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DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO, Born in Mumbai in 1964 and graduated from Mumbai University, Completed his Ph.D from ICT, 1991,Matunga, Mumbai, India, in Organic Chemistry, The thesis topic was Synthesis of Novel Pyrethroid Analogues, Currently he is working with AFRICURE PHARMA, ROW2TECH, NIPER-G, Department of Pharmaceuticals, Ministry of Chemicals and Fertilizers, Govt. of India as ADVISOR, earlier assignment was with GLENMARK LIFE SCIENCES LTD, as CONSUlTANT, Retired from GLENMARK in Jan2022 Research Centre as Principal Scientist, Process Research (bulk actives) at Mahape, Navi Mumbai, India. Total Industry exp 32 plus yrs, Prior to joining Glenmark, he has worked with major multinationals like Hoechst Marion Roussel, now Sanofi, Searle India Ltd, now RPG lifesciences, etc. He has worked with notable scientists like Dr K Nagarajan, Dr Ralph Stapel, Prof S Seshadri, etc, He did custom synthesis for major multinationals in his career like BASF, Novartis, Sanofi, etc., He has worked in Discovery, Natural products, Bulk drugs, Generics, Intermediates, Fine chemicals, Neutraceuticals, GMP, Scaleups, etc, he is now helping millions, has 9 million plus hits on Google on all Organic chemistry websites. His friends call him Open superstar worlddrugtracker. His New Drug Approvals, Green Chemistry International, All about drugs, Eurekamoments, Organic spectroscopy international, etc in organic chemistry are some most read blogs He has hands on experience in initiation and developing novel routes for drug molecules and implementation them on commercial scale over a 32 PLUS year tenure till date Feb 2023, Around 35 plus products in his career. He has good knowledge of IPM, GMP, Regulatory aspects, he has several International patents published worldwide . He has good proficiency in Technology transfer, Spectroscopy, Stereochemistry, Synthesis, Polymorphism etc., He suffered a paralytic stroke/ Acute Transverse mylitis in Dec 2007 and is 90 %Paralysed, He is bound to a wheelchair, this seems to have injected feul in him to help chemists all around the world, he is more active than before and is pushing boundaries, He has 100 million plus hits on Google, 2.5 lakh plus connections on all networking sites, 100 Lakh plus views on dozen plus blogs, 227 countries, 7 continents, He makes himself available to all, contact him on +91 9323115463, email amcrasto@gmail.com, Twitter, @amcrasto , He lives and will die for his family, 90% paralysis cannot kill his soul., Notably he has 38 lakh plus views on New Drug Approvals Blog in 227 countries......https://newdrugapprovals.wordpress.com/ , He appreciates the help he gets from one and all, Friends, Family, Glenmark, Readers, Wellwishers, Doctors, Drug authorities, His Contacts, Physiotherapist, etc He has total of 32 International and Indian awards

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Recent Posts

Cipepofol

June 2, 2026 2:36 am / Leave a comment


Cipepofol

CAS1637741-58-2

MW 204.31 g/mol MF C14H20O

2-[(1R)-1-cyclopropylethyl]-6-propan-2-ylphenol

FDA 2026, APPROVALS 2026, Cypsedo, HSK 3486, CS-0064163, GTPL 10812, HSK-3486, HY-116152, M3WGS532VY

  • OriginatorSichuan Haisco Pharmaceutical
  • ClassCyclopropanes; General anaesthetics; Phenols; Small molecules
  • Mechanism of ActionGABA A receptor agonists
  • RegisteredAnaesthesia; Sedation
  • 10 Apr 2026Sichuan Haisco Pharmaceutical plans a phase III trial for Anesthesia (In Children, In adolescents) (IV) in May 2026 (NCT07510945)
  • 28 Aug 2024No recent reports of development identified for preclinical development in Sedation in USA (IV, Infusion)
  • 01 Aug 2024Zhongda Hospital plans a clinical trial for Sedation (IV) in August 2024 (NCT06538883)

To induce general anesthesia in adults undergoing surgery

Cipepofol (also known as ciprofol or HSK3486) is a novel, short-acting intravenous anesthetic and sedative. As a structural analog of propofol, it targets \(GABA_{A}\) receptors but is 4 to 6 times more potent. It offers faster recovery, improved cardiovascular stability, and significantly less injection pain than propofol.

Key Clinical Advantages

  • Superior Efficacy: Requires a lower dose to achieve the same sedative depth as propofol.
  • Better Safety Profile: Associated with a lower incidence of injection pain, reduced respiratory depression, and better hemodynamic (blood pressure) stability.
  • Fast Acting: Characterized by rapid onset and quick recovery times, making it ideal for procedures like gastrointestinal endoscopy, bronchoscopy, and general anesthesia induction.

Recent Developments

  • FDA Approval: Cipepofol (sold under the brand name CYPSEDO) officially received U.S. FDA marketing approval, becoming the first China-originated innovative intravenous anesthetic to enter the global market.
  • Ongoing Trials: Clinical trials and post-marketing studies are actively evaluating its safety in specific populations, such as elderly patients and children.

Cipepofol (INNTooltip International Nonproprietary Name, USANTooltip United States Adopted Name), also known as ciprofol or by its developmental code name HSK3486, is a general anesthetic related to propofol which is used for anesthesia and sedation.[1][2][3][4] The drug is used by intravenous infusion.[1] A short-acting and highly selective γ-aminobutyric acid positive allosteric modulator,[5] ciprofol is 4 to 6 times more potent than other phenol derivatives such as propofol or fospropofol.[6]

In May 2026, cipepofol was approved by the US FDA.[7] Manufactured by Haisco Pharmaceutical Group of Chengdu, Sichuan, China, ciprofol underwentphase I and II trials in Australia and China.[8][9][10] In these early studies, ciprofol was comparable in efficacy to propofol and was associated with fewer adverse events.[4][6][11][12][13][14][15][16][17][18]

Physical properties

Ciprofol is an optically active 2,6-disubstituted alkylphenol with a cyclopropylethyl group incorporated at the second carbon atom. This cyclopropyl group increases the steric effects and introduces stereoselective effects over its anesthetic properties. These properties appear to increase the anesthetic potency of ciprofol, when compared with propofol.[9]

Medical use

Ciprofol is used for the intravenous induction of general anesthesia.[3][4] Studies published in 2022 and 2023 found it was efficacious as a general anesthetic in patients undergoing gynecological surgery[6][11] and kidney transplantation,[19] as well as for endoscopic procedures such as bronchoscopy,[15][20] esophagogastroduodenoscopy and colonoscopy.[21][22]

Ciprofol has also been used for sedation of critically ill patients undergoing mechanical ventilation in the intensive care unit,[23] as well as for the treatment of agitation and delirium in that patient population.[24] When combined with mild therapeutic hypothermia, ciprofol may also be useful as a cerebral protective agent in the setting of cerebral ischemia-reperfusion injury.[25]

Experimental use

In experimental models of isoproterenol-induced myocardial infarction (using mice as subjects), ciprofol appears to protect the heart against oxidative damage, inflammation and apoptosis of cardiac muscle cells.[26]

SYN

US20240132445,

https://patentscope.wipo.int/search/en/detail.jsf?docId=US428011434&_cid=P12-MPW0XO-91017-1

PAT

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2014180305&_cid=P12-MPW0R4-87054-1

Example 16

[-cyclopropylethyl] -6 -isopropylphenol (compound 16)

2- [(lR)-l-cyclopropylethyl]-6-isopropyl -phenol

Preparation methods of Examples 16-17:

2-(1-Cyclopropylethyl-6-isopropylphenol (compound 3) 600 mg was used for resolution. Preparation conditions: (Instrument: Agilent 1260/CH-Y-J0404; Column: CHIRALPAK OJ-H (4.6 mm < 250 mm, 5 μm) No.: OJ-H-27; Mobile phase: A: isopropanol, B: n-hexane; Flow rate: 1.0 mL/min; Back pressure: 100 bar; Column temperature: 35°C; Wavelength: 210 nm; Period: 10 min)

Two optical isomers were obtained after separation: peak 1 (retention time: 10.72 min, 280 mg, pale yellow liquid, ee%=99%) and peak 2 (retention time: 13.58 min, 280 mg, pale yellow liquid, ee%=99%).

峰 1 : MS m/z(ESI): 203.1(Ml).

toMR (400 MHz,CDCl3 ) ： δ 7.14(dd， 1H)， δ 7.08(dd， 1H)， 6.91 (t， 1H)， 4.93 (s, 1H), 3.22-3.14(m, 1H)， 2.55-2.48 (m, 1H)， 1.33 (d, 6H)， 1.28 (d, 3H)， 1.10-1.05 (m， 1H)， 0.60-0.58 (m, 1H)， 0.49-0.46 (m， 1H)， 0.25-0.18 (m, 2H).

峰 2: MS m/z(ESI): 203.1(Ml).

iHNMR (400 MHz,CDCl3) ： 57.14(dd, 1H)， δ 7.08(dd， 1H)， 6.93 (t, 1H)， 4.93 (s 1H), 3.22-3.15(m, 1H)， 2.55-2.48 (m， 1H)， 1.32 (d， 6H)， 1.28 (d， 3H)， 1.10-1.04 (m， 1H)， 0.60-0.58 (m, 1H)， 0.49-0.46 (m, 1H)， 0.25-0.18 (m, 2H).

