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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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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

POLIDOCANOL

November 3, 2021 2:41 am / Leave a comment


Polidocanol skeletal.svg
Molecular Structure of 3055-99-0 (3,6,9,12,15,18,21,24,27-Nonaoxanonatriacontan-1-ol)

POLIDOCANOL

Synonym: Polidocanol; C12E9, Dodecyl nonaethylene glycol ether, Dodecylnonaglycol, Polidocanol, Polyoxyethylene (9) lauryl ether; trade names: Asclera, Aethoxysklerol and Varithena; Laureth-9; Dodecylnonaoxyethylene glycol monoether

IUPAC/Chemical Name: 3,6,9,12,15,18,21,24,27-nonaoxanonatriacontan-1-ol

3055-99-0
Chemical Formula: C30H62O10
Exact Mass: 582.4343Polidocanol 
CAS Registry Number: 9002-92-0 
CAS Name: a-Dodecyl-w-hydroxypoly(oxy-1,2-ethanediyl) 
Additional Names: polyethylene glycol (9) monododecyl ether; dodecyl alcohol polyoxyethylene ether; hydroxypolyethoxydodecane; laureth 9; polyoxyethylene lauryl ether 
Trademarks: Aethoxysklerol (Kreussler); Aetoxisclerol (Dexo); Atlas G-4829 (ICI); Hetoxol L-9 (Heterene Chem.)Line Formula: C12H25(OCH2CH2)nOH 
Literature References: Contains an average of nine ethylene oxide units and has an average mol wt ~600. Prepd by reaction of ethylene oxide and dodecyl alcohol: Pertsemlides, Soehring, Arzneim.-Forsch.10, 990 (1960). Toxicology: H. S. Zipf et al.,ibid.7, 162 (1957). Review of clinical experience: P. M. Goldman, J. Dermatol. Surg. Oncol.15, 204-209 (1989). 
Properties: Sol in water, ethanol, toluene. Miscible with hot mineral, natural and synthetic oils; with fats and fatty alcohols. LD50 in mice (mg/kg): 1170 orally, 125 i.v. (Zipf). 
Toxicity data: LD50 in mice (mg/kg): 1170 orally, 125 i.v. (Zipf) 
Use: Solvent; nonionic emulsifier; pharmaceutic aid (surfactant); spermaticide. 
Therap-Cat: Anesthetic (topical); antipruritic; sclerosing agent. 
Keywords: Anesthetic (Local); Antipruritic; Sclerosing Agent.

EINECS221-284-4
CAS No.3055-99-0Density1.007 g/cm3
PSA103.30000LogP4.04900
Solubility Melting Point33-36 °C
FormulaC30H62O10Boiling Point615.857 °C at 760 mmHg
Molecular Weight582.43Flash Point326.259 °C

Polidocanol is a local anaesthetic and antipruritic component of ointments and bath additives. It relieves itching caused by eczema and dry skin.[1] It has also been used to treat varicose veins,[2] hemangiomas, and vascular malformations.[3] It is formed by the ethoxylation of dodecanol.

Polidocanol is a local anaesthetic and antipruritic component of ointments and bath additives. It relieves itching caused by eczema and dry skin. It is formed by the ethoxylation of dodecanol. The substance is also used as a sclerosant, an irritant injected to treat varicose veins, under the trade names Asclera, Aethoxysklerol and Varithena. Polidocanol causes fibrosis inside varicose veins, occluding the lumen of the vessel, and reducing the appearance of the varicosity. The FDA has approved polidocanol injections for the treatment of small varicose (less than 1 mm in diameter) and reticular veins (1 to 3 mm in diameter). Polidocanol works by damaging the cell lining of blood vessels, causing them to close and eventually be replaced by other types of tissue.

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Yu, Zeqiong; Bo, Shaowei; Wang, Huiyuan; Li, Yu; Yang, Zhigang; Huang, Yongzhuo; Jiang, Zhong-Xing. Application of Monodisperse PEGs in Pharmaceutics: Monodisperse Polidocanols. Molecular Pharmaceutics. Volume 14. Issue 10. Pages 3473-3479. 2017.

SYN 2

Jiang, Zhongxing; Yu, Zeqiong. Process for preparation of monodisperse nona-polyethylene glycol dodecyl alcohol monoether and sulfate. Assignee Wuhan University, Peop. Rep. China. CN 106316802. (2017).

Sclerotherapy

Polidocanol is also used as a sclerosant, an irritant injected to treat varicose veins, under the trade names Asclera, Aethoxysklerol[4] and Varithena.[5] Polidocanol causes fibrosis inside varicose veins, occluding the lumen of the vessel, and reducing the appearance of the varicosity.

