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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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Idarucizumab

April 26, 2016 10:45 am / Leave a comment


Idarucizumab

(Praxbind®) Approved

An antidote for rapid reversal of dabigatran-induced anticoagulation indicated for emergency surgery (urgent procedures) and life-threatening or uncontrolled bleeding in patients treated with dabigatran.

BI-655075

CAS No.1362509-93-0

1- 225-Immunoglobulin G1, anti-(dabigatran) (human-Mus musculus γ1-chain) (225→219′)-disulfide with immunoglobulin G1, anti-(dabigatran) (human-Mus musculus κ-chain)

Other Names

  • BI 655075
  • Idarucizumab
  • Praxbind

Protein Sequence

Sequence Length: 444, 225, 219multichain; modified (modifications unspecified)

Idarucizumab, sold under the brand name Praxbind, is a monoclonal antibody designed for the reversal of anticoagulant effects ofdabigatran.[1][2]

This drug was developed by Boehringer Ingelheim Pharmaceuticals. A large study sponsored by the manufacturer found that idarucizumab effectively reversed anticoagulation by dabigatran within minutes.[3] It was FDA approved in October 2015.[4] In the United States the wholesale cost is $3500 US.[5]

On October 16, 2015, the U. S. Food and Drug Administration granted accelerated approval to idarucizumab (Praxbind  Injection, Boehringer Ingelheim Pharmaceuticals, Inc.) for the treatment of patients treated with dabigatran (Pradaxa) when reversal of the anticoagulant effects of dabigatran is needed for emergency surgery/urgent procedures, or in life-threatening or uncontrolled bleeding.
The approval was based on three randomized, placebo-controlled trials enrolling a total of 283 healthy volunteers who received either dabigatran and idarucizumab or dabigatran and placebo.  The primary endpoint in healthy volunteer trials was the reduction of unbound dabigatran to undetectable levels after the administration of 5 g idarucizumab.  This reduction of dabigatran plasma concentration was observed over the entire 24 hour observation period.
These trials are supported by an ongoing open-label trial in which data from 123 patients receiving dabigatran who had life-threatening or uncontrolled bleeding, or who required emergency surgery/urgent procedures was available for evaluation.  This open-label trial continues to enroll and follow patients. The primary endpoint is the reversal of dabigatran’s anticoagulant effect (measured by ecarin clotting time or dilute thrombin time) in the first four hours after administration of 5 g idarucizumab. In these 123 patients, the anticoagulant effect of dabigatran was completely reversed in more than 89% of patients within four hours of receiving idarucizumab.  Between 12 and 24 hours after idarucizumab administration, elevated coagulation parameters have been observed in a limited number of patients.
Safety data were evaluated in 224 healthy volunteers who received at least one dose of idarucizumab and 123 patients who received idarucizumab. Headache was the most common adverse event reported in more than 5% of healthy volunteers.  Among the 123 patients treated with idarucizumab in the ongoing open-label trial, adverse events reported in more than 5% of patients were hypokalemia, delirium, constipation, pyrexia and pneumonia.
Praxbind is the first approved reversal agent. It is specific for dabigatran.
Continued approval for this indication may be contingent upon the results of completion of the ongoing open-label trial.
The recommended dose for idarucizumab is 5 g (2.5g per vial) administered intravenously as two consecutive 2.5 g infusions or bolus injection by injecting both vials consecutively one after another via syringe.