PAT

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References

References

  1.  “Sichuan Haisco Pharmaceutical”. AdisInsight. 28 August 2024. Retrieved 1 October 2025.
  2.  “Ciprofol (Cipepofol): A γ-Aminobutyric Acid Receptor Agonist for Induction of Anesthesia”. Chemistry and Pharmacology of Drug Discovery. Wiley. 2024. pp. 251–274. doi:10.1002/9781394225156.ch12. ISBN 978-1-394-22512-5. Retrieved 1 October 2025.
  3.  Wang X, Wang X, Liu J, Zuo YX, Zhu QM, Wei XC, et al. (March 2022). “Effects of ciprofol for the induction of general anesthesia in patients scheduled for elective surgery compared to propofol: a phase 3, multicenter, randomized, double-blind, comparative study”. European Review for Medical and Pharmacological Sciences. 26 (5): 1607–1617. PMID 35302207.
  4.  Zeng Y, Wang DX, Lin ZM, Liu J, Wei XC, Deng J, et al. (February 2022). “Efficacy and safety of HSK3486 for the induction and maintenance of general anesthesia in elective surgical patients: a multicenter, randomized, open-label, propofol-controlled phase 2 clinical trial”. European Review for Medical and Pharmacological Sciences. 26 (4): 1114–1124. PMID 35253166.
  5.  Liao J, Li M, Huang C, Yu Y, Chen Y, Gan J, et al. (2022). “Pharmacodynamics and Pharmacokinetics of HSK3486, a Novel 2,6-Disubstituted Phenol Derivative as a General Anesthetic”. Frontiers in Pharmacology. 13 830791. doi:10.3389/fphar.2022.830791. PMC 8851058. PMID 35185584.
  6.  Chen BZ, Yin XY, Jiang LH, Liu JH, Shi YY, Yuan BY (August 2022). “The efficacy and safety of ciprofol use for the induction of general anesthesia in patients undergoing gynecological surgery: a prospective randomized controlled study”. BMC Anesthesiology. 22 (1) 245. doi:10.1186/s12871-022-01782-7. PMC 9347095. PMID 35922771.
  7.  “Novel Drug Approvals for 2026”. U.S. Food and Drug Administration. 29 May 2026. Retrieved 31 May 2026.
  8.  Lu M, Liu J, Wu X, Zhang Z (2023). “Ciprofol: A Novel Alternative to Propofol in Clinical Intravenous Anesthesia?”. BioMed Research International. 2023 7443226. doi:10.1155/2023/7443226. PMC 9879693. PMID 36714027.
  9.  Qin L, Ren L, Wan S, Liu G, Luo X, Liu Z, et al. (May 2017). “Design, Synthesis, and Evaluation of Novel 2,6-Disubstituted Phenol Derivatives as General Anesthetics”. Journal of Medicinal Chemistry. 60 (9): 3606–3617. doi:10.1021/acs.jmedchem.7b00254. PMID 28430430.
  10.  Nair A, Seelam S (2022). “Ciprofol- a game changing intravenous anesthetic or another experimental drug!”. Saudi Journal of Anaesthesia. 16 (2): 258–259. doi:10.4103/sja.sja_898_21. PMC 9009555. PMID 35431734.
  11.  Man Y, Xiao H, Zhu T, Ji F (March 2023). “Study on the effectiveness and safety of ciprofol in anesthesia in gynecological day surgery: a randomized double-blind controlled study”. BMC Anesthesiology. 23 (1) 92. doi:10.1186/s12871-023-02051-x. PMC 10039513. PMID 36964501.
  12.  Chen X, Guo P, Yang L, Liu Z, Yu D (2022). “Comparison and Clinical Value of Ciprofol and Propofol in Intraoperative Adverse Reactions, Operation, Resuscitation, and Satisfaction of Patients under Painless Gastroenteroscopy Anesthesia”. Contrast Media & Molecular Imaging. 2022 9541060. doi:10.1155/2022/9541060. PMC 9314164. PMID 35935320.
  13.  Zhong J, Zhang J, Fan Y, Zhu M, Zhao X, Zuo Z, et al. (May 2023). “Efficacy and safety of Ciprofol for procedural sedation and anesthesia in non-operating room settings”. Journal of Clinical Anesthesia. 85 111047. doi:10.1016/j.jclinane.2022.111047. PMID 36599219. S2CID 255468218.
  14.  Liang P, Dai M, Wang X, Wang D, Yang M, Lin X, et al. (June 2023). “Efficacy and safety of ciprofol vs. propofol for the induction and maintenance of general anaesthesia: A multicentre, single-blind, randomised, parallel-group, phase 3 clinical trial”. European Journal of Anaesthesiology. 40 (6): 399–406. doi:10.1097/EJA.0000000000001799. PMC 10155686. PMID 36647565.
  15.  Luo Z, Tu H, Zhang X, Wang X, Ouyang W, Wei X, et al. (March 2022). “Efficacy and Safety of HSK3486 for Anesthesia/Sedation in Patients Undergoing Fiberoptic Bronchoscopy: A Multicenter, Double-Blind, Propofol-Controlled, Randomized, Phase 3 Study”. CNS Drugs. 36 (3): 301–313. doi:10.1007/s40263-021-00890-1. PMC 8927014. PMID 35157236.
  16.  Hu C, Ou X, Teng Y, Shu S, Wang Y, Zhu X, et al. (November 2021). “Sedation Effects Produced by a Ciprofol Initial Infusion or Bolus Dose Followed by Continuous Maintenance Infusion in Healthy Subjects: A Phase 1 Trial”. Advances in Therapy. 38 (11): 5484–5500. doi:10.1007/s12325-021-01914-4. PMC 8523013. PMID 34559359.
  17.  Teng Y, Ou M, Wang X, Zhang W, Liu X, Liang Y, et al. (September 2021). “Efficacy and safety of ciprofol for the sedation/anesthesia in patients undergoing colonoscopy: Phase IIa and IIb multi-center clinical trials”. European Journal of Pharmaceutical Sciences. 164 105904. doi:10.1016/j.ejps.2021.105904. PMID 34116176.
  18.  Zhu Q, Luo Z, Wang X, Wang D, Li J, Wei X, et al. (April 2023). “Efficacy and safety of ciprofol versus propofol for the induction of anesthesia in adult patients: a multicenter phase 2a clinical trial”. International Journal of Clinical Pharmacy. 45 (2): 473–482. doi:10.1007/s11096-022-01529-x. PMC 10147789. PMID 36680620.
  19.  Qin K, Qin WY, Ming SP, Ma XF, Du XK (July 2022). “Effect of ciprofol on induction and maintenance of general anesthesia in patients undergoing kidney transplantation”. European Review for Medical and Pharmacological Sciences. 26 (14): 5063–5071. PMID 35916802.
  20.  Wu B, Zhu W, Wang Q, Ren C, Wang L, Xie G (2022). “Efficacy and safety of ciprofol-remifentanil versus propofol-remifentanil during fiberoptic bronchoscopy: A prospective, randomized, double-blind, non-inferiority trial”. Frontiers in Pharmacology. 13 1091579. doi:10.3389/fphar.2022.1091579. PMC 9812563. PMID 36618929.
  21.  Li J, Wang X, Liu J, Wang X, Li X, Wang Y, et al. (August 2022). “Comparison of ciprofol (HSK3486) versus propofol for the induction of deep sedation during gastroscopy and colonoscopy procedures: A multi-centre, non-inferiority, randomized, controlled phase 3 clinical trial”. Basic & Clinical Pharmacology & Toxicology. 131 (2): 138–148. doi:10.1111/bcpt.13761. PMC 9543620. PMID 35653554.
  22.  Long YQ, Feng CD, Ding YY, Feng XM, Liu H, Ji FH, et al. (2022). “Esketamine as an Adjuvant to Ciprofol or Propofol Sedation for Same-Day Bidirectional Endoscopy: Protocol for a Randomized, Double-Blind, Controlled Trial With Factorial Design”. Frontiers in Pharmacology. 13 821691. doi:10.3389/fphar.2022.821691. PMC 8975265. PMID 35370640.
  23.  Liu Y, Yu X, Zhu D, Zeng J, Lin Q, Zang B, et al. (May 2022). “Safety and efficacy of ciprofol vs. propofol for sedation in intensive care unit patients with mechanical ventilation: a multi-center, open label, randomized, phase 2 trial”. Chinese Medical Journal. 135 (9): 1043–1051. doi:10.1097/CM9.0000000000001912. PMC 9276409. PMID 34924506.
  24.  Liu GL, Wu GZ, Ge D, Zhou HJ, Cui S, Gao K, et al. (2023). “Efficacy and safety of ciprofol for agitation and delirium in the ICU: A multicenter, single-blind, 3-arm parallel randomized controlled trial study protocol”. Frontiers in Medicine. 9 1024762. doi:10.3389/fmed.2022.1024762. PMC 9868613. PMID 36698817.
  25.  Wang YC, Wu MJ, Zhou SL, Li ZH (January 2023). “Protective effects of combined treatment with ciprofol and mild therapeutic hypothermia during cerebral ischemia-reperfusion injury”. World Journal of Clinical Cases. 11 (3): 487–492. doi:10.12998/wjcc.v11.i3.487. PMC 9923870. PMID 36793629.
  26.  Yang Y, Xia Z, Xu C, Zhai C, Yu X, Li S (2022). “Ciprofol attenuates the isoproterenol-induced oxidative damage, inflammatory response and cardiomyocyte apoptosis”. Frontiers in Pharmacology. 13 1037151. doi:10.3389/fphar.2022.1037151. PMC 9723392. PMID 36483733.
  27.  Vittori A, Di Fabio C, Cascella M, Marinangeli F, Francia E, Mascilini I, et al. (January 2026). “Advantages of Ciprofol with Special Consideration of Pediatric Anesthesia”. Children (Basel, Switzerland). 13 (2). doi:10.3390/children13020188. PMC 12939459. PMID 41749542.
  28.  Liu SB, Yao X, Tao J, Yang JJ, Zhao YY, Liu DW, et al. (March 2023). “Population total and unbound pharmacokinetics and pharmacodynamics of ciprofol and M4 in subjects with various renal functions”. British Journal of Clinical Pharmacology. 89 (3): 1139–1151. doi:10.1111/bcp.15561. PMID 36217805. S2CID 252818288.
  29.  Hu Y, Li X, Liu J, Chen H, Zheng W, Zhang H, et al. (December 2022). “Safety, pharmacokinetics and pharmacodynamics of a novel γ-aminobutyric acid (GABA) receptor potentiator, HSK3486, in Chinese patients with hepatic impairment”. Annals of Medicine. 54 (1): 2769–2780. doi:10.1080/07853890.2022.2129433. PMC 9559057. PMID 36217101.
  30.  Li X, Yang D, Li Q, Wang H, Wang M, Yan P, et al. (2021). “Safety, Pharmacokinetics, and Pharmacodynamics of a Single Bolus of the γ-aminobutyric Acid (GABA) Receptor Potentiator HSK3486 in Healthy Chinese Elderly and Non-elderly”. Frontiers in Pharmacology. 12 735700. doi:10.3389/fphar.2021.735700. PMC 8430033. PMID 34512361.
  31.  Ding YY, Long YQ, Yang HT, Zhuang K, Ji FH, Peng K (December 2022). “Efficacy and safety of ciprofol for general anaesthesia induction in elderly patients undergoing major noncardiac surgery: A randomised controlled pilot trial”. European Journal of Anaesthesiology. 39 (12): 960–963. doi:10.1097/EJA.0000000000001759. PMID 36214498. S2CID 252779399.
  32.  Duan G, Lan H, Shan W, Wu Y, Xu Q, Dong X, et al. (April 2023). “Clinical effect of different doses of ciprofol for induction of general anesthesia in elderly patients: A randomized, controlled trial”. Pharmacology Research & Perspectives. 11 (2) e01066. doi:10.1002/prp2.1066. PMC 9944862. PMID 36811327. S2CID 257098376.
  33.  Yang Y, Xia Z, Xu C, Zhai C, Yu X, Li S (2022). “Ciprofol attenuates the isoproterenol-induced oxidative damage, inflammatory response and cardiomyocyte apoptosis”. Frontiers in Pharmacology. 13 1037151: 1037151. doi:10.3389/fphar.2022.1037151. PMC 9723392. PMID 36483733.
  34.  Bian Y, Zhang H, Ma S, Jiao Y, Yan P, Liu X, et al. (January 2021). “Mass balance, pharmacokinetics and pharmacodynamics of intravenous HSK3486, a novel anaesthetic, administered to healthy subjects”. British Journal of Clinical Pharmacology. 87 (1): 93–105. doi:10.1111/bcp.14363. PMID 32415708. S2CID 218658207.

