DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO, Worlddrugtracker, Born in Mumbai in 1964 and graduated from Mumbai University, Completed his PhD from ICT ,1991, Mumbai, India, in Organic chemistry, The thesis topic was Synthesis of Novel Pyrethroid Analogues, Currently he is working with AFRICURE PHARMA as ADVISOR earlier GLENMARK LS Research centre as consultant,Principal Scientist, Process Research (bulk actives) at Mahape, Navi Mumbai, India. Prior to joining Glenmark, he worked with major multinationals like Hoechst Marion Roussel, now sSanofi, Searle India ltd, now Rpg lifesciences, etc. he is now helping millions, has million hits on google on all organic chemistry websites. His New Drug Approvals, Green Chemistry International, Eurekamoments 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 year tenure, good knowledge of IPM, GMP, Regulatory aspects, he has several international drug patents published worldwide . He gas good proficiency in Technology transfer, Spectroscopy, Stereochemistry, Synthesis, polymorphism etc He suffered a paralytic stroke in dec 2007 and is bound to a wheelchair, this seems to have injected feul in him to help chemists around the world, he is more active than before and is pushing boundaries, he has one lakh connections on all networking sites, He makes himself available to all, contact him on +91 9323115463, [email protected]

Chemically Induced Pluripotent Stem Cells

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Aug 022013

A combination of seven small-molecule compounds can be used to generate induced pluripotent stem cells

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Anti-tumoral Metabolites in Orange Peel

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Aug 022013

Flavonoid 5-demethylnobiletin is metabolized to compounds that show anti-tumoral properties

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Microgels for Glucose-Dependent Insulin Release

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Aug 022013

A group of American scientists developed microgels that release insulin in response to changing blood glucose levels

10 Top-selling Diabetes Drugs – 2012

diabetes 1 Response »

Aug 012013

By Eric Palmer

http://www.fiercepharma.com/special-reports/10-top-selling-diabetes-drugs-2012?page=0,0&utm_medium=nl&utm_source=internal

The prevalence of diabetes is growing globally, and with that the size of the diabetes drug market. There are more than 370 million people in the world with diabetes, about 90% of those with Type 2 diabetes. More children are developing the disease and more people are dying from diabetes, and so more and more people need treatment. Standard & Poor’s has estimated the annual market will hit $58 billion by 2018, from about $35 billion today.Read more:

http://www.fiercepharma.com/special-reports/10-top-selling-diabetes-drugs-2012?page=0,0&utm_medium=nl&utm_source=internal

check these videos

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FDA Lifts Clinical Hold on Canada company Cangene’s Hemophilia Compound

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Jul 312013

FDA lifts clinical hold on Cangene’s hemophilia compound IB1001

WINNIPEG, July 29, 2013 /CNW/ – Cangene Corporation (Cangene) today announces that the U.S. Food and Drug Administration (FDA) has lifted the clinical hold previously placed on clinical trials evaluating the safety and efficacy of IB1001, a recombinant Factor IX (rFIX) product being developed for the treatment and prevention of bleeding episodes with hemophilia B.

http://www.pharmalive.com/fda-lifts-clinical-hold-on-cangenes-hemophilia-compoun

IB1001 is an intravenous recombinant Factor IX (rFIX) being developed for the treatment and prevention of bleeding episodes in people with hemophilia B. The IB1001 development program includes a comprehensive set of pharmacokinetic, safety, and efficacy data from a Phase 3 clinical trial in people affected by hemophilia B, including a surgery sub-study.

A biologics license application (BLA) was submitted to the U.S. Food and Drug Administration (FDA) in March 2012 and a Marketing Authorization Application (MAA) was submitted to the European Medicines Agency (EMA) in October 2011.

In July 2012, IB1001 was put on a clinical hold by the FDA due to a higher than expected rate of host cell antibody development in people treated with IB1001.

Cangene Corporation (TSX: CNJ) has completed its previously announced acquisition of the worldwide rights to investigational hemophilia compound IB1001 (recombinant FIX), as well as Inspiration’s rights to two product candidates in pre-clinical development: IB1007 (recombinant FVIIa) and IB1008 (recombinant FVIII) from Ipsen (Euronext: IPN; ADR: IPSEY) and Inspiration Biopharmaceuticals, Inc., in connection with Inspiration’s bankruptcy proceedings.

