General Information of Drug (ID: DM053KT)

Drug Name
Aprepitant
Synonyms
Aprepitant [USAN]; L 754030; MK 0869; Emend (TN); L-754030; MK-0869; ONO-7436; Aprepitant (JAN/USAN/INN); MK-869, L-754030, Emend, Aprepitant; 3-(((2R,3S)-3-(p-Fluorophenyl)-2-(((alphaR)-alpha-methyl-3,5-bis(trifluoromethyl)benzyl)oxy)morpholino)methyl)-Delta(2)-1,2,4-triazolin-5-one; 3-(((2R,3S)-3-(p-Fluorophenyl)-2-(((alphaR)-alpha-methyl-3,5-bis(trifluoromethyl)benzyl)oxy)morpholino)methyl)-delta(sup 2)-1,2,4-triazolin-5-one; 5-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholin-4-yl]methyl]-1,2-dihydro-1,2,4-triazol-3-one; 5-[[(2S,3R)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholin-4-yl]methyl]-1,2-dihydro-1,2,4-triazol-3-one; 5-{[(2R,3S)-2-{(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy}-3-(4-fluorophenyl)morpholin-4-yl]methyl}-2,4-dihydro-3H-1,2,4-triazol-3-one
Indication
Disease Entry ICD 11 Status REF
Depression 6A70-6A7Z Approved [1], [2]
Nausea MD90 Approved [3], [4]
Solid tumour/cancer 2A00-2F9Z Phase 3 [5]
Therapeutic Class
Antiemetics
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 2 Molecular Weight (mw) 534.4
Topological Polar Surface Area (xlogp) 4.2
Rotatable Bond Count (rotbonds) 6
Hydrogen Bond Donor Count (hbonddonor) 2
Hydrogen Bond Acceptor Count (hbondacc) 12
ADMET Property
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 2: low solubility and high permeability [6]
Bioavailability
The bioavailability of drug is 60-65% [7]
Clearance
The apparent plasma clearance of drug is 62-90 mL/min [8]
Elimination
0% of drug is excreted from urine in the unchanged form [6]
Half-life
The concentration or amount of drug in body reduced by one-half in 9 - 13 hours [9]
Metabolism
The drug is metabolized via the CYP1A2 and CYP2C19 [7]
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 3.3413 micromolar/kg/day [10]
Unbound Fraction
The unbound fraction of drug in plasma is 0.05% [9]
Vd
The volume of distribution (Vd) of drug is 70 L [8]
Chemical Identifiers
Formula
C23H21F7N4O3
IUPAC Name
3-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholin-4-yl]methyl]-1,4-dihydro-1,2,4-triazol-5-one
Canonical SMILES
C[C@H](C1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F)O[C@@H]2[C@@H](N(CCO2)CC3=NNC(=O)N3)C4=CC=C(C=C4)F
InChI
InChI=1S/C23H21F7N4O3/c1-12(14-8-15(22(25,26)27)10-16(9-14)23(28,29)30)37-20-19(13-2-4-17(24)5-3-13)34(6-7-36-20)11-18-31-21(35)33-32-18/h2-5,8-10,12,19-20H,6-7,11H2,1H3,(H2,31,32,33,35)/t12-,19+,20-/m1/s1
InChIKey
ATALOFNDEOCMKK-OITMNORJSA-N
Cross-matching ID
PubChem CID
135413536
ChEBI ID
CHEBI:499361
CAS Number
170729-80-3
DrugBank ID
DB00673
TTD ID
D0GU4K
VARIDT ID
DR01398
INTEDE ID
DR0125
ACDINA ID
D00042

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Substance-P receptor (TACR1) TTZPO1L NK1R_HUMAN Antagonist [11]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [12]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4)
Main DME
DE4LYSA CP3A4_HUMAN Substrate [13]
Mephenytoin 4-hydroxylase (CYP2C19) DEGTFWK CP2CJ_HUMAN Substrate [14]
Cytochrome P450 1A2 (CYP1A2) DEJGDUW CP1A2_HUMAN Substrate [14]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease Depression
ICD Disease Classification 6A70-6A7Z
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Substance-P receptor (TACR1) DTT TACR1 7.40E-01 0.02 0.07
Substance-P receptor (TACR1) DTT TACR1 8.57E-01 -0.02 -0.18
P-glycoprotein 1 (ABCB1) DTP P-GP 1.19E-01 -1.32E-01 -2.77E-01
P-glycoprotein 1 (ABCB1) DTP P-GP 1.65E-01 -1.47E-01 -4.48E-01
Cytochrome P450 1A2 (CYP1A2) DME CYP1A2 6.73E-02 6.49E-02 3.07E-01
Cytochrome P450 1A2 (CYP1A2) DME CYP1A2 6.45E-01 2.07E-02 1.74E-01
Mephenytoin 4-hydroxylase (CYP2C19) DME CYP2C19 7.39E-01 1.54E-02 4.74E-02
Mephenytoin 4-hydroxylase (CYP2C19) DME CYP2C19 4.64E-02 -8.21E-02 -7.11E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 4.66E-01 4.25E-02 1.20E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 4.75E-01 5.15E-02 3.64E-01
Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Same Disease as Aprepitant
DDI Drug Name DDI Drug ID Severity Mechanism Disease REF
Vilazodone DM4LECQ Moderate Decreased metabolism of Aprepitant caused by Vilazodone mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [58]
Nefazodone DM4ZS8M Moderate Decreased metabolism of Aprepitant caused by Nefazodone mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [59]
Escitalopram DMFK9HG Minor Decreased metabolism of Aprepitant caused by Escitalopram mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [60]
OPC-34712 DMHG57U Major Decreased metabolism of Aprepitant caused by OPC-34712 mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [61]
Coadministration of a Drug Treating the Disease Different from Aprepitant (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Tretinoin DM49DUI Moderate Decreased metabolism of Aprepitant caused by Tretinoin mediated inhibition of CYP450 enzyme. Acne vulgaris [ED80] [59]
Repaglinide DM5SXUV Moderate Decreased metabolism of Aprepitant caused by Repaglinide mediated inhibition of CYP450 enzyme. Acute diabete complication [5A2Y] [62]
Pioglitazone DMKJ485 Moderate Decreased metabolism of Aprepitant caused by Pioglitazone mediated inhibition of CYP450 enzyme. Acute diabete complication [5A2Y] [59]
Nateglinide DMLK2QH Moderate Increased metabolism of Aprepitant caused by Nateglinide mediated induction of CYP450 enzyme. Acute diabete complication [5A2Y] [59]
Glipizide DMZA5PQ Moderate Increased metabolism of Aprepitant caused by Glipizide mediated induction of CYP450 enzyme. Acute diabete complication [5A2Y] [59]
Ivosidenib DM8S6T7 Major Increased metabolism of Aprepitant caused by Ivosidenib mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [63]
Midostaurin DMI6E0R Moderate Decreased metabolism of Aprepitant caused by Midostaurin mediated inhibition of CYP450 enzyme. Acute myeloid leukaemia [2A60] [64]
Oliceridine DM6MDCF Major Decreased metabolism of Aprepitant caused by Oliceridine mediated inhibition of CYP450 enzyme. Acute pain [MG31] [65]
Donepezil DMIYG7Z Minor Decreased metabolism of Aprepitant caused by Donepezil mediated inhibition of CYP450 enzyme. Alzheimer disease [8A20] [66]
Ivabradine DM0L594 Major Decreased metabolism of Aprepitant caused by Ivabradine mediated inhibition of CYP450 enzyme. Angina pectoris [BA40] [67]
Bepridil DM0RKS4 Moderate Decreased metabolism of Aprepitant caused by Bepridil mediated inhibition of CYP450 enzyme. Angina pectoris [BA40] [59]
Dronedarone DMA8FS5 Moderate Decreased metabolism of Aprepitant caused by Dronedarone mediated inhibition of CYP450 enzyme. Angina pectoris [BA40] [68]
Nifedipine DMSVOZT Moderate Decreased metabolism of Aprepitant caused by Nifedipine mediated inhibition of CYP450 enzyme. Angina pectoris [BA40] [59]
Methylphenobarbital DMDSWAG Moderate Increased metabolism of Aprepitant caused by Methylphenobarbital mediated induction of CYP450 enzyme. Anxiety disorder [6B00-6B0Z] [69]
