This HTML5 document contains 61 embedded RDF statements represented using HTML+Microdata notation.

The embedded RDF content will be recognized by any processor of HTML5 Microdata.

Namespace Prefixes

PrefixIRI
n2http://linked.opendata.cz/resource/drugbank/drug/
dctermshttp://purl.org/dc/terms/
n6http://linked.opendata.cz/resource/AHFS/
foafhttp://xmlns.com/foaf/0.1/
n7http://linked.opendata.cz/resource/drugbank/dosage/
n15http://linked.opendata.cz/resource/drugbank/drug/DB08827/identifier/chebi/
n10http://www.drugs.com/
n11http://www.rxlist.com/
n19http://bio2rdf.org/drugbank:
n17http://linked.opendata.cz/resource/drugbank/drug/DB08827/identifier/wikipedia/
admshttp://www.w3.org/ns/adms#
n4http://linked.opendata.cz/resource/drugbank/patent/
rdfhttp://www.w3.org/1999/02/22-rdf-syntax-ns#
owlhttp://www.w3.org/2002/07/owl#
n3http://linked.opendata.cz/ontology/drugbank/
n8http://linked.opendata.cz/resource/drugbank/property/
n14http://linked.opendata.cz/resource/drugbank/drug/DB08827/identifier/kegg-drug/
n13http://linked.opendata.cz/resource/drugbank/drug/DB08827/identifier/drugbank/
xsdhhttp://www.w3.org/2001/XMLSchema#
n16http://linked.opendata.cz/resource/drugbank/drug/DB08827/identifier/national-drug-code-directory/
n20http://linked.opendata.cz/resource/atc/
n5http://linked.opendata.cz/ontology/sukl/drug/

Statements

Subject Item
n2:DB08827
rdf:type
n3:Drug
n3: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).
n3:dosage
n7:271B5771-363D-11E5-9242-09173F13E4C5 n7:271B5772-363D-11E5-9242-09173F13E4C5 n7:271B5770-363D-11E5-9242-09173F13E4C5
n3: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
n3:group
approved
n3:halfLife
Lomitapide half-life is about 39.7 hours.
n3: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).
owl:sameAs
n19:DB08827
dcterms:title
Lomitapide
adms:identifier
n13:DB08827 n14:D09637 n15:72297 n16:76431-110-01 n17:Lomitapide
n3: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.
n3:patent
n4:5712279 n4:5739135 n4:7932268 n4:6492365
n3:routeOfElimination
About 52.9-59.5% is eliminated by the urine and 33.4-35.1% is eliminated by the feces.
n3:synonym
AEGR 733 BMS 201038
n3:toxicity
Contra-indicated in pregnancy, and moderate to severe hepatic insufficiency (Child-Pugh category B or C). Severe GI adverse reactions may occur.
n3:volumeOfDistribution
The steady state volume of distribution is about 985-1292 L.
n5:hasAHFSCode
n6:24-06-92
n3:foodInteraction
Avoid grapefruit juice, which will likely increase lomitapide plasma concentrations. When taking lomitapide with food, the risk of GI side effects is increased.
n3:proteinBinding
Plasma protein binding is about 99.8%
n3:salt
foaf:page
n10:juxtapid.html n11:juxtapid-drug.htm
n3:IUPAC-Name
n8:271B5774-363D-11E5-9242-09173F13E4C5
n3:InChI
n8:271B577A-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n8:271B5779-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n8:271B5776-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n8:271B5777-363D-11E5-9242-09173F13E4C5
n3:SMILES
n8:271B5778-363D-11E5-9242-09173F13E4C5
n3:logP
n8:271B5773-363D-11E5-9242-09173F13E4C5
n5:hasATCCode
n20:C10AX12
n3:H-Bond-Acceptor-Count
n8:271B5780-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n8:271B5781-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n8:271B577B-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n8:271B577C-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n8:271B577E-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n8:271B577D-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n8:271B577F-363D-11E5-9242-09173F13E4C5
n3: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%.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
182431-12-5
n3:category
n3:Bioavailability
n8:271B5786-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n8:271B5788-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n8:271B5789-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n8:271B5785-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n8:271B5784-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n8:271B5787-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n8:271B5775-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n8:271B5782-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n8:271B5783-363D-11E5-9242-09173F13E4C5