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Read all about Organic Spectroscopy on ORGANIC SPECTROSCOPY INTERNATIONAL 

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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 GLENMARK PHARMACEUTICALS LTD, Research Centre as Principal Scientist, Process Research (bulk actives) at Mahape, Navi Mumbai, India. Total Industry exp 30 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, Dr T.V. Radhakrishnan and Dr B. K. Kulkarni, 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 30 year tenure till date Dec 2017, 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 9 million plus hits on Google, 2.5 lakh plus connections on all networking sites, 50 Lakh plus views on dozen plus blogs, He makes himself available to all, contact him on +91 9323115463, email, Twitter, @amcrasto , He lives and will die for his family, 90% paralysis cannot kill his soul., Notably he has 19 lakh plus views on New Drug Approvals Blog in 216 countries...... , He appreciates the help he gets from one and all, Friends, Family, Glenmark, Readers, Wellwishers, Doctors, Drug authorities, His Contacts, Physiotherapist, etc

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CFDA Approves Clinical Trials for Novel China AIDS Treatment


China’s SFDA Ready to Fast-Track Approvals of Peramivir, a Flu Treatment


(1S,2S,3S,4R)-3-[(1S)-1-acetamido-2-ethyl-butyl]-4- (diaminomethylideneamino)-2-hydroxy-cyclopentane- 1-carboxylic acid

8th, APRIL 2013

In the wake of the growing bird flu outbreak, China’s SFDA will fast-track approvals of a flu treatment – not a vaccine – known as peramivir (peramivir sodium chloride injection). The drug is a neuraminidase inhibitor, which works by preventing the virus from moving from an infected cell to infect other cells. Guangzhou Nanxin Pharma has been approved to produce the medicine, and it expects to begin distributing the drug in 30 days. Other China pharmas have also filed for approval to make the drug or conduct human clinical trials

Peramivir is an experimental antiviral drug developed by BioCryst Pharmaceuticals for the treatment of influenza. It has been authorized for the emergency use of treatment of certain hospitalized patients with known or suspected 2009 H1N1 influenza.[1]

Peramivir is a neuraminidase inhibitor, acting as a transition-state analogue inhibitor of influenza neuraminidase and thereby preventing new viruses from emerging from infected cells.

The development of peramivir is supported by the US Department of Health and Human Services as part of the US government’s effort to prepare against the threat of an influenza pandemic.[2]

Peramivir is already available in Japan as RAPIACTA (R) and also available in South Korea as PERAMIFLU. Peramivir is currently the only intravenous option for treating swine flu. The drug is in Phase III studies in US.[3][4]

Use in treating Influenza A (H1N1) “Swine Flu”

In October 2009, it was reported that the experimental antiviral drug peramivir had been effective in treating serious cases of swine flu.[5] On October 23, the U.S. Food and Drug Administration (FDA) issued an Emergency Use Authorization for Peramivir, allowing the use of the drug in intravenous form for hospitalized patients only in cases where the other available methods of treatment are ineffective or unavailable;[6] for instance, if oseltamivir (Tamiflu) resistance develops and a person is unable to take Relenza via the inhaled route. The Emergency Use Authorization expired on June 23, 2010.

Biocryst also donated 1200 courses of treatment to the US department of Health and Human Services.[7]

According to a research report published in June 2011, a novel variant of swine flu has emerged in Asia with a genetic adaptation giving some resistance to Roche’s (ROG.VX) Tamiflu and GlaxoSmithKline’s (GSK.L) Relenza, the two mainstay drugs used to tackle the disease. There was no significant reduction in sensitivity to Peramivir. [8]

Initial treatment courses are for 5 to 10 days duration. Treatment beyond 10 days is permitted depending on clinical presentation such as critical illness (e.g., respiratory failure or intensive care unit admission), continued viral shedding or unresolved clinical influenza illness.[9]

