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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
Juxtapidcapsule10 mgoralAegerion Pharmaceuticals Canada Ltd2014-05-06Not applicableCanada
Juxtapidcapsule5 mg/1oralAegerion Pharmaceuticals, Inc.2013-01-03Not applicableUs
Juxtapidcapsule40 mg/1oralAegerion Pharmaceuticals, Inc.2013-01-03Not applicableUs
Juxtapidcapsule20 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
Juxtapidcapsule20 mg/1oralAegerion Pharmaceuticals, Inc.2013-01-03Not applicableUs
Juxtapidcapsule5 mgoralAegerion Pharmaceuticals Canada Ltd2014-05-06Not applicableCanada
Juxtapidcapsule30 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 KeyInChIKey=MBBCVAKAJPKAKM-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
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
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).
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.
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
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal AbsorptionNot AvailableNot Available
Blood Brain BarrierNot AvailableNot Available
Caco-2 permeableNot AvailableNot Available
P-glycoprotein substrateNot AvailableNot Available
P-glycoprotein inhibitor INot AvailableNot Available
P-glycoprotein inhibitor IINot AvailableNot Available
Renal organic cation transporterNot AvailableNot Available
CYP450 2C9 substrateNot AvailableNot Available
CYP450 2D6 substrateNot AvailableNot Available
CYP450 3A4 substrateNot AvailableNot Available
CYP450 1A2 substrateNot AvailableNot Available
CYP450 2C9 inhibitorNot AvailableNot Available
CYP450 2D6 inhibitorNot AvailableNot Available
CYP450 2C19 inhibitorNot AvailableNot Available
CYP450 3A4 inhibitorNot AvailableNot Available
CYP450 inhibitory promiscuityNot AvailableNot Available
Ames testNot AvailableNot Available
CarcinogenicityNot AvailableNot Available
BiodegradationNot AvailableNot Available
Rat acute toxicityNot AvailableNot applicable
hERG inhibition (predictor I)Not AvailableNot Available
hERG inhibition (predictor II)Not AvailableNot Available
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Capsuleoral10 mg
Capsuleoral10 mg/1
Capsuleoral20 mg/1
Capsuleoral20 mg
Capsuleoral30 mg/1
Capsuleoral40 mg/1
Capsuleoral5 mg/1
Capsuleoral5 mg
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
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
Interactions
Drug Interactions
Drug
AcebutololThe serum concentration of Acebutolol can be increased when it is combined with Lomitapide.
AcetaminophenThe serum concentration of Acetaminophen can be increased when it is combined with Lomitapide.
Acetylsalicylic acidThe serum concentration of Acetylsalicylic acid can be increased when it is combined with Lomitapide.
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Lomitapide.
AldosteroneThe serum concentration of Aldosterone can be increased when it is combined with Lomitapide.
AlitretinoinThe serum concentration of Alitretinoin can be increased when it is combined with Lomitapide.
AlprazolamThe serum concentration of Lomitapide can be increased when it is combined with Alprazolam.
AmbrisentanThe serum concentration of Ambrisentan can be increased when it is combined with Lomitapide.
AmiodaroneThe serum concentration of Lomitapide can be increased when it is combined with Amiodarone.
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Lomitapide.
AmlodipineThe serum concentration of Lomitapide can be increased when it is combined with Amlodipine.
ApixabanThe serum concentration of Apixaban can be increased when it is combined with Lomitapide.
AprepitantThe serum concentration of Lomitapide can be increased when it is combined with Aprepitant.
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Lomitapide.
Arsenic trioxideThe serum concentration of Arsenic trioxide can be increased when it is combined with Lomitapide.
AtazanavirThe serum concentration of Lomitapide can be increased when it is combined with Atazanavir.
AtenololThe serum concentration of Atenolol can be increased when it is combined with Lomitapide.
AtomoxetineThe serum concentration of Lomitapide can be increased when it is combined with Atomoxetine.
AtorvastatinThe serum concentration of Lomitapide can be increased when it is combined with Atorvastatin.
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Lomitapide.
BetamethasoneThe serum concentration of Betamethasone can be increased when it is combined with Lomitapide.
BexaroteneThe serum concentration of Lomitapide can be decreased when it is combined with Bexarotene.
BicalutamideThe serum concentration of Lomitapide can be increased when it is combined with Bicalutamide.
BoceprevirThe serum concentration of Lomitapide can be increased when it is combined with Boceprevir.
BortezomibThe serum concentration of Lomitapide can be increased when it is combined with Bortezomib.
BosentanThe serum concentration of Lomitapide can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Lomitapide.
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Lomitapide.
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Lomitapide.
CabazitaxelThe serum concentration of Cabazitaxel can be increased when it is combined with Lomitapide.
CaffeineThe serum concentration of Caffeine can be increased when it is combined with Lomitapide.
CamptothecinThe serum concentration of Camptothecin can be increased when it is combined with Lomitapide.
CanagliflozinThe serum concentration of Canagliflozin can be increased when it is combined with Lomitapide.
CarbamazepineThe metabolism of Lomitapide can be increased when combined with Carbamazepine.
CarbamazepineThe serum concentration of Carbamazepine can be increased when it is combined with Lomitapide.
CarfilzomibThe serum concentration of Carfilzomib can be increased when it is combined with Lomitapide.
CeritinibThe serum concentration of Lomitapide can be increased when it is combined with Ceritinib.
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Lomitapide.
ChlorpromazineThe serum concentration of Chlorpromazine can be increased when it is combined with Lomitapide.
CholestyramineCholestyramine can cause a decrease in the absorption of Lomitapide resulting in a reduced serum concentration and potentially a decrease in efficacy.
CilostazolThe serum concentration of Lomitapide can be increased when it is combined with Cilostazol.
CimetidineThe serum concentration of Lomitapide can be increased when it is combined with Cimetidine.
CiprofloxacinThe serum concentration of Lomitapide can be increased when it is combined with Ciprofloxacin.
CisplatinThe serum concentration of Cisplatin can be increased when it is combined with Lomitapide.
CitalopramThe serum concentration of Citalopram can be increased when it is combined with Lomitapide.
ClarithromycinThe serum concentration of Lomitapide can be increased when it is combined with Clarithromycin.
ClemastineThe serum concentration of Lomitapide can be increased when it is combined with Clemastine.
ClobazamThe serum concentration of Clobazam can be increased when it is combined with Lomitapide.
ClomifeneThe serum concentration of Clomifene can be increased when it is combined with Lomitapide.
ClonidineThe serum concentration of Clonidine can be increased when it is combined with Lomitapide.
ClopidogrelThe serum concentration of Clopidogrel can be increased when it is combined with Lomitapide.
ClotrimazoleThe serum concentration of Lomitapide can be increased when it is combined with Clotrimazole.
ClozapineThe serum concentration of Clozapine can be increased when it is combined with Lomitapide.
CobicistatThe serum concentration of Lomitapide can be increased when it is combined with Cobicistat.
CobimetinibThe serum concentration of Cobimetinib can be increased when it is combined with Lomitapide.
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Lomitapide.
ColesevelamColesevelam can cause a decrease in the absorption of Lomitapide resulting in a reduced serum concentration and potentially a decrease in efficacy.
ColestipolColestipol can cause a decrease in the absorption of Lomitapide resulting in a reduced serum concentration and potentially a decrease in efficacy.
ConivaptanThe serum concentration of Lomitapide can be increased when it is combined with Conivaptan.
Conjugated Equine EstrogensThe serum concentration of Conjugated Equine Estrogens can be increased when it is combined with Lomitapide.
CrizotinibThe serum concentration of Lomitapide can be increased when it is combined with Crizotinib.
CyclosporineThe serum concentration of Lomitapide can be increased when it is combined with Cyclosporine.
Dabigatran etexilateThe serum concentration of Dabigatran etexilate can be increased when it is combined with Lomitapide.
DabrafenibThe serum concentration of Lomitapide can be decreased when it is combined with Dabrafenib.
DabrafenibThe serum concentration of Dabrafenib can be increased when it is combined with Lomitapide.
DactinomycinThe serum concentration of Dactinomycin can be increased when it is combined with Lomitapide.
DalfopristinThe serum concentration of Lomitapide can be increased when it is combined with Dalfopristin.
DanazolThe serum concentration of Lomitapide can be increased when it is combined with Danazol.
DapagliflozinThe serum concentration of Dapagliflozin can be increased when it is combined with Lomitapide.
DarunavirThe serum concentration of Lomitapide can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Lomitapide can be increased when it is combined with Dasatinib.
DaunorubicinThe serum concentration of Daunorubicin can be increased when it is combined with Lomitapide.
DebrisoquinThe serum concentration of Debrisoquin can be increased when it is combined with Lomitapide.
DeferasiroxThe serum concentration of Lomitapide can be decreased when it is combined with Deferasirox.
DelavirdineThe serum concentration of Lomitapide can be increased when it is combined with Delavirdine.
DexamethasoneThe serum concentration of Lomitapide can be decreased when it is combined with Dexamethasone.
DexamethasoneThe serum concentration of Dexamethasone can be increased when it is combined with Lomitapide.
DiazepamThe serum concentration of Diazepam can be increased when it is combined with Lomitapide.
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be increased when it is combined with Lomitapide.
DigitoxinThe serum concentration of Digitoxin can be increased when it is combined with Lomitapide.
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Lomitapide.
DihydroergotamineThe serum concentration of Lomitapide can be increased when it is combined with Dihydroergotamine.
DihydrotestosteroneThe serum concentration of Dihydrotestosterone can be increased when it is combined with Lomitapide.
DiltiazemThe serum concentration of Lomitapide can be increased when it is combined with Diltiazem.
DipyridamoleThe serum concentration of Dipyridamole can be increased when it is combined with Lomitapide.
DocetaxelThe serum concentration of Docetaxel can be increased when it is combined with Lomitapide.
DofetilideThe serum concentration of Dofetilide can be increased when it is combined with Lomitapide.
DomperidoneThe serum concentration of Domperidone can be increased when it is combined with Lomitapide.
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Lomitapide.
DoxycyclineThe serum concentration of Lomitapide can be increased when it is combined with Doxycycline.
DronedaroneThe serum concentration of Lomitapide can be increased when it is combined with Dronedarone.
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Lomitapide.
EfavirenzThe serum concentration of Lomitapide can be decreased when it is combined with Efavirenz.
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Lomitapide.
EnzalutamideThe serum concentration of Lomitapide can be decreased when it is combined with Enzalutamide.
EpinastineThe serum concentration of Epinastine can be increased when it is combined with Lomitapide.
ErlotinibThe serum concentration of Erlotinib can be increased when it is combined with Lomitapide.
ErythromycinThe serum concentration of Lomitapide can be increased when it is combined with Erythromycin.
Eslicarbazepine acetateThe serum concentration of Lomitapide can be decreased when it is combined with Eslicarbazepine acetate.
EstradiolThe serum concentration of Estradiol can be increased when it is combined with Lomitapide.
EstriolThe serum concentration of Estriol can be increased when it is combined with Lomitapide.
EstroneThe serum concentration of Estrone can be increased when it is combined with Lomitapide.
EthanolEthanol may increase the hepatotoxic activities of Lomitapide.
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be increased when it is combined with Lomitapide.
EtoposideThe serum concentration of Etoposide can be increased when it is combined with Lomitapide.
EtravirineThe serum concentration of Lomitapide can be decreased when it is combined with Etravirine.
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Lomitapide.
EzetimibeThe serum concentration of Ezetimibe can be increased when it is combined with Lomitapide.
FesoterodineThe serum concentration of Fesoterodine can be increased when it is combined with Lomitapide.
FexofenadineThe serum concentration of Fexofenadine can be increased when it is combined with Lomitapide.
FidaxomicinThe serum concentration of Fidaxomicin can be increased when it is combined with Lomitapide.
FlibanserinThe serum concentration of Flibanserin can be increased when it is combined with Lomitapide.
FluconazoleThe serum concentration of Lomitapide can be increased when it is combined with Fluconazole.
Fluticasone furoateThe serum concentration of Fluticasone furoate can be increased when it is combined with Lomitapide.
FluvoxamineThe serum concentration of Lomitapide can be increased when it is combined with Fluvoxamine.
FosamprenavirThe serum concentration of Lomitapide can be increased when it is combined with Fosamprenavir.
FosaprepitantThe serum concentration of Lomitapide can be increased when it is combined with Fosaprepitant.
FosphenytoinThe metabolism of Lomitapide can be increased when combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Lomitapide can be increased when it is combined with Fusidic Acid.
GefitinibThe serum concentration of Gefitinib can be increased when it is combined with Lomitapide.
GemcitabineThe serum concentration of Gemcitabine can be increased when it is combined with Lomitapide.
Glycerol PhenylbutyrateThe serum concentration of Lomitapide can be increased when it is combined with Glycerol Phenylbutyrate.
GrazoprevirThe serum concentration of Grazoprevir can be increased when it is combined with Lomitapide.
GrepafloxacinThe serum concentration of Grepafloxacin can be increased when it is combined with Lomitapide.
HaloperidolThe serum concentration of Haloperidol can be increased when it is combined with Lomitapide.
HydrocodoneThe serum concentration of Hydrocodone can be increased when it is combined with Lomitapide.
HydrocortisoneThe serum concentration of Hydrocortisone can be increased when it is combined with Lomitapide.
IbuprofenThe serum concentration of Ibuprofen can be increased when it is combined with Lomitapide.
IdelalisibThe serum concentration of Lomitapide can be increased when it is combined with Idelalisib.
IloperidoneThe serum concentration of Lomitapide can be increased when it is combined with Iloperidone.
ImatinibThe serum concentration of Lomitapide can be increased when it is combined with Imatinib.
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Lomitapide.
IndacaterolThe serum concentration of Indacaterol can be increased when it is combined with Lomitapide.
IndinavirThe serum concentration of Lomitapide can be increased when it is combined with Indinavir.
IndomethacinThe serum concentration of Indomethacin can be increased when it is combined with Lomitapide.
IrinotecanThe serum concentration of Irinotecan can be increased when it is combined with Lomitapide.
IsavuconazoniumThe serum concentration of Lomitapide can be increased when it is combined with Isavuconazonium.
IsoniazidThe serum concentration of Lomitapide can be increased when it is combined with Isoniazid.
IsradipineThe serum concentration of Lomitapide can be increased when it is combined with Isradipine.
ItraconazoleThe serum concentration of Lomitapide can be increased when it is combined with Itraconazole.
IvacaftorThe serum concentration of Lomitapide can be increased when it is combined with Ivacaftor.
IvermectinThe serum concentration of Ivermectin can be increased when it is combined with Lomitapide.
KetazolamThe serum concentration of Ketazolam can be increased when it is combined with Lomitapide.
KetoconazoleThe serum concentration of Lomitapide can be increased when it is combined with Ketoconazole.
LamivudineThe serum concentration of Lamivudine can be increased when it is combined with Lomitapide.
LamotrigineThe serum concentration of Lamotrigine can be increased when it is combined with Lomitapide.
LansoprazoleThe serum concentration of Lansoprazole can be increased when it is combined with Lomitapide.
LapatinibThe serum concentration of Lomitapide can be increased when it is combined with Lapatinib.
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Lomitapide.
LenalidomideThe serum concentration of Lenalidomide can be increased when it is combined with Lomitapide.
LenvatinibThe serum concentration of Lenvatinib can be increased when it is combined with Lomitapide.
LevetiracetamThe serum concentration of Levetiracetam can be increased when it is combined with Lomitapide.
LevofloxacinThe serum concentration of Levofloxacin can be increased when it is combined with Lomitapide.
LevomilnacipranThe serum concentration of Levomilnacipran can be increased when it is combined with Lomitapide.
LinagliptinThe serum concentration of Linagliptin can be increased when it is combined with Lomitapide.
LoperamideThe serum concentration of Loperamide can be increased when it is combined with Lomitapide.
LopinavirThe serum concentration of Lomitapide can be increased when it is combined with Lopinavir.
LosartanThe serum concentration of Losartan can be increased when it is combined with Lomitapide.
LovastatinThe serum concentration of Lomitapide can be increased when it is combined with Lovastatin.
LuliconazoleThe serum concentration of Lomitapide can be increased when it is combined with Luliconazole.
LurasidoneThe serum concentration of Lomitapide can be increased when it is combined with Lurasidone.
MannitolThe serum concentration of Mannitol can be increased when it is combined with Lomitapide.
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Lomitapide.
MethylprednisoloneThe serum concentration of Methylprednisolone can be increased when it is combined with Lomitapide.
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Lomitapide.
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Lomitapide.
MifepristoneThe serum concentration of Lomitapide can be increased when it is combined with Mifepristone.
MipomersenLomitapide may increase the hepatotoxic activities of Mipomersen.
MirabegronThe serum concentration of Mirabegron can be increased when it is combined with Lomitapide.
MitotaneThe serum concentration of Lomitapide can be decreased when it is combined with Mitotane.
MitoxantroneThe serum concentration of Mitoxantrone can be increased when it is combined with Lomitapide.
