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Identification
NameLomitapide
Accession NumberDB08827
TypeSmall Molecule
GroupsApproved
DescriptionLomitapide is a microsomal triglyceride transfer protein (MTP) inhibitor used in homozygous familial hypercholesterolemia (HoFH) patients. It is marketed under the name Juxtapid (R).
Structure
Thumb
Synonyms
AEGR 733
BMS 201038
External Identifiers
  • AEGR-773
  • BMS 201038
  • BMS-201038-04
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
JuxtapidCapsule40 mg/1OralAegerion Pharmaceuticals, Inc.2013-01-03Not applicableUs
JuxtapidCapsule5 mgOralAegerion Pharmaceuticals Canada Ltd2014-05-06Not applicableCanada
JuxtapidCapsule10 mg/1OralAegerion Pharmaceuticals, Inc.2013-01-03Not applicableUs
JuxtapidCapsule60 mg/1OralAegerion Pharmaceuticals, Inc.2013-01-03Not applicableUs
JuxtapidCapsule10 mgOralAegerion Pharmaceuticals Canada Ltd2014-05-06Not applicableCanada
JuxtapidCapsule20 mg/1OralAegerion Pharmaceuticals, Inc.2013-01-03Not applicableUs
JuxtapidCapsule20 mgOralAegerion Pharmaceuticals Canada Ltd2014-05-06Not applicableCanada
JuxtapidCapsule30 mg/1OralAegerion Pharmaceuticals, Inc.2013-01-03Not applicableUs
JuxtapidCapsule5 mg/1OralAegerion Pharmaceuticals, Inc.2013-01-03Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
LojuxtaNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Lomitapide mesylate
202914-84-9
Thumb
  • InChI Key: QKVKOFVWUHNEBX-UHFFFAOYSA-N
  • Monoisotopic Mass: 789.267111357
  • Average Mass: 789.826
DBSALT000110
Categories
UNII82KUB0583F
CAS number182431-12-5
WeightAverage: 693.7204
Monoisotopic: 693.278996673
Chemical FormulaC39H37F6N3O2
InChI KeyMBBCVAKAJPKAKM-UHFFFAOYSA-N
InChI
InChI=1S/C39H37F6N3O2/c40-38(41,42)25-46-36(50)37(33-13-5-3-10-30(33)31-11-4-6-14-34(31)37)21-7-8-22-48-23-19-28(20-24-48)47-35(49)32-12-2-1-9-29(32)26-15-17-27(18-16-26)39(43,44)45/h1-6,9-18,28H,7-8,19-25H2,(H,46,50)(H,47,49)
IUPAC Name
N-(2,2,2-trifluoroethyl)-9-[4-(4-{2-[4-(trifluoromethyl)phenyl]benzamido}piperidin-1-yl)butyl]-9H-fluorene-9-carboxamide
SMILES
FC(F)(F)CNC(=O)C1(CCCCN2CCC(CC2)NC(=O)C2=C(C=CC=C2)C2=CC=C(C=C2)C(F)(F)F)C2=CC=CC=C2C2=CC=CC=C12
Pharmacology
IndicationUsed 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).
Structured Indications
PharmacodynamicsLomitapide directly inhibits microsomal triglyceride transfer protein (MTP).
Mechanism of actionWithin 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.
TargetKindPharmacological actionActionsOrganismUniProt ID
Microsomal triglyceride transfer protein large subunitProteinyes
antagonist
HumanP55157 details
Related Articles
AbsorptionIn 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%.
Volume of distribution

The steady state volume of distribution is about 985-1292 L.

Protein bindingPlasma protein binding is about 99.8%
Metabolism

Lomitapide is mainly metabolized by CYP3A4 to it's inactive metabolites, M1 and M3. CYP enzymes that metabolize lomitapide to a minor extent include CYP 1A2,2B6,2C8,2C19.

Route of eliminationAbout 52.9-59.5% is eliminated by the urine and 33.4-35.1% is eliminated by the feces.
Half lifeLomitapide half-life is about 39.7 hours.
