Elucidating Heterocyclic Chemistry in Pharmaceuticals

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Jun 162013

Researchers at the Scripps Research Institute advance heteorcylic chemistry trhough new reagents and reaction-tracking techniques.

http://www.pharmtech.com/pharmtech/Ingredients+Insider/Elucidating-Heterocyclic-Chemistry-in-Pharmaceutic/ArticleStandard/Article/detail/814894?contextCategoryId=43497

jun 2, 2013
By: Patricia Van Arnum
Pharmaceutical Technology

Patricia Van Arnum

Heterocyclic compounds play an important role in medicinal chemistry and drug synthesis. Like any important functional class of compounds, developments that facilitate their production or elucidate their reaction mechanisms are significant for process chemists in the pharmaceutical industry. In two separate developments, researchers at The Scripps Research Institute (TSRI) in La Jolla, California recently reported on the use of zinc sulfinates as reagents for the direct chemical functionalization of nitrogen-based heterocycles and on reaction-tracking tools to better elucidate copper-catalyzed reactions in making triazoles.

The art of antibody process development –Drug Discovery Today

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Jun 152013

Figure 1. Schematic of an antibody. Pfizer’s developmental compound tremelimumab is an antibody of subclass IgG2 and is composed of four proteins linked by disulfide bonds. Many antibodies are glycosylated, meaning that polysaccharide structures are covalently attached to the proteins at distinct sites. An antibody can have several domains that have activity, including the variable regions on the arms of the heavy and light chains, which bind to antigens, and the Fc domains, which can mediate effector functions. Adapted with permission from Pfizer, Inc.

S1359644608001475

The art of antibody process development

Drug Discovery Today

Volume 13, Issues 13–14, July 2008, Pages 613–618

Global Biologics, Pfizer Global Research & Development, Chesterfield, MO, United States
Biopharmaceutical drug development is an intricate path that spans a dozen years from discovery through registration. The development of a therapeutic antibody presents substantial challenges, particularly with respect to the creation and implementation of manufacturing process technologies. Process development and large scale biotherapeutic manufacturing is an art generally only practiced within industry. As a consequence, these technologies may be seen as something of a ‘black box’ by many in the medical community. This article provides insight into the current art of antibody process development leading to market entry of novel, life-saving medicines.
http://www.sciencedirect.com/science/article/pii/S1359644608001475

http://dx.doi.org/10.1016/j.drudis.2008.04.005,

Cempra Provides Guidance on the Clinical Program Required for Regulatory Approval for Solithromycin for Community-Acquired Bacterial Pneumonia (CABP)

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Jun 142013

solithromycin

(3aS,4R,7S,9R,10R,11R,13R,15R,15aR)-1-[4-[4-(3-aminophenyl)-1H-1,2,3-triazol-1-yl]butyl]-4-ethyl-7-fluorooctahydro-11-methoxy-3a,7,9,11,13,15-hexamethyl-10-{[3,4,6-trideoxy-3-(dimethylamino)-β-D–xylo-hexopyranosyl]oxy}-2H-Oxacyclotetradecino[4,3-d]oxazole-2,6,8,14(1H,7H,9H)-tetrone

Identifiers

Legal status	Phase III clinical trials, North America, South America, Europe
Routes	oral, intravenous
CAS number	760981-83-7

Cempra Provides Guidance on the Clinical Program Required for Regulatory …
The Herald | HeraldOnline.com
The Phase 3 solithromycin clinical program in CABP will be planned to consist of an oral trial and an intravenous (IV)-to-oral clinical trial. Cempra followed the CABP guidance that the FDA proposed in a November, 2011, meeting of the Anti-Infective …

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http://www.heraldonline.com/2013/06/13/4944834/cempra-provides-guidance-on-the.html

Solithromycin (formerly known as CEM-101 and OP-1068) is a novel ketolide antibiotic undergoing clinical development for the treatment of community-acquired pneumonia (CAP) and other infections.It is expected to be the first macrolide antibiotic available in intravenous, oral, and pediatric suspension formulations in over 20 years.