References

  1.  Statement On A Nonproprietary Name Adopted By The USAN Council – Idarucizumab, American Medical Association.
  2.  World Health Organization (2013). “International Nonproprietary Names for Pharmaceutical Substances (INN). Proposed INN: List 109” (PDF). WHO Drug Information 27 (2).
  3.  Pollack, Charles V.; Reilly, Paul A.; Eikelboom, John; Glund, Stephan; Verhamme, Peter; Bernstein, Richard A.; Dubiel, Robert; Huisman, Menno V.; Hylek, Elaine M. (2015-08-06).“Idarucizumab for Dabigatran Reversal”. The New England Journal of Medicine 373 (6): 511–520. doi:10.1056/NEJMoa1502000. ISSN 1533-4406. PMID 26095746.
  4.  “Press Announcements – FDA approves Praxbind, the first reversal agent for the anticoagulant Pradaxa”. http://www.fda.gov. Retrieved 2015-10-17.
  5.  Elia, Joe. “Dabigatran-Reversal Agent Price Set”. Retrieved 20 October 2015.
Idarucizumab
Monoclonal antibody
Type Fab fragment
Source Humanized (from mouse)
Target Dabigatran
Clinical data
Trade names Praxbind
Identifiers
CAS Number 1362509-93-0
ATC code V03AB37 (WHO)
IUPHAR/BPS 8298
ChemSpider none
Chemical data
Formula C2131H3299N555O671S11
Molar mass 47.8 kg/mol

/////Idarucizumab

FDA approves Praxbind, Idarucizumab the first reversal agent for the anticoagulant Pradaxa

October 17, 2015 1:05 am / Leave a comment


10/16/2015 01:07 PM EDT
The FDA has granted accelerated approval to Praxbind (idarucizumab) for use in patients who are taking the anticoagulant Pradaxa (dabigatran) during emergency situations when there is a need to reverse Pradaxa’s blood-thinning effects.

October 16, 2015

Release

The U.S. Food and Drug Administration today granted accelerated approval to Praxbind (idarucizumab) for use in patients who are taking the anticoagulant Pradaxa (dabigatran) during emergency situations when there is a need to reverse Pradaxa’s blood-thinning effects.

“The anticoagulant effects of Pradaxa are important and life-saving for some patients, but there are situations where reversal of the drug’s effects is medically necessary,” said Richard Pazdur, M.D., director of the Office of Hematology and Oncology Products in the FDA’s Center for Drug Evaluation and Research. “Today’s approval offers the medical community an important tool for managing patients taking Pradaxa in emergency or life-threatening situations when bleeding can’t be controlled.”

The FDA approved Pradaxa in 2010 to prevent stroke and systemic blood clots in patients with atrial fibrillation, as well as for the treatment and prevention of deep venous thrombosis and pulmonary embolism. Praxbind is the first reversal agent approved specifically for Pradaxa and works by binding to the drug compound to neutralize its effect. Praxbind solution is for intravenous injection.

The safety and effectiveness of Praxbind were studied in three trials involving a total of 283 healthy volunteers taking Pradaxa (i.e., people who did not require an anticoagulant). In the healthy volunteers who were given Praxbind, there was an immediate reduction in the amount of Pradaxa in participants’ blood (measured as unbound dabigatran plasma concentration) that lasted for a period of at least 24 hours. In this study, the most common side effect from use of Praxbind was headache.

Another trial included 123 patients taking Pradaxa who received Praxbind due to uncontrolled bleeding or because they required emergency surgery. In this ongoing trial, based on laboratory testing, the anticoagulant effect of Pradaxa was fully reversed in 89 percent of patients within four hours of receiving Praxbind. In this patient trial, the most common side effects were low potassium (hypokalemia), confusion, constipation, fever and pneumonia.

Reversing the effect of Pradaxa exposes patients to the risk of blood clots and stroke from their underlying disease (such as atrial fibrillation). The Praxbind labeling recommends patients resume their anticoagulant therapy as soon as medically appropriate, as determined by their health care provider.

Praxbind is approved under the FDA’s accelerated approval program, which allows the agency to approve drugs for serious conditions that fill an unmet medical need based on an effect on a surrogate or an intermediate clinical endpoint that is reasonably likely to predict a clinical benefit to patients. The program is designed to provide patients with earlier access to promising new drugs, but the company will be required to submit additional clinical information after approval to confirm the drug’s clinical benefit.

Praxbind and Pradaxa are both marketed by Boehringer Ingelheim of Ridgefield, Connecticut.