ClearanceNot Available
ToxicityContra-indicated in pregnancy, and moderate to severe hepatic insufficiency (Child-Pugh category B or C). Severe GI adverse reactions may occur.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
AcebutololThe serum concentration of Acebutolol can be increased when it is combined with Lomitapide.Approved
AcetaminophenThe serum concentration of Acetaminophen can be increased when it is combined with Lomitapide.Approved
Acetylsalicylic acidThe serum concentration of Acetylsalicylic acid can be increased when it is combined with Lomitapide.Approved, Vet Approved
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Lomitapide.Approved
AldosteroneThe serum concentration of Aldosterone can be increased when it is combined with Lomitapide.Experimental
AlitretinoinThe serum concentration of Alitretinoin can be increased when it is combined with Lomitapide.Approved, Investigational
AlprazolamThe serum concentration of Lomitapide can be increased when it is combined with Alprazolam.Approved, Illicit, Investigational
AmbrisentanThe serum concentration of Ambrisentan can be increased when it is combined with Lomitapide.Approved, Investigational
AmiodaroneThe serum concentration of Lomitapide can be increased when it is combined with Amiodarone.Approved, Investigational
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Lomitapide.Approved
AmlodipineThe serum concentration of Lomitapide can be increased when it is combined with Amlodipine.Approved
ApixabanThe serum concentration of Apixaban can be increased when it is combined with Lomitapide.Approved
AprepitantThe serum concentration of Lomitapide can be increased when it is combined with Aprepitant.Approved, Investigational
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Lomitapide.Approved, Investigational
Arsenic trioxideThe serum concentration of Arsenic trioxide can be increased when it is combined with Lomitapide.Approved, Investigational
AtazanavirThe serum concentration of Lomitapide can be increased when it is combined with Atazanavir.Approved, Investigational
AtenololThe serum concentration of Atenolol can be increased when it is combined with Lomitapide.Approved
AtomoxetineThe serum concentration of Lomitapide can be increased when it is combined with Atomoxetine.Approved
AtorvastatinThe serum concentration of Lomitapide can be increased when it is combined with Atorvastatin.Approved
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Lomitapide.Approved, Investigational
BetamethasoneThe serum concentration of Betamethasone can be increased when it is combined with Lomitapide.Approved, Vet Approved
BexaroteneThe serum concentration of Lomitapide can be decreased when it is combined with Bexarotene.Approved, Investigational
BicalutamideThe serum concentration of Lomitapide can be increased when it is combined with Bicalutamide.Approved
BoceprevirThe serum concentration of Lomitapide can be increased when it is combined with Boceprevir.Approved
BortezomibThe serum concentration of Lomitapide can be increased when it is combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Lomitapide can be decreased when it is combined with Bosentan.Approved, Investigational
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Lomitapide.Approved
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Lomitapide.Approved
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Lomitapide.Approved, Investigational
CabazitaxelThe serum concentration of Cabazitaxel can be increased when it is combined with Lomitapide.Approved
CaffeineThe serum concentration of Caffeine can be increased when it is combined with Lomitapide.Approved
CamptothecinThe serum concentration of Camptothecin can be increased when it is combined with Lomitapide.Experimental
CanagliflozinThe serum concentration of Canagliflozin can be increased when it is combined with Lomitapide.Approved
CarbamazepineThe metabolism of Lomitapide can be increased when combined with Carbamazepine.Approved, Investigational
CarfilzomibThe serum concentration of Carfilzomib can be increased when it is combined with Lomitapide.Approved
CeritinibThe serum concentration of Lomitapide can be increased when it is combined with Ceritinib.Approved
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Lomitapide.Withdrawn
ChlorpromazineThe serum concentration of Chlorpromazine can be increased when it is combined with Lomitapide.Approved, Vet Approved
CholestyramineCholestyramine can cause a decrease in the absorption of Lomitapide resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
CilostazolThe serum concentration of Lomitapide can be increased when it is combined with Cilostazol.Approved
CimetidineThe serum concentration of Lomitapide can be increased when it is combined with Cimetidine.Approved
CiprofloxacinThe serum concentration of Lomitapide can be increased when it is combined with Ciprofloxacin.Approved, Investigational
CisplatinThe serum concentration of Cisplatin can be increased when it is combined with Lomitapide.Approved
CitalopramThe serum concentration of Citalopram can be increased when it is combined with Lomitapide.Approved
ClarithromycinThe serum concentration of Lomitapide can be increased when it is combined with Clarithromycin.Approved
ClemastineThe serum concentration of Lomitapide can be increased when it is combined with Clemastine.Approved
ClobazamThe serum concentration of Clobazam can be increased when it is combined with Lomitapide.Approved, Illicit
ClomifeneThe serum concentration of Clomifene can be increased when it is combined with Lomitapide.Approved, Investigational
ClonidineThe serum concentration of Clonidine can be increased when it is combined with Lomitapide.Approved
ClopidogrelThe serum concentration of Clopidogrel can be increased when it is combined with Lomitapide.Approved, Nutraceutical
ClotrimazoleThe serum concentration of Lomitapide can be increased when it is combined with Clotrimazole.Approved, Vet Approved
ClozapineThe serum concentration of Clozapine can be increased when it is combined with Lomitapide.Approved
CobicistatThe serum concentration of Lomitapide can be increased when it is combined with Cobicistat.Approved
CobimetinibThe serum concentration of Cobimetinib can be increased when it is combined with Lomitapide.Approved
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Lomitapide.Approved
ColesevelamColesevelam can cause a decrease in the absorption of Lomitapide resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
ColestipolColestipol can cause a decrease in the absorption of Lomitapide resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
ConivaptanThe serum concentration of Lomitapide can be increased when it is combined with Conivaptan.Approved, Investigational
Conjugated Equine EstrogensThe serum concentration of Conjugated Equine Estrogens can be increased when it is combined with Lomitapide.Approved
CrizotinibThe serum concentration of Lomitapide can be increased when it is combined with Crizotinib.Approved
CyclosporineThe serum concentration of Lomitapide can be increased when it is combined with Cyclosporine.Approved, Investigational, Vet Approved
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Lomitapide.Approved
DabrafenibThe serum concentration of Lomitapide can be decreased when it is combined with Dabrafenib.Approved
DactinomycinThe serum concentration of Dactinomycin can be increased when it is combined with Lomitapide.Approved
DalfopristinThe serum concentration of Lomitapide can be increased when it is combined with Dalfopristin.Approved
DanazolThe serum concentration of Lomitapide can be increased when it is combined with Danazol.Approved
DapagliflozinThe serum concentration of Dapagliflozin can be increased when it is combined with Lomitapide.Approved
DarunavirThe serum concentration of Lomitapide can be increased when it is combined with Darunavir.Approved
DasatinibThe serum concentration of Lomitapide can be increased when it is combined with Dasatinib.Approved, Investigational
DaunorubicinThe serum concentration of Daunorubicin can be increased when it is combined with Lomitapide.Approved
DebrisoquinThe serum concentration of Debrisoquin can be increased when it is combined with Lomitapide.Approved
DeferasiroxThe serum concentration of Lomitapide can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe serum concentration of Lomitapide can be increased when it is combined with Delavirdine.Approved
DexamethasoneThe serum concentration of Lomitapide can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DiazepamThe serum concentration of Diazepam can be increased when it is combined with Lomitapide.Approved, Illicit, Vet Approved
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be increased when it is combined with Lomitapide.Approved
DigitoxinThe serum concentration of Digitoxin can be increased when it is combined with Lomitapide.Approved
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Lomitapide.Approved
DihydroergotamineThe serum concentration of Lomitapide can be increased when it is combined with Dihydroergotamine.Approved
DihydrotestosteroneThe serum concentration of Dihydrotestosterone can be increased when it is combined with Lomitapide.Illicit
DiltiazemThe serum concentration of Lomitapide can be increased when it is combined with Diltiazem.Approved
DipyridamoleThe serum concentration of Dipyridamole can be increased when it is combined with Lomitapide.Approved
DocetaxelThe serum concentration of Docetaxel can be increased when it is combined with Lomitapide.Approved, Investigational
DofetilideThe serum concentration of Dofetilide can be increased when it is combined with Lomitapide.Approved
DomperidoneThe serum concentration of Domperidone can be increased when it is combined with Lomitapide.Approved, Investigational, Vet Approved
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Lomitapide.Approved, Investigational
DoxycyclineThe serum concentration of Lomitapide can be increased when it is combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe serum concentration of Lomitapide can be increased when it is combined with Dronedarone.Approved
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Lomitapide.Approved
EfavirenzThe serum concentration of Lomitapide can be decreased when it is combined with Efavirenz.Approved, Investigational
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Lomitapide.Approved, Investigational
EnzalutamideThe serum concentration of Lomitapide can be decreased when it is combined with Enzalutamide.Approved
EpinastineThe serum concentration of Epinastine can be increased when it is combined with Lomitapide.Approved, Investigational
ErlotinibThe serum concentration of Erlotinib can be increased when it is combined with Lomitapide.Approved, Investigational
ErythromycinThe serum concentration of Lomitapide can be increased when it is combined with Erythromycin.Approved, Vet Approved
Eslicarbazepine acetateThe serum concentration of Lomitapide can be decreased when it is combined with Eslicarbazepine acetate.Approved
EstradiolThe serum concentration of Estradiol can be increased when it is combined with Lomitapide.Approved, Investigational, Vet Approved
EstriolThe serum concentration of Estriol can be increased when it is combined with Lomitapide.Approved, Vet Approved
EstroneThe serum concentration of Estrone can be increased when it is combined with Lomitapide.Approved
EthanolEthanol may increase the hepatotoxic activities of Lomitapide.Approved
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be increased when it is combined with Lomitapide.Approved
EtoposideThe serum concentration of Etoposide can be increased when it is combined with Lomitapide.Approved
EtravirineThe serum concentration of Lomitapide can be decreased when it is combined with Etravirine.Approved
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Lomitapide.Approved
EzetimibeThe serum concentration of Ezetimibe can be increased when it is combined with Lomitapide.Approved
FesoterodineThe serum concentration of Fesoterodine can be increased when it is combined with Lomitapide.Approved
FexofenadineThe serum concentration of Fexofenadine can be increased when it is combined with Lomitapide.Approved
FidaxomicinThe serum concentration of Fidaxomicin can be increased when it is combined with Lomitapide.Approved
FlibanserinThe serum concentration of Flibanserin can be increased when it is combined with Lomitapide.Approved
FluconazoleThe serum concentration of Lomitapide can be increased when it is combined with Fluconazole.Approved
Fluticasone furoateThe serum concentration of Fluticasone furoate can be increased when it is combined with Lomitapide.Approved
FluvoxamineThe serum concentration of Lomitapide can be increased when it is combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe serum concentration of Lomitapide can be increased when it is combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Lomitapide can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Lomitapide can be increased when combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Lomitapide can be increased when it is combined with Fusidic Acid.Approved
GefitinibThe serum concentration of Gefitinib can be increased when it is combined with Lomitapide.Approved, Investigational
GemcitabineThe serum concentration of Gemcitabine can be increased when it is combined with Lomitapide.Approved
Glycerol PhenylbutyrateThe serum concentration of Lomitapide can be increased when it is combined with Glycerol Phenylbutyrate.Approved
GrazoprevirThe serum concentration of Grazoprevir can be increased when it is combined with Lomitapide.Approved
GrepafloxacinThe serum concentration of Grepafloxacin can be increased when it is combined with Lomitapide.Withdrawn
HaloperidolThe serum concentration of Haloperidol can be increased when it is combined with Lomitapide.Approved
HydrocodoneThe serum concentration of Hydrocodone can be increased when it is combined with Lomitapide.Approved, Illicit
HydrocortisoneThe serum concentration of Hydrocortisone can be increased when it is combined with Lomitapide.Approved, Vet Approved
IbuprofenThe serum concentration of Ibuprofen can be increased when it is combined with Lomitapide.Approved
IdelalisibThe serum concentration of Lomitapide can be increased when it is combined with Idelalisib.Approved
IloperidoneThe serum concentration of Lomitapide can be increased when it is combined with Iloperidone.Approved
ImatinibThe serum concentration of Lomitapide can be increased when it is combined with Imatinib.Approved
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Lomitapide.Approved
IndacaterolThe serum concentration of Indacaterol can be increased when it is combined with Lomitapide.Approved
IndinavirThe serum concentration of Lomitapide can be increased when it is combined with Indinavir.Approved
IndomethacinThe serum concentration of Indomethacin can be increased when it is combined with Lomitapide.Approved, Investigational
IrinotecanThe serum concentration of Irinotecan can be increased when it is combined with Lomitapide.Approved, Investigational
IsavuconazoniumThe serum concentration of Lomitapide can be increased when it is combined with Isavuconazonium.Approved, Investigational