Solithromycin exhibits excellent in vitro activity against a broad spectrum of Gram-positive respiratory tract pathogens, including macrolide-resistant strains. Solithromycin has activity against a wide variety of pathogens, and further research is being conducted for other infections.

May 2011: Solithromycin is in a Phase 2 clinical trial for serious community-acquired bacterial pneumonia (CABP) and in a Phase 1 clinical trial with an intravenous formulation.

September 2011 : Encouraging results from the phase 2 clinical trial versus levofloxacin were reported.

DRUG SCALEUP AND MANUFACTURING INTERNATIONAL BY DR ANTHONY M CRASTO, WORLD DRUG TRACKER

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Jun 142013

http://drug-scaleup-and-manufacturing.webnode.com/news/my-website-on-scaleup-of-organic-compounds/

Tumor Immunotherapy Efficacy Increased In Both Breast And Prostate Cancer Preclinical Models With Addition Of Galectin Inhibitor

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Jun 132013

Tumor Immunotherapy Efficacy Increased In Both Breast And Prostate Cancer …
Daily Markets
NORCROSS, Ga., June 12, 2013 /PRNewswire-USNewswire/ — Galectin Therapeutics (GALT), the leading developer of therapeutics that target galectin proteins to treat fibrosis and cancer, today announced that preclinical studies have shown that … The …

http://www.dailymarkets.com/stock/2013/06/12/tumor-immunotherapy-efficacy-increased-in-both-breast-and-prostate-cancer-preclinical-models-with-addition-of-galectin-inhibitor/

Aphios, VivaCell to Develop Cannabinoid-Based Drugs for MS, CNS Disorders

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Jun 132013

Aphios, VivaCell to Develop Cannabinoid-Based Drugs for MS, CNS Disorders
Genetic Engineering News
Aphios and VivaCell have executed research and commercialization agreements to develop these drug candidates through preclinical studies, clinical development, and commercialization in the U.S. and Europe. Researchers at the University of Córdoba and …

http://www.genengnews.com/gen-news-highlights/aphios-vivacell-to-develop-cannabinoid-based-drugs-for-ms-cns-disorders/81248471/

Emory University launches drug commercialization venture

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Jun 132013

Emory University

Urvaksh Karkaria: Staff Writer- Atlanta Business Chronicle

Emory University launches drug commercialization venture

DRIVE will provide the financial, business, project management and regulatory expertise to effectively move drugs through pre-clinical testing – a stage of drug development often termed the “Valley of Death” — and into proof-of-concept clinical trials.

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http://www.bizjournals.com/atlanta/blog/a-healthy-conversation/2013/06/emory-university-launches.html

Celgene arthritis drug maintains efficacy at 52 weeks-study

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Jun 132013

apremilast

Celgene arthritis drug maintains efficacy at 52 weeks-study
Reuters
The U.S. biotechnology company had previously released positive data from the 500-patient Phase III trial called Palace-1 that compared its drug, apremilast, to a placebo through 16 weeks of treatment. The data being presented at the European League …

http://in.reuters.com/article/2013/06/11/celgene-arthritis-idINL2N0EN21P20130611

Apremilast is an orally available small molecule inhibitor of PDE4 being developed by Celgene for ankylosing spondylitis, psoriasis, and psoriatic arthritis.The drug is currently in phase III trials for the three indications. Apremilast, an anti-inflammatory drug, specifically inhibits phosphodiesterase 4. In general the drug works on an intra-cellular basis to moderate proinflammatory and anti-inflammatory mediator production.

Medical Use [Apremilast is being tested for its efficacy in treating “psoriasis, psoriatic arthritis and other chronic inflammatory diseases such as ankylosing spondylitis, Behcet’s disease, and rheutmatoid arthritis.”

Apremilast is being tested for its efficacy in treating “psoriasis, psoriatic arthritis and other chronic inflammatory diseases such as ankylosing spondylitis, Behcet’s disease, and rheutmatoid arthritis.”