Cilostazol DMZMSCT Major Decreased metabolism of Aprepitant caused by Cilostazol mediated inhibition of CYP450 enzyme. Arterial occlusive disease [BD40] [67]
Budesonide DMJIBAW Moderate Decreased metabolism of Aprepitant caused by Budesonide mediated inhibition of CYP450 enzyme. Asthma [CA23] [70]
Dalfopristin DM4LTKV Moderate Decreased metabolism of Aprepitant caused by Dalfopristin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [71]
Clarithromycin DM4M1SG Moderate Decreased metabolism of Aprepitant caused by Clarithromycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [59]
Rabeprazole DMMZXIW Moderate Decreased metabolism of Aprepitant caused by Rabeprazole mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [59]
Telithromycin DMZ4P3A Moderate Decreased metabolism of Aprepitant caused by Telithromycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [59]
Cariprazine DMJYDVK Moderate Decreased metabolism of Aprepitant caused by Cariprazine mediated inhibition of CYP450 enzyme. Bipolar disorder [6A60] [72]
Pexidartinib DMS2J0Z Major Decreased metabolism of Aprepitant caused by Pexidartinib mediated inhibition of CYP450 enzyme. Bone/articular cartilage neoplasm [2F7B] [73]
Ixabepilone DM2OZ3G Moderate Decreased metabolism of Aprepitant caused by Ixabepilone mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [74]
Lapatinib DM3BH1Y Moderate Decreased metabolism of Aprepitant caused by Lapatinib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [75]
HKI-272 DM6QOVN Major Decreased metabolism of Aprepitant caused by HKI-272 mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [76]
LY2835219 DM93VBZ Moderate Decreased metabolism of Aprepitant caused by LY2835219 mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [77]
Esterified estrogens DM9KZDO Moderate Decreased metabolism of Aprepitant caused by Esterified estrogens mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [59]
Tucatinib DMBESUA Moderate Decreased metabolism of Aprepitant caused by Tucatinib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [59]
Palbociclib DMD7L94 Moderate Decreased metabolism of Aprepitant caused by Palbociclib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [67]
Letrozole DMH07Y3 Moderate Decreased metabolism of Aprepitant caused by Letrozole mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [59]
Quinestrol DMJ6H1Z Moderate Decreased metabolism of Aprepitant caused by Quinestrol mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [59]
Tamoxifen DMLB0EZ Moderate Decreased metabolism of Aprepitant caused by Tamoxifen mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [59]
Cabazitaxel DMPAZHC Moderate Decreased metabolism of Aprepitant caused by Cabazitaxel mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [74]
Bosutinib DMTI8YE Major Decreased metabolism of Aprepitant caused by Bosutinib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [78]
Estradiol DMUNTE3 Moderate Decreased metabolism of Aprepitant caused by Estradiol mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [59]
Atorvastatin DMF28YC Moderate Decreased metabolism of Aprepitant caused by Atorvastatin mediated inhibition of CYP450 enzyme. Cardiovascular disease [BA00-BE2Z] [79]
PF-04449913 DMSB068 Moderate Decreased metabolism of Aprepitant caused by PF-04449913 mediated inhibition of CYP450 enzyme. Chronic myelomonocytic leukaemia [2A40] [80]
Indacaterol DMQJHR7 Minor Decreased metabolism of Aprepitant caused by Indacaterol mediated inhibition of CYP450 enzyme. Chronic obstructive pulmonary disease [CA22] [81]
Phenylbutazone DMAYL0T Moderate Increased metabolism of Aprepitant caused by Phenylbutazone mediated induction of CYP450 enzyme. Chronic pain [MG30] [59]
Dihydrocodeine DMB0FWL Moderate Decreased metabolism of Aprepitant caused by Dihydrocodeine mediated inhibition of CYP450 enzyme. Chronic pain [MG30] [71]
Anisindione DM2C48U Moderate Increased metabolism of Aprepitant caused by Anisindione mediated induction of CYP450 enzyme. Coagulation defect [3B10] [82]
Irinotecan DMP6SC2 Moderate Decreased metabolism of Aprepitant caused by Irinotecan mediated inhibition of CYP450 enzyme. Colorectal cancer [2B91] [74]
Drospirenone DM1A9W3 Moderate Increased metabolism of Aprepitant caused by Drospirenone mediated induction of CYP450 enzyme. Contraceptive management [QA21] [83]
Levonorgestrel DM1DP7T Moderate Increased metabolism of Aprepitant caused by Levonorgestrel mediated induction of CYP450 enzyme. Contraceptive management [QA21] [83]
Ulipristal DMBNI20 Minor Decreased metabolism of Aprepitant caused by Ulipristal mediated inhibition of CYP450 enzyme. Contraceptive management [QA21] [67]
Levobupivacaine DM783CH Moderate Decreased metabolism of Aprepitant caused by Levobupivacaine mediated inhibition of CYP450 enzyme. Corneal disease [9A76-9A78] [67]
Cocaine DMSOX7I Moderate Decreased metabolism of Aprepitant caused by Cocaine mediated inhibition of CYP450 enzyme. Corneal disease [9A76-9A78] [71]
Alfentanil DMVO0UB Major Decreased metabolism of Aprepitant caused by Alfentanil mediated inhibition of CYP450 enzyme. Corneal disease [9A76-9A78] [84]
Mifepristone DMGZQEF Moderate Decreased metabolism of Aprepitant caused by Mifepristone mediated inhibition of CYP450 enzyme. Cushing syndrome [5A70] [85]
Osilodrostat DMIJC9X Moderate Decreased metabolism of Aprepitant caused by Osilodrostat mediated inhibition of CYP450 enzyme. Cushing syndrome [5A70] [67]
Ivacaftor DMZC1HS Major Decreased metabolism of Aprepitant caused by Ivacaftor mediated inhibition of CYP450 enzyme. Cystic fibrosis [CA25] [67]
MK-8228 DMOB58Q Moderate Decreased metabolism of Aprepitant caused by MK-8228 mediated inhibition of CYP450 enzyme. Cytomegaloviral disease [1D82] [59]
Rivaroxaban DMQMBZ1 Moderate Decreased metabolism of Aprepitant caused by Rivaroxaban mediated inhibition of CYP450 enzyme. Deep vein thrombosis [BD71] [78]
Polatuzumab vedotin DMF6Y0L Moderate Decreased metabolism of Aprepitant caused by Polatuzumab vedotin mediated inhibition of CYP450 enzyme. Diffuse large B-cell lymphoma [2A81] [86]
[3H]estrone-3-sulphate DMGPF0N Moderate Decreased metabolism of Aprepitant caused by [3H]estrone-3-sulphate mediated inhibition of CYP450 enzyme. Discovery agent [N.A.] [71]
Oxybutynine DMJPBAX Moderate Decreased metabolism of Aprepitant caused by Oxybutynine mediated inhibition of CYP450 enzyme. Discovery agent [N.A.] [59]
Diazepam DM08E9O Moderate Decreased metabolism of Aprepitant caused by Diazepam mediated inhibition of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [87]
Primidone DM0WX6I Moderate Increased metabolism of Aprepitant caused by Primidone mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [59]
Felbamate DM1V5ZS Moderate Increased metabolism of Aprepitant caused by Felbamate mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [59]
Oxcarbazepine DM5PU6O Moderate Increased metabolism of Aprepitant caused by Oxcarbazepine mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [59]
Tiagabine DMKSQG0 Moderate Decreased metabolism of Aprepitant caused by Tiagabine mediated inhibition of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [59]
Stiripentol DMMSDOY Moderate Decreased metabolism of Aprepitant caused by Stiripentol mediated inhibition of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [67]
Fosphenytoin DMOX3LB Moderate Increased metabolism of Aprepitant caused by Fosphenytoin mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [59]
Clonazepam DMTO13J Moderate Decreased metabolism of Aprepitant caused by Clonazepam mediated inhibition of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [87]
Phenobarbital DMXZOCG Moderate Increased metabolism of Aprepitant caused by Phenobarbital mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [59]
Eslicarbazepine DMZREFQ Moderate Increased metabolism of Aprepitant caused by Eslicarbazepine mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [59]
Cannabidiol DM0659E Minor Decreased metabolism of Aprepitant caused by Cannabidiol mediated inhibition of CYP450 enzyme. Epileptic encephalopathy [8A62] [67]
Mefenamic acid DMK7HFI Moderate Increased metabolism of Aprepitant caused by Mefenamic acid mediated induction of CYP450 enzyme. Female pelvic pain [GA34] [59]
Bay 80-6946 DMLOS5R Moderate Decreased metabolism of Aprepitant caused by Bay 80-6946 mediated inhibition of CYP450 enzyme. Follicular lymphoma [2A80] [88]
Tazemetostat DMWP1BH Major Decreased metabolism of Aprepitant caused by Tazemetostat mediated inhibition of CYP450 enzyme. Follicular lymphoma [2A80] [89]
Solifenacin DMG592Q Moderate Decreased metabolism of Aprepitant caused by Solifenacin mediated inhibition of CYP450 enzyme. Functional bladder disorder [GC50] [90]
Mirabegron DMS1GYT Minor Decreased metabolism of Aprepitant caused by Mirabegron mediated inhibition of CYP450 enzyme. Functional bladder disorder [GC50] [91]
Itraconazole DMCR1MV Moderate Decreased metabolism of Aprepitant caused by Itraconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [59]
Miconazole DMPMYE8 Moderate Decreased metabolism of Aprepitant caused by Miconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [59]
Ketoconazole DMPZI3Q Moderate Decreased metabolism of Aprepitant caused by Ketoconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [59]
Ripretinib DM958QB Moderate Decreased metabolism of Aprepitant caused by Ripretinib mediated inhibition of CYP450 enzyme. Gastrointestinal stromal tumour [2B5B] [78]
Avapritinib DMK2GZX Major Decreased metabolism of Aprepitant caused by Avapritinib mediated inhibition of CYP450 enzyme. Gastrointestinal stromal tumour [2B5B] [67]
Colchicine DM2POTE Major Decreased metabolism of Aprepitant caused by Colchicine mediated inhibition of CYP450 enzyme. Gout [FA25] [92]
Sulfinpyrazone DMEV954 Moderate Increased metabolism of Aprepitant caused by Sulfinpyrazone mediated induction of CYP450 enzyme. Gout [FA25] [59]
Ergotamine DMKR3C5 Moderate Decreased metabolism of Aprepitant caused by Ergotamine mediated inhibition of CYP450 enzyme. Headache [8A80-8A84] [93]
Eplerenone DMF0NQR Major Decreased metabolism of Aprepitant caused by Eplerenone mediated inhibition of CYP450 enzyme. Heart failure [BD10-BD1Z] [94]
Digitoxin DMWVIGP Moderate Decreased metabolism of Aprepitant caused by Digitoxin mediated inhibition of CYP450 enzyme. Heart failure [BD10-BD1Z] [59]
Telaprevir DMMRV29 Moderate Decreased metabolism of Aprepitant caused by Telaprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [59]
Daclatasvir DMSFK9V Moderate Decreased metabolism of Aprepitant caused by Daclatasvir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [78]
Rifapentine DMCHV4I Moderate Increased metabolism of Aprepitant caused by Rifapentine mediated induction of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [59]
MK-1439 DM215WE Minor Decreased metabolism of Aprepitant caused by MK-1439 mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [95]
Fosamprenavir DM4W9B3 Moderate Decreased metabolism of Aprepitant caused by Fosamprenavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [59]
Cobicistat DM6L4H2 Moderate Decreased metabolism of Aprepitant caused by Cobicistat mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [59]
Dolutegravir DMCZGRE Minor Decreased metabolism of Aprepitant caused by Dolutegravir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [96]
Saquinavir DMG814N Moderate Decreased metabolism of Aprepitant caused by Saquinavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [59]
Etravirine DMGV8QU Moderate Decreased metabolism of Aprepitant caused by Etravirine mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [97]
Rilpivirine DMJ0QOW Moderate Decreased metabolism of Aprepitant caused by Rilpivirine mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [78]
Amprenavir DMLMXE0 Moderate Decreased metabolism of Aprepitant caused by Amprenavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [59]
Darunavir DMN3GCH Moderate Decreased metabolism of Aprepitant caused by Darunavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [59]
Atazanavir DMSYRBX Moderate Decreased metabolism of Aprepitant caused by Atazanavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [59]
Maraviroc DMTL94F Moderate Decreased metabolism of Aprepitant caused by Maraviroc mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [98]
Fluvastatin DM4MDJY Moderate Increased metabolism of Aprepitant caused by Fluvastatin mediated induction of CYP450 enzyme. Hyper-lipoproteinaemia [5C80] [59]
BMS-201038 DMQTAGO Major Decreased metabolism of Aprepitant caused by BMS-201038 mediated inhibition of CYP450 enzyme. Hyper-lipoproteinaemia [5C80] [78]
Aliskiren DM1BV7W Moderate Decreased metabolism of Aprepitant caused by Aliskiren mediated inhibition of CYP450 enzyme. Hypertension [BA00-BA04] [99]
Losartan DM72JXH Moderate Increased metabolism of Aprepitant caused by Losartan mediated induction of CYP450 enzyme. Hypertension [BA00-BA04] [59]
Levamlodipine DM92S6N Moderate Decreased metabolism of Aprepitant caused by Levamlodipine mediated inhibition of CYP450 enzyme. Hypertension [BA00-BA04] [99]
Felodipine DMOSW35 Moderate Decreased metabolism of Aprepitant caused by Felodipine mediated inhibition of CYP450 enzyme. Hypertension [BA00-BA04] [59]
Irbesartan DMTP1DC Moderate Increased metabolism of Aprepitant caused by Irbesartan mediated induction of CYP450 enzyme. Hypertension [BA00-BA04] [59]
Conivaptan DM1V329 Moderate Decreased metabolism of Aprepitant caused by Conivaptan mediated inhibition of CYP450 enzyme. Hypo-osmolality/hyponatraemia [5C72] [100]
Tolvaptan DMIWFRL Moderate Decreased metabolism of Aprepitant caused by Tolvaptan mediated inhibition of CYP450 enzyme. Hypo-osmolality/hyponatraemia [5C72] [101]
Fludrocortisone DMUDIR8 Moderate Decreased metabolism of Aprepitant caused by Fludrocortisone mediated inhibition of CYP450 enzyme. Hypo-osmolality/hyponatraemia [5C72] [59]
Retapamulin DM9JXB7 Minor Decreased metabolism of Aprepitant caused by Retapamulin mediated inhibition of CYP450 enzyme. Impetigo [1B72] [102]
Lesinurad DMUR64T Moderate Increased metabolism of Aprepitant caused by Lesinurad mediated induction of CYP450 enzyme. Inborn purine/pyrimidine/nucleotide metabolism error [5C55] [103]
Suvorexant DM0E6S3 Major Decreased metabolism of Aprepitant caused by Suvorexant mediated inhibition of CYP450 enzyme. Insomnia [7A00-7A0Z] [104]
Amobarbital DM0GQ8N Moderate Increased metabolism of Aprepitant caused by Amobarbital mediated induction of CYP450 enzyme. Insomnia [7A00-7A0Z] [59]
Triazolam DMETYK5 Moderate Decreased metabolism of Aprepitant caused by Triazolam mediated inhibition of CYP450 enzyme. Insomnia [7A00-7A0Z] [87]
Tasimelteon DMLOQ1V Moderate Decreased metabolism of Aprepitant caused by Tasimelteon mediated inhibition of CYP450 enzyme. Insomnia [7A00-7A0Z] [105]
ITI-007 DMUQ1DO Major Decreased metabolism of Aprepitant caused by ITI-007 mediated inhibition of CYP450 enzyme. Insomnia [7A00-7A0Z] [106]
Quazepam DMY4D87 Moderate Decreased metabolism of Aprepitant caused by Quazepam mediated inhibition of CYP450 enzyme. Insomnia [7A00-7A0Z] [87]
Estazolam DMZGXUM Moderate Decreased metabolism of Aprepitant caused by Estazolam mediated inhibition of CYP450 enzyme. Insomnia [7A00-7A0Z] [87]
Alosetron DML2A03 Moderate Increased metabolism of Aprepitant caused by Alosetron mediated induction of CYP450 enzyme. Irritable bowel syndrome [DD91] [59]
Naloxegol DML0B41 Major Decreased metabolism of Aprepitant caused by Naloxegol mediated inhibition of CYP450 enzyme. Large intestine motility disorder [DB32] [67]
Pemigatinib DM819JF Major Decreased metabolism of Aprepitant caused by Pemigatinib mediated inhibition of CYP450 enzyme. Liver cancer [2C12] [67]
Crizotinib DM4F29C Moderate Decreased metabolism of Aprepitant caused by Crizotinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [59]
Brigatinib DM7W94S Major Decreased metabolism of Aprepitant caused by Brigatinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [78]
Ceritinib DMB920Z Moderate Decreased metabolism of Aprepitant caused by Ceritinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [107]
Lurbinectedin DMEFRTZ Major Decreased metabolism of Aprepitant caused by Lurbinectedin mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [108]
PF-06463922 DMKM7EW Moderate Increased metabolism of Aprepitant caused by PF-06463922 mediated induction of CYP450 enzyme. Lung cancer [2C25] [59]
Osimertinib DMRJLAT Moderate Decreased metabolism of Aprepitant caused by Osimertinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [109]
Pralsetinib DMWU0I2 Moderate Decreased metabolism of Aprepitant caused by Pralsetinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [110]
Capmatinib DMYCXKL Moderate Decreased metabolism of Aprepitant caused by Capmatinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [111]
Selpercatinib DMZR15V Major Decreased metabolism of Aprepitant caused by Selpercatinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [67]
Halofantrine DMOMK1V Major Decreased metabolism of Aprepitant caused by Halofantrine mediated inhibition of CYP450 enzyme. Malaria [1F40-1F45] [112]
Hydroxychloroquine DMSIVND Moderate Decreased metabolism of Aprepitant caused by Hydroxychloroquine mediated inhibition of CYP450 enzyme. Malaria [1F40-1F45] [78]
Idelalisib DM602WT Moderate Decreased metabolism of Aprepitant caused by Idelalisib mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [59]
GDC-0199 DMH0QKA Major Decreased metabolism of Aprepitant caused by GDC-0199 mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [78]
IPI-145 DMWA24P Moderate Decreased metabolism of Aprepitant caused by IPI-145 mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [113]
Acalabrutinib DM7GCVW Major Decreased metabolism of Aprepitant caused by Acalabrutinib mediated inhibition of CYP450 enzyme. Mature B-cell lymphoma [2A85] [114]
Ibrutinib DMHZCPO Major Decreased metabolism of Aprepitant caused by Ibrutinib mediated inhibition of CYP450 enzyme. Mature B-cell lymphoma [2A85] [115]
Ponatinib DMYGJQO Moderate Decreased metabolism of Aprepitant caused by Ponatinib mediated inhibition of CYP450 enzyme. Mature B-cell lymphoma [2A85] [116]
Vemurafenib DM62UG5 Moderate Increased metabolism of Aprepitant caused by Vemurafenib mediated induction of CYP450 enzyme. Melanoma [2C30] [59]
Selumetinib DMC7W6R Major Decreased metabolism of Aprepitant caused by Selumetinib mediated inhibition of CYP450 enzyme. Melanoma [2C30] [117]
LGX818 DMNQXV8 Major Decreased metabolism of Aprepitant caused by LGX818 mediated inhibition of CYP450 enzyme. Melanoma [2C30] [118]
Dabrafenib DMX6OE3 Moderate Increased metabolism of Aprepitant caused by Dabrafenib mediated induction of CYP450 enzyme. Melanoma [2C30] [59]
Dienestrol DMBSXI0 Moderate Decreased metabolism of Aprepitant caused by Dienestrol mediated inhibition of CYP450 enzyme. Menopausal disorder [GA30] [71]
Ethinyl estradiol DMODJ40 Moderate Increased metabolism of Aprepitant caused by Ethinyl estradiol mediated induction of CYP450 enzyme. Menopausal disorder [GA30] [119]
Ubrogepant DM749I3 Moderate Decreased metabolism of Aprepitant caused by Ubrogepant mediated inhibition of CYP450 enzyme. Migraine [8A80] [120]
Almogran DM7I64Z Moderate Decreased metabolism of Aprepitant caused by Almogran mediated inhibition of CYP450 enzyme. Migraine [8A80] [59]
Flibanserin DM70DTN Major Decreased metabolism of Aprepitant caused by Flibanserin mediated inhibition of CYP450 enzyme. Mood disorder [6A60-6E23] [121]
Panobinostat DM58WKG Moderate Decreased metabolism of Aprepitant caused by Panobinostat mediated inhibition of CYP450 enzyme. Multiple myeloma [2A83] [74]
Siponimod DM2R86O Major Decreased metabolism of Aprepitant caused by Siponimod mediated inhibition of CYP450 enzyme. Multiple sclerosis [8A40] [78]
Fedratinib DM4ZBK6 Moderate Decreased metabolism of Aprepitant caused by Fedratinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [59]
Nilotinib DM7HXWT Moderate Decreased metabolism of Aprepitant caused by Nilotinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [122]
Ruxolitinib DM7Q98D Minor Decreased metabolism of Aprepitant caused by Ruxolitinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [67]
Dasatinib DMJV2EK Moderate Decreased metabolism of Aprepitant caused by Dasatinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [74]
Busulfan DMXYJ9C Moderate Decreased metabolism of Aprepitant caused by Busulfan mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [74]
Modafinil DMYILBE Minor Decreased metabolism of Aprepitant caused by Modafinil mediated inhibition of CYP450 enzyme. Narcolepsy [7A20] [78]
Netupitant DMEKAYI Moderate Decreased metabolism of Aprepitant caused by Netupitant mediated inhibition of CYP450 enzyme. Nausea/vomiting [MD90] [71]
Entrectinib DMMPTLH Major Decreased metabolism of Aprepitant caused by Entrectinib mediated inhibition of CYP450 enzyme. Non-small cell lung cancer [2C25] [78]
Sibutramine DMFJTDI Minor Decreased metabolism of Aprepitant caused by Sibutramine mediated inhibition of CYP450 enzyme. Obesity [5B80-5B81] [123]
Benzphetamine DMIJATC Moderate Decreased metabolism of Aprepitant caused by Benzphetamine mediated inhibition of CYP450 enzyme. Obesity [5B80-5B81] [59]
Levomethadyl Acetate DM06HG5 Major Decreased metabolism of Aprepitant caused by Levomethadyl Acetate mediated inhibition of CYP450 enzyme. Opioid use disorder [6C43] [124]
S-297995 DM26IH8 Moderate Decreased metabolism of Aprepitant caused by S-297995 mediated inhibition of CYP450 enzyme. Opioid use disorder [6C43] [67]
Naproxen DMZ5RGV Moderate Increased metabolism of Aprepitant caused by Naproxen mediated induction of CYP450 enzyme. Osteoarthritis [FA00-FA05] [59]
Olaparib DM8QB1D Major Decreased metabolism of Aprepitant caused by Olaparib mediated inhibition of CYP450 enzyme. Ovarian cancer [2C73] [78]
Rucaparib DM9PVX8 Moderate Decreased metabolism of Aprepitant caused by Rucaparib mediated inhibition of CYP450 enzyme. Ovarian cancer [2C73] [59]
Ibuprofen DM8VCBE Moderate Increased metabolism of Aprepitant caused by Ibuprofen mediated induction of CYP450 enzyme. Pain [MG30-MG3Z] [59]
Buprenorphine DMPRI8G Moderate Decreased metabolism of Aprepitant caused by Buprenorphine mediated inhibition of CYP450 enzyme. Pain [MG30-MG3Z] [125]
Hydrocodone DMQ2JO5 Major Decreased metabolism of Aprepitant caused by Hydrocodone mediated inhibition of CYP450 enzyme. Pain [MG30-MG3Z] [126]
Pimavanserin DMR7IVC Moderate Decreased metabolism of Aprepitant caused by Pimavanserin mediated inhibition of CYP450 enzyme. Parkinsonism [8A00] [127]
Abametapir DM2RX0I Moderate Decreased metabolism of Aprepitant caused by Abametapir mediated inhibition of CYP450 enzyme. Pediculosis [1G00] [128]
Lefamulin DME6G97 Moderate Decreased metabolism of Aprepitant caused by Lefamulin mediated inhibition of CYP450 enzyme. Pneumonia [CA40] [129]
Hydrocortisone DMGEMB7 Moderate Decreased metabolism of Aprepitant caused by Hydrocortisone mediated inhibition of CYP450 enzyme. Postoperative inflammation [1A00-CA43] [59]
Ergonovine DM0VEC1 Moderate Decreased metabolism of Aprepitant caused by Ergonovine mediated inhibition of CYP450 enzyme. Postpartum haemorrhage [JA43] [130]
Lonafarnib DMGM2Z6 Major Decreased metabolism of Aprepitant caused by Lonafarnib mediated inhibition of CYP450 enzyme. Premature ageing appearance [LD2B] [131]
Enzalutamide DMGL19D Moderate Decreased metabolism of Aprepitant caused by Enzalutamide mediated inhibition of CYP450 enzyme. Prostate cancer [2C82] [132]
Darolutamide DMV7YFT Minor Decreased metabolism of Aprepitant caused by Darolutamide mediated inhibition of CYP450 enzyme. Prostate cancer [2C82] [133]
Bicalutamide DMZMSPF Moderate Decreased metabolism of Aprepitant caused by Bicalutamide mediated inhibition of CYP450 enzyme. Prostate cancer [2C82] [59]
Tamsulosin DM5QF9V Moderate Decreased metabolism of Aprepitant caused by Tamsulosin mediated inhibition of CYP450 enzyme. Prostate hyperplasia [GA90] [134]
Silodosin DMJSBT6 Moderate Decreased metabolism of Aprepitant caused by Silodosin mediated inhibition of CYP450 enzyme. Prostate hyperplasia [GA90] [135]
Dutasteride DMQ4TJK Moderate Decreased metabolism of Aprepitant caused by Dutasteride mediated inhibition of CYP450 enzyme. Prostate hyperplasia [GA90] [136]
Everolimus DM8X2EH Major Decreased clearance of Aprepitant due to the transporter inhibition by Everolimus. Renal cell carcinoma [2C90] [137]
Axitinib DMGVH6N Moderate Decreased metabolism of Aprepitant caused by Axitinib mediated inhibition of CYP450 enzyme. Renal cell carcinoma [2C90] [59]
Temsirolimus DMS104F Moderate Decreased metabolism of Aprepitant caused by Temsirolimus mediated inhibition of CYP450 enzyme. Renal cell carcinoma [2C90] [138]
Meloxicam DM2AR7L Moderate Increased metabolism of Aprepitant caused by Meloxicam mediated induction of CYP450 enzyme. Rheumatoid arthritis [FA20] [59]
Upadacitinib DM32B5U Moderate Decreased metabolism of Aprepitant caused by Upadacitinib mediated inhibition of CYP450 enzyme. Rheumatoid arthritis [FA20] [139]
Flurbiprofen DMGN4BY Moderate Increased metabolism of Aprepitant caused by Flurbiprofen mediated induction of CYP450 enzyme. Rheumatoid arthritis [FA20] [59]
Dexamethasone DMMWZET Moderate Decreased metabolism of Aprepitant caused by Dexamethasone mediated inhibition of CYP450 enzyme. Rheumatoid arthritis [FA20] [59]
Quetiapine DM1N62C Moderate Decreased metabolism of Aprepitant caused by Quetiapine mediated inhibition of CYP450 enzyme. Schizophrenia [6A20] [140]
Aripiprazole DM3NUMH Moderate Decreased metabolism of Aprepitant caused by Aripiprazole mediated inhibition of CYP450 enzyme. Schizophrenia [6A20] [141]
Pimozide DMW83TP Major Decreased metabolism of Aprepitant caused by Pimozide mediated inhibition of CYP450 enzyme. Schizophrenia [6A20] [78]
Fentanyl DM8WAHT Major Decreased metabolism of Aprepitant caused by Fentanyl mediated inhibition of CYP450 enzyme. Sensation disturbance [MB40] [78]
Sufentanil DMU7YEL Moderate Decreased metabolism of Aprepitant caused by Sufentanil mediated inhibition of CYP450 enzyme. Sensation disturbance [MB40] [59]
Avanafil DM75CXN Major Decreased metabolism of Aprepitant caused by Avanafil mediated inhibition of CYP450 enzyme. Sexual dysfunction [HA00-HA01] [142]
Tadalafil DMJZHT1 Moderate Decreased metabolism of Aprepitant caused by Tadalafil mediated inhibition of CYP450 enzyme. Sexual dysfunction [HA00-HA01] [143]
Vardenafil DMTBGW8 Moderate Decreased metabolism of Aprepitant caused by Vardenafil mediated inhibition of CYP450 enzyme. Sexual dysfunction [HA00-HA01] [144]
Voxelotor DMCS6M5 Moderate Decreased metabolism of Aprepitant caused by Voxelotor mediated inhibition of CYP450 enzyme. Sickle-cell disorder [3A51] [59]
LDE225 DMM9F25 Major Decreased metabolism of Aprepitant caused by LDE225 mediated inhibition of CYP450 enzyme. Skin cancer [2C30-2C37] [145]
Telotristat ethyl DMDIYFZ Moderate Increased metabolism of Aprepitant caused by Telotristat ethyl mediated induction of CYP450 enzyme. Small intestine developmental anomaly [DA90] [67]
Larotrectinib DM26CQR Moderate Decreased metabolism of Aprepitant caused by Larotrectinib mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [78]
Methylprednisolone DM4BDON Moderate Decreased metabolism of Aprepitant caused by Methylprednisolone mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [59]
Ifosfamide DMCT3I8 Moderate Decreased metabolism of Aprepitant caused by Ifosfamide mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [74]
Docetaxel DMDI269 Moderate Decreased metabolism of Aprepitant caused by Docetaxel mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [146]
Trabectedin DMG3Y89 Moderate Decreased metabolism of Aprepitant caused by Trabectedin mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [74]
Armodafinil DMGB035 Minor Decreased metabolism of Aprepitant caused by Armodafinil mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [78]
Etoposide DMNH3PG Moderate Decreased metabolism of Aprepitant caused by Etoposide mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [74]
Prednisolone DMQ8FR2 Moderate Decreased metabolism of Aprepitant caused by Prednisolone mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [59]
Norethindrone DMTY169 Moderate Increased metabolism of Aprepitant caused by Norethindrone mediated induction of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [119]
Taxol DMUOT9V Moderate Decreased metabolism of Aprepitant caused by Taxol mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [74]
Doxorubicin DMVP5YE Moderate Decreased metabolism of Aprepitant caused by Doxorubicin mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [74]
Warfarin DMJYCVW Moderate Increased metabolism of Aprepitant caused by Warfarin mediated induction of CYP450 enzyme. Supraventricular tachyarrhythmia [BC81] [82]
Fostamatinib DM6AUHV Moderate Decreased metabolism of Aprepitant caused by Fostamatinib mediated inhibition of CYP450 enzyme. Thrombocytopenia [3B64] [147]
Apixaban DM89JLN Moderate Decreased metabolism of Aprepitant caused by Apixaban mediated inhibition of CYP450 enzyme. Thrombosis [DB61-GB90] [67]
Brilinta DMBR01X Moderate Decreased metabolism of Aprepitant caused by Brilinta mediated inhibition of CYP450 enzyme. Thrombosis [DB61-GB90] [67]
Cabozantinib DMIYDT4 Moderate Decreased metabolism of Aprepitant caused by Cabozantinib mediated inhibition of CYP450 enzyme. Thyroid cancer [2D10] [148]
Sirolimus DMGW1ID Moderate Decreased metabolism of Aprepitant caused by Sirolimus mediated inhibition of CYP450 enzyme. Transplant rejection [NE84] [59]
Tacrolimus DMZ7XNQ Moderate Decreased metabolism of Aprepitant caused by Tacrolimus mediated inhibition of CYP450 enzyme. Transplant rejection [NE84] [59]
Saxagliptin DMGXENV Moderate Decreased metabolism of Aprepitant caused by Saxagliptin mediated inhibition of CYP450 enzyme. Type 2 diabetes mellitus [5A11] [67]
Elagolix DMB2C0E Moderate Decreased metabolism of Aprepitant caused by Elagolix mediated inhibition of CYP450 enzyme. Uterine fibroid [2E86] [149]
Fluticasone DMGCSVF Moderate Decreased metabolism of Aprepitant caused by Fluticasone mediated inhibition of CYP450 enzyme. Vasomotor/allergic rhinitis [CA08] [78]
Propafenone DMPIBJK Moderate Decreased metabolism of Aprepitant caused by Propafenone mediated inhibition of CYP450 enzyme. Ventricular tachyarrhythmia [BC71] [150]
Amiodarone DMUTEX3 Moderate Decreased metabolism of Aprepitant caused by Amiodarone mediated inhibition of CYP450 enzyme. Ventricular tachyarrhythmia [BC71] [59]
⏷ Show the Full List of 217 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG
DIG Name DIG ID PubChem CID Functional Classification
FD&C blue no. 1 E00263 19700 Colorant
Mannitol E00103 6251 Diluent; Flavoring agent; Lyophilization aid; Plasticizing agent; Tonicity agent
Sodium lauryl sulfate E00464 3423265 Emulsifying agent; Modified-release agent; Penetration agent; Solubilizing agent; Surfactant; lubricant
Sodium stearyl fumarate E00545 23665634 lubricant
Eisenoxyd E00585 56841934 Colorant
FD&C red no. 3 E00629 Not Available Colorant
Ferric hydroxide oxide yellow E00539 23320441 Colorant
Ferrosoferric oxide E00231 14789 Colorant
Poloxamer 407 E00646 Not Available Emulsifying agent; Solubilizing agent; Surfactant
Potassium hydroxide E00233 14797 Alkalizing agent
Propylene glycol E00040 1030 Antimicrobial preservative; Humectant; Plasticizing agent; Solvent
Saccharose E00091 5988 Binding agent; Coating agent; Cryoprotectant; Diluent; Flavoring agent; Suspending agent; Viscosity-controlling agent
Silicon dioxide E00670 Not Available Anticaking agent; Opacifying agent; Viscosity-controlling agent
Titanium dioxide E00322 26042 Coating agent; Colorant; Opacifying agent
Tocophersolan E00679 Not Available Antioxidant; Binding agent; Emulsifying agent; Ointment base; Solubilizing agent; Surfactant; Suspending agent
Water E00035 962 Solvent
⏷ Show the Full List of 16 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Aprepitant 125 mg capsule 125 mg Oral Capsule Oral
Aprepitant 40 mg capsule 40 mg Oral Capsule Oral
Aprepitant 80 mg capsule 80 mg Oral Capsule Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
2 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009602)
3 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3490).
4 Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77.
5 ClinicalTrials.gov (NCT00571168) Efficacy and Safety of Aprepitant in Subjects With Multiple Myeloma During and After High-dose Chemotherapy. U.S. National Institutes of Health.
6 BDDCS applied to over 900 drugs
7 FDA approval: ado-trastuzumab emtansine for the treatment of patients with HER2-positive metastatic breast cancer. Clin Cancer Res. 2014 Sep 1;20(17):4436-41.
8 An FDA phase I clinical trial of quinacrine sterilization (QS). Int J Gynaecol Obstet. 2003 Oct;83 Suppl 2:S45-9.
9 Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
10 Estimating the safe starting dose in phase I clinical trials and no observed effect level based on QSAR modeling of the human maximum recommended daily dose
11 Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists. J Med Chem. 2009 May 14;52(9):3039-46.
12 Improving the prediction of the brain disposition for orally administered drugs using BDDCS. Adv Drug Deliv Rev. 2012 Jan;64(1):95-109.
13 Lack of effect of aprepitant on the pharmacokinetics of docetaxel in cancer patients. Cancer Chemother Pharmacol. 2005 Jun;55(6):609-16.
14 Cytochrome P450 3A4 is the major enzyme involved in the metabolism of the substance P receptor antagonist aprepitant. Drug Metab Dispos. 2004 Nov;32(11):1287-92.
15 Expression levels and activation of a PXR variant are directly related to drug resistance in osteosarcoma cell lines. Cancer. 2007 Mar 1;109(5):957-65.
16 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
17 Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310(3):1062-75.
18 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
19 Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772.
20 Potent mechanism-based inhibition of CYP3A4 by imatinib explains its liability to interact with CYP3A4 substrates. Br J Pharmacol. 2012 Apr;165(8):2787-98.
21 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
22 The metabolism of zidovudine by human liver microsomes in vitro: formation of 3'-amino-3'-deoxythymidine. Biochem Pharmacol. 1994 Jul 19;48(2):267-76.
23 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
24 Roles of cytochromes P450 1A2, 2A6, and 2C8 in 5-fluorouracil formation from tegafur, an anticancer prodrug, in human liver microsomes. Drug Metab Dispos. 2000 Dec;28(12):1457-63.
25 Effects of polyunsaturated fatty acids on prostaglandin synthesis and cyclooxygenase-mediated DNA adduct formation by heterocyclic aromatic amines in human adenocarcinoma colon cells. Mol Carcinog. 2004 Jul;40(3):180-8.
26 Endoxifen and other metabolites of tamoxifen inhibit human hydroxysteroid sulfotransferase 2A1 (hSULT2A1). Drug Metab Dispos. 2014 Nov;42(11):1843-50.
27 Cytochrome P450 1A2 (CYP1A2) activity and risk factors for breast cancer: a cross-sectional study. Breast Cancer Res. 2004;6(4):R352-65.
28 PharmGKB summary: pathways of acetaminophen metabolism at the therapeutic versus toxic doses. Pharmacogenet Genomics. 2015 Aug;25(8):416-26.
29 The effect of apigenin on pharmacokinetics of imatinib and its metabolite N-desmethyl imatinib in rats. Biomed Res Int. 2013;2013:789184.
30 The influence of metabolic gene polymorphisms on urinary 1-hydroxypyrene concentrations in Chinese coke oven workers. Sci Total Environ. 2007 Aug 1;381(1-3):38-46.
31 Identification of P450 enzymes involved in metabolism of verapamil in humans. Naunyn Schmiedebergs Arch Pharmacol. 1993 Sep;348(3):332-7.
32 Metabolism and metabolic inhibition of xanthotoxol in human liver microsomes. Evid Based Complement Alternat Med. 2016;2016:5416509.
33 High-dose rabeprazole/amoxicillin therapy as the second-line regimen after failure to eradicate H. pylori by triple therapy with the usual doses of a proton pump inhibitor, clarithromycin and amoxicillin. Hepatogastroenterology. 2003 Nov-Dec;50(54):2274-8.
34 Progesterone and testosterone hydroxylation by cytochromes P450 2C19, 2C9, and 3A4 in human liver microsomes. Arch Biochem Biophys. 1997 Oct 1;346(1):161-9.
35 Cytochrome P450 pharmacogenetics and cancer. Oncogene. 2006 Mar 13;25(11):1679-91.
36 CYP2C19*17 is associated with decreased breast cancer risk. Breast Cancer Res Treat. 2009 May;115(2):391-6.
37 Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
38 Cytochromes of the P450 2C subfamily are the major enzymes involved in the O-demethylation of verapamil in humans. Naunyn Schmiedebergs Arch Pharmacol. 1995 Dec;353(1):116-21.
39 Diclofenac and its derivatives as tools for studying human cytochromes P450 active sites: particular efficiency and regioselectivity of P450 2Cs. Biochemistry. 1999 Oct 26;38(43):14264-70.
40 A mechanistic approach to antiepileptic drug interactions. Ann Pharmacother. 1998 May;32(5):554-63.
41 Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver. Gastroenterology. 2001 Feb;120(2):525-33.
42 Possible involvement of multiple human cytochrome P450 isoforms in the liver metabolism of propofol. Br J Anaesth. 1998 Jun;80(6):788-95.
43 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
44 MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
45 Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade. Cancer Lett. 2016 Jan 1;370(1):153-64.
46 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
47 Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
48 Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
49 Association of genetic polymorphisms in the influx transporter SLCO1B3 and the efflux transporter ABCB1 with imatinib pharmacokinetics in patients with chronic myeloid leukemia. Ther Drug Monit. 2011 Apr;33(2):244-50.
50 Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
51 Netupitant and palonosetron trigger NK1 receptor internalization in NG108-15 cells. Exp Brain Res. 2014 Aug;232(8):2637-44.
52 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
53 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
54 Stress-related neuropeptides and alcoholism: CRH, NPY and beyond. Alcohol. 2009 November; 43(7): 491-498.
55 A review of drug options in age-related macular degeneration therapy and potential new agents. Expert Opin Pharmacother. 2006 Dec;7(17):2355-68.
56 Efficacy and safety of casopitant mesylate, a neurokinin 1 (NK1)-receptor antagonist, in prevention of chemotherapy-induced nausea and vomiting in patients receiving cisplatin-based highly emetogenicchemotherapy: a randomised, double-blind, placebo-controlled trial. Lancet Oncol. 2009 Jun;10(6):549-58.
57 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 360).
58 Product Information. Viibryd (vilazodone). Trovis Pharmaceuticals LLC, New Haven, CT.
59 Product Information. Emend (aprepitant). Merck & Company Inc, West Point, PA.
60 Product Information. Celexa (citalopram). Forest Pharmaceuticals, St. Louis, MO.
61 Product Information. Rexulti (brexpiprazole). Otsuka American Pharmaceuticals Inc, Rockville, MD.
62 Bidstrup TB, Bjornsdottir I, Sidelmann UG, Thomsen MS, Hansen KT "CYP2C8 and CYP3A4 are the principal enzymes involved in the human in vitro biotransformation of the insulin secretagogue repaglinide." Br J Clin Pharmacol 56 (2003): 305-14. [PMID: 12919179]
63 Product Information. Tibsovo (ivosidenib). Agios Pharmaceuticals, Cambridge, MA.
64 Dutreix C, Munarini F, Lorenzo S, Roesel J, Wang Y "Investigation into CYP3A4-mediated drug-drug interactions on midostaurin in healthy volunteers." Cancer Chemother Pharmacol 72 (2013): 1223-34. [PMID: 24085261]
65 Product Information. Olinvyk (oliceridine). Trevena Inc, Chesterbrook, PA.
66 Product Information. Aricept (donepezil). Pfizer US Pharmaceuticals, New York, NY.
67 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
68 Product Information. Multaq (dronedarone). sanofi-aventis , Bridgewater, NJ.
69 Product Information. Diabinese (chlorpropamide). Pfizer US Pharmaceuticals, New York, NY.
70 Bolland MJ, Bagg W, Thomas MG, Lucas JA, Ticehurst R, Black PN "Cushing's syndrome due to interaction between inhaled corticosteroids and itraconazole." Ann Pharmacother 38 (2004): 46-9. [PMID: 14742792]
71 Product Information. Emend (aprepitant). Merck &amp Company Inc, West Point, PA.
72 Product Information. Vraylar (cariprazine). Actavis Pharma, Inc., Parsippany, NJ.
73 Product Information. Turalio (pexidartinib). Daiichi Sankyo, Inc., Parsippany, NJ.
74 Charasson V, Haaz MC, Robert J "Determination of Drug Interactions Occurring with the Metabolic Pathways of Irinotecan." Drug Metab Dispos 30 (2002): 731-733. [PMID: 12019202]
75 Product Information. Tykerb (lapatinib). Novartis Pharmaceuticals, East Hanover, NJ.
76 Abbas R, Hug BA, Leister C, Burns J, Sonnichsen D "Pharmacokinetics of oral neratinib during co-administration of ketoconazole in healthy subjects." Br J Clin Pharmacol 71 (2011): 522-7. [PMID: 21395644]
77 Product Information. Verzenio (abemaciclib). Lilly, Eli and Company, Indianapolis, IN.
78 Cerner Multum, Inc. "Australian Product Information.".
79 Agbin NE, Brater DC, Hall SD "Interaction of diltiazem with lovastatin and pravastatin." Clin Pharmacol Ther 61 (1997): 201. [PMID: 9797793]
80 Product Information. Daurismo (glasdegib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
81 Product Information. Arcapta Neohaler (indacaterol). Novartis Pharmaceuticals, East Hanover, NJ.
82 Hermans JJ, Thijssen HH "Human liver microsomal metabolism of the enantiomers of warfarin and acenocoumarol: P450 isozyme diversity determines the differences in their pharmacokinetics." Br J Pharmacol 110 (1993): 482-90. [PMID: 8220911]
83 Faculty of Sexual & Reproductive Healthcare "FSRH Clinical Guidance: Drug Interactions with Hormonal Contraception.".
84 Bartkowski RR, Goldberg ME, Larijani GE, Boerner T "Inhibition of alfentanil metabolism by erythromycin." Clin Pharmacol Ther 46 (1989): 99-102. [PMID: 2501060]
85 Product Information. Korlym (mifepristone). Corcept Therapeutics Incorporated, Menlo Park, CA.
86 Product Information. Polivy (polatuzumab vedotin). Genentech, South San Francisco, CA.
87 Dresser GK, Spence JD, Bailey DG "Pharmacokinetic-pharmacodynamic consequences and clinical relevance of cytochrome P450 3A4 inhibition." Clin Pharmacokinet 38 (2000): 41-57. [PMID: 10668858]
88 Product Information. Aliqopa (copanlisib). Bayer Pharmaceutical Inc, West Haven, CT.
89 Product Information. Tazverik (tazemetostat). Epizyme, Inc, Cambridge, MA.
90 Product Information. VESIcare (solifenacin). GlaxoSmithKline, Research Triangle Park, NC.
91 Product Information. Myrbetriq (mirabegron). Astellas Pharma US, Inc, Deerfield, IL.
92 Akdag I, Ersoy A, Kahvecioglu S, Gullulu M, Dilek K "Acute colchicine intoxication during clarithromycin administration in patients with chronic renal failure." J Nephrol 19 (2006): 515-7. [PMID: 17048210]
93 Ausband SC, Goodman PE "An unusual case of clarithromycin associated ergotism." J Emerg Med 4 (2001): 411-3. [PMID: 11728770]
94 Product Information. Inspra (eplerenone). Searle, Chicago, IL.
95 Product Information. Pifeltro (doravirine). Merck & Company Inc, Whitehouse Station, NJ.
96 Product Information. Tivicay (dolutegravir). ViiV Healthcare, Research Triangle Park, NC.
97 Product Information. Intelence (etravirine). Ortho Biotech Inc, Bridgewater, NJ.
98 Product Information. Selzentry (maraviroc). Pfizer U.S. Pharmaceuticals Group, New York, NY.
99 Canadian Pharmacists Association.
100 Product Information. Vaprisol (conivaptan). Cumberland Pharmaceuticals Inc, Nashville, TN.
101 Product Information. Samsca (tolvaptan). Otsuka American Pharmaceuticals Inc, Rockville, MD.
102 Product Information. Altabax (retapamulin topical). GlaxoSmithKline, Research Triangle Park, NC.
103 Product Information. Zurampic (lesinurad). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
104 Product Information. Belsomra (suvorexant). Merck & Company Inc, Whitehouse Station, NJ.
105 Product Information. Hetlioz (tasimelteon). Vanda Pharmaceuticals Inc, Rockville, MD.
106 Product Information. Caplyta (lumateperone). Intra-Cellular Therapies, Inc., New York, NY.
107 Product Information. Zykadia (ceritinib). Novartis Pharmaceuticals, East Hanover, NJ.
108 Product Information. Zepzelca (lurbinectedin). Jazz Pharmaceuticals, Palo Alto, CA.
109 Product Information. Tagrisso (osimertinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
110 Product Information. Gavreto (pralsetinib). Blueprint Medicines Corporation, Cambridge, MA.
111 Product Information. Tabrecta (capmatinib). Novartis Pharmaceuticals, East Hanover, NJ.
112 Abernethy DR, Wesche DL, Barbey JT, et al. "Stereoselective halofantrine disposition and effect: concentration-related QTc prolongation." Br J Clin Pharmacol 51 (2001): 231-7. [PMID: 11298069]
113 Product Information. Copiktra (duvelisib). Verastem, Inc., Needham, MA.
114 Product Information. Calquence (acalabrutinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
115 Product Information. Imbruvica (ibrutinib). Pharmacyclics Inc, Sunnyvale, CA.
116 Product Information. Iclusig (ponatinib). Ariad Pharmaceuticals Inc, Cambridge, MA.
117 Product Information. Koselugo (selumetinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
118 Product Information. Braftovi (encorafenib). Array BioPharma Inc., Boulder, CO.
119 Faculty of Sexual & Reproductive Healthcare "FSRH Clinical Guidance: Drug Interactions with Hormonal Contraception.".
120 Product Information. Ubrelvy (ubrogepant). Allergan Inc, Irvine, CA.
121 Product Information. Addyi (flibanserin). Sprout Pharmaceuticals, Raleigh, NC.
122 Product Information. Tasigna (nilotinib). Novartis Pharmaceuticals, East Hanover, NJ.
123 Product Information. Meridia (sibutramine). Knoll Pharmaceutical Company, Whippany, NJ.
124 Product Information. Orlaam (levomethadyl acetate) Roxanne Laboratories Inc, Columbus, OH.
125 Product Information. Buprenex (buprenorphine). Reckitt and Colman Pharmaceutical, Richmond, VA.
126 Hutchinson MR, Menelaou A, Foster DJ, Coller JK, Somogyi AA "CYP2D6 and CYP3A4 involvement in the primary oxidative metabolism of hydrocodone by human liver microsomes." Br J Clin Pharmacol 57 (2004): 287-97. [PMID: 14998425]
127 Product Information. Nuplazid (pimavanserin). Accelis Pharma, East Windsor, NJ.
128 Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ.
129 Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA.
130 Francis H, Tyndall A, Webb J "Severe vascular spasm due to erythromycin-ergotamine interaction." Clin Rheumatol 3 (1984): 243-6. [PMID: 6236021]
131 Product Information. Zokinvy (lonafarnib). Eiger BioPharmaceuticals, Palo Alto, CA.
132 Product Information. Xtandi (enzalutamide). Astellas Pharma US, Inc, Deerfield, IL.
133 Product Information. Nubeqa (darolutamide). Bayer HealthCare Pharmaceuticals Inc., Whippany, NJ.
134 Franco-Salinas G, de la Rosette JJ, Michel MC "Pharmacokinetics and pharmacodynamics of tamsulosin in its modified-release and oral controlled absorption system formulations." Clin Pharmacokinet 49 (2010): 177-88. [PMID: 20170206]
135 Product Information. Rapaflo (silodosin). Watson Pharmaceuticals, Corona, CA.
136 Product Information. Duagen (dutasteride). GlaxoSmithKline Healthcare, Pittsburgh, PA.
137 Product Information. Afinitor (everolimus). Novartis Pharmaceuticals, East Hanover, NJ.
138 Product Information. Torisel (temsirolimus). Wyeth-Ayerst Laboratories, Philadelphia, PA.
139 Product Information. Rinvoq (upadacitinib). AbbVie US LLC, North Chicago, IL.
140 DeVane CL, Nemeroff CB "Clinical pharmacokinetics of quetiapine - An atypical antipsychotic." Clin Pharmacokinet 40 (2001): 509-22. [PMID: 11510628]
141 Product Information. Abilify (aripiprazole). Bristol-Myers Squibb, Princeton, NJ.
142 Product Information. Stendra (avanafil). Vivus Inc, Mountain View, CA.
143 Product Information. Cialis (tadalafil). Lilly, Eli and Company, Indianapolis, IN.
144 Product Information. Levitra (vardenafil). Bayer, West Haven, CT.
145 Product Information. Odomzo (sonidegib). Novartis Pharmaceuticals, East Hanover, NJ.
146 Aronson JK, Grahame-Smith DG "Clinical pharmacology: adverse drug interactions." Br Med J 282 (1981): 288-91. [PMID: 6779990]
147 Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.
148 Product Information. Cometriq (cabozantinib). Exelixis Inc, S San Francisco, CA.
149 Product Information. Orilissa (elagolix). AbbVie US LLC, North Chicago, IL.
150 Product Information. Rythmol SR (propafenone). GlaxoSmithKline, Research Triangle Park, NC.