Further reading

Clinical data
Other namesCiprofol; CS-0064163; CS0064163; GTPL10812; GTPL-10812; HSK-3486; HSK3486; HY-116152; HY116152; (R)-2-(1-Cyclopropylethyl)-6-isopropylphenol
Routes of
administration		Intravenous infusion[1]
Drug classGABAA receptor positive allosteric modulator
Pharmacokinetic data
MetabolismLiver glucuronidation
ExcretionKidney
Identifiers
IUPAC name
CAS Number1637741-58-2 
PubChem CID86301664
DrugBankDB16295 
ChemSpider76794458 
UNIIM3WGS532VY
KEGGD12449 
ChEMBLChEMBL4094894 
Chemical and physical data
FormulaC14H20O
Molar mass204.313 g·mol−1
3D model (JSmol)Interactive image
SMILES
InChI

////////cipepofol, FDA 2026, APPROVALS 2026, Cypsedo, HSK 3486, CS-0064163, GTPL 10812, HSK-3486, HY-116152, M3WGS532VY, ANAESTHETIC

Fudapirine

May 31, 2026 2:48 am / Leave a comment


Fudapirine

CAS 1859978-72-5

MFC34H33ClN2O2 MW537.1 g/mol

(1R,2S)-1-[5-(4-chlorophenyl)-2-methoxy-3-pyridinyl]-4-(dimethylamino)-2-naphthalen-1-yl-1-phenylbutan-2-ol

(1R,2S)-1-[5-(4-chlorophenyl)-2-methoxypyridin-3-yl]-4-(dimethylamino)-2-(naphthalen-1-yl)-1-phenylbutan-2-ol
antibacterial, Sudapyridine, WX-081, WX 081, 7X86XPE5TG,

  • A Phase III Study of Oral Sudapyridine (WX-081) Tablets in Rifampicin-Resistant Pulmonary Tuberculosis PatientsCTID: NCT05824871Phase: Phase 3Status: RecruitingDate: 2025-06-29
  • Drug-Drug Interaction and Food Effect of Sudapyridine(WX-081) With Itraconazole and Rifampin in Healthy Chinese AdultsCTID: NCT06701136Phase: Phase 1Status: Not yet recruitingDate: 2025-02-12
  • Sudapyridine (WX-081) in Healthy VolunteersCTID: NCT06117514Phase: Phase 1Status: CompletedDate: 2023-11-07
  • Evaluation of Early Bactericidal Activity and Safety in Pulmonary Tuberculosis With WX-081CTID: NCT04608955Phase: Phase 2Status: CompletedDate: 2023-09-11

Fudapirine (also known as sudapyridine or WX-081) is a novel, next-generation antimycobacterial drug primarily being developed to treat tuberculosis (TB). It belongs to a chemical class called diarylquinolines, making it a close analogue of bedaquiline, an already established drug used for drug-resistant tuberculosis.Key Facts About FudapirinePrimary Function: It displays powerful anti-mycobacterial activity against Mycobacterium tuberculosis strains.

Mechanism: As a diarylquinoline, it selectively inhibits bacterial ATP synthase, effectively cutting off the energy supply that the tuberculosis bacteria need to survive and replicate.Development Stage: According to pharmacology databases like the IUPHAR/BPS Guide to PHARMACOLOGY, the drug has advanced into Phase III clinical evaluation.Official Naming: While initially designated as WX-081, the World Health Organization (WHO) assigned it the International Nonproprietary Name (INN) fudapirine in early 2025.Other Applications: Beyond standard TB, researchers are investigating its therapeutic potential against non-tuberculous mycobacterial (NTM) infections.

PAT

https://patentscope.wipo.int/search/en/detail.jsf;jsessionid=6D72E4125E9DD99079BEE19ECCE38CED.wapp2nC?docId=WO2017121323&_cid=P22-MPT687-41395-1

Step 5: 
Synthesis of 
1-(5-(4-chlorophenyl)-2-methoxypyridin-3-yl)-4-(dimethylamino)-2-(naphth-1-yl)-1-phenylbut-2-ol

Titration of n-butyllithium : Under nitrogen protection, 1.00 g 

of diphenylacetic acid (Alfa, 4.71 mmol) was added to 10 mL of tetrahydrofuran to form a colorless and transparent solution. A hexane solution of 

n-butyllithium was slowly added dropwise to this solution using a syringe. The solution was observed to turn yellow locally during the addition, but the yellow color quickly disappeared. The endpoint was reached when a yellow solution formed after one drop and did not fade within half a minute. The volumes of 

n-butyllithium were recorded (1.927 mL and 1.985 mL, with an average volume of 1.95 mL). Therefore, the concentration of 

the n-butyllithium hexane solution used was 2.42 mol/L. 

[0171]TMP (2.74 kg, 19.3 mol) was dissolved in anhydrous tetrahydrofuran (12 L). The reaction temperature was cooled to -65°C using a dry ice-acetone bath, and then 

n-butyllithium (8 L, 19.3 mol, 2.42 mol/L n-hexane solution) was added dropwise. The temperature was controlled between -20°C and -78°C. The reaction system was observed to gradually change color from light yellow to red to deep red, eventually forming a yellow suspension. Stirring was continued at this temperature for 30 minutes. Then, the reaction temperature was lowered to -75°C to -80°C, and over 4–6 hours, a solution of 

3-benzyl-5-(4-chlorophenyl)-2-methoxypyridine (4.08 kg, 12.9 mol) in anhydrous tetrahydrofuran (6 L) was slowly added dropwise. The temperature was maintained between -65°C and -78°C, and a mild exothermic reaction with a deep red color was observed. After the initial addition was complete, a solution of 3-(dimethylamino)-1-(naphth-1-yl)propyl-1-one (3.26 kg, 12.9 mol, 90% purity) in anhydrous tetrahydrofuran (2.0 L) was slowly added dropwise over 2–4 hours. The system exhibited significant exothermic activity, and the flow rate was controlled to maintain the temperature at -65°C to -78°C. After the addition was complete, the temperature was maintained at -65°C to -78°C, and stirring was continued for another half hour. HPLC analysis showed that the content of 

3-benzyl-5-(4-chlorophenyl)-2-methoxypyridine was less than 10%. The reaction solution was slowly added to a saturated 

ammonium chloride solution (40 L) for quenching, and the mixture was separated. The aqueous phase was extracted with ethyl acetate (30 L). The combined organic phases were washed and separated with saturated brine (30 L). The organic phases were concentrated under reduced pressure at 40–50 °C to obtain a yellow oily crude product (13.5 kg). The crude product was stirred in a mixed solvent of ethyl acetate/n-heptane (4 L, 1/4) at 5–15 °C for 16 hours to precipitate a white solid. The product was filtered, and the filter cake was slurried with ethanol (4 L × 2). After filtration, the filter cake was vacuum dried to constant weight (50 °C, 24–48 hours) to obtain the target compound 1-(5-(4-chlorophenyl)-2-methoxypyridin-3-yl)-4-(dimethylamino)-2-(naphth-1-yl)-1-phenylbut-2-ol (1.83 kg, yield 23.23%), a white solid. HPLC identification showed that isomer A accounted for 88.3% and isomer B accounted for 4.8%. 

1 H NMR (400MHz, CDCl 3 )δ: 8.85(d,J＝2.3Hz,1H),8.64(d,J＝8.7Hz,1H),8.32(d,J＝2.4Hz,1H),7. 98-7.86(m,2H),7.72-7.61(m,2H),7.57(d,J＝8.4Hz,2H),7.54-7.43(m,3 H),7.33(t,J＝7.8Hz,1H),7.20-7.17(m,2H),6.95-6.87(m,3H),5.85(s,1 H),4.17(s,3H),2.60-2.51(m,1H),2.19-2.04(m,2H),2.01-1.97(m,7H).

