U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Approval Year

Unknown
139594
Substance Class Protein
Created
by admin
on Sat Dec 16 09:19:35 UTC 2023
Edited
by admin
on Sat Dec 16 09:19:35 UTC 2023
Protein Type TRANSPORTER
Protein Sub Type ATP-BINDING CASSETTE TRANSPORTER
Sequence Origin HUMAN
Sequence Type COMPLETE
Record UNII
22ES734693
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
MULTIDRUG RESISTANCE PROTEIN 1
Common Name English
MDR1
Common Name English
PGY1
Common Name English
ATP-BINDING CASSETTE SUB-FAMILY B MEMBER 1
Common Name English
PGP-1
Common Name English
MULTIDRUG RESISTANCE PROTEIN 1 (HUMAN)
Common Name English
P-GP
Common Name English
GP170
Common Name English
MGC163296
Common Name English
CD-243
Code English
CLCS
Common Name English
P-GLYCOPROTEIN 1
Common Name English
MDR-1
Common Name English
ATP-BINDING CASSETTE B1
Common Name English
ABC20
Common Name English
ABCB1
Common Name English
P-GLYCOPROTEIN
Common Name English
CD243
Common Name English
Classification Tree Code System Code
UCSF-FDA TRANSPORTAL ABCB1
Created by admin on Sat Dec 16 09:19:53 UTC 2023 , Edited by admin on Sat Dec 16 09:19:53 UTC 2023
EC (ENZYME CLASS) EC 3.6.3.44
Created by admin on Sat Dec 16 09:19:53 UTC 2023 , Edited by admin on Sat Dec 16 09:19:53 UTC 2023
Code System Code Type Description
CAS
1646537-23-6
Created by admin on Sat Dec 16 09:19:53 UTC 2023 , Edited by admin on Sat Dec 16 09:19:53 UTC 2023
PRIMARY
UNIPROT
P08183
Created by admin on Sat Dec 16 09:19:53 UTC 2023 , Edited by admin on Sat Dec 16 09:19:53 UTC 2023
PRIMARY
FDA UNII
22ES734693
Created by admin on Sat Dec 16 09:19:53 UTC 2023 , Edited by admin on Sat Dec 16 09:19:53 UTC 2023
PRIMARY
Glycosylation Type HUMAN
Glycosylation Link Type Site
N 1_91
N 1_94
N 1_99
O 1_419
Related Record Type Details
Structure of REGORAFENIB ANHYDROUS
INHIBITOR -> TRANSPORTER
Regorafenib inhibits Pgp and BCRP in vitro.
Structure of VENETOCLAX
INHIBITOR -> TRANSPORTER
Structure of CAPTOPRIL
INHIBITOR -> TRANSPORTER
Structure of COPANLISIB
SUBSTRATE -> TRANSPORTER
Structure of KETOCONAZOLE
INHIBITOR -> TRANSPORTER
Structure of LML-134
NON-SUBSTRATE -> TRANSPORTER
Structure of MGS-0039
NON-SUBSTRATE -> TRANSPORTER
Structure of NILOTINIB
INHIBITOR -> TRANSPORTER
Structure of BMS-962212
NON-SUBSTRATE -> TRANSPORTER
Structure of TAMATINIB
SUBSTRATE -> TRANSPORTER
Structure of MOTESANIB
INHIBITOR -> TRANSPORTER
Structure of N-DESMETHYL ENTRECTINIB
SUBSTRATE -> TRANSPORTER
Structure of KETOCONAZOLE
SUBSTRATE -> TRANSPORTER
Structure of Tildacerfont
INHIBITOR -> TRANSPORTER
Structure of NINTEDANIB
SUBSTRATE -> TRANSPORTER
Structure of SOTORASIB
SUBSTRATE -> TRANSPORTER
Structure of VOXILAPREVIR
SUBSTRATE -> TRANSPORTER
Structure of FENTANYL
SUBSTRATE -> TRANSPORTER
Structure of TOFACITINIB
SUBSTRATE -> TRANSPORTER
Structure of INDACATEROL
SUBSTRATE -> TRANSPORTER
In vitro investigations indicated that indacaterol is a low affinity substrate for the efflux pump P-gp.
