Tag Archives: Phase II

TAK-733 & CH4987655 (Allosteric MEK Inhibitors)

Posted on February 4, 2011 by mcb

The mitogen-activated protein kinase (MAPK) signalling cascade is one of the key pathways regulating cell proliferation and differentiation and aberrant activation of this pathway is implicated in a number of cancers. Targeting components of the cascade thus has the potential … Continue reading →

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Discovery of PF-232798 (CCR5 Antagonist)

Posted on January 6, 2011 by mcb

CCR5 antagonists prevent entry of HIV into host cells by binding to the CCR5 co-receptor and stopping the gp120-CD4 complex from making the crucial interaction with CCR5 that leads to fusion of the viral and host cell membranes (see Wikipedia article … Continue reading →

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Discovery of LX2931 (Sphingosine 1-Phosphate Lyase Inhibitor) & Phase IIa Data

Posted on December 20, 2010 by mcb

Fingolimod (FTY720, Gilenya), an immunosuppresive agent with activity purported to be mediated by binding of it’s phosphorylated derivative to the sphingosine-1-phosphate receptor 1 (S1P1), was approved earlier in the year as the first orally administered disease modifying therapy for the treatment … Continue reading →

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Discovery of PF-04457845 (FAAH Inhibitor)

Posted on December 15, 2010 by mcb

In this latest publication from the Pfizer labs, the authors describe their continuing efforts to identify urea-based, irreversible inhibitors of fatty acid amide hydrolase (FAAH).  Inhibition of FAAH and the concomitant elevation of endogenous levels of fatty acid amides has … Continue reading →

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