"目录号: HY-14668
Others-
Lomitapide(AEGR-733; BMS-201038)甲磺酸盐是高效MTP蛋白抑制剂，体外IC50值为8nM。
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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--
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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
NCT00730236
Aegerion Pharmaceuticals, Inc.-FDA Office of Orphan Products Development
Homozygous Familial Hypercholesterolemia
December 2007
Phase 3
NCT00690443
Aegerion Pharmaceuticals, Inc.
Hypercholesterolemia
May 2008
Phase 2
NCT00405067
Aegerion Pharmaceuticals, Inc.
Hypercholesterolemia
May 2006
Phase 2
NCT00559962
Aegerion Pharmaceuticals, Inc.
Hyperlipidemia
October 2007
Phase 2
NCT00474240
Aegerion Pharmaceuticals, Inc.
Hypercholesterolemia
April 2007
Phase 2
NCT00730236
Aegerion Pharmaceuticals, Inc.-FDA Office of Orphan Products Development
Homozygous Familial Hypercholesterolemia
December 2007
Phase 3
NCT00690443
Aegerion Pharmaceuticals, Inc.
Hypercholesterolemia
May 2008
Phase 2
NCT00405067
Aegerion Pharmaceuticals, Inc.
Hypercholesterolemia
May 2006
Phase 2
NCT00559962
Aegerion Pharmaceuticals, Inc.
Hyperlipidemia
October 2007
Phase 2
NCT00474240
Aegerion Pharmaceuticals, Inc.
Hypercholesterolemia
April 2007
Phase 2
NCT02080455
Aegerion Pharmaceuticals, Inc.
Effect of Atorvastatin on the Pharmacokinetics of Lomitapide
February 2014
Phase 1
NCT02173158
Aegerion Pharmaceuticals, Inc.
Familial Hypercholesterolemia - Homozygous
April 2014
Phase 3
NCT02044419
Aegerion Pharmaceuticals, Inc.
Healthy
October 2013
Phase 1
NCT02135705
Aegerion Pharmaceuticals, Inc.
Homozygous Familial Hypercholesterolemia
March 2014
NCT00943306
Aegerion Pharmaceuticals, Inc.
Familial Hypercholesterolemia
September 2009
Phase 3
NCT02080468
Aegerion Pharmaceuticals, Inc.
Healthy
February 2014
Phase 1
NCT01915771
Aegerion Pharmaceuticals, Inc.
Intra-subject Variability of Pharmacokinetics
August 2013
Phase 1
NCT02765841
Aegerion Pharmaceuticals, Inc.
Homozygous Familial Hypercholesterolemia
May 2016
Phase 3
NCT02399839
Aegerion Pharmaceuticals, Inc.
Pregnancy
October 2014
NCT02399852
Aegerion Pharmaceuticals, Inc.
Homozygous Familial Hypercholesterolemia
April 2015
NCT01760187
Aegerion Pharmaceuticals, Inc.-Richmond Pharmacology Limited
Healthy Volunteer
November 2012
Phase 1
NCT01556906
Aegerion Pharmaceuticals, Inc.-University of Pennsylvania-Doris Duke Charitable Foundation
Homozygous Familial Hypercholesterolemia
June 2003
Phase 2
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References
[1].Sulsky R, et al. 5-Carboxamido-1,3,2-dioxaphosphorinanes, potent inhibitors of MTP. Bioorg Med Chem Lett. 2004 Oct 18;14(20):5067-70.
[2].Lomitapide. Am J Cardiovasc Drugs. 2011 Oct 1;11(5):347-52.
[3].Perry CM. Lomitapide: a review of its use in adults with homozygous familial hypercholesterolemia. Am J Cardiovasc Drugs. 2013 Aug;13(4):285-96.