Structure of RIVAROXABAN
SUBSTRATE -> TRANSPORTER
Structure of LURASIDONE
NON-SUBSTRATE -> TRANSPORTER
Structure of ICOTINIB
INHIBITOR -> TRANSPORTER
Structure of TEPOTINIB
INHIBITOR -> TRANSPORTER
Structure of FIDAXOMICIN
INHIBITOR -> TRANSPORTER
IC50
Structure of RISDIPLAM
SUBSTRATE -> TRANSPORTER
IN VITRO
WEAK
Structure of BRIGATINIB
SUBSTRATE -> TRANSPORTER
Structure of NIROGACESTAT
SUBSTRATE -> TRANSPORTER
Structure of MURIZATOCLAX
INHIBITOR -> TRANSPORTER
Structure of BOCEPREVIR
SUBSTRATE -> TRANSPORTER
Structure of PASIREOTIDE
INHIBITOR -> TRANSPORTER
Structure of Erythromycin
INHIBITOR -> TRANSPORTER
Structure of CASPOFUNGIN
NON-SUBSTRATE -> TRANSPORTER
Structure of ELIGLUSTAT
SUBSTRATE -> TRANSPORTER
Structure of TICAGRELOR
SUBSTRATE -> TRANSPORTER
Structure of NIRAPARIB
SUBSTRATE -> TRANSPORTER
Niraparib is a substrate of P-gp and BCRP in vitro.
Structure of GS-563117
SUBSTRATE -> TRANSPORTER
IN VITRO
Structure of TEMSAVIR
SUBSTRATE -> TRANSPORTER
Drugs that induce or inhibit CYP3A, P-gp, and BCRP may affect temsavir plasma concentrations.
Structure of TOLVAPTAN
SUBSTRATE -> TRANSPORTER
Structure of TENOFOVIR ALAFENAMIDE
SUBSTRATE -> TRANSPORTER
Structure of INDINAVIR
SUBSTRATE -> TRANSPORTER
Structure of TAMOXIFEN
INHIBITOR -> TRANSPORTER
Structure of ARTESUNATE
SUBSTRATE -> TRANSPORTER
Structure of Erythromycin
SUBSTRATE -> TRANSPORTER
Structure of VEMURAFENIB
SUBSTRATE -> TRANSPORTER
Structure of SITAGLIPTIN
SUBSTRATE -> TRANSPORTER
Structure of REMDESIVIR
SUBSTRATE -> TRANSPORTER
Structure of QUINIDINE
INHIBITOR -> TRANSPORTER
Structure of LORCASERIN
NON-INHIBITOR -> TRANSPORTER
Structure of DACLATASVIR
SUBSTRATE -> TRANSPORTER
Structure of ICARIIN
INHIBITOR -> TRANSPORTER
Structure of ALECTINIB
INHIBITOR -> TRANSPORTER
Structure of NALDEMEDINE
SUBSTRATE -> TRANSPORTER
Structure of ELACRIDAR
INHIBITOR -> TRANSPORTER
Structure of TENULIN
INHIBITOR -> TARGET
Structure of ZANUBRUTINIB
SUBSTRATE -> TRANSPORTER
Structure of ELISMETREP
NON-SUBSTRATE -> TRANSPORTER
Structure of ODANACATIB
SUBSTRATE -> TRANSPORTER
Structure of PF-06273340
SUBSTRATE -> TRANSPORTER
Substance designed to be a strong substrate to limit brain availability
EFFLUX RATIO
Structure of ENCORAFENIB
SUBSTRATE -> TRANSPORTER
Structure of BEROTRALSTAT
SUBSTRATE -> TRANSPORTER
Structure of LINAGLIPTIN
SUBSTRATE -> TRANSPORTER
Structure of ETOPOSIDE
SUBSTRATE -> TRANSPORTER
Structure of AMIODARONE
INHIBITOR -> TRANSPORTER
Structure of LOMITAPIDE
NON-SUBSTRATE -> TRANSPORTER
Structure of GEFITINIB
INHIBITOR -> TRANSPORTER
Structure of TARIQUIDAR
INHIBITOR -> TARGET
Structure of TEPOTINIB
SUBSTRATE -> TRANSPORTER
Structure of QUERCETIN
INHIBITOR -> TRANSPORTER
Structure of ZOSUQUIDAR
INHIBITOR -> TARGET
Structure of RELUGOLIX
SUBSTRATE -> TRANSPORTER
Relugolix is a substrate for intestinal P-gp.Co-administration with rifampin (P-gp and strong CYP3A inducer) decreased the AUC and Cmax of relugolix by 55% and 23%, respectively.