IsoniazidThe serum concentration of Lomitapide can be increased when it is combined with Isoniazid.Approved
IsradipineThe serum concentration of Lomitapide can be increased when it is combined with Isradipine.Approved
ItraconazoleThe serum concentration of Lomitapide can be increased when it is combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Lomitapide can be increased when it is combined with Ivacaftor.Approved
IvermectinThe serum concentration of Ivermectin can be increased when it is combined with Lomitapide.Approved, Vet Approved
KetazolamThe serum concentration of Ketazolam can be increased when it is combined with Lomitapide.Approved
KetoconazoleThe serum concentration of Lomitapide can be increased when it is combined with Ketoconazole.Approved, Investigational
LamivudineThe serum concentration of Lamivudine can be increased when it is combined with Lomitapide.Approved, Investigational
LamotrigineThe serum concentration of Lamotrigine can be increased when it is combined with Lomitapide.Approved, Investigational
LansoprazoleThe serum concentration of Lansoprazole can be increased when it is combined with Lomitapide.Approved, Investigational
LapatinibThe serum concentration of Lomitapide can be increased when it is combined with Lapatinib.Approved, Investigational
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Lomitapide.Approved
LenalidomideThe serum concentration of Lenalidomide can be increased when it is combined with Lomitapide.Approved
LenvatinibThe serum concentration of Lenvatinib can be increased when it is combined with Lomitapide.Approved
LevetiracetamThe serum concentration of Levetiracetam can be increased when it is combined with Lomitapide.Approved, Investigational
LevofloxacinThe serum concentration of Levofloxacin can be increased when it is combined with Lomitapide.Approved, Investigational
LevomilnacipranThe serum concentration of Levomilnacipran can be increased when it is combined with Lomitapide.Approved
LinagliptinThe serum concentration of Linagliptin can be increased when it is combined with Lomitapide.Approved
LoperamideThe serum concentration of Loperamide can be increased when it is combined with Lomitapide.Approved
LopinavirThe serum concentration of Lomitapide can be increased when it is combined with Lopinavir.Approved
LosartanThe serum concentration of Losartan can be increased when it is combined with Lomitapide.Approved
LovastatinThe serum concentration of Lovastatin can be increased when it is combined with Lomitapide.Approved, Investigational
LuliconazoleThe serum concentration of Lomitapide can be increased when it is combined with Luliconazole.Approved
LumacaftorThe metabolism of Lomitapide can be increased when combined with Lumacaftor.Approved
LurasidoneThe serum concentration of Lomitapide can be increased when it is combined with Lurasidone.Approved
MannitolThe serum concentration of Mannitol can be increased when it is combined with Lomitapide.Approved, Investigational
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Lomitapide.Approved
MethylprednisoloneThe serum concentration of Methylprednisolone can be increased when it is combined with Lomitapide.Approved, Vet Approved
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Lomitapide.Approved, Investigational
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Lomitapide.Approved, Illicit
MifepristoneThe serum concentration of Lomitapide can be increased when it is combined with Mifepristone.Approved, Investigational
MipomersenLomitapide may increase the hepatotoxic activities of Mipomersen.Approved
MirabegronThe serum concentration of Mirabegron can be increased when it is combined with Lomitapide.Approved
MitotaneThe serum concentration of Lomitapide can be decreased when it is combined with Mitotane.Approved
MitoxantroneThe serum concentration of Mitoxantrone can be increased when it is combined with Lomitapide.Approved, Investigational
ModafinilThe serum concentration of Lomitapide can be decreased when it is combined with Modafinil.Approved, Investigational
MorphineThe serum concentration of Morphine can be increased when it is combined with Lomitapide.Approved, Investigational
Mycophenolate mofetilThe serum concentration of Mycophenolate mofetil can be increased when it is combined with Lomitapide.Approved, Investigational
NadololThe serum concentration of Nadolol can be increased when it is combined with Lomitapide.Approved
NafcillinThe serum concentration of Lomitapide can be decreased when it is combined with Nafcillin.Approved
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Lomitapide.Approved
NaloxoneThe serum concentration of Naloxone can be increased when it is combined with Lomitapide.Approved, Vet Approved
NefazodoneThe serum concentration of Lomitapide can be increased when it is combined with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of Lomitapide can be increased when it is combined with Nelfinavir.Approved
NetupitantThe serum concentration of Lomitapide can be increased when it is combined with Netupitant.Approved
NevirapineThe serum concentration of Lomitapide can be increased when it is combined with Nevirapine.Approved
NicardipineThe serum concentration of Lomitapide can be increased when it is combined with Nicardipine.Approved
NifedipineThe serum concentration of Nifedipine can be increased when it is combined with Lomitapide.Approved
NilotinibThe serum concentration of Lomitapide can be increased when it is combined with Nilotinib.Approved, Investigational
NimodipineThe serum concentration of Nimodipine can be increased when it is combined with Lomitapide.Approved
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Lomitapide.Approved
NizatidineThe serum concentration of Nizatidine can be increased when it is combined with Lomitapide.Approved
OlanzapineThe serum concentration of Olanzapine can be increased when it is combined with Lomitapide.Approved, Investigational
OlaparibThe serum concentration of Lomitapide can be increased when it is combined with Olaparib.Approved
OmbitasvirThe serum concentration of Ombitasvir can be increased when it is combined with Lomitapide.Approved
OsimertinibThe serum concentration of Lomitapide can be increased when it is combined with Osimertinib.Approved
PaclitaxelThe serum concentration of Paclitaxel can be increased when it is combined with Lomitapide.Approved, Vet Approved
PalbociclibThe serum concentration of Lomitapide can be increased when it is combined with Palbociclib.Approved
PanobinostatThe serum concentration of Panobinostat can be increased when it is combined with Lomitapide.Approved, Investigational
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Lomitapide.Approved
PentobarbitalThe metabolism of Lomitapide can be increased when combined with Pentobarbital.Approved, Vet Approved
PhenobarbitalThe metabolism of Lomitapide can be increased when combined with Phenobarbital.Approved
PhenytoinThe metabolism of Lomitapide can be increased when combined with Phenytoin.Approved, Vet Approved
PimozideThe serum concentration of Pimozide can be increased when it is combined with Lomitapide.Approved
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Lomitapide.Approved
PomalidomideThe serum concentration of Pomalidomide can be increased when it is combined with Lomitapide.Approved
PonatinibThe serum concentration of Ponatinib can be increased when it is combined with Lomitapide.Approved
PosaconazoleThe serum concentration of Lomitapide can be increased when it is combined with Posaconazole.Approved, Investigational, Vet Approved
PravastatinThe serum concentration of Pravastatin can be increased when it is combined with Lomitapide.Approved
PrazosinThe serum concentration of Prazosin can be increased when it is combined with Lomitapide.Approved
PrednisoloneThe serum concentration of Prednisolone can be increased when it is combined with Lomitapide.Approved, Vet Approved
PrednisoneThe serum concentration of Prednisone can be increased when it is combined with Lomitapide.Approved, Vet Approved
PrimidoneThe metabolism of Lomitapide can be increased when combined with Primidone.Approved, Vet Approved
ProgesteroneThe serum concentration of Progesterone can be increased when it is combined with Lomitapide.Approved, Vet Approved
PropofolThe serum concentration of Lomitapide can be increased when it is combined with Propofol.Approved, Investigational, Vet Approved
PropranololThe serum concentration of Propranolol can be increased when it is combined with Lomitapide.Approved, Investigational
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Lomitapide.Approved
QuetiapineThe serum concentration of Quetiapine can be increased when it is combined with Lomitapide.Approved
QuinidineThe serum concentration of Lomitapide can be increased when it is combined with Quinidine.Approved
QuinineThe serum concentration of Quinine can be increased when it is combined with Lomitapide.Approved
QuinupristinThe serum concentration of Lomitapide can be increased when it is combined with Quinupristin.Approved
RanitidineThe serum concentration of Ranitidine can be increased when it is combined with Lomitapide.Approved
RanolazineThe serum concentration of Lomitapide can be increased when it is combined with Ranolazine.Approved, Investigational
ReserpineThe serum concentration of Reserpine can be increased when it is combined with Lomitapide.Approved
RifabutinThe metabolism of Lomitapide can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Lomitapide can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Lomitapide can be increased when combined with Rifapentine.Approved
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Lomitapide.Approved, Investigational
RisperidoneThe serum concentration of Risperidone can be increased when it is combined with Lomitapide.Approved, Investigational
RitonavirThe serum concentration of Lomitapide can be increased when it is combined with Ritonavir.Approved, Investigational
RivaroxabanThe serum concentration of Rivaroxaban can be increased when it is combined with Lomitapide.Approved
RomidepsinThe serum concentration of Romidepsin can be increased when it is combined with Lomitapide.Approved, Investigational
