Thursday, November 8, 2012
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Bromodomain containing 4 (BRD4);
In vitro and rodent studies identified BRD4 inhibitors that
could help treat inflammation. Fragment-based screening, chemical synthesis
and in vitro testing of sulfonamide analogs of quinazolinone
identified a lead compound as a nanomolar inhibitor of BRD4. In a human
monocyte-based inflammation assay, the lead compound blocked lipopolysaccharide
IL-6 production with a low micromolar EC50 value. In normal mice
and rats, the lead compound showed oral bioavailability and good
pharmacokinetics. Future studies could include testing the compound in animal
models of inflammation.
an inhibitor of the bromodomain and extra terminal domain
family of bromodomain-containing proteins including BRD4, is in Phase II
testing to treat diabetes and atherosclerosis and Phase I testing to treat
Alzheimer's disease (AD).
Mitsubishi Tanabe Pharma Corp.
S.A. have OTX015,
a synthetic small molecule inhibitor of BET BRD2,
and BRD4, in Phase I testing to treat cancer.
Published online Nov. 8, 2012
Patent and licensing status
Fish, P. et al. J. Med.
published online Oct. 25, 2012;
Contact: Dafydd R. Owen,
Pfizer Worldwide R&D, Cambridge, Mass.
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