Structure of BICTEGRAVIR
SUBSTRATE -> TRANSPORTER
Structure of DAPAGLIFLOZIN
SUBSTRATE -> TRANSPORTER
Structure of ABROCITINIB
SUBSTRATE -> TRANSPORTER
Structure of LONAFARNIB
INHIBITOR -> TRANSPORTER
Structure of OMBITASVIR
SUBSTRATE -> TRANSPORTER
Structure of SELEXIPAG
SUBSTRATE -> TRANSPORTER
Structure of IVOSIDENIB
SUBSTRATE -> TRANSPORTER
Structure of DEFLAZACORT
SUBSTRATE -> TRANSPORTER
Structure of ATORVASTATIN
SUBSTRATE -> TRANSPORTER
Structure of CLARITHROMYCIN
INHIBITOR -> TRANSPORTER
Structure of RANOLAZINE
INHIBITOR -> TRANSPORTER
Structure of RIPRETINIB
SUBSTRATE -> TRANSPORTER
Structure of IDELALISIB
SUBSTRATE -> TRANSPORTER
Structure of LORLATINIB
INHIBITOR -> TRANSPORTER
Structure of DAUNORUBICIN
SUBSTRATE -> TRANSPORTER
Structure of OCTREOTIDE
SUBSTRATE -> TARGET
Structure of DOMPERIDONE
SUBSTRATE -> TRANSPORTER
Structure of Belumosudil
INHIBITOR -> TRANSPORTER
Inhibits at clinically relevant concentrations.
Structure of ROLAPITANT
NON-SUBSTRATE -> TRANSPORTER
Structure of CABOTEGRAVIR
SUBSTRATE -> TRANSPORTER
Cabotegravir is a substrate of P-gp and BCRP in vitro; however, because of its high permeability, no alteration in cabotegravir absorption is expected with coadministration of P-gp or BCRP inhibitors.
Structure of RIFAMYCIN
SUBSTRATE -> TRANSPORTER
Structure of BAFETINIB
INHIBITOR -> TRANSPORTER
Structure of RIFAMPIN
INDUCER -> TRANSPORTER
Structure of PIBRENTASVIR
INHIBITOR -> TRANSPORTER
Structure of BRYOSTATIN 1
INHIBITOR -> TRANSPORTER
Structure of GALBANIC ACID
INHIBITOR -> TRANSPORTER
Structure of FIDAXOMICIN
SUBSTRATE -> TRANSPORTER
Structure of BRANEBRUTINIB
INHIBITOR -> TRANSPORTER
Structure of TRABECTEDIN
SUBSTRATE -> TRANSPORTER
Structure of Colchicine
SUBSTRATE -> TRANSPORTER
Structure of SAQUINAVIR
SUBSTRATE -> TRANSPORTER
Structure of MIVEBRESIB
SUBSTRATE -> TRANSPORTER
Structure of ZANUBRUTINIB
INHIBITOR -> TRANSPORTER
Structure of EPIRUBICIN
SUBSTRATE -> TRANSPORTER
Structure of Selpercatinib
INHIBITOR -> TRANSPORTER
Structure of ERDAFITINIB
INHIBITOR -> TRANSPORTER
Structure of Fluometacyl
SUBSTRATE -> TRANSPORTER
WEAK
Structure of PRUCALOPRIDE
SUBSTRATE -> TRANSPORTER
Structure of ATAZANAVIR
INHIBITOR -> TRANSPORTER
WEAK
IC50
Structure of CITALOPRAM
SUBSTRATE -> TRANSPORTER
in vitro ER in the MDCK-MDR1 cell line from National Institutes of Health. Weak substrate in-vivo.
