lomitapide Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
microsomal triglyceride transfer protein (MTP) inhibitors 4721 182431-12-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • lomitapide
  • juxtapid
  • BMS-201038
  • lomitapide mesylate
  • lojuxta
  • lomitapide mesilate
  • BMS201038
  • BMS 201038
an anticholesteremic agent and microsomal triglycide transfer protein inhibitor
  • Molecular weight: 693.73
  • Formula: C39H37F6N3O2
  • CLOGP: 7
  • LIPINSKI: 2
  • HAC: 5
  • HDO: 2
  • TPSA: 61.44
  • ALOGS: -6.89
  • ROTB: 12

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
40 mg O

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 16.30 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 8.70 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.00 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 39.70 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Dec. 21, 2012 FDA AEGERION

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Therapy cessation 1086.01 38.30 279 3558 26350 46655875
Weight decreased 414.73 38.30 240 3597 210609 46471616
Diarrhoea 360.93 38.30 322 3515 559280 46122945
Product used for unknown indication 205.43 38.30 36 3801 503 46681722
Flatulence 201.05 38.30 79 3758 28799 46653426
Low density lipoprotein increased 191.07 38.30 52 3785 5948 46676277
Diet noncompliance 129.46 38.30 22 3815 253 46681972
Abdominal pain upper 114.86 38.30 95 3742 145210 46537015
Inappropriate schedule of product administration 110.83 38.30 68 3769 64945 46617280
Blood cholesterol increased 97.94 38.30 53 3784 39960 46642265
Nausea 94.36 38.30 186 3651 687268 45994957
Product dose omission issue 71.21 38.30 78 3759 168442 46513783
Product administered to patient of inappropriate age 57.04 38.30 17 3820 2679 46679546
Abdominal discomfort 57.02 38.30 66 3771 151099 46531126
Abdominal distension 49.68 38.30 44 3793 73307 46608918
Hepatic enzyme increased 47.47 38.30 45 3792 81742 46600483
Non-high-density lipoprotein cholesterol increased 44.84 38.30 8 3829 124 46682101
Liver function test increased 44.31 38.30 26 3811 22800 46659425

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Therapy cessation 499.15 53.67 125 1627 15012 29935714
Weight decreased 349.36 53.67 170 1582 150751 29799975
Diarrhoea 210.61 53.67 164 1588 333939 29616787
Product used for unknown indication 186.04 53.67 30 1722 356 29950370
Flatulence 132.87 53.67 47 1705 18082 29932644
Low density lipoprotein increased 111.13 53.67 29 1723 3987 29946739
Product dose omission issue 101.07 53.67 64 1688 91567 29859159
Diet noncompliance 89.98 53.67 14 1738 129 29950597
Abdominal discomfort 63.59 53.67 38 1714 48753 29901973
Blood cholesterol increased 63.37 53.67 27 1725 16943 29933783
Inappropriate schedule of product administration 57.15 53.67 33 1719 39695 29911031
Product administered to patient of inappropriate age 54.42 53.67 15 1737 2528 29948198

Pharmacologic Action:

SourceCodeDescription
ATC C10AX12 CARDIOVASCULAR SYSTEM
LIPID MODIFYING AGENTS
LIPID MODIFYING AGENTS, PLAIN
Other lipid modifying agents
FDA MoA N0000182141 Cytochrome P450 3A4 Inhibitors
FDA MoA N0000185503 P-Glycoprotein Inhibitors
FDA MoA N0000186778 Microsomal Triglyceride Transfer Protein Inhibitors
FDA EPC N0000186779 Microsomal Triglyceride Transfer Protein Inhibitor
CHEBI has role CHEBI:35821 hypocholesteremic agent
CHEBI has role CHEBI:72298 microsomal triglyceride transfer protein inhibitors

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Familial hypercholesterolemia - homozygous indication 238078005

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.28 acidic
pKa2 13.97 acidic
pKa3 8.71 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Microsomal triglyceride transfer protein large subunit Cytosolic other INHIBITOR IC50 8.10 WOMBAT-PK CHEMBL

External reference:

IDSource
D09637 KEGG_DRUG
4032035 VUID
N0000186142 NUI
202914-84-9 SECONDARY_CAS_RN
4032035 VANDF
C1176233 UMLSCUI
CHEBI:72297 CHEBI
CHEMBL354541 ChEMBL_ID
CHEMBL2105662 ChEMBL_ID
DB08827 DRUGBANK_ID
C473731 MESH_SUPPLEMENTAL_RECORD_UI
9853053 PUBCHEM_CID
7439 IUPHAR_LIGAND_ID
9120 INN_ID
82KUB0583F UNII
1364478 RXNORM
196706 MMSL
29025 MMSL
30485 MMSL
d07939 MMSL
014810 NDDF
014811 NDDF
716228008 SNOMEDCT_US
716229000 SNOMEDCT_US
864003008 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Juxtapid HUMAN PRESCRIPTION DRUG LABEL 1 76431-105 CAPSULE 5 mg ORAL NDA 33 sections
Juxtapid HUMAN PRESCRIPTION DRUG LABEL 1 76431-110 CAPSULE 10 mg ORAL NDA 33 sections
Juxtapid HUMAN PRESCRIPTION DRUG LABEL 1 76431-120 CAPSULE 20 mg ORAL NDA 33 sections
Juxtapid HUMAN PRESCRIPTION DRUG LABEL 1 76431-130 CAPSULE 30 mg ORAL NDA 33 sections
Juxtapid HUMAN PRESCRIPTION DRUG LABEL 1 76431-140 CAPSULE 40 mg ORAL NDA 33 sections
Juxtapid HUMAN PRESCRIPTION DRUG LABEL 1 76431-160 CAPSULE 60 mg ORAL NDA 33 sections