  1.  “Peramivir authorized for Emergency use”. LifeHugger. 2009-12-04. Retrieved 2009-12-04.
  2.  “HHS Pursues Advance Development of New Influenza Antiviral Drug” (Press release). USDepartment of Health and Human Services. 2007-01-04. Retrieved 2007-05-25.
  3.  “Evaluation of the Efficacy and Safety of Peramivir in Subjects With Uncomplicated Acute Influenza”.National Institutes of Health. 2007-03-16. Retrieved 2007-05-25.
  4.  “Evaluation of the Efficacy and Safety of Peramivir in Adults With Acute Serious or Potentially Life-Threatening Influenza”National Institutes of Health. 2007-03-28. Retrieved 2007-05-25.
  5.  “Life-Saving H1N1 Drug Unavailable to Most”CBS Evening News (Atlanta, GA, USA: CBS Interactive). 2009-10-19. Retrieved 2009-10-20.
  6.  “Emergency Use Authorization Granted For BioCryst’s Peramivir”Reuters. 2009-10-24.
  7.  “FDA Authorizes Emergency Use of Intravenous Antiviral Peramivir for 2009 H1N1 Influenza for Certain Patients, Settings”Reuters. 2009-10-24.
  8.  Hirschler, Ben (2011-06-10). “Swine flu starting to show resistance to drugs”Reuters.
  9.  “Peramivir: Dosage and Administration”. LifeHugger. 2009-12-04. Retrieved 2009-12-04.

TLC388 (Lipotecan®) Taiwan Liposome Company Hepatic cancer drug candidate gets fast track approval status from SFDA

TLC388 (Lipotecan®) structure can be figured out from a link below of a poster


The str can be concluded from above picture from a poster by TLC BIO

TLC388 (Lipotecan) is a potent Topoisomerase-1 inhibitor and it can disrupt both Sonic Hedgehog and HIF1-α pathways to overcome cancer drug resistance and inhibit angiogenesis induced by tumor hypoxia. This phase I first-in-human study of Lipotecan examined the MTD, safety, anti-tumor activity and pharmacokinetic profiles of TLC388 in patients with advanced incurable solid tumors.

Methods: Lipotecan was administered intravenously on day 1, 8 and 15 of a 28-day cycle. Patients underwent safety assessments regularly and tumor assessments every other cycle. Pharmacokinetic samples were drawn on days 1, 8 and 15 of cycles 1 and 2 for all treated patients.

MAR19 2013

China SFDA has granted fast track approval status to Taiwan Liposome company hepatic cancer drug  Lipotecan, shortening the review period. The drug will enter Phase 2 clinical trials  in China in the second half of this year. Lipotecan has been granted orphan drug status by US FDA and EU EMEA for the treatment of hepatocellular carcinoma (HCC)

Nexavar is the standard of care in first line advanced liver cancer patients. Lipotecan as a second-line treatment allows patients who have failed prior treatment with Nexavar to maintain a six month course of the disease without progressing

Lipotecan is a  second generation camptothecin drug emphasize on modification on E-ring with a group which not only stabilizes the active site but also functions as a strong radio-sensitizer to overcome radio- and chemo-resistance that is frequently encountered in clinical therapies, enabling Lipotecan® to tailor at unmet needs.

Pfizer Gains China Approval of Kinase-Specific Lung Cancer Drug, Xalkori (crizotinib)

File:Crizotinib structure.svg

Xalkori, crizotinib,

Crizotinib; 877399-52-5; Xalkori; PF-2341066; PF-02341066; (R)-crizotinib; 877399-52-5

Molecular Formula: C21H22Cl2FN5O
Molecular Weight: 450.336683 g/mol

Crizotinib an inhibitor of receptor tyrosine kinase for the treatment of non-small cell lung cancer (NSCLC). Verification of the presence of ALK fusion gene is done by Abbott Molecular’s Vysis ALK Break Apart FISH Probe Kit. This verification is used to select for patients suitable for treatment. FDA approved in August 26, 2011.

Crizotinib (1), an anaplastic lymphoma kinase (ALK) receptor tyrosine kinase inhibitor approved by the U.S. Food and Drug Administration in 2011, is efficacious in ALK and ROS positive patients

Feb 25, 2013

Pfizer has been granted China approval for Xalkori (crizotinib), an innovative treatment for patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) that is anaplastic lymphoma kinase (ALK) positive. The ALK-positive variation, which comprises between 3% and 5% of all NSCLC tumors, must be proved by a biomarker test. Pfizer said China’s approval came just eleven months after it submitted a new drug application to the SFDA for Xalkori

Crizotinib (trade name Xalkori,[1] Pfizer), is an anti-cancer drug acting as an ALK (anaplastic lymphoma kinase) and ROS1 (c-ros oncogene 1) inhibitor, approved for treatment of some non-small cell lung carcinoma (NSCLC) in the US and some other countries, and undergoing clinical trials testing its safety and efficacy in anaplastic large cell lymphoma, neuroblastoma, and other advanced solid tumors in both adults and children.[2]

