Molecule Details
InChIKeyMBBCVAKAJPKAKM-UHFFFAOYSA-N
Canonical SMILESO=C(NC1CCN(CCCCC2(C(=O)NCC(F)(F)F)c3ccccc3-c3ccccc32)CC1)c1ccccc1-c1ccc(C(F)(F)F)cc1
Clinical Status Data-mined Candidate
Targets (Human+Pathogen)2
Pfam Stratification Cross-Family
Avg pChEMBL8.7
SourceChEMBL;BindingDB
2D Structure
2D structure
Activity Profile
DrugBank Annotations
DrugBank ID DB08827
Drug NameLomitapide
CAS Number182431-12-5
Groups approved investigational
ATC Codes C10AX12
DescriptionLomitapide is a microsomal triglyceride transfer protein (MTP) inhibitor used in homozygous familial hypercholesterolemia (HoFH) patients. It is marketed under the name Juxtapid (R).

Categories: Cytochrome P-450 CYP3A Inhibitors Cytochrome P-450 CYP3A Substrates Cytochrome P-450 CYP3A4 Inhibitors Cytochrome P-450 CYP3A4 Inhibitors (weak) Cytochrome P-450 CYP3A4 Substrates Cytochrome P-450 CYP3A4 Substrates (strength unknown) Cytochrome P-450 CYP3A4 Substrates with a Narrow Therapeutic Index Cytochrome P-450 Enzyme Inhibitors Cytochrome P-450 Substrates Hepatotoxic Agents Heterocyclic Compounds, Fused-Ring Hypolipidemic Agents Hypolipidemic Agents Indicated for Hyperlipidemia Lipid Modifying Agents Lipid Modifying Agents, Plain Microsomal Triglyceride Transfer Protein Inhibitor Microsomal Triglyceride Transfer Protein Inhibitors Narrow Therapeutic Index Drugs Non-statin Hypolipidemic Agents Indicated for Hyperlipidemia P-glycoprotein inhibitors
Cross-references: BindingDB: 50098320 ChEBI: 72297 CHEMBL354541 ChemSpider: 8028764 Drugs Product Database (DPD): 22241 D09637 PharmGKB: PA166114922 PubChem:9853053 PubChem:175427108 RxCUI: 1364479 Wikipedia: Lomitapide ZINC: ZINC000027990463
Target Activities (2)
Target Gene Organism Category Pfam pChEMBL Type Source
Q99707 MTR Homo sapiens Human PF02310 PF02607 PF02965 PF00809 PF02574 9.3 IC50 ChEMBL
P55157 MTTP Homo sapiens Human PF19444 PF01347 8.1 IC50 ChEMBL;BindingDB
DrugBank Target Actions (4)
Target Gene Target Name Action Type
P08684 CYP3A4 Cytochrome P450 3A4 substrate enzymes
P55157 MTTP Microsomal triglyceride transfer protein large subunit antagonist targets
P55157 MTTP Microsomal triglyceride transfer protein large subunit inhibitor targets
P08183 ABCB1 ATP-dependent translocase ABCB1 inhibitor transporters