EFFLUX RATIO
Structure of DOCETAXEL
SUBSTRATE -> TRANSPORTER
Structure of EVEROLIMUS
SUBSTRATE -> TRANSPORTER
Structure of ELAGOLIX
SUBSTRATE -> TRANSPORTER
Structure of LAPATINIB
INHIBITOR -> TRANSPORTER
Structure of DUVELISIB
INHIBITOR -> TRANSPORTER
Structure of ALPELISIB
INHIBITOR -> TRANSPORTER
The in vitro study result indicated that alpelisib is a weak P-gp inhibitor with a Ki of 98.6 μM (R0900459).
Ki
Structure of TACROLIMUS
SUBSTRATE -> TRANSPORTER
Structure of AGI-16903
SUBSTRATE -> TRANSPORTER
Structure of DESMETHYLLOPERAMIDE C-11
SUBSTRATE -> TARGET
Measures P-gp function
Structure of DACOMITINIB ANHYDROUS
INHIBITOR -> TRANSPORTER
Structure of SAXAGLIPTIN ANHYDROUS
SUBSTRATE -> TRANSPORTER
Structure of CARVEDILOL
INHIBITOR -> TRANSPORTER
Structure of GLASDEGIB
INHIBITOR -> TRANSPORTER
Structure of MK-8189
NON-SUBSTRATE -> TRANSPORTER
Transporter studies indicate high potential for CNS penetration.
Structure of Selpercatinib
SUBSTRATE -> TRANSPORTER
Structure of DABIGATRAN ETEXILATE
SUBSTRATE -> TRANSPORTER
Structure of TERFENADINE
INHIBITOR -> TRANSPORTER
Structure of BENZNIDAZOLE
SUBSTRATE -> TRANSPORTER
Structure of MURIZATOCLAX
SUBSTRATE -> TRANSPORTER
Structure of NALOXEGOL
SUBSTRATE -> TRANSPORTER
Structure of LUSUTROMBOPAG
SUBSTRATE -> TARGET
Structure of PALBOCICLIB
SUBSTRATE -> TRANSPORTER
Structure of RANITIDINE
SUBSTRATE -> TRANSPORTER
Structure of LOPERAMIDE
SUBSTRATE -> TRANSPORTER
in vitro ER in the MDCK-MDR1 cell line from National Institutes of Health
EFFLUX RATIO
Structure of SITRAVATINIB
INHIBITOR -> TRANSPORTER
Inhibits the ABCB1 efflux pump by inhibiting the hydrolysis of ATP
Structure of CISPLATIN
SUBSTRATE -> TRANSPORTER
Structure of DILTIAZEM
SUBSTRATE -> TRANSPORTER
Structure of TALAZOPARIB
SUBSTRATE -> TRANSPORTER
Co-administration of talazoparib with certain P-gp inhibitors including amiodarone, carvedilol, clarithromycin, itraconazole, and verapamil in the clinical studies (PRP-001, PRP-002, ABRAZO and EMBRACA) increased talazoparib exposure by 44.7%, in conjunction with an increased rate of Talzenna dose reductions (41%).
Gramicidin
SUBSTRATE -> TRANSPORTER
Structure of EPACADOSTAT
SUBSTRATE -> TRANSPORTER
Structure of STIRIPENTOL
INHIBITOR -> TARGET
IC50
Structure of BIRICODAR
INHIBITOR -> TARGET
Structure of MC225 F-18
RADIOLIGAND->TARGET
Acts as a substrate selective over BCRP
Structure of Hydroxyurea
SUBSTRATE -> TRANSPORTER
Structure of PGP-4008
INHIBITOR -> TARGET
Selective inhibitor of P-glycoprotein (P-gp) that does not affect the activity of multidrug resistance-related protein 1
Structure of UPADACITINIB
SUBSTRATE -> TRANSPORTER
Structure of RITONAVIR
SUBSTRATE -> TRANSPORTER
Structure of ELIGLUSTAT
INHIBITOR -> TRANSPORTER
IC50
Structure of OSPEMIFENE
SUBSTRATE -> TRANSPORTER
The sponsor evaluated ospemifene as a potential substrate for transporters in a P-gp in vitro study. No in vivo transporter studies were conducted.