Generic Licensing News, Featured product, Bosentan

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Jun 122013

Generic Licensing News

http://www.leadformix.com/ef1/preview_campaign.php?lf1=900485181e199412625317a3906967

Click here to contact Zack Systems SpA about this product.

BOSENTAN

Bosentan is a dual endothelin receptor antagonist important in the treatment of pulmonary artery hypertension (PAH).

Bosentan belongs to a class of drugs known as endothelin receptor antagonists (ERAs). Patients with PAH have elevated levels of endothelin, a potent blood vessel constrictor, in their plasma and lung tissue. Bosentan blocks the binding of endothelin to its receptors, thereby negating endothelin’s deleterious effects.

bosentan

Bosentan is a dual endothelin receptor antagonist used in the treatment of pulmonary artery hypertension (PAH). It is licensed in the United States, the European Union and other countries by Actelion Pharmaceuticals for the management of PAH under the trade name Tracleer.

Bosentan is indicated mainly for the treatment of pulmonary hypertension. In 2007, bosentan was approved in the European Union also for reducing the number of new digital ulcers in patients with systemic sclerosis and ongoing digital ulcer disease.Bosentan is a competitive antagonist of endothelin-1 at the endothelin-A (ET-A) and endothelin-B (ET-B) receptors. Under normal conditions, endothelin-1 binding of ET-A or ET-B receptors causes pulmonary vasoconstriction. By blocking this interaction, bosentan decreases pulmonary vascular resistance. Bosentan has a slightly higher affinity for ET-A than ET-B.

In the United States, bosentan is indicated for the treatment of pulmonary arterial hypertension (WHO Group I) in patients with WHO Class II-IV symptoms, to improve exercise capacity and decrease the rate of clinical worsening.^[1]

Warnings

Due to potential hepatotoxicity, the FDA requires monthly monitoring of liver function tests while taking Bosentan.

Bosentan use requires hematocrit monitoring due to potential onset of anemia. ^[2]

Hormone-based contraception is not possible in women taking Bosentan, due to a pharmacokinetic interaction. ^[3]

Bosentan is absolutely contraindicated in pregnancy because of its teratogenicity. Category X.

volleyball

ViroPharma Receives Orphan Drug Designation For Maribavir In Europe

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Jun 122013

Maribavir

ViroPharma Receives Orphan Drug Designation For Maribavir In Europe
The Herald | HeraldOnline.com
We commend the European Commission for providing incentives such as this for the development of drugs for rare and life threatening diseases.” ViroPharma is currently conducting two Phase 2 dose ranging studies of oral maribavir at one of three doses …

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http://www.heraldonline.com/2013/06/11/4934867/viropharma-receives-orphan-drug.html

Maribavir (originally named 1263W94) is an experimental oral antiviral drug candidate licensed by ViroPharma from GlaxoSmithKline in 2003 for the prevention and treatment of human cytomegalovirus (HCMV) disease in hematopoietic stem cell/bone marrow transplant patients. The mechanism by which maribavir inhibits HCMV replication is by inhibition of an HCMV encoded protein kinase enzyme called UL97 or pUL97. Maribavir showed promise in Phase II clinical trials and was granted fast track status, but failed to meet study goals in a Phase III trial. However, the dosage used in the Phase III trial may have been too low to be efficacious.

A Phase II study with maribavir demonstrated that prophylaxis with maribavir displayed strong antiviral activity, as measured by statistically significant reduction in the rate of reactivation of CMV in recipients of hematopoietic stem cell/bone marrow transplants. In an intent-to-treat analysis of the first 100 days after the transplant, the number of subjects who required pre-emptive anti-CMV therapy was statistically significantly reduced with maribavir compared to placebo.

ViroPharma conducted a Phase III clinical study to evaluate the prophylactic use for the prevention of cytomegalovirus disease in recipients of allogeneic stem cell transplant patients. In February 2009, ViroPharma announced that the Phase III study failed to achieve its goal, showing no significant difference between maribavir and a placebo at reducing the rate at which CMV DNA levels were detected in patients.