The transaction was slated to close on February 15, 2013.

Pursuant to the terms of the agreement, Cangene will pay approximately US $5.9 million upfront and up to $50 million in potential additional commercial milestones as well net sales payments equivalent to tiered double-digit percentage of IB1001 annual net sales.

http://canadianprivateequity.com/cangene-closes-56-million-acquisition-of-inspirations-ib1001-hemophilia-b-product/2013/02/20/

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Perrigo Buying Elan For $8.6B

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Jul 302013

U.S. drugmaker Perrigo agreed to buy Ireland’s Elan for $8.6 billion in a deal that should allow the rapidly growing company to reduce its tax bill and boost its royalty stream.

Perrigo Co. said it would pay Elan Corp.’s investors $6.25 per share in cash and $10.25 in Perrigo stock, an 11% premium over Elan’s closing price on July 26. Elan shares in Dublin surged 13% higher to 12.58 euros ($16.71), above Perrigo’s offer price, following news of the takeover.

http://www.dddmag.com/news/2013/07/perrigo-buying-elan-86b

Indian biopharma giant Biocon clocks revenue worth $121 mn

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Jul 302013

Kiran Mazumdar-Shaw, chairman and managing director, Biocon.

Indian biopharma giant Biocon reported healthy growth of 22 percent for Q1 FY14 riding on the back of an increased geographical footprint in the emerging markets

Bangalore: Indian biopharma giant Biocon reported healthy growth of 22 percent for Q1 FY14. The firm clocked revenues worth $121 million (Rs723 crore), EBITDA of $29.50 million (Rs175 crore); and profit after tax (PAT) of $15.80 million (Rs94 crore).

Biocon’s India-focused branded formulations vertical as well as research services continue to grow at a steady pace

B Family Album -Structural Biology: First structures of class B G protein-coupled receptors may aid drug hunts

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Jul 292013

Two new G-Protein Coupled Receptor structures, the glucagon receptor (computer model with extracellular domain) and corticotropin-releasing factor receptor, showing their location on the GPCR family tree.

A computer model of a full-length glucagon receptor (left) and a crystal structure of a corticotropin-releasing factor receptor (right) add details of class B receptors to the class A structures already on the GPCR family tree.

Credit: Katya Kadyshevskaya

As many as 30% of drugs on the market target G protein-coupled receptors (GPCRs), a family of signaling conduits that snake back and forth across cell membranes. But there are several classes of these proteins, and scientists’ knowledge of the structures is almost entirely restricted to just one, the class A subtype. So drugs could be missing a lot of targets. Aim could improve, however, now that researchers have the first two reports of class B GPCR structures (Nature 2013, DOI: 10.1038/nature12357 and10.1038/nature12393

read all at

http://cen.acs.org/articles/91/i30/B-Family-Album.html

Tesaro begins phase III trial of niraparib for treatment of ovarian cancer

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Jul 292013

niraparib

MK-4827

MK-4827 Formula: C19H20N4O

MK-4827 Storage: at -20 ℃ 2 years
MK-4827 CAS No.: 1038915-60-4

MK-4827 is an inhibitor of PARP 1 and 2 with IC50 = 3.8 and 2.1 nM, respectively, currently in clinical trials. In a whole cell assay, it inhibited PARP activity with EC50 = 4 nM and inhibited proliferation of cancer cells with mutant BRCA-1 and BRCA-2 with CC50 in the 10-100 nM range. MK-4827 was well tolerated in vivo and demonstrated efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer

TESARO, Inc. an oncology-focused biopharmaceutical company, today announced that it has initiated patient enrollment in a Phase 3 trial of niraparib, an inhibitor of poly ADP-ribose polymerase (PARP), for the treatment of ovarian cancer. This trial, referred to as NOVA, will evaluate a single daily 300 milligram dose of niraparib in 360 patients with high grade serous, platinum sensitive, relapsed ovarian cancer compared to placebo.
Read more:

http://www.benzinga.com/news/13/07/3773861/tesaro-initiates-phase-3-trial-of-niraparib-for-treatment-of-patients-with-ovaria?utm_source=feedburner&utm_medium=feed&utm_campaign=Feed%3A+benzinga+%28Benzinga+News+Feed%29

