"目录号: HY-14668
Lomitapide(AEGR-733; BMS-201038)甲磺酸盐是高效MTP蛋白抑制剂，体外IC50值为8nM。
相关产品
SBE-β-CD-MPTP hydrochloride-Cyclosporin A-Etomoxir-Auranofin-GKT137831-Ceruletide-Acetylcysteine-JC-1-BPTES-Brassinolide-FCCP-IPTG-MTT-RSL3 1S,3R--
生物活性
Description
Lomitapide mesylate(AEGR-733; BMS-201038) is an inhibitor of microsomal triglyceride-transfer protein (MTP) wtih in vitro IC50 of 8 nM.IC50 value: 8 nM [1]Target: MTP inhibitorLomitapide is a small-molecule, microsomal triglyceride transfer protein (MTP) inhibitor, for the treatment of both familial and primary hypercholesterolemia. Oral, once-daily lomitapide will be targeted at patients resistant to HMG-CoA reductase inhibitors (statins) either due to abnormalities in liver function or to discontinuation because of muscle pain.
Clinical Trial
Aegerion Pharmaceuticals, Inc.-FDA Office of Orphan Products Development
Homozygous Familial Hypercholesterolemia
December 2007
Phase 3
Aegerion Pharmaceuticals, Inc.
Hypercholesterolemia
May 2008
Phase 2
Aegerion Pharmaceuticals, Inc.
Hypercholesterolemia
May 2006
Phase 2
Aegerion Pharmaceuticals, Inc.
Hyperlipidemia
October 2007
Phase 2
Aegerion Pharmaceuticals, Inc.
Hypercholesterolemia
April 2007
Phase 2
Aegerion Pharmaceuticals, Inc.-FDA Office of Orphan Products Development
Homozygous Familial Hypercholesterolemia
December 2007
Phase 3
Aegerion Pharmaceuticals, Inc.
Hypercholesterolemia
May 2008
Phase 2
Aegerion Pharmaceuticals, Inc.
Hypercholesterolemia
May 2006
Phase 2
Aegerion Pharmaceuticals, Inc.
Hyperlipidemia
October 2007
Phase 2
Aegerion Pharmaceuticals, Inc.
Hypercholesterolemia
April 2007
Phase 2
Aegerion Pharmaceuticals, Inc.
Effect of Atorvastatin on the Pharmacokinetics of Lomitapide
February 2014
Phase 1
Aegerion Pharmaceuticals, Inc.
Familial Hypercholesterolemia - Homozygous
April 2014
Phase 3
Aegerion Pharmaceuticals, Inc.
Healthy
October 2013
Phase 1
Aegerion Pharmaceuticals, Inc.
Homozygous Familial Hypercholesterolemia
March 2014
Aegerion Pharmaceuticals, Inc.
Familial Hypercholesterolemia
September 2009
Phase 3
Aegerion Pharmaceuticals, Inc.
Healthy
February 2014
Phase 1
Aegerion Pharmaceuticals, Inc.
Intra-subject Variability of Pharmacokinetics
August 2013
Phase 1
Aegerion Pharmaceuticals, Inc.
Homozygous Familial Hypercholesterolemia
May 2016
Phase 3
Aegerion Pharmaceuticals, Inc.
Pregnancy
October 2014
Aegerion Pharmaceuticals, Inc.
Homozygous Familial Hypercholesterolemia
April 2015
Aegerion Pharmaceuticals, Inc.-Richmond Pharmacology Limited
Healthy Volunteer
November 2012
Phase 1
Aegerion Pharmaceuticals, Inc.-University of Pennsylvania-Doris Duke Charitable Foundation
Homozygous Familial Hypercholesterolemia
June 2003
Phase 2
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References
[2].Lomitapide. Am J Cardiovasc Drugs. 2011 Oct 1;11(5):347-52.