ModafinilThe serum concentration of Lomitapide can be decreased when it is combined with Modafinil.
MorphineThe serum concentration of Morphine can be increased when it is combined with Lomitapide.
Mycophenolate mofetilThe serum concentration of Mycophenolate mofetil can be increased when it is combined with Lomitapide.
NadololThe serum concentration of Nadolol can be increased when it is combined with Lomitapide.
NafcillinThe serum concentration of Lomitapide can be decreased when it is combined with Nafcillin.
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Lomitapide.
NaloxoneThe serum concentration of Naloxone can be increased when it is combined with Lomitapide.
NefazodoneThe serum concentration of Lomitapide can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Lomitapide can be increased when it is combined with Nelfinavir.
NetupitantThe serum concentration of Lomitapide can be increased when it is combined with Netupitant.
NevirapineThe serum concentration of Lomitapide can be increased when it is combined with Nevirapine.
NicardipineThe serum concentration of Lomitapide can be increased when it is combined with Nicardipine.
NifedipineThe serum concentration of Nifedipine can be increased when it is combined with Lomitapide.
NilotinibThe serum concentration of Lomitapide can be increased when it is combined with Nilotinib.
NimodipineThe serum concentration of Nimodipine can be increased when it is combined with Lomitapide.
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Lomitapide.
NizatidineThe serum concentration of Nizatidine can be increased when it is combined with Lomitapide.
OlanzapineThe serum concentration of Olanzapine can be increased when it is combined with Lomitapide.
OlaparibThe serum concentration of Lomitapide can be increased when it is combined with Olaparib.
OmbitasvirThe serum concentration of Ombitasvir can be increased when it is combined with Lomitapide.
OsimertinibThe serum concentration of Lomitapide can be increased when it is combined with Osimertinib.
PaclitaxelThe serum concentration of Paclitaxel can be increased when it is combined with Lomitapide.
PalbociclibThe serum concentration of Lomitapide can be increased when it is combined with Palbociclib.
PanobinostatThe serum concentration of Panobinostat can be increased when it is combined with Lomitapide.
PazopanibThe serum concentration of Lomitapide can be increased when it is combined with Pazopanib.
PentobarbitalThe metabolism of Lomitapide can be increased when combined with Pentobarbital.
PhenobarbitalThe metabolism of Lomitapide can be increased when combined with Phenobarbital.
PhenobarbitalThe serum concentration of Phenobarbital can be increased when it is combined with Lomitapide.
PhenytoinThe metabolism of Lomitapide can be increased when combined with Phenytoin.
PhenytoinThe serum concentration of Phenytoin can be increased when it is combined with Lomitapide.
PimozideThe serum concentration of Pimozide can be increased when it is combined with Lomitapide.
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Lomitapide.
PomalidomideThe serum concentration of Pomalidomide can be increased when it is combined with Lomitapide.
PonatinibThe serum concentration of Ponatinib can be increased when it is combined with Lomitapide.
PosaconazoleThe serum concentration of Lomitapide can be increased when it is combined with Posaconazole.
PravastatinThe serum concentration of Pravastatin can be increased when it is combined with Lomitapide.
PrazosinThe serum concentration of Prazosin can be increased when it is combined with Lomitapide.
PrednisoloneThe serum concentration of Prednisolone can be increased when it is combined with Lomitapide.
PrednisoneThe serum concentration of Prednisone can be increased when it is combined with Lomitapide.
PrimidoneThe metabolism of Lomitapide can be increased when combined with Primidone.
ProgesteroneThe serum concentration of Progesterone can be increased when it is combined with Lomitapide.
PropofolThe serum concentration of Lomitapide can be increased when it is combined with Propofol.
PropranololThe serum concentration of Propranolol can be increased when it is combined with Lomitapide.
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Lomitapide.
QuetiapineThe serum concentration of Quetiapine can be increased when it is combined with Lomitapide.
QuinidineThe serum concentration of Lomitapide can be increased when it is combined with Quinidine.
QuinineThe serum concentration of Quinine can be increased when it is combined with Lomitapide.
QuinupristinThe serum concentration of Lomitapide can be increased when it is combined with Quinupristin.
RanitidineThe serum concentration of Ranitidine can be increased when it is combined with Lomitapide.
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Lomitapide.
ReserpineThe serum concentration of Reserpine can be increased when it is combined with Lomitapide.
RifabutinThe metabolism of Lomitapide can be increased when combined with Rifabutin.
RifampicinThe metabolism of Lomitapide can be increased when combined with Rifampicin.
RifampicinThe serum concentration of Rifampicin can be increased when it is combined with Lomitapide.
RifapentineThe metabolism of Lomitapide can be increased when combined with Rifapentine.
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Lomitapide.
RisperidoneThe serum concentration of Risperidone can be increased when it is combined with Lomitapide.
RitonavirThe serum concentration of Lomitapide can be increased when it is combined with Ritonavir.
RivaroxabanThe serum concentration of Rivaroxaban can be increased when it is combined with Lomitapide.
RomidepsinThe serum concentration of Romidepsin can be increased when it is combined with Lomitapide.
Salicylic acidThe serum concentration of Salicylic acid can be increased when it is combined with Lomitapide.
SaquinavirThe serum concentration of Lomitapide can be increased when it is combined with Saquinavir.
SelexipagThe serum concentration of Selexipag can be increased when it is combined with Lomitapide.
SildenafilThe serum concentration of Lomitapide can be increased when it is combined with Sildenafil.
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Lomitapide.
SiltuximabThe serum concentration of Lomitapide can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Lomitapide can be increased when it is combined with Simeprevir.
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Lomitapide.
SitagliptinThe serum concentration of Sitagliptin can be increased when it is combined with Lomitapide.
SofosbuvirThe serum concentration of Sofosbuvir can be increased when it is combined with Lomitapide.
SorafenibThe serum concentration of Sorafenib can be increased when it is combined with Lomitapide.
SparfloxacinThe serum concentration of Sparfloxacin can be increased when it is combined with Lomitapide.
SphingosineThe serum concentration of Sphingosine can be increased when it is combined with Lomitapide.
St. John's WortThe serum concentration of Lomitapide can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Lomitapide can be increased when it is combined with Stiripentol.
SulfisoxazoleThe serum concentration of Lomitapide can be increased when it is combined with Sulfisoxazole.
TacrolimusThe serum concentration of Tacrolimus can be increased when it is combined with Lomitapide.
TamoxifenThe serum concentration of Tamoxifen can be increased when it is combined with Lomitapide.
Taurocholic AcidThe serum concentration of Taurocholic Acid can be increased when it is combined with Lomitapide.
Technetium Tc-99m sestamibiThe serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Lomitapide.
TelaprevirThe serum concentration of Lomitapide can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Lomitapide can be increased when it is combined with Telithromycin.
TemsirolimusThe serum concentration of Temsirolimus can be increased when it is combined with Lomitapide.
TicagrelorThe serum concentration of Lomitapide can be increased when it is combined with Ticagrelor.
TiclopidineThe serum concentration of Lomitapide can be increased when it is combined with Ticlopidine.
TimololThe serum concentration of Timolol can be increased when it is combined with Lomitapide.
TipranavirThe serum concentration of Lomitapide can be increased when it is combined with Tipranavir.
TocilizumabThe serum concentration of Lomitapide can be decreased when it is combined with Tocilizumab.
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Lomitapide.
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Lomitapide.
ToremifeneThe serum concentration of Toremifene can be increased when it is combined with Lomitapide.
Trastuzumab emtansineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Lomitapide.
UlipristalThe serum concentration of Ulipristal can be increased when it is combined with Lomitapide.
UmeclidiniumThe serum concentration of Umeclidinium can be increased when it is combined with Lomitapide.
VecuroniumThe serum concentration of Vecuronium can be increased when it is combined with Lomitapide.
VenlafaxineThe serum concentration of Lomitapide can be increased when it is combined with Venlafaxine.
VerapamilThe serum concentration of Lomitapide can be increased when it is combined with Verapamil.
VinblastineThe serum concentration of Vinblastine can be increased when it is combined with Lomitapide.
VincristineThe serum concentration of Vincristine can be increased when it is combined with Lomitapide.
VismodegibThe serum concentration of Vismodegib can be increased when it is combined with Lomitapide.
VoriconazoleThe serum concentration of Lomitapide can be increased when it is combined with Voriconazole.
WarfarinThe serum concentration of Warfarin can be increased when it is combined with Lomitapide.
ZidovudineThe serum concentration of Zidovudine can be increased when it is combined with Lomitapide.
ZiprasidoneThe serum concentration of Lomitapide can be increased when it is combined with Ziprasidone.
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.

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 September 26, 2016 02:22