[0172]Step 6: Synthesis of (1R,2S)-1-(5-(4-chlorophenyl)-2-methoxypyridin-3-yl)-4-(dimethylamino)-2-(naphth-1-yl)-1-phenylbut-2-ol compound I-2

Method 1: 

[0175]Two parallel batches were prepared: R-(-)-binaphthol phosphate (519.3 g, 1.49 mol) was suspended in DMSO (1.0 L) and heated to 50 °C with stirring until dissolved and clear. 1-(5-(4-chlorophenyl)-2-methoxypyridin-3-yl)-4-(dimethylamino)-2-(naphthaleneethanol-1-yl)-1-phenylbutyl-2-ol (910 g, 1.49 mol, isomer A content 88.3%) was added to an ethanol (24 L) solution, and the DMSO (1.0 L) solution of R-(-)-binaphthol phosphate prepared above was added dropwise over 1–2 hours with stirring (196 rpm). Undissolved particulate compounds began to dissolve, but a more viscous emulsion formed. After the addition was complete, the reaction mixture was stirred at 15–35 °C for 16 hours. The reaction solution was heated to reflux in an oil bath and refluxed for 1 hour. Heating was then stopped, and the reaction solution was cooled to 15–35°C and stirred for 16 hours. The reaction solution was filtered (two batches were combined for processing). Due to the high viscosity of the solids, filtration was slow. The filter cake was slurried three times with ethanol (20 liters). The combined organic phases were concentrated to constant weight to obtain a yellow oily substance (5 kg). Water (10 liters) and ethyl acetate (5 liters) were added to this crude product. The pH of the system was adjusted to 11 with a 10% cold 

sodium hydroxide aqueous solution, and stirring was continued for 1 hour. Then, the mixture was separated. A large amount of solid precipitated from the system. The solid obtained by filtration was isomer A (350 g, purity 97%, white solid). The filtrate was concentrated under reduced pressure at 50°C to constant weight, and ethanol (1.0 L) was added. The mixture was stirred at 15-35°C for 16 hours, filtered, and the filter cake was washed three times with ethanol (400 mL) to obtain a white solid. The solid was dried under vacuum to constant weight (50°C, 24-48 hours) to obtain compound I-2 (400 g, purity 95%, ee value greater than 99.5%, yield 24%), a white solid. 

1 H NMR (400MHz, CDCl 

3 )δ: 8.85(d,J＝2.3Hz,1H),8.64(d,J＝8.7Hz,1H),8.32(d,J＝2.4Hz,1H),7. 98-7.86(m,2H),7.72-7.61(m,2H),7.57(d,J＝8.4Hz,2H),7.54-7.43(m,3 H),7.33(t,J＝7.8Hz,1H),7.20-7.17(m,2H),6.95-6.87(m,3H),5.85(s,1 H),4.17(s,3H),2.60-2.51(m,1H),2.19-2.04(m,2H),2.01-1.97(m,7H).

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PAT

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Fosrugocrixan

May 29, 2026 2:35 am / Leave a comment


Fosrugocrixan

CAS 2408145-38-8

MF C19H26N5O4PS2, MW483.5 g/mol

[(2R)-2-[[2-amino-5-[(1S)-1-phenylethyl]sulfanyl-[1,3]thiazolo[4,5-d]pyrimidin-7-yl]amino]-4-methylpentyl] dihydrogen phosphate

(2R)-2-[(2-amino-5-{[(1S)-1-phenylethyl]sulfanyl}[1,3]thiazolo[4,5-d]pyrimidin-7-yl)amino]-4-methylpentyl dihydrogen phosphate
CX3C chemokine receptor 1 (CX3CR1) antagonist, antiinflammatory, 4ZXD25SC4S, KAND-145, KAND 145

  • OriginatorKancera
  • DeveloperNovakand Pharma
  • ClassAnti-inflammatories; Antineoplastics; Small molecules
  • Mechanism of ActionChemokine CXCL13 inhibitors
  • Phase IOvarian cancer
  • PreclinicalChronic lymphocytic leukaemia
  • No development reportedInflammation
  • 22 Sep 2025Kancera is now called Novakand Pharma
  • 28 Apr 2025No recent reports of development identified for preclinical development in Ovarian-cancer in Sweden (IV)
  • 03 May 2024Efficacy and adverse event data from a phase I trials in healthy volunteers released by Kancera

Fosrugocrixan (also known by its developmental code KAND145) is a novel, small-molecule drug candidate acting as a selective antagonist for CX3C chemokine receptor 1 (CX3CR1), commonly known as the fractalkine receptor.

Key Characteristics and Mechanism

  • Drug Class: It represents a first-in-class small molecule immune modulator.
  • Phosphate Prodrug: Fosrugocrixan is designed as a soluble phosphate prodrug. Once inside the body (in vivo), it converts into its active drug form, rugocrixan (formerly KAND567).
  • Mechanism of Action: By blocking the CX3CR1 fractalkine pathway, it controls and prevents the trafficking of disease-promoting immune cells. This blockage provides potent anti-inflammatory activity.

Clinical Development and Targets

The drug is being actively developed by Novakand Pharma (a company formerly known as Kancera). Its primary therapeutic targets span several conditions driven by runaway inflammation and immune responses:

  • Cardiovascular Diseases: Specifically targeted to manage conditions where hyper-inflammation damages tissue (such as post-myocardial infarction or heart conditions).
  • Autoimmune & Inflammatory Diseases: Evaluated for broad anti-inflammatory potential.
  • Oncology: Investigated for its ability to regulate the tumor microenvironment.

SYN

WO 2020008064

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2020008064&_cid=P21-MPQB4Y-95682-1

SYN

Karlström et al. J. Med. Chem., 2013, 56, 3177-3190

https://pubs.acs.org/doi/10.1021/jm3012273

PAT

https://patentscope.wipo.int/search/en/detail.jsf;jsessionid=25F7EEC83623D484A1CFC460F518D56A.wapp2nB?docId=US458057934&_cid=P21-MPQAOO-82527-1

(2R)-2-[(2-Amino-5-{[(1S)-1-phenylethyl]sulfanyl}[1,3]thiazolo[4,5-d]pyrimidin-7-yl)amino]-4-methylpentyl dihydrogen phosphate (B), are known to act as antagonists of the fractalkine receptor (CX3CR1) (Karlström et al. J. Med. Chem., 2013, 56, 3177-3190; WO 2020/008064)

PAT

https://patentscope.wipo.int/search/en/detail.jsf?docId=US336567291&_cid=P21-MPQAYT-90868-1

Example 1

Preparation of (2R)-2-[(2-Amino-5-{[(1S)-1-phenylethyl]sulfanyl}[1,3]thiazolo[4,5-d]pyrimidin-7-yl)amino]-4-methylpentyl dihydrogen phosphate

Phosphorus oxychloride (337 mg, 2.2 mmol) was dissolved in THE (0.75 mL) and water (25 mg, 1.4 mmol) was added. The mixture was cooled in an ice-bath and pyridine (111 mg, 113 μL, 1.4 mmol) was added followed by (2R)-2-[(2-amino-5-{[(1S)-1-phenylethyl]sulfanyl}-[1,3] thiazolo[4,5-d]pyrimidin-7-yl)amino]-4-methylpentan-1-ol hydrochloride (110 mg, 0.25 mmol) (Karlstr6m S., et al., J. Med. Chem., 2013, 56, 3177-3190; WO 2006/107258). The reaction mixture was stirred at ice-bath temperature for 1 h. To a mixture of phosphorus oxychloride (337 mg, 2.2 mmol) and water (25 mg, 1.4 mmol) in THE was added, at ice-bath temperature pyridine (111 mg, 113 μL, 1.4 mmol). Half of this mixture was added to the reaction mixture described above. The reaction mixture was stirred at ice-bath temperature for another 1 h. Water (3 mL) was added and the reaction mixture was stirred for 15 min at ice-bath temperature and 20 min at room temperature. DCM (3 mL) was added and the phases were separated. The aqueous phase was extracted with another portion of DCM (3 mL) and the organic phases were combined. At this point the product started to precipitate as a pale-yellow gum in the organic phase. MeOH was added and the now homogeneous solution was transferred to a round-bottomed flask and was evaporated to yield 120 mg of crude product, which according to HPLC was ca. 93% pure. The crude material was dissolved in a MeOH/water mixture and the pH was adjusted to about 6-7 with 1 M NaOH. The material was purified by preparative HPLC (basic method). The pure fractions were pooled, evaporated, and dried in vacuum. The product was assumed to be the diammonium salt after purification. 1H NMR (600 MHz, CD 3OD) δ H ppm 7.43-7.47 (m, 2H) 7.30-7.35 (m, 2H) 7.20-7.24 (m, 1H) 5.08 (q, J=7.03 Hz, 1H) 4.59-4.68 (m, 1H) 3.92 (ddd, J=10.12, 5.67, 4.30 Hz, 1H) 3.88 (dt, J=10.12, 4.94 Hz, 1H) 1.74 (d, J=7.03 Hz, 3H) 1.71-1.79 (m, 1H) 1.68 (ddd, J=13.87, 9.54, 5.67 Hz, 1H) 1.57 (ddd, J=13.87, 8.54, 5.33 Hz, 1H) 0.98 (d, J=6.71 Hz, 3H) 0.96 (d, J=6.56 Hz, 3H). MS (ESI +) m/z 484 [M+H] +.

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Fosizensertib

May 28, 2026 2:32 am / Leave a comment


Fosizensertib

CAS 2905377-00-4

MF C22H21F2N4O5P MW490.4 g/mol

[(2S)-1-[[5-[2-[1-(difluoromethyl)pyrazol-4-yl]ethynyl]pyridine-3-carbonyl]-methylamino]-3-phenylpropan-2-yl] dihydrogen phosphate

(2S)-1-(5-{[1-(difluoromethyl)-1H-pyrazol-4-yl]ethynyl}-Nmethylpyridine-3-carboxamido)-3-phenylpropan-2-yl dihydrogen
phosphate
receptor-interacting serine/threonine protein (RIP-1) kinase inhibitor, ABBV-668, ABBV 668, 6GA6XSX5SL

Fosizensertib (also known by the developmental code ABBV-668) is an investigational small molecule drug being evaluated for the treatment of ulcerative colitis and other chronic autoimmune or inflammatory conditions.