Biological Activity of MK-4827:
MK-4827 is a potent, selective, PARP 1/2 inhibitor with IC50 of 3.8 and 2.1 nM for PARP1 and 2, respectively. MK-4827 possesses potential antineoplastic activity. In a whole cell assay, MK-4827 prevented PARP activity with an EC50 of 4 nM, enhancing the accumulation of DNA strand breaks and promoting genomic instability and apoptosis. MK-4827 induces selective synthetic lethality in homologous recombination (HR) repair deficient tumors with BRCA1 / 2 loss and tumor cell lines with non-BRCA-related HR defects, supporting clinical utility in sporadic tumors. MK-4827 reveals good pharmacokinetic properties and is currently in phase I clin. trials. The phase I clinical trials for MK-4827 is ongoing in the treatment of solid tumors.

References on MK-4827:
1. Study of the Safety and Efficacy of MK-4827 Given With Temozolomide in Participants With Advanced Cancer (MK-4827-014 AM1).2. A Study of MK4827 in Participants With Advanced Solid Tumors or Hematologic Malignancies (MK-4827-001 AM8).

3. PARP inhibitor MK4827
Abstract
An inhibitor of Poly (ADP-ribose) polymerase (PARP) with potential Antineoplastic Activity. PARP Inhibitor MK4827 inhibits PARP Activity, ENHANCING the accumulation of DNA Strand Breaks and promoting genomic instability and apoptosis. The PARP family of Proteins detect and repair single strand DNA breaks by the base-excision repair (BER) pathway.

4. Glendenning J, Tutt A. PARP inhibitors – Current Status and the Walk towards Early Breast cancer. Breast. 2011 Oct; 20 Suppl 3: S12-9.
Abstract
… Early Phase Trials with efficacy endpoints have been presented for the PARP inhibitors AG014699, olaparib, veliparib, iniparib and MK4827. The results of the first phase II trials exploring monotherapy PARP inhibitor strategies, which are based on revisiting the concept of synthetic lethality, have emerged and are reviewed herein. The clinical trials that have or are exploring combinations with DNA damaging therapy in these contexts are discussed with particular reference to breast cancer, as are biomarkers that have been proposed and are being investigated to develop optimal drug schedule and patient selection criteria for these DNA repair targeting approaches.

5. Jones, Philip; Altamura, Sergio; Boueres, Julia et al. Discovery of 2 – {4 – [(3S)-Piperidin-3-yl] phenyl}-2H-INDAZOLE-7-carboxamide (MK-4827): A Novel Oral Poly (ADP-ribose) polymerase (PARP) Inhibitor efficacious in BRCA-1 and -2 Mutant Tumors. Journal of Medicinal Chemistry (2009), 52 (22), 7170-7185.
Abstract
… We Disclose the Development of a novel series of 2-phenyl-2H-indazole-7-carboxamides as poly (ADP-ribose) polymerase (PARP) 1 and 2 inhibitors. This series was optimized to improve enzyme and cellular activity, and the resulting PARP inhibitors display antiproliferation activities against BRCA-1 and BRCA-2 deficient cancer cells, with high selectivity over BRCA proficient cells. Extrahepatic oxidation by CYP450 1A1 and 1A2 was identified as a metabolic concern, and strategies to improve pharmacokinetic properties are reported. These efforts culminated in the identification of 2 – {4 – [(3S)-piperidin-3-yl] phenyl}-2H-indazole-7-carboxamide 56 (MK-4827), which displays good pharmacokinetic properties and is currently in phase I clinical trials. This compound displays excellent PARP 1 and 2 inhibition with IC50 = 3.8 and 2.1 nM, respectively, and in a whole cell assay, it inhibited PARP activity with EC50 = 4 nM and inhibited proliferation of cancer cells with mutant BRCA-1 and BRCA-2 with CC50 in the 10? 100 nM range. Compound 56 was well tolerated in vivo and demonstrated efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer.