Identification

Name
Lomitapide
Accession Number
DB08827
Type
Small Molecule
Groups
Approved
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).

Structure
Thumb
Synonyms
  • AEGR 733
  • BMS 201038
External IDs
AEGR-733 / AEGR-773 / BMS 201038 / BMS-201038-01 / BMS-201038-04
Product Ingredients
IngredientUNIICASInChI Key
Lomitapide mesylateX4S83CP54E202914-84-9QKVKOFVWUHNEBX-UHFFFAOYSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
JuxtapidCapsule5 mgOralAegerion Pharmaceuticals2014-05-06Not applicableCanada
JuxtapidCapsule60 mg/1OralAegerion Pharmaceuticals2013-01-03Not applicableUs
JuxtapidCapsule5 mg/1OralAegerion Pharmaceuticals2013-01-03Not applicableUs
JuxtapidCapsule30 mg/1OralAegerion Pharmaceuticals2013-01-03Not applicableUs
JuxtapidCapsule10 mgOralAegerion Pharmaceuticals2014-05-06Not applicableCanada
JuxtapidCapsule10 mg/1OralAegerion Pharmaceuticals2013-01-03Not applicableUs
JuxtapidCapsule40 mg/1OralAegerion Pharmaceuticals2013-01-03Not applicableUs
JuxtapidCapsule20 mgOralAegerion Pharmaceuticals2014-05-06Not applicableCanada
JuxtapidCapsule20 mg/1OralAegerion Pharmaceuticals2013-01-03Not applicableUs
International/Other Brands
Lojuxta
Categories
UNII
82KUB0583F
CAS number
182431-12-5
Weight
Average: 693.7204
Monoisotopic: 693.278996673
Chemical Formula
C39H37F6N3O2
InChI Key
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

Pharmacology

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).

Structured Indications
Pharmacodynamics

Lomitapide directly inhibits microsomal triglyceride transfer protein (MTP).

Mechanism of action

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.

TargetActionsOrganism
AMicrosomal triglyceride transfer protein large subunit
antagonist
Human
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%.

Volume of distribution

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

Protein binding

Plasma 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 elimination

About 52.9-59.5% is eliminated by the urine and 33.4-35.1% is eliminated by the feces.

Half life

Lomitapide half-life is about 39.7 hours.

Clearance
Not Available
Toxicity

Contra-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
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Lomitapide.Approved
AmiodaroneThe serum concentration of Lomitapide can be increased when it is combined with Amiodarone.Approved, Investigational
AprepitantThe serum concentration of Lomitapide can be increased when it is combined with Aprepitant.Approved, Investigational
AtazanavirThe serum concentration of Lomitapide can be increased when it is combined with Atazanavir.Approved, Investigational
AtomoxetineThe serum concentration of Lomitapide can be increased when it is combined with Atomoxetine.Approved
AtorvastatinThe risk or severity of adverse effects can be increased when Lomitapide is combined with Atorvastatin.Approved
BoceprevirThe serum concentration of Lomitapide can be increased when it is combined with Boceprevir.Approved, Withdrawn
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 risk or severity of adverse effects can be increased when Bromocriptine is combined with Lomitapide.Approved, Investigational
CabergolineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Lomitapide.Approved
CarbamazepineThe metabolism of Lomitapide can be increased when combined with Carbamazepine.Approved, Investigational
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
CholestyramineCholestyramine can cause a decrease in the absorption of Lomitapide resulting in a reduced serum concentration and potentially a decrease in efficacy.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
ClotrimazoleThe serum concentration of Lomitapide can be increased when it is combined with Clotrimazole.Approved, Vet Approved
CobicistatThe serum concentration of Lomitapide can be increased when it is combined with Cobicistat.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
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
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
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
DihydroergocornineThe risk or severity of adverse effects can be increased when Dihydroergocornine is combined with Lomitapide.Approved
DihydroergocristineThe risk or severity of adverse effects can be increased when Dihydroergocristine is combined with Lomitapide.Experimental
DihydroergocryptineThe risk or severity of adverse effects can be increased when Dihydroergocryptine is combined with Lomitapide.Experimental
DihydroergotamineThe serum concentration of Lomitapide can be increased when it is combined with Dihydroergotamine.Approved
DiltiazemThe serum concentration of Lomitapide can be increased when it is combined with Diltiazem.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
EnzalutamideThe serum concentration of Lomitapide can be decreased when it is combined with Enzalutamide.Approved
ErgonovineThe risk or severity of adverse effects can be increased when Ergonovine is combined with Lomitapide.Approved
ErgotamineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Lomitapide.Approved
ErythromycinThe serum concentration of Lomitapide can be increased when it is combined with Erythromycin.Approved, Vet Approved
EthanolEthanol may increase the hepatotoxic activities of Lomitapide.Approved
EverolimusThe serum concentration of Everolimus 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
FluvastatinThe serum concentration of Fluvastatin 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
IdelalisibThe serum concentration of Lomitapide can be increased when it is combined with Idelalisib.Approved
ImatinibThe serum concentration of Lomitapide can be increased when it is combined with Imatinib.Approved
IndinavirThe serum concentration of Lomitapide can be increased when it is combined with Indinavir.Approved
IsavuconazoniumThe serum concentration of Lomitapide can be increased when it is combined with Isavuconazonium.Approved, Investigational
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
KetoconazoleThe serum concentration of Lomitapide can be increased when it is combined with Ketoconazole.Approved, Investigational
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Lomitapide.Approved
LisurideThe risk or severity of adverse effects can be increased when Lisuride is combined with Lomitapide.Approved, Investigational
LopinavirThe serum concentration of Lomitapide can be increased when it is combined with Lopinavir.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
Lysergic Acid DiethylamideThe risk or severity of adverse effects can be increased when Lysergic Acid Diethylamide is combined with Lomitapide.Illicit, Investigational, Withdrawn
MetergolineThe risk or severity of adverse effects can be increased when Metergoline is combined with Lomitapide.Experimental
MethylergometrineThe risk or severity of adverse effects can be increased when Methylergometrine is combined with Lomitapide.Approved
MethysergideThe risk or severity of adverse effects can be increased when Methysergide is combined with Lomitapide.Approved
MevastatinThe serum concentration of Mevastatin can be increased when it is combined with Lomitapide.Experimental
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
MitotaneThe serum concentration of Lomitapide can be decreased when it is combined with Mitotane.Approved
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Lomitapide.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
NicergolineThe risk or severity of adverse effects can be increased when Nicergoline is combined with Lomitapide.Approved, Investigational
NilotinibThe serum concentration of Lomitapide can be increased when it is combined with Nilotinib.Approved, Investigational
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Lomitapide.Approved
OlaparibThe serum concentration of Lomitapide can be increased when it is combined with Olaparib.Approved
OsimertinibThe serum concentration of Lomitapide can be increased when it is combined with Osimertinib.Approved
PalbociclibThe serum concentration of Lomitapide can be increased when it is combined with Palbociclib.Approved
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
PergolideThe risk or severity of adverse effects can be increased when Pergolide is combined with Lomitapide.Approved, Investigational, Vet Approved, Withdrawn
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
PitavastatinThe serum concentration of Pitavastatin 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
PrimidoneThe metabolism of Lomitapide can be increased when combined with Primidone.Approved, Vet Approved
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Lomitapide.Approved
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Lomitapide.Approved, Investigational
RibociclibThe serum concentration of Lomitapide can be increased when it is combined with Ribociclib.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
RosuvastatinThe serum concentration of Rosuvastatin can be increased when it is combined with Lomitapide.Approved
SaquinavirThe serum concentration of Lomitapide can be increased when it is combined with Saquinavir.Approved, Investigational
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
St. John's WortThe serum concentration of Lomitapide can be decreased when it is combined with St. John's Wort.Investigational, 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
TelaprevirThe serum concentration of Lomitapide can be increased when it is combined with Telaprevir.Approved, Withdrawn
TelithromycinThe serum concentration of Lomitapide can be increased when it is combined with Telithromycin.Approved
TergurideThe risk or severity of adverse effects can be increased when Terguride is combined with Lomitapide.Experimental
TiclopidineThe serum concentration of Lomitapide can be increased when it is combined with Ticlopidine.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
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Lomitapide.Approved, Investigational
UbidecarenoneThe serum concentration of Ubidecarenone can be increased when it is combined with Lomitapide.Approved, Experimental
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
VincristineThe serum concentration of Vincristine can be increased when it is combined with Lomitapide.Approved, Investigational
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
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

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
KEGG Drug
D09637
PubChem Compound
9853053
PubChem Substance
175427108
ChemSpider
8028764
BindingDB
50098320
ChEBI
72297
ChEMBL
CHEMBL354541
PharmGKB
PA166114922
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Lomitapide
ATC Codes
C10AX12 — Lomitapide
AHFS Codes
  • 24:06.92 — Miscellaneous Antilipemic Agents
FDA label
Download (930 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedNot AvailableEffect of Atorvastatin on the Pharmacokinetics of Lomitapide1
1CompletedNot AvailableHealthy Volunteers2
1CompletedNot AvailableIntra-subject Variability of Pharmacokinetics1
1CompletedTreatmentHealthy Volunteers1
2CompletedTreatmentHomozygous Familial Hypercholesterolemia1
2CompletedTreatmentHypercholesterolaemia3
2CompletedTreatmentHyperlipidemias1
3Active Not RecruitingTreatmentFamilial Hypercholesterolemia - Homozygous1
3CompletedTreatmentHomozygous Familial Hypercholesterolemia1
3CompletedTreatmentHypercholesterolemia, Familial1
3WithdrawnTreatmentHomozygous Familial Hypercholesterolemia1
Not AvailableEnrolling by InvitationNot AvailableHomozygous Familial Hypercholesterolemia1
Not AvailableEnrolling by InvitationNot AvailablePregnancy1
Not AvailableNot Yet RecruitingNot AvailableHomozygous Familial Hypercholesterolemia1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
CapsuleOral10 mg
CapsuleOral10 mg/1
CapsuleOral20 mg/1
CapsuleOral20 mg
CapsuleOral30 mg/1
CapsuleOral40 mg/1
CapsuleOral5 mg
CapsuleOral5 mg/1
CapsuleOral60 mg/1
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5739135No2012-12-122015-04-14Us
US5712279No1996-02-212016-02-21Us
US6492365No1999-12-102019-12-10Us
US8618135No2005-03-072025-03-07Us
US7932268No2007-08-192027-08-19Us
US9265758No2005-03-072025-03-07Us
US9433617No2005-03-072025-03-07Us
US9364470No2005-03-072025-03-07Us

Properties

State
Solid
Experimental Properties
Not 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 FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This 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.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Fluorenes
Sub Class
Not Available
Direct Parent
Fluorenes
Alternative Parents
Biphenyls and derivatives / Trifluoromethylbenzenes / Benzamides / Benzoyl derivatives / Aralkylamines / Piperidines / Fatty amides / Amino acids and derivatives / Secondary carboxylic acid amides / Trialkylamines
show 7 more
Substituents
Fluorene / Biphenyl / Trifluoromethylbenzene / Benzamide / Benzoic acid or derivatives / Benzoyl / Aralkylamine / Monocyclic benzene moiety / Fatty amide / Piperidine
show 23 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
piperidines, benzamides, fluorenes, (trifluoromethyl)benzenes (CHEBI:72297)

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). Requ...
Gene Name
MTTP
Uniprot ID
P55157
Uniprot Name
Microsomal triglyceride transfer protein large subunit
Molecular Weight
99350.255 Da

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
Inhibitor
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 react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
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
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da

Drug created on January 03, 2013 13:34 / Updated on November 22, 2017 12:37