FDA grants breakthrough therapy designation to Boehringer’s Idarucizumab, BI 655075

June 30, 2014 5:04 am / Leave a comment


  • 1-​225-​Immunoglobulin G1, anti-​(dabigatran) (human-​Mus musculus γ1-​chain) (225→219′)​-​disulfide with immunoglobulin G1, anti-​(dabigatran) (human-​Mus musculus κ-​chain)Protein SequenceSequence Length: 444, 225, 219

BI 655075, Idarucizumab

  • Idarucizumab [INN]
  • UNII-97RWB5S1U6

 CAS 1362509-93-0

Treatment of dabigatran associated haemorrhage

 

The US Food and Drug Administration (FDA) has granted breakthrough therapy designation for Boehringer Ingelheim Pharmaceuticals’ idarucizumab, an investigational fully humanised antibody fragment being studied as a specific antidote for Pradaxa.
Boehringer Ingelheim Pharmaceuticals Medicine & Regulatory Affairs senior vice-president Sabine Luik said: “We are committed to innovative research and to advancing care in patients taking Pradaxa.

http://www.pharmaceutical-technology.com/news/newsfda-grants-breakthrough-therapy-designation-boehringers-idarucizumab-4304367

http://apps.who.int/trialsearch/Trial.aspx?TrialID=EUCTR2013-004813-41-EE

http://www.ema.europa.eu/ema/index.jsp?curl=pages/medicines/pips/EMEA-001438-PIP01-13/pip_001159.jsp&mid=WC0b01ac058001d129

  1. IDARUCIZUMAB (BI 655075)
    • What is it?  It is a humanized antibody fragment directed against dabigatran; generated from mouse monoclonal antibody against dabigatran; humanized and reduced to a FAb fragment.
    • What anticoagulant drugs might it reverse?  Dabigatran.
    • Clinical trial status:  (a) A phase 3 study of patients on dabigatran with major bleeding or needing emergency surgery is in the planning stages and will likely start in 2014. (b) A phase 1 study to determine the effect of idarucizumab on coagulation tests in dabigatran-treated healthy volunteers has been completed (NCT01688830), another two are ongoing (NCT01955720; NCT02028780).

June 26, 2014

Pradaxa Antidote, Idarucizumab Designated Breakthrough Therapy

Boehringer Ingelheim announced that the FDA has granted Breakthrough Therapy designation to idarucizumab, an investigational fully humanized antibody fragment (Fab), being evaluated as a specific antidote for Pradaxa (dabigatran etexilate mesylate).

Data from a Phase 1 trial demonstrated that idarucizumab was able to achieve immediate, complete, and sustained reversal of dabigatran-induced anticoagulation in healthy humans. The on-set of action of the antidote was detected immediately following a 5-minute infusion while thrombin time was reversed with idarucizumab. Reversal of the anticoagulation effect was complete and sustained in 7 of 9 subjects who received the 2g dose and in 8 out of 8 subjects who received the 4g dose. The 1g dose resulted in complete reversal of anticoagulation effect; however, after approximately 30 minutes there was some return of the anticoagulation effects of dabigatran.

RELATED: Anticoagulant Dosing Conversions

A global Phase 3 study, RE-VERSE AD, is underway in patients taking Pradaxa who have uncontrolled bleeding or require emergency surgery or procedures. Currently there are no specific antidotes for newer oral anticoagulants.

Pradaxa is approved to reduce the risk of stroke and systemic embolism in non-valvular atrial fibrillation (AF). Treatment of deep vein thrombosis (DVT) and pulmonary embolism (PE) in patients who have been treated with parenteral anticoagulant for 5–10 days. To reduce risk of recurrent DVT/PE in patients who have been previously treated.

For more information call (800) 542-6257 or visit Boehringer-Ingelheim.com.

P/0069/2014: European Medicines Agency decision of 17 March 2014 on the agreement of apaediatric investigation plan and on the granting of a deferral for idarucizumab (EMEA-001438-PIP01-13)