Thursday, May 2, 2013
This week in therapeutics
Publication and contact
SEC24 family member A (SEC24A); proprotein
convertase subtilisin/kexin type 9 (PCSK9);
lipoprotein receptor (LDLR)
Mouse studies suggest
inhibiting SEC24A could help treat hypercholesterolemia and related metabolic
indications. In mice, a Sec24a deficiency decreased hepatic secretion of Pcsk9
and increased Ldlr expression compared with no Sec24a deficiency. In the
Sec24a-deficient mice, circulating levels of high-density lipoprotein,
low-density lipoprotein and total cholesterol were lower than those in
nondeficient controls. Next steps include testing the effects of SEC24A
knockdown in human hepatocytes.
AMG 145, a human mAb against
PCSK9 from Amgen
Inc., is in Phase III testing to treat
hypercholesterolemia, hyperlipidemia and dyslipidemia.
a human mAb targeting PCSK9 from Regeneron
Pharmaceuticals Inc. and Sanofi,
is in Phase III testing to treat hypercholesterolemia.
a PCSK9 inhibitor from Pfizer
Inc., is in Phase II testing to treat hypercholesterolemia
and acute coronary syndrome.
Published online May 2, 2013
Unpatented; available for
partnering or licensing from the University
Contact: Robin Rasor, University of
Michigan, Ann Arbor, Mich.
Chen, X.-W. et al. eLife;
published online April 9, 2013;
Contact: David Ginsburg, University of Michigan, Ann Arbor,
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