  1. FDA approves Xalkori with companion diagnostic for a type of late-stage lung cancer. U.S. Food and Drug Administration.
  2. NCT00932451 An Investigational Drug, PF-02341066, Is Being Studied In Patients With Advanced Non-Small Cell Lung Cancer With A Specific Gene Profile Involving The Anaplastic Lymphoma Kinase (ALK) Gene

Crizotinib the core structure is a substituted pyridine, the 3 – position of the ether as a chiral center adjacent, so with Mitsunobu reaction to complete, as is a typical Mitsunobu SN2 reaction, the reaction chiral center occurs in reverse, so easy to control, no racemization occurs. Pyridine substituted at position 5 by Suzuki reaction constructed.
Compound 1 The activation of the hydroxyl groups of methanesulfonyl chloride, and then with a 4 – iodopyrazole reaction 2 , 2 to 4 Suzuki reaction conversion can be used, but will generate a large quantity of the reaction product of their coupling, the first 2 converted to a Grignard reagent, and then with a boronic acid ester of 3 reaction 4 .



(R)-3-[l-(2,6-Dichloro-3-fluoro-phenyl)-ethoxy]-5-(l-piperidin-4-yl-lH-py- razol-4-yl)-pyridin-2-ylamine, also known as Crizotinib, is represented by the Formula (I):

Formula (I)

Crizotinib is a potent small-molecule inhibitor of c-Met/HGFR (hepatocyte growth factor receptor) kinase and ALK (anaplastic lymphoma kinase) activity. Enantiomerically pure compound of formula I was first disclosed in US Patent No. 7,858,643. Additionally, the racemate of compound of formula I was disclosed in U.S. patent application 2006/0128724, both of these references discloses similar methods for the synthesis of Compound of Formula I.

Conventionally, the compounds of formula I are prepared by reacting Bis(pinacolato)diboron with protected 5-bromo-3-[l-(2,6-dichloro-3-fluoro-phenyl)-ethoxy]-pyridin-2-ylamine in the presence of Pd catalyst. The obtained product after deprotection is reacted with N- protected 4-(4-bromo-pyrazol-l-yl)-piperidine in the presence of Pd Catalyst. The obtained product is filtered through celite pad and purified by Column Chromatography. The final product of formula I was obtained by deprotection of the purified compound by using HCl/dioxane. US Patent No. 7,858,643 provides enantiomerically pure aminoheteroaryl compounds, particularly aminopyridines and aminopyrazines, having protein tyrosine kinase activity. More particularly, US 7,858,643 describes process for the preparation of 3-[(lR)-l-(2,6- dichloro-3-fluorophenyl)ethoxy]-5-(l-piperidin-4-ylpyrazol-4-yl)pyridin-2-amine. The Scheme is summarized below in Scheme- 1 :


wherein, “Boc” means tert-butoxycarbonyl; and a) (Boc)2, DMF, Dimethylaminopyridine b) Pd(dppf)Cl2, KOAc, Dichloromethane; c) HC1, Dioxane, Dichloromethane; d) Pd(PPh3)2Cl2, Na2C03, DME/H20; e) 4M HCl/Dioxane, Dichloromethane

A similar process has been disclosed in the U.S. patent application 2006/0128724 for the preparation of Crizotinib. J. Jean Cui et. al. in J. Med. Chem. 2011, 54, 6342-6363, also provides a similar process for the preparation of Crizotinib and its derivatives.

However, above mentioned synthetic process requires stringent operational conditions such as filtration at several steps through celite pad. Also column chromatography is required at various steps which is not only tedious but also results in significant yield loss. Another disadvantage of above process involves extensive use of palladium catalysts, hence metal scavengers are required to remove palladium content from the desired product at various steps which makes this process inefficient for commercial scale.

Yet another disadvantage of above process is the cost of Bis(pinacolato)diboron. This reagent is used in excess in the reaction mixture resulting in considerable cost, especially during large-scale syntheses.