Mechanism of Action

  • Target: It acts as a selective inhibitor of receptor-interacting serine/threonine-protein kinase 1 (RIPK1), an enzyme that plays a critical role in regulating cellular inflammation and necroptosis (programmed cell death).
  • Prodrug Design: Fosizensertib functions as a phosphate prodrug. When administered, it is essentially inactive in vitro (inhibiting RIPK1 by less than 10%).
  • Bioactivation: Once inside the body, it undergoes in vivo dephosphorylation to convert into its active metabolite (Compound 2), which strongly inhibits RIPK1 activity to suppress inflammatory pathways.

According to resources like the IUPHAR/BPS Guide to Pharmacology and PubChem, its core chemical metrics include:

Fosizensertib was assigned its International Nonproprietary Name (INN) by the World Health Organization (WHO). Developed by the pharmaceutical company AbbVie, it is classified as a clinical candidate intended for oral administration. It is currently restricted strictly to laboratory research and clinical evaluation settings and is not approved for general prescription or veterinary use.

PAT

[WO2023018643A1]

https://patentscope.wipo.int/search/en/detail.jsf;jsessionid=66762EE22EF5E77E0FC927179EB58712.wapp2nB?docId=WO2023018643&_cid=P21-MPOVCH-38336-1

(S)-1-(5-((1-(difluoromethyl)-1H-pyrazol-4-yl)ethynyl)-N-methylnicotinamido)-3-phenylpropan-2-yl dihydrogen phosphate;

Examples #18 and 19: (S)–di–tert–butyl (1–(5–((1–(difluoromethyl)–1H–pyrazol–4– yl)ethynyl)–N–methylnicotinamido)–3–phenylpropan–2–yl) phosphate (Example #18) and (S)–1–(5–((1–(difluoromethyl)–1H–pyrazol–4–yl)ethynyl)–N–methylnicotinamido)–3– phenylpropan–2–yl dihydrogen phosphate (Example #19)

[0173] To a solution of (S)-5-((1-(difluoromethyl)-1H-pyrazol-4-yl)ethynyl)-N-(2-hydroxy- 3-phenylpropyl)-N-methylnicotinamide (Example #2) (500 mg, 1.22 mmol) in N-Methyl-2- pyrrolidinone (1000 mL) was added di-tert-butyl diethylphosphoramidite (304 mg, 1.22 mmol) and 1H-tetrazole (10.8 mL, 4.87 mmol) in one portion at 20 °C under N2. The mixture was stirred at 40 °C for 3 hours. Hydrogen peroxide (5.0 mL, 49 mmol) was added to the solution at 0 °C, and the mixture was stirred for an additional 2 hours. The mixture was poured into saturated Na2SO3 (75 mL) and extracted with ethyl acetate (EtOAc) (3 × 100 mL). The organic phase was washed with brine (100 mL), dried over Na2SO4, concentrated under reduced pressure to give the crude t-butyl phosphate ester, which was chromatographed on silica gel (petroleum ether: ethyl acetate=1:1-1:4) to provide (S)-di-tert-butyl (1-(5-((1-(difluoromethyl)-1H-pyrazol-4- yl)ethynyl)-N-methylnicotinamido)-3-phenylpropan-2-yl) phosphate (Example #18) (384 mg, 0.64 mmol, 52% yield). LC/MS (Table B, Method aa) Rt = 1,73 min; MS m/z: 545.20 (M-tBu)+; 1H NMR (400 MHz, DMSO-d6) δ 8.76 – 8.40 (m, 3H), 8.15 – 7.60 (m, 3H), 7.27-7.01 (m, 5H), 4.78-4.46 (br m, 1H), 3.75-2.72 (m, 7H), 1.50-1.18 (m, 18H). tBu = tert–butyl; Et = ethyl.

[0174] A flask was charged with (S)-di-tert-butyl (1-(5-((1-(difluoromethyl)-1H-pyrazol-4- yl)ethynyl)-N-methylnicotinamido)-3-phenylpropan-2-yl) phosphate (Example #18) (381 mg, .632 mmol), dichloromethane (DCM) (5 mL) and trifluoroacetic acid (TFA) (0.61 mL, 7.9 mmol) and stirred at room temperature for approximately 19 hours. The mixture was concentrated under reduced pressure, then purified via reverse phase liquid chromatography (Atlantis® Prep T3 Phenomenex 5 μm 19 x 50 mm column, 5 to 95 acetonitrile (MeCN):water (formic acid buffer) at 1 mL/minute) to provide the title compound, Example #19 (230 mg, 0.47 mmol, 74% yield). LC/MS (Table B, Method ff) Rt = 1.96 min; MS m/z: 491.0 (M+H)+; 1H NMR (400 MHz,

DMSO-d6) δ 8.78 – 8.69 (m, 1H), 8.65 – 8.57 (m, 1H), 8.44 (d, J = 1.0 Hz, 1H), 8.14 – 8.08 (m, 1H), 8.03 – 7.99 (m, 1H), 7.97 (s, 1H), 7.88 – 7.84 (m, 1H), 7.76 (s, 1H), 7.73 – 7.69 (m, 1H), 7.35 – 7.28 (m, 2H), 7.27 – 7.21 (m, 1H), 7.19 – 7.12 (m, 1H), 7.03 (br d, J = 7.5 Hz, 1H), 4.80 – 4.73 (m, 1H), 4.52 – 4.45 (m, 1H), 3.84 – 3.76 (m, 1H), 3.66 (br d, J = 13.5 Hz, 1H), 3.33 (br dd, J = 9.5, 13.5 Hz, 1H), 3.27 – 3.11 (m, 1H), 3.08 – 3.00 (m, 1H), 2.97 (s, 1H), 2.95 (br s, 1H), 2.92 (s, 2H), 2.90 – 2.85 (m, 1H), 2.79 – 2.69 (m, 1H), 2.07 (s, 1H), 1.78 (s, 1H), 1.74 (s, 1H).

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References

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Bulevirtide-gmod

May 27, 2026 2:32 am / Leave a comment


Bulevirtide-gmod

CAS 2012558-47-1.

MF C248H355N65O72 MW 5399 g/mol

FDA 2026, APPROVALS 2026, 5/22/2026, Hepcludex, WKM56H3TLB

To treat chronic hepatitis delta virus infection in adults without cirrhosis or with compensated cirrhosis


N-myristoyl-glycyl-L-threonyl-L-asparagyl-L-leucyl-L-seryl-L-valyl-L-prolyl-L-asparagyl-L-prolyl-L-leucyl-glycyl-L-phenylalanyl-L-phenylalanyl-L-prolyl-L-alpha-aspartyl-L-histidyl-L-glutaminyl-L-leucyl-L-alpha-aspartyl-L-prolyl-L-alanyl-L-phenylalanyl-glycyl-L-alanyl-L-asparagyl-L-seryl-L-asparagyl-L-asparagyl-L-prolyl-L-alpha-aspartyl-L-tryptophyl-L-alpha-aspartyl-L-phenylalanyl-L-asparagyl-L-prolyl-L-asparagyl-L-lysyl-L-alpha-aspartyl-L-histidyl-L-tryptophyl-L-prolyl-L-alpha-glutamyl-L-alanyl-L-asparagyl-L-lysyl-L-valyl-glycinamide

(4S)-4-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-4-amino-2-[[(2S)-1-[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-4-amino-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-1-[(2S)-4-amino-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S,3R)-3-hydroxy-2-[[2-(tetradecanoylamino)acetyl]amino]butanoyl]amino]-4-oxobutanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]-3-methylbutanoyl]pyrrolidine-2-carbonyl]amino]-4-oxobutanoyl]pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-phenylpropanoyl]pyrrolidine-2-carbonyl]amino]-3-carboxypropanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-5-oxopentanoyl]amino]-4-methylpentanoyl]amino]-3-carboxypropanoyl]pyrrolidine-2-carbonyl]amino]propanoyl]amino]-3-phenylpropanoyl]amino]acetyl]amino]propanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-4-oxobutanoyl]amino]-4-oxobutanoyl]pyrrolidine-2-carbonyl]amino]-3-carboxypropanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-carboxypropanoyl]amino]-3-phenylpropanoyl]amino]-4-oxobutanoyl]pyrrolidine-2-carbonyl]amino]-4-oxobutanoyl]amino]hexanoyl]amino]-3-carboxypropanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]pyrrolidine-2-carbonyl]amino]-5-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-oxopentanoic acid

Bulevirtide-gmod, sold under the brand name Hepcludex, is the first and only FDA-approved medication for treating chronic hepatitis delta virus (HDV) infection in adults. Developed by Gilead Sciences, it received accelerated approval from the U.S. Food and Drug Administration (FDA) on May 22, 2026, filling a critical gap for patients with this severe viral liver disease.

Indication and Clinical Use

  • Target Patient Profile: Approved for adults with chronic HDV who have compensated cirrhosis or no cirrhosis.
  • The Clinical Need: HDV only occurs as a co-infection in individuals who already have Hepatitis B (HBV). It is considered the most aggressive form of viral hepatitis, often accelerating liver scarring (fibrosis), liver failure, and liver cancer.
  • Basis of Approval: The FDA granted accelerated approval based on Phase 3 MYR301 study data, which demonstrated a significant reduction in viral HDV RNA and the normalization of alanine aminotransferase (ALT) liver enzymes.

Mechanism of Action

Bulevirtide-gmod is a first-in-class entry inhibitor. It works by binding to and blocking the sodium taurocholate co-transporting polypeptide (NTCP) receptor on liver cells. Because HDV and HBV rely on this specific receptor to enter hepatocytes, the drug successfully disrupts the viral life cycle and prevents the virus from spreading to healthy liver cells.

Dosage and Administration

  • Form: Supplied as a lyophilized powder for injection.
  • Dose: The recommended dose is 8.5 mg once daily.
  • Administration: Delivered via subcutaneous injection (under the skin).