Salicylic acidThe serum concentration of Salicylic acid can be increased when it is combined with Lomitapide.Approved, Vet Approved
SaquinavirThe serum concentration of Lomitapide can be increased when it is combined with Saquinavir.Approved, Investigational
SelexipagThe serum concentration of Selexipag can be increased when it is combined with Lomitapide.Approved
SildenafilThe serum concentration of Lomitapide can be increased when it is combined with Sildenafil.Approved, Investigational
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Lomitapide.Approved
SiltuximabThe serum concentration of Lomitapide can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Lomitapide can be increased when it is combined with Simeprevir.Approved
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Lomitapide.Approved
SitagliptinThe serum concentration of Sitagliptin can be increased when it is combined with Lomitapide.Approved, Investigational
SofosbuvirThe serum concentration of Sofosbuvir can be increased when it is combined with Lomitapide.Approved
SorafenibThe serum concentration of Sorafenib can be increased when it is combined with Lomitapide.Approved, Investigational
SparfloxacinThe serum concentration of Sparfloxacin can be increased when it is combined with Lomitapide.Approved
SphingosineThe serum concentration of Sphingosine can be increased when it is combined with Lomitapide.Experimental
St. John's WortThe serum concentration of Lomitapide can be decreased when it is combined with St. John's Wort.Nutraceutical
StiripentolThe serum concentration of Lomitapide can be increased when it is combined with Stiripentol.Approved
SulfisoxazoleThe serum concentration of Lomitapide can be increased when it is combined with Sulfisoxazole.Approved, Vet Approved
TacrolimusThe serum concentration of Tacrolimus can be increased when it is combined with Lomitapide.Approved, Investigational
TamoxifenThe serum concentration of Tamoxifen can be increased when it is combined with Lomitapide.Approved
Taurocholic AcidThe serum concentration of Taurocholic Acid can be increased when it is combined with Lomitapide.Experimental
Technetium Tc-99m sestamibiThe serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Lomitapide.Approved
TelaprevirThe serum concentration of Lomitapide can be increased when it is combined with Telaprevir.Approved
TelithromycinThe serum concentration of Lomitapide can be increased when it is combined with Telithromycin.Approved
TemsirolimusThe serum concentration of Temsirolimus can be increased when it is combined with Lomitapide.Approved
TicagrelorThe serum concentration of Lomitapide can be increased when it is combined with Ticagrelor.Approved
TiclopidineThe serum concentration of Lomitapide can be increased when it is combined with Ticlopidine.Approved
TimololThe serum concentration of Timolol can be increased when it is combined with Lomitapide.Approved
TipranavirThe serum concentration of Lomitapide can be increased when it is combined with Tipranavir.Approved, Investigational
TocilizumabThe serum concentration of Lomitapide can be decreased when it is combined with Tocilizumab.Approved
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Lomitapide.Approved
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Lomitapide.Approved, Investigational
ToremifeneThe serum concentration of Toremifene can be increased when it is combined with Lomitapide.Approved, Investigational
Trastuzumab emtansineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Lomitapide.Approved
UlipristalThe serum concentration of Ulipristal can be increased when it is combined with Lomitapide.Approved
UmeclidiniumThe serum concentration of Umeclidinium can be increased when it is combined with Lomitapide.Approved
VecuroniumThe serum concentration of Vecuronium can be increased when it is combined with Lomitapide.Approved
VenetoclaxThe serum concentration of Venetoclax can be increased when it is combined with Lomitapide.Approved
VenlafaxineThe serum concentration of Lomitapide can be increased when it is combined with Venlafaxine.Approved
VerapamilThe serum concentration of Lomitapide can be increased when it is combined with Verapamil.Approved
VinblastineThe serum concentration of Vinblastine can be increased when it is combined with Lomitapide.Approved
VincristineThe serum concentration of Vincristine can be increased when it is combined with Lomitapide.Approved, Investigational
VismodegibThe serum concentration of Vismodegib can be increased when it is combined with Lomitapide.Approved
VoriconazoleThe serum concentration of Lomitapide can be increased when it is combined with Voriconazole.Approved, Investigational
WarfarinThe serum concentration of Warfarin can be increased when it is combined with Lomitapide.Approved
ZidovudineThe serum concentration of Zidovudine can be increased when it is combined with Lomitapide.Approved
ZiprasidoneThe serum concentration of Lomitapide can be increased when it is combined with Ziprasidone.Approved
Food Interactions
  • Avoid grapefruit juice, which will likely increase lomitapide plasma concentrations.