The FDA has approved polidocanol injections for the treatment of small varicose (less than 1 mm in diameter) and reticular veins (1 to 3 mm in diameter). Polidocanol works by damaging the cell lining of blood vessels, causing them to close and eventually be replaced by other types of tissue.[6][7] Polidocanol in the form of Varithena injected in the greater saphenous vein can cause the eruption of varicose and spider veins throughout the lower leg. This procedure should be done with caution and with the knowledge that the appearance of the leg may be forever compromised.

Pure polidocanol for pharmaceutical use

On March 30th,2010 the FDA approved Polidocanol under the trade name Asclera. Polidocanol is a sclerosing agent indicated to treat uncomplicated spider veins (varicose veins ≤1 mm in diameter) and uncomplicated reticular veins (varicose veins 1 to 3 mm in diameter) in the lower extremities. Varicose veins develop when the small valves inside the veins no longer work properly, allowing the blood to flow backwards and then pool in the vein.
When injected intravenously, Polidocanol works by locally damaging the endothelium of the blood vessel, causing platelets to aggregate at the site of damage and attach to the venous wall. Eventually, a dense network of platelets, cellular debris and fibrin occludes the vessel, which is then replaced with connective fibrous tissue. As one would expect for this type of molecule and also the mechanism of action, there is believed to be no specific molecular target for Polidocanol.
Polidocanol is a large ‘small molecule’ drug (Molecular Weight of 583 g.mol-1), with a mean half-life of 1.5 hr. Polidocanol is administrated intravenously and the strength of the solution and the volume injected depend on the size and extent of the varicose veins. Thus, the recommended dosage is 0.1 to 0.3 mL for each injection (Asclera 0.5% for spider veins and Asclera 1% for reticular veins) into each varicose vein, and a maximum recommended volume per treatment session of 10 mL.
Polidocanol’s chemical structure is 2-[2-[2-[2-[2-[2-[2-[2-[2-(dodecyloxy)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethanol. It is a non-ionic detergent, similar to polyethylene glycol (PEG) in structure, consisting of two components, a polar hydrophilic (dodecyl alcohol) and an apolar hydrophobic (polyethylene oxide – the part in brackets in the chemical structure) chain.

References

  1. ^ “E45 itch relief cream”. netdoctor.co.uk. Retrieved 2007-07-12.
  2. ^ Star P, Connor DE, Parsi K (April 2018). “Novel developments in foam sclerotherapy: Focus on Varithena® (polidocanol endovenous microfoam) in the management of varicose veins”. Phlebology. 33 (3): 150–162. doi:10.1177/0268355516687864. PMID 28166694.
  3. ^ Gao Z, Zhang Y, Li W, Shi C (January 2018). “Effectiveness and safety of polidocanol for the treatment of hemangiomas and vascular malformations: A meta-analysis”. Dermatologic Therapy. 31 (1). doi:10.1111/dth.12568. PMID 29082587.
  4. ^ Sclerotherapy, Laurence Z Rosenberg, MD, eMedicine.com
  5. ^ “Varithena™ (polidocanol injectable foam) For Intravenous Use. Full Prescribing Information” (PDF). Biocompatibles, Inc. Archived from the original (PDF) on 4 August 2016. Retrieved 1 October 2015.
  6. ^ Facts and Companies: Varicose Vein Treatment Approved
  7. ^ “Asclera Full Prescribing Information in Drug Reference Encyclopedia”. Retrieved 2010-04-11.
Clinical data
Other namesPolydocanolLaureth 9Macrogol lauryl etherLauromacrogolPEG-9 lauryl alcoholPOE-9 lauryl alcoholDodecylpolyethyleneglycoletherHydroxyl polyethoxy dodecaneOxypolyethoxydodecane
AHFS/Drugs.comInternational Drug Names
Pregnancy
category		Topical: allowed
Injection: contraindication in months 1–3 and after week 36
Routes of
administration		topical, subcutaneous injection
ATC codeC05BB02 (WHO)
Legal status
Legal statusOTC (topical), ℞ (injection)
Identifiers
showIUPAC name
CAS Number9002-92-0 
3055-99-0
PubChem CID656641
ChemSpider570993 
UNII0AWH8BFG9A
KEGGD01993 
ChEMBLChEMBL1201751 
ECHA InfoCard100.019.351 
Chemical and physical data
FormulaC30H62O10
Molar mass582.816 g·mol−1
3D model (JSmol)Interactive image
showSMILES
showInChI
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////////POLIDOCANOL, Anesthetic ,  Antipruritic, Sclerosing Agent,

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