AUTHOR OF THIS BLOG

DR ANTHONY MELVIN CRASTO, WORLDDRUGTRACKER

Generic Licensing News, Featured product, Bosentan

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Jun 122013
 

Generic Licensing News

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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.

  1. http://www.tracleer.com/pdf/09%20276%2001%2000%200809_Tra%20PI_4%20Pg_081409pdf.pdf
  2. http://www.ionchannels.org/showabstract.php?pmid=15875338
  3. http://www.ionchannels.org/showabstract.php?pmid=15875338

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Clovis Oncology Shares Double on Trial Data for Cancer Drug,CO-1686

 phase 1, Uncategorized  Comments Off on Clovis Oncology Shares Double on Trial Data for Cancer Drug,CO-1686
Jun 042013
 

Colorado-based Clovis said in a statement today. The drug, CO-1686, is in the first of three phases of testing typically required before U.S. regulatory approval.

http://www.businessweek.com/news/2013-06-03/clovis-oncology-shares-almost-double-on-ovarian-drug-trial-data

by WORLD DRUG TRACKER

DR ANTHONY CRASTO

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Selumetinib is the first drug ever to show significant benefit for patients with advanced uveal melanoma

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Jun 042013
 

Two Array Invented MEK Inhibitors Showcased At ASCO
Sacramento Bee
AstraZeneca began a pivotal trial with selumetinib (an Array-invented drug) in thyroid cancer in May 2013 and expects to begin a Phase 3 trial in non-small cell lung cancer during the second half of 2013.

http://www.sacbee.com/2013/06/03/5466446/two-array-invented-mek-inhibitors.html

Two Array BioPharma-invented MEK inhibitors, selumetinib and MEK162, were showcased at the 49th annual meeting of the American Society of Clinical Oncology (ASCO).

 

by WORLD DRUG TRACKER

DR ANTHONY CRASTO

 

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Experimental Drug Shows Benefits Against Melanoma in Early Study, Lambrolizumab activates body’s immune system to kill cancerous cells, researchers say

 Uncategorized  Comments Off on Experimental Drug Shows Benefits Against Melanoma in Early Study, Lambrolizumab activates body’s immune system to kill cancerous cells, researchers say
Jun 032013
 

Experimental Drug Shows Benefits Against Melanoma in Early Study
U.S. News & World Report
SUNDAY, June 2 (HealthDay News) — A new drug called lambrolizumab appears to improve outcomes in patients with advanced melanoma, according to the results of a phase 1 trial. Lambrolizumab is an antibody that works by revealing the cancer to the immune system so it can mount a response and kill the cancer cells with few serious side effects, the researchers said.

read all at

http://health.usnews.com/health-news/news/articles/2013/06/02/experimental-drug-shows-benefits-against-melanoma-in-early-study

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by WORLD DRUG TRACKER

DR ANTHONY CRASTO

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Discovery of Unexpectedly Active Group-Introduction of a sulfoximine group into anticancer candidates shows that sometimes sticking to the unconventional pays off

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May 312013
 

thumbnail image: Discovery of Unexpectedly Active Group

Introduction of a sulfoximine group into anticancer candidates shows that sometimes sticking to the unconventional pays off

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A Drug Discovery Detective Story-Biological activity of small-molecule RNA polymerase (RNAP) inhibitors revealed to come from polymeric impurity

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May 312013
 

thumbnail image: A Drug Discovery Detective Story

Biological activity of small-molecule RNA polymerase (RNAP) inhibitors revealed to come from polymeric impurity

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Researchers identify novel class of drugs for prostate cancers

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May 292013
 

Photo of Dr. Ganesh Raj, an associate professor of urology at UT Southwestern Medical Center.

http://www.sciencecodex.com/researchers_identify_novel_class_of_drugs_for_prostate_cancers-112935

(Photo Credit: UT Southwestern Medical Center)

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