Safety and Side Effects

  • Boxed Warning: The drug carries a prominent warning regarding the risk of severe acute exacerbations of hepatitis D and B if treatment is discontinued. Stopping the medication can cause severe, life-threatening viral flares, requiring close medical monitoring for at least 6 months post-treatment.
  • Common Side Effects: The most frequent adverse reactions of patients) include:
    • Injection site reactions
    • Headache
    • Abdominal pain
    • Fatigue
    • Pruritus (itching)

Bulevirtide, sold under the brand name Hepcludex, is an antiviral medication used for the treatment of chronic hepatitis D (in the presence of hepatitis B).[8]

The most common side effects include raised levels of bile salts in the blood and reactions at the site of injection.[8]

Bulevirtide works by attaching to and blocking a receptor (target) through which the hepatitis delta and hepatitis B viruses enter liver cells.[8] By blocking the entry of the virus into the cells, it limits the ability of HDV to replicate and its effects in the body, reducing symptoms of the disease.[8]

Bulevirtide was approved for medical use in the European Union in July 2020,[8] and in Canada in August 2025.[5]

Medical uses

Bulevirtide is indicated for the treatment of chronic hepatitis delta virus (HDV) infection in plasma (or serum) HDV-RNA positive adult patients with compensated liver disease.[8][10]

Pharmacology

Mechanism of action

Bulevirtide binds and inactivates the sodium/bile acid cotransporter, blocking both hepatitis B and hepatitis D viruses from entering hepatocytes.[11]

The hepatitis B virus uses its surface lipopeptide pre-S1 for docking to mature liver cells via their sodium/bile acid cotransporter (NTCP) and subsequently entering the cells. Myrcludex B is a synthetic N-acylated pre-S1[12][13] that can also dock to NTCP, blocking the virus’s entry mechanism.[14]

Bulevirtide is also effective against hepatitis D because the hepatitis D virus uses the same entry receptor as the hepatitis B virus and is only effective in the presence of a hepatitis B virus infection.[14]

Pre-clinical data in mice suggests that pharmacological inhibition of NTCP-mediated bile salt uptake may also be effective to lower hepatic bile salt accumulation in cholestatic conditions. This reduces hepatocellular damage.[15] An increased ratio of phospholipid to bile salts seen in bile upon NTCP inhibition may further contribute to the protective effect as bile salts are less toxic in presence of phospholipids.[16]

Structural formula

Bulevirtide is a 47-amino acid peptide with the following sequence:[17]

CH3(CH2)12CO–Gly–Thr–Asn–Leu–Ser–Val–Pro-Asn-Pro-Leu-Gly-Phe-Phe-Pro-Asp–His–Gln-Leu-Asp-Pro-Ala-Phe-Gly-Ala-Asn-Ser-Asn-Asn-Pro-Asp-Trp-Asp-Phe-Asn-Pro-Asn-Lys-Asp-His-Trp-Pro-Glu-Ala-Asn-Lys-Val-Gly-NH2 (C13H27CO-GTNLSVPNPLGFFPDHQLDPAFGANSNNPDWDFNPNKDHWPEANKVG-NH2)

SYN

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2024073572&_cid=P11-MPNG4J-82875-1

PATENTS

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References

References

  1.  Deterding K, Wedemeyer H (2019). “Beyond Pegylated Interferon-Alpha: New Treatments for Hepatitis Delta”. AIDS Reviews. 21 (3): 126–134. doi:10.24875/AIDSRev.19000080. PMID 31532397. S2CID 202674681.
  2.  “Hepcludex (bulevirtide acetate)”. Therapeutic Goods Administration (TGA). 12 August 2024. Retrieved 12 October 2024.
  3.  “Therapeutic Goods (Poisons Standard—June 2024) Instrument 2024”. Federal Register of Legislation. 30 May 2024. Retrieved 10 June 2024.
  4.  “Hepcludex (Gilead Sciences Pty Ltd)”. Therapeutic Goods Administration (TGA). 13 September 2024. Retrieved 15 September 2024.
  5.  “Hepcludex Product information”. Health Canada. 8 August 2025. Retrieved 20 August 2025.
  6.  “Summary Basis of Decision for Hepcludex”. Drug and Health Products Portal. 29 September 2025. Retrieved 12 October 2025.
  7.  “Hepcludex 2 mg powder for solution for injection – Summary of Product Characteristics (SmPC)”. (emc). 30 March 2022. Retrieved 1 July 2022.
  8.  “Hepcludex EPAR”. European Medicines Agency (EMA). 26 May 2020. Retrieved 12 August 2020. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  9.  “Hepcludex Product information”. Union Register of medicinal products. Retrieved 3 March 2023.
  10.  “Summary of opinion: Hepcludex” (PDF). European Medicines Agency (EMA). 28 May 2020.
  11.  Francisco EM (29 May 2020). “Hepcludex”. European Medicines Agency (EMA). Archived from the original on 15 June 2020. Retrieved 6 August 2020.
  12.  Volz T, Allweiss L, Ben MBarek M, Warlich M, Lohse AW, Pollok JM, et al. (May 2013). “The entry inhibitor Myrcludex-B efficiently blocks intrahepatic virus spreading in humanized mice previously infected with hepatitis B virus”. Journal of Hepatology. 58 (5): 861–867. doi:10.1016/j.jhep.2012.12.008. PMID 23246506.
  13.  Abbas Z, Abbas M (August 2015). “Management of hepatitis delta: Need for novel therapeutic options”. World Journal of Gastroenterology. 21 (32): 9461–9465. doi:10.3748/wjg.v21.i32.9461. PMC 4548107. PMID 26327754.
  14.  Spreitzer H (14 September 2015). “Neue Wirkstoffe – Myrcludex B”. Österreichische Apothekerzeitung (in German) (19/2015): 12.
  15.  Na+ -taurocholate cotransporting polypeptide inhibition has hepatoprotective effects in cholestasis in mice. Slijepcevic D, Roscam Abbing RLP, Fuchs CD, Haazen LCM, Beuers U, Trauner M, Oude Elferink RPJ, van de Graaf SFJ. Hepatology. 2018 Sep;68(3):1057-1069. doi: 10.1002/hep.29888
  16.  Roscam Abbing RL, Slijepcevic D, Donkers JM, Havinga R, Duijst S, Paulusma CC, et al. (January 2020). “Blocking Sodium-Taurocholate Cotransporting Polypeptide Stimulates Biliary Cholesterol and Phospholipid Secretion in Mice”. Hepatology. 71 (1): 247–258. doi:10.1002/hep.30792. PMC 7003915. PMID 31136002.
  17.  Sauter M, Blank A, Stoll F, Lutz N, Haefeli WE, Burhenne J (September 2021). “Intact plasma quantification of the large therapeutic lipopeptide bulevirtide”. Analytical and Bioanalytical Chemistry. 413 (22): 5645–5654. doi:10.1007/s00216-021-03384-7. PMC 8410713. PMID 34018034.
Clinical data
Pronunciation/bjuːˈlɛvɪrtaɪd/
byoo-LEH-vir-tyde
Trade namesHepcludex
Other namesMyrB, Myrcludex-B[1]
License dataUS DailyMed: Bulevirtide
Pregnancy
category		AU: B1[2]
Routes of
administration		Subcutaneous
ATC codeJ05AX28 (WHO)
Legal status
Legal statusAU: S4 (Prescription only)[3][4][2]CA: ℞-only[5][6]UK: POM (Prescription only)[7]EU: Rx-only[8][9]
Identifiers
CAS Number2012558-47-1
DrugBankDB15248
ChemSpider129157549
UNIIWKM56H3TLB
KEGGD11877as salt: D11878
ChEMBLChEMBL4297711
Chemical and physical data
FormulaC248H355N65O72
Molar mass5398.951 g·mol−1
3D model (JSmol)Interactive image
SMILES
InChI

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Flormotridazum (18F)

May 26, 2026 2:29 am / Leave a comment


Flormotridazum (18F)

CAS 2798832-03-6

MF C23H29Cl18FN5O4 MW492.961

2-tert-butyl-4-chloro-5-[(3-{[4-({2-[2-(18F)fluoroethoxy]ethoxy}methyl)-1H-1,2,3-triazol-1-yl]methyl}phenyl)methoxy]pyridazin-3(2H)-one

3(2H)-Pyridazinone, 4-chloro-2-(1,1-dimethylethyl)-5-[[3-[[4-[[2-[2-(fluoro-18F)ethoxy]ethoxy]methyl]-1H-1,2,3-triazol-1-yl]methyl]phenyl]methoxy]-

2-tert-butyl-4-chloro-5-[(3-{[4-({2-[2-(18F)fluoroethoxy]ethoxy}methyl)-1H-1,2,3-triazol-1-yl]methyl}phenyl)methoxy]pyridazin-3(2H)-one

imaging agent, 7AR6ZH8YUU

Flormotridaz (18F) (also referred to by its International Nonproprietary Name, flormotridazum) is an advanced radiopharmaceutical compound utilized in nuclear medicine. It is specifically engineered as a radioactive diagnostic tracer containing the fluorine-18 positron-emitting isotope.

Core Characteristics & Chemical Profile

  • Substance Classification: Radioactive Diagnostic Agent / Small Molecule.
  • Mechanism Basis: It shares core structural similarities and structural lineage with pyridazinone-based mitochondrial complex 1 (MC-1) inhibitors, heavily linking its functionality to target-specific tissues with high metabolic or mitochondrial activity.

Mechanism and Clinical Application

Like related fluorine-18 labeled pyridazinone analogues, this agent is designed for Positron Emission Tomography (PET) imaging workflows. [1]

  1. Administration: The agent is administered intravenously as a sterile unit dose before scanning.
  2. Cellular Targeting: It binds selectively to specific intracellular molecular targets (such as mitochondrial pathways) within highly active tissues.
  3. PET Imaging: As the Fluorine-18 radioisotope decays, it emits positrons. These positrons encounter electrons to produce gamma rays, which the PET scanner captures to map high-resolution, three-dimensional metabolic layouts of internal organ systems.