US Patent No. 7,825,137 also discloses a process for the preparation of Crizotinib where Boc protected 4-(4-iodo-pyrazol-l-yl)-piperidine is first reacted with Bis(pinacolato)diboron in the presence of Pd catalyst. The reaction mixture is filtered through a bed of celite and the obtained filtrate is concentrated and purified by silica gel chromatography to give to form tert-butyl-4-[4-(4,4,5,5-tetramethyl-l,3,2-dioxaborolan-2-yl)-lH-pyrazol-l-yl]piperidine-l- carboxylate. To this compound, 5-bromo-3-[l-(2,6-dichloro-3-fluoro-phenyl)-ethoxy]- pyridin-2-ylamine is added in the presence of a Pd catalyst. The reaction mixture is stirred for 16h at 87°C. The reaction mixture is filtered through celite pad and the concentrated filtrate is purified on silica gel column to obtain (4-{6-amino-5-[(R)-l-(2,6-dichloro-3-fluoro- phenyl)-ethoxy]-pyri- din-3-yl}-pyrazol-l-yl)-piperidine-l-carboxylic acid tert-butyl ester of 95% purity. To the solution of resulting compound in dichloromethane 4N HCl/Dioxane is added and thereby getting the reaction suspension is filtered in Buchner funnel lined with filter paper. The obtained solid is dissolved in HPLC water and pH is adjusted to 10 with the addition of Na2C03 Compound is extracted using dichloroform and is purified on a silica gel column by eluting with CH2Cl2 MeOH/NEt3 system to obtain Crizotinib. The scheme is summarized below in scheme 2:

Formula (i) Formula (ii)

Formula (iii) Formula (ii) ula (iv)

Formula (v) Formula (I)


Preparation of Crizotinib:

To a stirred solution of Tert-butyl 4-(4-{ 6-amino-5-[(li?)-l-(2,6-dichloro-3- fluorophenyl)ethoxy]pyridin-3 -yl } – lH-pyrazol- 1 -yl)piperidine- 1 -carboxylate (material obtained in Example 3) (l.Og, 0.00181 moles) in dichloromethane (-13 ml) at 0°C was added 4.0 M dioxane HQ (6.7 ml, 0.0272 moles). Reaction mixture was stirred at room temperature for 4h. After the completion of reaction monitored by TLC, solid was filtered and washed with dichloromethane (10 ml). The obtained solid was dissolved in water (20 ml); aqueous layer was extracted with dichloromethane (10×2). The pH of aqueous layer was adjusted to 9-10 with Na2C03 and compound was extracted with dichloromethane (10 x 3), combined organic layers were washed with water (20 ml), evaporated under vacuum to get solid product. The solid was stirred with ether (10 ml), filtered off, washed well with ether, dried under vacuum to get Crizotinib.

Yield: 0.45g (55 %)

HPLC Purity: 99.35 %

1HNMR (400 MHz, CDC13) δ: 7.76 (d, J = 1.6 Hz, 1H), 7.56 (s, 1H), 7.49 (s, 1H), 7.30 (dd, J = 9.2 Hz), 7.0 (m, 1H), 6.86 (d, J = 1.6 Hz, 1H), 6.09 ( q, J= 6.8 Hz, 1H), 4.75 (brs, 1H), 4.19 (m, 1H), 3.25 (m, 2H), 2.76 (m, 2H), 2.16 (m, 2H), 1.92 (m, 2H), 1.85 (d, J= 6.8 Hz, 3H), 1.67 (brs, 1H)



A novel approach for the synthesis of Crizotinib (1) is described. In addition, new efficient procedures have been developed for the preparation of (S)-1-(2,6-dichloro-3-fluorophenyl)ethanol (2) and tert-butyl 4-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl)piperidine-1-carboxylate (4), the key intermediates required for the synthesis of Crizotinib.

Graphical abstract

Full-size image (16 K)


4-(4-Iodo-1H-pyrazol-1-yl)piperidine is a key intermediate in the synthesis of Crizotinib. We report a robust three-step synthesis that has successfully delivered multi-kilogram quantities of the key intermediate. The process includes nucleophilic aromatic substitution of 4-chloropyridine with pyrazole, followed by hydrogenation of the pyridine moiety and subsequent iodination of the pyrazole which all required optimization to ensure successful scale-up.

Graphical abstract

Full-size image (6 K)


Org. Process Res. Dev., 2011, 15 (5), pp 1018–1026
DOI: 10.1021/op200131n
Abstract Image

A robust six-step process for the synthesis of crizotinib, a novel c-Met/ALK inhibitor currently in phase III clinical trials, has been developed and used to deliver over 100 kg of API. The process includes a Mitsunobu reaction, a chemoselective reduction of an arylnitro group, and a Suzuki coupling, all of which required optimization to ensure successful scale-up. Conducting the Mitsunobu reaction in toluene and then crystallizing the product from ethanol efficiently purged the reaction byproduct. A chemoselective arylnitro reduction and subsequent bromination reaction afforded the key intermediate 6. A highly selective Suzuki reaction between 6 and pinacol boronate 8, followed by Boc deprotection, completed the synthesis of crizotinib 1.

3-[(1R)-1-(2,6-Dichloro-3-fluorophenyl)ethoxy]-5-[1-(piperidin-4-yl)-1H-pyrazol-4-yl]pyridin-2-amine 1

crizotinib1 (20.7 kg, 80%) as a white solid.

Mp 192 °C;

1H NMR (400 MHz, CDCl3) δ: 7.78 (d, J = 1.8 Hz, 1H), 7.58 (s, 1H), 7.52 (s, 1H), 7.31 (dd, J = 9.0, 4.9 Hz, 1H), 7.06 (m, 1H), 6.89 (d, J = 1.7 Hz, 1H), 6.09 (q, 1H), 4.79 (br s, 2H), 4.21 (m, 1H), 3.26 (m, 2H), 2.78 (m, 2H), 2.17 (m, 2H), 1.90 (m, 2H), 1.87 (d, J = 6.7 Hz, 3H), 1.63 (br s, 1H).

13C NMR (100.6 MHz, CDCl3) δ: 157.5 (d, J = 250.7 Hz), 148.9, 139.8, 137.0, 135.7, 135.6, 129.9, 129.0 (d, J = 3.7 Hz), 122.4, 122.1 (d, J = 19.0 Hz), 119.9, 119.3, 116.7 (d, J = 23.3 Hz), 115.0, 72.4, 59.9, 45.7, 34.0, 18.9.

LC-MS: found m/z 450.0, 451.0, 452.0, 453.0, 454.0, 455.0.

Anal. Calcd for C21H22Cl2FN5O: C, 56.01; H, 4.92; N, 15.55. Found: C, 56.08; H, 4.94; N, 15.80.

Cui, J. J.; Botrous, I.; Shen, H.; Tran-Dube, M. B.; Nambu, M. D.; Kung, P.-P.; Funk, L. A.; Jia, L.; Meng, J. J.; Pairish, M. A.; McTigue, M.; Grodsky, N.; Ryan, K.; Alton, G.; Yamazaki, S.; Zou, H.; Christensen, J. G.; Mroczkowski, B.Abstracts of Papers; 235th ACS National Meeting, New Orleans, LA, United States, April 6–10, 2008.

Cui, J. J.; Funk, L. A.; Jia, L.; Kung, P.-P.; Meng, J. J.; Nambu, M. D.; Pairish, M. A.; Shen, H.; Tran-Dube, M. B. U.S. Pat. Appl. U. S. 2006/0046991 A1, 2006.
WO2010048131A1 * Oct 20, 2009 Apr 29, 2010 Vertex Pharmaceuticals Incorporated C-met protein kinase inhibitors
WO2011042389A2 * Oct 4, 2010 Apr 14, 2011 Bayer Cropscience Ag Phenylpyri(mi)dinylazoles
US7825137 Nov 23, 2006 Nov 2, 2010 Pfizer Inc. Method of treating abnormal cell growth
US7858643 Aug 26, 2005 Dec 28, 2010 Agouron Pharmaceuticals, Inc. Crizotinib, a c-Met protein kinase inhibitor anticancer agent; 3-[(R)-1-(2,6-dichloro-3-fluoro-phenyl)-ethoxy]-5-(1-piperidin-4-yl-1H-pyrazol-4-yl)-pyridin-2-ylamine is crizotinib
US20060128724 Aug 26, 2005 Jun 15, 2006 Agouron Pharmaceuticals, Inc. Pyrazole-substituted aminoheteroaryl compounds as protein kinase inhibitors
1 J. JEAN CUI J. MED. CHEM. vol. 54, 2011, pages 6342 – 6363
2 ORG. PROCESS RES. DEV. vol. 15, 2011, pages 1018 – 1026
3 * PIETER D. DE KONING ET AL: “Fit-for-Purpose Development of the Enabling Route to Crizotinib (PF-02341066)“, ORGANIC PROCESS RESEARCH & DEVELOPMENT, vol. 15, no. 5, 16 September 2011 (2011-09-16), pages 1018-1026, XP055078841, ISSN: 1083-6160, DOI: 10.1021/op200131n

State Food and Drug Administration, China Grants Approval to Sihuan Pharmaceutical for Clinical Trial of Innovative Drug — Pinoxacin Hydrochloride

HONG KONG, Feb. 22, 2013, Sihuan Pharmaceutical Holdings Group Ltd. a leading pharmaceutical company with the largest cardio-cerebral vascular (“CCV”) drug franchise in China’s prescription market, today announced that Pinoxacin Hydrochloride, a Category 1.1 new drug developed by the Company’s innovative drug research and development team, received Approval for Clinical Studies from the State Food and Drug Administration. Phase I of clinical studies are set to begin in the first half of this year. It is the fourth Category 1 innovative drug for which the Company has received Approval for Clinical Studies.

