21:04 , Jan 15, 2019 |  BC Innovations  |  Distillery Therapeutics

Cancer

INDICATION: Brain cancer In vitro , patient sample, cell culture and rat studies identified an inhibitor of thrombin-mediated PAR1 activation that could help treat glioblastoma. In tumor samples from patients, PAR1 expression was higher than...
20:33 , May 23, 2017 |  BC Innovations  |  Distillery Techniques

Drug platforms

TECHNOLOGY: Structural analyses Crystallographic analyses of a PAR2 variant bound to PAR2 inhibitors could guide the design of therapies for cancer, inflammation and other PAR2-dependent diseases. The PAR2 variant contained point mutations in nine thermostabilizing...
23:34 , May 1, 2017 |  BC Extra  |  Clinical News

Paper identifies MOA of PAR2 antagonists

In a paper published in Nature , researchers at the Heptares Therapeutics Ltd. subsidiary of Sosei Group Corp. (Tokyo:4565) and AstraZeneca plc (LSE:AZN; NYSE:AZN) identified the binding mechanism of two protease-activated receptor 2 (PAR2) antagonists,...
07:00 , Sep 15, 2016 |  BC Innovations  |  Targets & Mechanisms

KOR-recting MS

Although the failed Phase II multiple sclerosis trial of Biogen Inc. 's anti-LINGO mAb in June dealt a blow to myelin repair, a slew of compounds acting by different mechanisms lies behind it in clinical...
07:00 , Sep 12, 2016 |  BC Week In Review  |  Company News

Merck, Aralez deal

Aralez purchased U.S. and Canadian rights to Zontivity vorapaxar from Merck. The protease-activated receptor 1 (PAR1) antagonist that inhibits thrombin-induced platelet activation is approved to reduce thrombotic cardiovascular events in patients with a history of...
07:00 , Aug 22, 2016 |  BC Week In Review  |  Company News

Merck sales and marketing update

Merck said it will discontinue marketing Zontivity vorapaxar in the U.S., effective Sept. 2. Merck said the decision was for “business reasons” and not related to safety and efficacy of Zontivity. As a result of...
07:00 , Jul 11, 2016 |  BC Week In Review  |  Clinical News

Zontivity vorapaxar regulatory update

EMA’s CHMP recommended expanding the label of Zontivity vorapaxar from Merck to include reduction of atherothrombotic events in adults with symptomatic peripheral arterial disease (PAD). The protease-activated receptor 1 (PAR1) antagonist that inhibits thrombin-induced platelet...
07:00 , Aug 27, 2015 |  BC Innovations  |  Distillery Techniques

Techniques: Atomic force microscopy (AFM) for measuring GPCR-ligand binding in lipid membranes

Assays and screens TECHNOLOGY: Binding assays An AFM-based method could measure binding affinities between ligands and GPCRs in lipid membranes. The method involves attaching a GPCR ligand to the tip of an oscillating cantilever moving...
08:00 , Mar 2, 2015 |  BC Week In Review  |  Clinical News

Zontivity vorapaxar: Additional Phase III data

Additional data from 3,623 patients with diabetes mellitus and a prior MI and without a history of stroke or transient ischemic attack in the double-blind Phase III TRA 2P-TIMI 50 trial showed that Zontivity vorapaxar...
08:00 , Feb 12, 2015 |  BC Innovations  |  Translation in Brief

Heptares up to PAR2

Heptares Therapeutics Ltd. has solved the long sought-after X-ray structure of Protease-activated receptor ( PAR2 ), a difficult-to-express GPCR that is activated by proteolytic cleavage. Now its partner AstraZeneca plc has used the structure to...