About: Lomitapide     Goto   Sponge   NotDistinct   Permalink

An Entity of Type : http://linked.opendata.cz/ontology/drugbank/Drug, within Data Space : linked.opendata.cz associated with source document(s)

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http://linked.open...gbank/description
  • Lomitapide is a microsomal triglyceride transfer protein (MTP) inhibitor used in homozygous familial hypercholesterolemia (HoFH) patients. It is marketed under the name Juxtapid (R). (en)
http://linked.open...y/drugbank/dosage
http://linked.open...generalReferences
  • # Cuchel M, Meagher EA, du Toit Theron H, Blom DJ, Marais AD, Hegele RA, Averna MR, Sirtori CR, Shah PK, Gaudet D, Stefanutti C, Vigna GB, Du Plessis AM, Propert KJ, Sasiela WJ, Bloedon LT, Rader DJ: Efficacy and safety of a microsomal triglyceride transfer protein inhibitor in patients with homozygous familial hypercholesterolaemia: a single-arm, open-label, phase 3 study. Lancet. 2012 Nov 1. pii: S0140-6736(12)61731-0. doi: 10.1016/S0140-6736(12)61731-0. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/23122768 # Cuchel M, Bloedon LT, Szapary PO, Kolansky DM, Wolfe ML, Sarkis A, Millar JS, Ikewaki K, Siegelman ES, Gregg RE, Rader DJ: Inhibition of microsomal triglyceride transfer protein in familial hypercholesterolemia. N Engl J Med. 2007 Jan 11;356(2):148-56. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17215532 (en)
http://linked.open...gy/drugbank/group
  • approved (en)
http://linked.open...drugbank/halfLife
  • Lomitapide half-life is about 39.7 hours. (en)
http://linked.open...ugbank/indication
  • Used in homozygous familial hypercholesterolemia (HoFH) patients to reduce low-density lipoprotein cholesterol (LDL-C), total cholesterol (TC), apolipoprotein B (apo B), and non-high-density lipoprotein cholesterol (non-HDL-C). (en)
sameAs
Title
  • Lomitapide (en)
adms:identifier
http://linked.open...mechanismOfAction
  • Within the lumen of the endoplasmic reticulum, lomitapide inhibits microsomal triglyceride transfer protein (MTP), which prevents the formation of apolipoprotein B, and, thus, the formation of VLDL and chylomicrons as well. Altogether, this leads to a reduction of low-density lipoprotein cholesterol. (en)
http://linked.open...y/drugbank/patent
http://linked.open...outeOfElimination
  • About 52.9-59.5% is eliminated by the urine and 33.4-35.1% is eliminated by the feces. (en)
http://linked.open.../drugbank/synonym
  • AEGR 733 (en)
  • BMS 201038 (en)
http://linked.open...drugbank/toxicity
  • Contra-indicated in pregnancy, and moderate to severe hepatic insufficiency (Child-Pugh category B or C). Severe GI adverse reactions may occur. (en)
http://linked.open...umeOfDistribution
  • The steady state volume of distribution is about 985-1292 L. (en)
http://linked.open.../drug/hasAHFSCode
http://linked.open...k/foodInteraction
  • When taking lomitapide with food, the risk of GI side effects is increased. (en)
  • Avoid grapefruit juice, which will likely increase lomitapide plasma concentrations. (en)
http://linked.open...nk/proteinBinding
  • Plasma protein binding is about 99.8% (en)
http://linked.open...ogy/drugbank/salt
  • (en)
foaf:page
http://linked.open...ugbank/IUPAC-Name
http://linked.open...gy/drugbank/InChI
http://linked.open...Molecular-Formula
http://linked.open.../Molecular-Weight
http://linked.open...noisotopic-Weight
http://linked.open...y/drugbank/SMILES
http://linked.open...ogy/drugbank/logP
http://linked.open...l/drug/hasATCCode
http://linked.open...nd-Acceptor-Count
http://linked.open...-Bond-Donor-Count
http://linked.open...drugbank/InChIKey
http://linked.open...urface-Area--PSA-
http://linked.open...nk/Polarizability
http://linked.open...bank/Refractivity
http://linked.open...atable-Bond-Count
http://linked.open...ugbank/absorption
  • In healthy patients, time to maximum lomitapide concentration is about 6 hours with a single dose of 60 mg. Lomitapide has an approximate absolute bioavailability of 7%. (en)
http://linked.open.../affectedOrganism
  • Humans and other mammals (en)
http://linked.open...casRegistryNumber
  • 182431-12-5 (en)
http://linked.open...drugbank/category
  • (en)
http://linked.open...k/Bioavailability
http://linked.open...bank/Ghose-Filter
http://linked.open...nk/MDDR-Like-Rule
http://linked.open...k/Number-of-Rings
http://linked.open...siological-Charge
http://linked.open...bank/Rule-of-Five
http://linked.open...tional-IUPAC-Name
http://linked.open...strongest-acidic-
http://linked.open...-strongest-basic-
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