BioCentury on BioBusiness,
Product Discovery & Development
Small molecules, RNAi enter clinic in race to target PCSK9 for lipid lowering
Monday, April 30, 2012
While antibody inhibitors of
proprotein convertase subtilisin/kexin 9 have begun to report proof-of-concept
data as lipid-lowering agents, other approaches to PCSK9 inhibition are just
now moving into the clinic. Small molecule programs could have an advantage
based on oral dosing, while RNAi-based approaches may prove useful for patients
with higher baseline levels of PCSK9.
The lead mAbs - REGN727 (SAR236553) from Regeneron
Pharmaceuticals Inc. and Sanofi,
Inc.'s AMG 145 - have shown impressive reductions in LDL-C levels when
added to statins. But they require subcutaneous injections once or twice a
month (see Cover Story).
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