Contextual Comparison

In clinical nuclear medicine, molecular tracers tagged with Fluorine-18 offer significant clinical benefits over older Single-Photon Emission Computed Tomography (SPECT) agents. Their 110-minute half-life allows them to be manufactured at centralized cyclotron facilities and distributed directly to regional medical centres as ready-to-use unit doses, eliminating the need for an on-site cyclotron

Flormotridaz (\(^{18}\text{F}\)):

  1. CN112807276B: “Preparation method and application of a pyridazinone myocardial perfusion PET radiopharmaceutical” (Covers the definitive radiosynthesis scheme).
  2. CN115947775A: “Method for preparing compound (I), compound (I), and uses thereof”.
  3. WO2024008073A1 / CN114832118B: “Compound I liquid composition, preparation method and use thereof” (Covers final formulation stabilization utilizing vitamin C and gentisic acid)

PAT

https://patents.google.com/patent/WO2024008073A1/zh

Compound I, chemically named 2-tert-butyl-4-chloro-5-((3-((4-((2-(2-fluoro[ 18F ]ethoxy)ethoxy)methyl)-1H-1,2,3-triazol-1-yl)methyl)benzyl)oxy)pyridazine-3(2H)-one. Chemical structural formula:Molecular formula : C₂₃H₂₉Cl₁₈FN₅O₄​

​Molecular weight: 492.97The mechanism of action of compound I as a myocardial perfusion PET imaging agent: Once compound I enters cardiomyocytes, it can rapidly interact with respiratory chain complex I (MC-I) in mitochondria and remain in the myocardium for a long time. Preliminary animal studies showed that it has high cardiac uptake and low hepatic uptake 15 minutes after injection, and maintains a good heart-liver ratio 60 minutes after injection, showing good potential for myocardial perfusion imaging.In this application, Compound I liquid composition or Compound I is used as a myocardial perfusion PET imaging agent.Precursor of Compound I: Chemical name is methyl 2-(2-((1-(3-(((1-(tert-butyl)-5-chloro-6-oxo-1,6-dihydropyridazin-4-yl)oxy)methyl)benzyl)-1H-1,2,3-triazol-4-yl)methoxy)ethoxy)ethyl-4-methylbenzenesulfonate, chemical structural formula is:Molecular formula : C30H36ClN5O7S

​Molecular weight: 646.16Amino polyethers (K222 ) are tribridged crown ether molecules with cavitary structures, and are typical nitrogen-containing cavitary ethers, belonging to the category of cavitary ethers. Due to their unique coordination properties, nitrogen-containing cavitary ethers can effectively and selectively complex transition metal and heavy metal cations, forming more stable complexes. Furthermore, they possess both lipophilic and hydrophilic properties, thus showing promising research potential.In existing technologies, the classic synthetic method for amino polyether (K 

​​222 ) is the highly diluted method proposed by Lehn et al., which is a typical non-template ion synthesis method. The specific steps involve dissolving the starting materials 1,8-diamino-3,6-dioxane and 1,8-diacyl chloride-3,6-dioxane in a large amount of benzene solvent and heating the reaction for 8 hours. Then, a reduction reaction with lithium aluminum hydride is performed for 24 hours, followed by column chromatography separation and recrystallization to obtain amino polyether (K 

​​222 ). This method requires a large amount of solvent, such as benzene, has a long synthetic route, is complex, has a low yield, and is not economically efficient. Besides the highly diluted method, another classic synthetic method for amino polyether (K​​222 ) is proposed by Kulstad and Malmsten, which uses Na 2CO 3 

as a template to obtain a sodium iodide complex of amino polyether (K ​​222 ) in acetonitrile , and then decomplexes it using a resin to obtain amino polyether (K ​​222 ). The specific steps are as follows: 1,2-bis(2-iodoethoxy)ethane and benzylamine are refluxed in acetonitrile solution for 3 days. An intermediate is then obtained through post-processing. This intermediate is recrystallized from acetone and filtered to obtain a NaI complex. This complex is then decomplexed under acidic conditions using cation exchange resins and anion exchange resins to prepare amino polyether (K222 ) . This method uses simple equipment, requires little solvent, and has relatively mild reaction conditions. However, the applicant has found that the decomplexing method using ion exchange resins fails to proceed when the sodium ion content decreases to a certain level, resulting in a low yield.

PAT

https://patents.google.com/patent/CN114773179B/en

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References

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Florensocatib

May 25, 2026 2:27 am / Leave a comment


Florensocatib

CAS 2762114-61-2

MF C23H23FN4O4 MW438.5 g/mol

(2S)-N-[(1S)-1-cyano-2-[2-fluoro-4-(3-methyl-2-oxo-1,3-benzoxazol-5-yl)phenyl]ethyl]-1,4-oxazepane-2-carboxamide

(2S)-N-{(1S)-1-cyano-2-[2-fluoro-4-(3-methyl-2-oxo-2,3-dihydro1,3-benzoxazol-5-yl)phenyl]ethyl}-1,4-oxazepane-2-
carboxamide
cathepsin inhibitor, HSK 31858, CHF 10196, DPP1-IN-1, RWC743JRK7

Florensocatib (originally designated as HSK31858 or CHF10196) is an investigative, highly potent, oral reversible inhibitor of dipeptidyl peptidase 1 (DPP1). It is being actively researched for its ability to reduce the frequency of pulmonary exacerbations in adults suffering from inflammatory respiratory diseases like bronchiectasis

Mechanism of Action

DPP1 (also known as cathepsin C) is a lysosomal protease enzyme responsible for activating neutrophil serine proteases (NSPs). In conditions like non-cystic fibrosis bronchiectasis, hyperactive neutrophils accumulate in the airways, causing severe tissue damage, chronic inflammation, and airway widening.

By inhibiting DPP1, florensocatib prevents the activation of these damaging enzymes, effectively targeting the primary driver of neutrophilic inflammation in the lungs.

Clinical Development & Trial Progress

Florensocatib is undergoing global evaluation across multiple advanced clinical trials:

  • The SAVE-BE Trial: An earlier clinical phase where the drug demonstrated high potency and favorable efficacy profiles in treating inflammatory lung conditions.
  • The HOPE-BE Trial: A definitive Phase III protocol launched to evaluate the long-term safety and overall reduction of pulmonary exacerbation frequencies specifically among Chinese adults.
  • Global Phase III Status: According to records on ClinicalTrials.gov, randomised, double-blind trials are evaluating the drug against a placebo in participants aged 12 to 85 for treatment windows stretching up to 78 weeks.

SYN

US11807635,

https://patentscope.wipo.int/search/en/detail.jsf?docId=US395653715&_cid=P21-MPKKTA-33002-1

Example 1: (S)—N—((S)-1-cyano-2-(2-fluoro-4-(3-methyl-2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)phenyl)ethyl)-1,4-oxazepane-2-carboxamide (Compound 1)

Step 4: (S)—N—((S)-1-cyano-2-(2-fluoro-4-(3-methyl-2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)phenyl)ethyl)-1,4-oxazepane-2-carboxamide (Compound 1)

      1D (0.32 g, 0.59 mmol) was dissolved in formic acid (2.5 mL) and upon completion of the addition, the mixture was reacted at 50° C. for 10 min. The reaction solution was concentrated to dryness and ethyl acetate (20 mL) was added. Then saturated aqueous sodium bicarbonate solution was added dropwise to adjust the pH to about 8. The organic layer was separated and the remaining aqueous layer was extracted with ethyl acetate (25 mL×3). The organic phases were combined, dried over anhydrous sodium sulfate, filtered and concentrated, and the residue was separated and purified by silica gel column chromatography (dichloromethane:methanol (v/v)=20:1) to obtain the title compound 1 (0.15 g, 58.0%). LC-MS (ESI): m/z=439.1 [M+H] +.
       1H NMR (400 MHz, CDCl 3) δ 7.43-7.22 (m, 5H), 7.12 (d, 1H), 5.19 (dd, 1H), 4.18-4.04 (m, 1H), 4.05-3.95 (m, 1H), 3.78 (m, 1H), 3.46 (s, 3H), 3.41-3.17 (m, 3H), 3.03-2.87 (m, 3H), 1.88 (m, 2H).

SYN

US11807635,

https://patentscope.wipo.int/search/en/detail.jsf?docId=US395653715&_cid=P21-MPKKYT-35548-1

PAT

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2022042591&_cid=P21-MPKKS9-32509-1

(S)-N-((S)-1-cyano-2-(2-fluoro-4-(3-methyl-2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)phenyl)ethyl)-1,4-oxazepane-2-carboxamide(compound 1)

Step 4: (S)-N-((S)-1-cyano-2-(2-fluoro-4-(3-methyl-2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)phenyl)ethyl)-1,4-oxazacycloheptane-2-carboxamide (Compound 1) 

[0360]

(S)-N-((S)-1-cyano-2-(2-fluoro-4-(3-methyl-2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)phenyl)ethyl)-1,4-oxazepane-2-carboxamide(compound 1)

[0361]1D (0.32 g, 0.59 mmol) was dissolved in formic acid (2.5 mL), and the mixture was reacted at 50 °C for 10 min after the addition was complete. The solution was concentrated to dryness, and ethyl acetate (20 mL) was added. The pH was adjusted to approximately 8 by dropwise addition of saturated sodium bicarbonate solution. The organic layer was separated and extracted with ethyl acetate (25 mL × 3). The organic phases were combined, dried over anhydrous sodium sulfate, filtered, concentrated, and the residue was purified by silica gel column chromatography (dichloromethane:methanol (v/v) = 20:1) to give title compound 1 (0.15 g, 58.0%). LC-MS (ESI): m/z = 439.1 [M+H] + . 

[0362]

1H NMR(400MHz,CDCl 3)δ7.43–7.22(m,5H),7.12(d,1H),5.19(dd,1H),4.18–4.04(m,1H),4.05–3.95(m,1H),3.78(m,1H),3.46(s,3H),3.41–3.17(m,3H),3.03–2.87(m,3H),1.88(m,2H).