Pinoxacin Hydrochloride is DPP-4 inhibitor class of oral hypoglycemic agents, a drug with a brand new structure for treating type II diabetes. It is clinically used to enhance the function of endogenous insulin for improving glycemic control, and long-term use can improve islet beta-cells function. Pre-clinical research has shown that DPP-4 inhibitors have potent in vitro and in vivo activities, a good selection profile, great stability and controllable quality, as well as better tolerance, with long-term administration showing a protective effect on pancreatic beta-cells. In addition, the DPP-4 inhibitor will not cause serious side effects such as weight gain and hypoglycaemia seen in traditional diabetes drugs. Pinoxacin Hydrochloride has good pharmacokinetic characteristics, high oral bioavailability, quick absorption, rapid onset and a longer duration. A once daily dosage is expected to keep the patients’ symptoms under control. The advantages of Pinoxacin Hydrochloride have proven the drug’s growth potential present in the market.

Celgene gains SFDA China, approval for marketing Revlimid (lenalidomide) to treat multiple myeloma


(RS)-3-(4-amino-1-oxo 1,3-dihydro-2H-isoindol- 2-yl)piperidine-2,6-dione


sun, feb17, 2013
Celgene Corporation was granted approval for Revlimid ® (lenalidomide) by the SFDA to treat multiple myeloma. The approval, which is the first for Celgene in China, includes an Import Drug License. Revlimid is indicated for use in combination with dexamethasone in patients with relapsed or refractory multiple myeloma who have received at least one prior therapy.
REVLIMID® is an oral immunomodulatory drug marketed in the United States and many international markets, in combination with dexamethasone, for treatment of patients with multiple myeloma who have received at least one prior therapy. It is also marketed in the United States and certain international markets for the treatment of transfusion-dependent anemia due to low- or intermediate-1-risk myelodysplastic syndromes, or MDS, associated with a deletion 5q cytogenetic abnormality with or without additional cytogenetic abnormalitie.Revlimid Worldwide annual sales in 2011 was $3.2bLenalidomide (Revlimid) is a derivative of thalidomideintroduced in 2004.It was initially intended as a treatment for multiple myeloma, for which thalidomide is an accepted therapeutic treatment. Lenalidomide has also shown efficacy in the class of hematological disorders known as myelodysplastic syndromes (MDS). Lenalidomide has significantly improved overall survival in myeloma (which generally carries a poor prognosis), although toxicity remains an issue for users. [1]It costs $163,381 per year for the average patient.[2]

Mechanism of action

Lenalidomide has been used to successfully treat both inflammatory disorders and cancers in the past 10 years. There are multiple mechanisms of action, and they can be simplified by organizing them as mechanisms of action in vitro and in vivo.[3] In vitro, lenalidomide has three main activities: direct anti-tumor effect, inhibition of the microenvironment support for tumor cells, and immunomodulatory role. In vivo, lenalidomide induces tumor cell apoptosis directly and indirectly by inhibition of bone marrow stromal cell support, by anti-angiogenic and anti-osteoclastogenic effects, and by immunomodulatory activity. Lenalidomide has a broad range of activities that can be exploited to treat many hematologic and solid cancers.

  1. McCarthy; Philip L. McCarthy, Kouros Owzar, Craig C. Hofmeister, et al. (May 10, 2012). “Lenalidomide after Stem-Cell Transplantation for Multiple Myeloma”N Engl J Med 366 (19): 1770–1781. doi:10.1056/NEJMoa1114083PMID 22571201.
  2. Badros, Ashraf Z. Badros (May 10, 2012). “Lenalidomide in Myeloma — A High-Maintenance Friend”N Engl J Med 366 (19): 1836–1838. doi:10.1056/NEJMe1202819PMID 22571206.
  3. Vallet S, Palumbo A, Raje N, Boccadoro M, Anderson KC (July 2008). “Thalidomide and lenalidomide: Mechanism-based potential drug combinations”. Leukemia & Lymphoma 49 (7): 1238–45. doi:10.1080/10428190802005191PMID 18452080.
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