  • When taking lomitapide with food, the risk of GI side effects is increased.
References
Synthesis ReferenceNot Available
General References
  1. 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. 2013 Jan 5;381(9860):40-6. doi: 10.1016/S0140-6736(12)61731-0. Epub 2012 Nov 2. [PubMed:23122768 ]
  2. 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:17215532 ]
External Links
ATC CodesC10AX12
AHFS Codes
  • 24:06.92
PDB EntriesNot Available
FDA labelDownload (930 KB)
MSDSNot Available
ADMET
Predicted ADMET featuresNot Available
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
CapsuleOral10 mg
CapsuleOral10 mg/1
CapsuleOral20 mg
CapsuleOral20 mg/1
CapsuleOral30 mg/1
CapsuleOral40 mg/1
CapsuleOral5 mg
CapsuleOral5 mg/1
CapsuleOral60 mg/1
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5712279 No1996-02-212016-02-21Us
US5739135 No2012-12-122015-04-14Us
US6492365 No1999-12-102019-12-10Us
US7932268 No2007-08-192027-08-19Us
US8618135 No2005-03-072025-03-07Us
US9265758 No2005-03-072025-03-07Us
Properties
StateSolid
Experimental PropertiesNot Available
Predicted Properties
PropertyValueSource
logP7.7ChemAxon
pKa (Strongest Acidic)10.35ChemAxon
pKa (Strongest Basic)9.02ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area61.44 Å2ChemAxon
Rotatable Bond Count12ChemAxon
Refractivity181.73 m3·mol-1ChemAxon
Polarizability68.08 Å3ChemAxon
Number of Rings6ChemAxon
Bioavailability0ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as fluorenes. These are compounds containing a fluorene moiety, which consists of two benzene rings connected through either a cyclopentane, cyclopentene, or cyclopenta-1,3-diene.
KingdomOrganic compounds
Super ClassBenzenoids
ClassFluorenes
Sub ClassNot Available
Direct ParentFluorenes
Alternative Parents
Substituents
  • Fluorene
  • Biphenyl
  • Benzoic acid or derivatives
  • Benzamide
  • Benzoyl
  • Aralkylamine
  • 4-aminopiperidine
  • Fatty acyl
  • Piperidine
  • Fatty amide
  • Monocyclic benzene moiety
  • Tertiary aliphatic amine
  • Tertiary amine
  • Secondary carboxylic acid amide
  • Carboxamide group
  • Azacycle
  • Organoheterocyclic compound
  • Carboxylic acid derivative
  • Carboxylic acid amide
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organofluoride
  • Organohalogen compound
  • Carbonyl group
  • Amine
  • Alkyl halide
  • Alkyl fluoride
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Protein heterodimerization activity
Specific Function:
Catalyzes the transport of triglyceride, cholesteryl ester, and phospholipid between phospholipid surfaces (PubMed:23475612, PubMed:8939939, PubMed:26224785, PubMed:25108285, PubMed:22236406). Required for the secretion of plasma lipoproteins that contain apolipoprotein B (PubMed:23475612, PubMed:8939939, PubMed:26224785).
Gene Name:
MTTP
Uniprot ID:
P55157
Molecular Weight:
99350.255 Da

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
no
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da

Transporters

Kind
Protein
Organism
Human
Pharmacological action
no
Actions
inhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
Comments
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Drug created on January 03, 2013 13:34 / Updated on December 07, 2016 02:48