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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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Roche may bid for Alexion, gets Erivedge EU approval


Erivedge , Vismodegib

The molecule also is known as GDC-0449 and RG3616.

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Vismodegib works by interfering with the membrane protein Smoothened, which provides positive signals to the Hh pathway. At present, there are no FDA-approved drugs targeting Hh signaling, although the pathway is the focus of investigation in a variety of cancers.

Meantime, Roche has obtained conditional European approval for Erivedge (vismodegib) for the treatment of adults with symptomatic metastatic basal cell carcinoma (BCC) or locally advanced BCC inappropriate for surgery or radiotherapy.

The Basel-based group noted that the approval makes Erivedge, a capsule taken once-a-day, the first licensed medicine for patients in the European Union “with this disfiguring and potentially life-threatening form of skin cancer”. Chief medical officer Hal Barron said the green light “is great news for patients with advanced basal cell carcinoma, who previously had no medicines to treat their disease”, adding that Erivedge substantially reduced tumour size in patients in clinical trials.

Under the conditional approval, Roche will provide additional data from an ongoing global safety study. Erivedge was approved by the US Food and Drug Administration in January 2012 following a priority review.

Vismodegib (trade name Erivedge) is a drug for the treatment of basal-cell carcinoma(BCC). The approval of vismodegib on January 30, 2012, represents the first Hedgehog signaling pathway targeting agent to gain U.S. Food and Drug Administration (FDA) approval.[1] The drug is also undergoing clinical trials for metastatic colorectal cancer,small-cell lung cancer, advanced stomach cancerpancreatic cancermedulloblastomaand chondrosarcoma as of June 2011.[2] The drug was developed by the biotechnology /pharmaceutical company Genentech, which is headquartered at South San Francisco, CaliforniaUSA.

Vismodegib is indicated for patients with basal cell carcinoma (BCC), which has metastasized to other parts of the body, relapsed after surgery, or cannot be treated with surgery or radiation.[3]

Hedgehog Activation.

The substance acts as a cyclopamine-competitive antagonist of the smoothened receptor (SMO) which is part of the hedgehog signaling pathway.[2] SMO inhibition causes the transcription factors GLI1 and GLI2 to remain inactive, which prevents the expression of tumor mediating genes within the hedgehog pathway.[4] This pathway is pathogenetically relevant in more than 90% of basal-cell carcinomas.[5]

Hedgehog pathway
Ligand-dependent Hedgehog signaling.


  1.  “Vismodegib, First Hedgehog Inhibitor, Approved for BCC Patients”.
  1.  “Vismodegib, First Hedgehog Inhibitor, Approved for BCC Patients”.
  2.  Molecule of the Month. June 2011.
  3.  “FDA approves Erivedge (vismodegib) capsule, the first medicine for adults with advanced basal cell carcinoma”.
  4.  “Vismodegib (GDC-0449) Smoothened Inhibitor – BioOncology”.
  5.  H. Spreitzer (4 July 2011). “Neue Wirkstoffe – Vismodegib”. Österreichische Apothekerzeitung (in German) (14/2011): 10.

Vismodegib is Hedgehog (Hg) path inhibitors. Pka = 3.8 (pyridinium cation); soluble 0.1μg/mL (pH = 7), 0.99mg/mL (pH = 1), logP = 2.7. Vismodegib can be synthesized by the following route:


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