ADVT

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References

/////////florensocatib, anax labs, cathepsin inhibitor, HSK 31858, CHF 10196, DPP1-IN-1, RWC743JRK7

Florcicaper (18F)

May 24, 2026 2:34 am / Leave a comment


Florcicaper (18F)

CAS 855927-17-2

MF C18H3318FO2, MW 299.4544

2-[(1S,2R)-2-(5-(18F)fluorotridecyl)cyclopropyl]acetic acid

2-((1S,2R)-2-(5-(FLUORO-18F)TRIDECYL)CYCLOPROPYL)ACETIC ACID
TRANS-9(RS)-18F-FLUORO-3,4(RS,RS)-METHYLENEHEPTADECANOIC ACID

rac-{(1R,2S)-2-[(5RS)-5-(18F)fluorotridecyl]cyclopropyl}aceticacid
imaging agent, CARDIOPET, (18F FCPHA), FDG79C95XB

CardioPET is: An F-18 labeled, modified fatty acid that provides insight into regions with decreased blood flow or metabolic insufficiency in the myocardium.; CardioPET may be used to: Identify patients that will benefit from PCI or revascularization and guide intervention, Assess myocardial viability, Evaluate CAD in patients that cannot exercise.; Agent: Muscle State Imaging Agent, Type: Fatty Acid (Labeled with Fluorine 18), Condition: Coronary Artery Disease, Status: completed enrollment.;This imaging agent exploits the dietary needs of the heart as it relates to glucose and fatty acids. By introducing a radio-labeled analog to the natural fatty acids utilized as an energy source by the heart we can visualize the anatomic location and state of the muscle within the areas defined by the specific coronary artery blood flow distribution and detect problems in advance of symptoms that would lead to a stress test.

Cardiopet is under investigation in clinical trial NCT01826773 (Cardiopet as PET Imaging Agent to Assess Myocardial Perfusion and Fatty Acid Uptake in Known or Suspected CAD Subjects).

A Phase I Study in Healthy Volunteers to Evaluate the Safety of CardioPET™ in Detection of Coronary Artery Disease

CTID: NCT00413647

Phase: Phase 1

Status: Completed

Date: 2013-06-12

PATENTS

CA-2876139-A1
CN-104684546-A
CN-114736112-A
CN-115141087-A
CN-115141087-B
CN-115141125-A
CN-115141125-B
CN-115181013-A
CN-115181013-B
CN-115850224-A
CN-115850224-B
CN-115959978-A
CN-115959978-B
CN-116041169-A
CN-116199658-A
CN-116217356-A
EP-2858630-A1
EP-4133284-A1
US-10533059-B2
US-11701429-B2
US-2015361110-A1
US-2017014528-A1
US-2020199249-A1
US-2020297854-A1
US-20230314449-A1
US-20230381092-A1
US-9409927-B2
WO-2013185032-A1
WO-2022082327-A1
WO-2023085674-A1
WO-2023236978-A1
WO-2023237092-A1

PAT

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2013185032&_cid=P11-MPJ5UV-89230-1

PAT

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2022082327&_cid=P11-MPJ5WJ-90048-1

ADVT

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References

//////////florcicaper (18F), anax labs, imaging agent, CARDIOPET, (18F FCPHA), FDG79C95XB

Fexlamose

May 23, 2026 2:42 am / Leave a comment


Fexlamose

CAS 1285607-08-0

MFC12H22O9S2 MW374.4 g/mol

(2S,3S,4S,5R,6R)-2-(sulfanylmethyl)-6-[(2R,3R,4S,5S,6S)-3,4,5-trihydroxy-6-(sulfanylmethyl)oxan-2-yl]oxyoxane-3,4,5-triol

6-thio-α-D-glucopyranosyl 6-thio-α-D-glucopyranoside; 6,6′-dithiotrehalose
mucolytic, AER-01, AER 01, VY9GAK6EVR, MUC-031, MUC031

Fexlamose (formerly known as AER-01) is an experimental inhaled small-molecule drug developed by Aer Therapeutics to treat muco-obstructive lung diseases like COPD (Chronic Obstructive Pulmonary Disease) and asthma. It is a thiol-modified carbohydrate designed to break down mucus plugs in the airways

How it Works

  • Mechanism: Fexlamose acts as a mucolytic by cleaving the disulfide bonds in mucus, thinning the thick secretions that block airways.
  • The Problem It Targets: While many respiratory drugs manage inflammation or relax airway muscles, currently no approved treatments directly tackle mucus plugs, which are a major cause of breathing difficulties in COPD.
  • Delivery: It is administered as an inhalation solution (or potentially a dry powder) directly into the lungs.
  • Current Clinical Status
  • Fexlamose is an investigational drug and is not yet approved for public use or commercial prescription.
  • Clinical Trials: It is undergoing Phase 2a clinical studies (such as the AER-01-002 trial) to evaluate its safety, tolerability, and efficacy in adults with moderate to severe COPD.
  • Study Design: These trials utilize specialized CT mucus plug scoring to identify patients who are most likely to benefit from the therapy.

SYN

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2017197360&_cid=P10-MPHQBA-11926-1

Syn

US-20230172885-A1

https://patentscope.wipo.int/search/en/detail.jsf?docId=US399239351&_cid=P10-MPHQQF-20898-1

Syn

US-20230181607-A1

https://patentscope.wipo.int/search/en/detail.jsf?docId=US399582635&_cid=P10-MPHQRV-21687-1

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References

//////////fexlamose, ANAX LABS, mucolytic, AER-01, AER 01, VY9GAK6EVR, MUC-031, MUC031

Famlasertib

May 22, 2026 2:29 am / Leave a comment


Famlasertib

CAS 2375591-69-6

MFC26H27ClN4O MW 447.0 g/mol

4-[[4-[3-(3-Chlorophenyl)-1H-pyrrolo[2,3-b]pyridin-5-yl]phenyl]methyl]-1-piperazineethanol

2-[4-({4-[3-(3-chlorophenyl)-1H-pyrrolo[2,3-b]pyridin-5-yl]phenyl}methyl)piperazin-1-yl]ethan-1-ol
serine/threonine kinase inhibitor, amyotrophic lateral sclerosis, Prosetin, WJP32276AY


Prosetin is an orally administered blocker of MAP4K under investigation for the treatment of amyotrophic lateral sclerosis.

Famlasertib (also known as Prosetin or Prostetin/12k) is a highly potent, small-molecule inhibitor targeting the mitogen-activated protein kinase kinase kinase kinase (MAP4K) family. It is an experimental drug primarily under investigation for its neuroprotective capabilities in treating neurodegenerative disorders like amyotrophic lateral sclerosis (ALS) and as an anti-invasive agent in certain cancers

  • Target Pathways: MAP4K4 (HGK), MLK1, and MLK3
  • Key Properties: Orally active, blood-brain barrier penetrant (CNS-penetrant)

Mechanism of Action

Famlasertib functions by blocking the activation of the MAP4K protein family, specifically demonstrating powerful inhibitory values (\(\text{IC}_{50}\)) against subfamilies like HGK (MAP4K4), MLK3, and MLK1. By inhibiting these kinases, the compound: [1]

  • Reduces Endoplasmic Reticulum (ER) Stress: It helps mitigate the unfolded protein response that triggers programmed cell death in neurons affected by misfolded protein accumulation.
  • Suppresses Inflammation: It blocks inflammatory pathways associated with neurodegeneration and cell damage.
  • Restrains Cell Motility: In oncology contexts, it disrupts kinase signaling linked to actin cytoskeleton remodeling, preventing malignant cells from migrating.

Primary Areas of Research

1. Amyotrophic Lateral Sclerosis (ALS)

In motor neuron models of ALS, cellular stress frequently triggers neurodegeneration. Because famlasertib easily passes through the blood-brain barrier, it is capable of directly shielding motor neurons from ER-stress-mediated cell death, extending cell viability in laboratory models.

2. Oncology (Medulloblastoma)

Recent findings published on bioRxiv indicate that famlasertib acts as a “migrastatic” agent in medulloblastoma (a type of pediatric brain tumor). It suppresses the highly invasive behavior and single-cell motility of tumor cells without exhibiting developmental toxicity.

SYN

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2020163594&_cid=P21-MPGALG-31359-1

PAT

https://patentscope.wipo.int/search/en/detail.jsf?docId=US317630245&_cid=P21-MPGALG-31359-1

Preparation of 2-(4-(4-(3-(3-Chlorophenyl)-1H-pyrrolo[2,3-b]pyridin-5-yl)benzyl)piperazin-1-yl)ethan-1-ol (Compound 12k)

Following the general procedure described above, with 4-(3-(3-chlorophenyl)-1-tosyl-1H-pyrrolo[2,3-b]pyridin-5-yl)benzaldehyde (10c, 418 mg, 0.86 mmol) and 1-(2-hydroxyethyl)piperazine (224 mg, 211 μL, 1.72 mmol, 2.0 eq) as the starting materials, 2-(4-(4-(3-(3-chlorophenyl)-1H-pyrrolo[2,3-b]pyridin-5-yl)benzyl)piperazin-1-yl)ethan-1-ol (12k) was isolated as an off-white solid (139.9 mg, 36% yield over two steps). 1H NMR (400 MHz, Methanol-d 4) δ 8.57 (d, J=2.0 Hz, 1H), 8.54 (d, J=2.0 Hz, 1H), 7.80 (s, 1H), 7.76 (d, J=8.3 Hz, 2H), 7.65 (t, J=1.9 Hz, 1H), 7.64-7.57 (m, 3H), 7.42 (t, J=7.9 Hz, 1H), 7.29 (ddd, J=8.0, 2.1, 1.0 Hz, 1H), 4.27 (s, 2H), 3.93-3.86 (m, 2H), 3.62 (s, 4H), 3.41 (s, 4H), 3.35-3.31 (m, 2H) ppm. HRMS (APCI +, m/z): calcd. for C 26H 28N 40Cl [M+H +]: 447.1952, found: 447.1954.

SYN

https://patentscope.wipo.int/search/en/detail.jsf?docId=US469942811&_cid=P21-MPGAUU-39605-1

ADVT

ANAX LABORATORIES

WEBSITE https://www.anaxlab.com/

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SEE MORE………Integrated Solutions, Manufacturing Solutions, Products,
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Phone : +91 897704 2010 /  +91 9177075735, Email : info@anaxlab.com

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References

PAT

///////famlasertib, serine/threonine kinase inhibitor, amyotrophic lateral sclerosis, Prosetin, WJP32276AY

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