Structure of POZIOTINIB
INHIBITOR -> TRANSPORTER
Structure of BARICITINIB
SUBSTRATE -> TRANSPORTER
Structure of LAPATINIB
SUBSTRATE -> TRANSPORTER
Structure of OTESECONAZOLE
INHIBITOR -> TRANSPORTER
Not clinically relevant in DDI study.
IC50
Structure of ITRACONAZOLE
INHIBITOR -> TRANSPORTER
Structure of ABEMACICLIB
INHIBITOR -> TRANSPORTER
IC50
Structure of DASABUVIR
SUBSTRATE -> TRANSPORTER
Structure of ELBASVIR
SUBSTRATE -> TRANSPORTER
Structure of ETRAVIRINE
INHIBITOR -> TRANSPORTER
WEAK
IC50
Structure of PANOBINOSTAT
SUBSTRATE -> TRANSPORTER
Structure of SIMEPREVIR
INHIBITOR -> TRANSPORTER
Simeprevir inhibited P-gp-dependent transport of paclitaxel in Caco-2 cells with an IC50 value of 64.4 ug/mL (Study NC113).
IC50
Structure of RUCAPARIB
SUBSTRATE -> TRANSPORTER
Structure of ZIDOVUDINE
SUBSTRATE -> TRANSPORTER
Structure of BALOXAVIR
SUBSTRATE -> TRANSPORTER
Structure of CARFILZOMIB
SUBSTRATE -> TRANSPORTER
Structure of BISBENZIMIDE ETHOXIDE
SUBSTRATE -> TRANSPORTER
Structure of VIBEGRON
SUBSTRATE -> TRANSPORTER
Structure of Olaparib
INHIBITOR -> TRANSPORTER
INHIBITOR
IC50
Structure of PONATINIB
NON-SUBSTRATE -> TRANSPORTER
Structure of N-Desmethylclobazam
SUBSTRATE -> TRANSPORTER
Structure of PACRITINIB
INHIBITOR -> TRANSPORTER
IC50
Structure of LAPATINIB
INHIBITOR -> TRANSPORTER
Structure of OP-1118
SUBSTRATE -> TRANSPORTER
Structure of DOXORUBICIN
SUBSTRATE -> TRANSPORTER
Structure of ESAXERENONE
SUBSTRATE -> TRANSPORTER
Structure of ELACRIDAR
INHIBITOR -> TRANSPORTER
Structure of LORCASERIN
NON-SUBSTRATE -> TRANSPORTER
Structure of FEDRATINIB
INHIBITOR -> TRANSPORTER
IC50
Structure of AZILSARTAN MEDOXOMIL
INHIBITOR -> TRANSPORTER
Structure of DACTINOMYCIN
SUBSTRATE -> TRANSPORTER
Structure of LEFAMULIN
SUBSTRATE -> TRANSPORTER
Structure of ULIXERTINIB
INHIBITOR -> TRANSPORTER
In ABCB1-overexpressing cells, ulixertinib antagonized MDR by attenuating the efflux function of ABCB1. A combination of ulixertinib with anticancer drugs to attenuate MDR mediated by ABCB1 or ABCG2 in cancer cells overexpressing these transporters.
Structure of REMIBRUTINIB
SUBSTRATE -> TRANSPORTER
VITAMIN E POLYETHYLENE GLYCOL SUCCINATE
INHIBITOR -> TRANSPORTER
Structure of TANGERETIN
INHIBITOR -> TRANSPORTER
Structure of DEXVERAPAMIL
INHIBITOR -> TRANSPORTER
Structure of Tamnorzatinib
INHIBITOR -> TRANSPORTER
Structure of PACLITAXEL
INDUCER -> TRANSPORTER
Structure of CORTICOSTERONE
SUBSTRATE -> TRANSPORTER
Structure of TRILACICLIB
SUBSTRATE -> TRANSPORTER
Structure of PASIREOTIDE
SUBSTRATE -> TRANSPORTER
Structure of LURBINECTEDIN
INHIBITOR -> TRANSPORTER
Structure of TELBIVUDINE
NON-SUBSTRATE -> TRANSPORTER
Structure of AVASIMIBE
INDUCER -> TRANSPORTER
Structure of BOSUTINIB
SUBSTRATE -> TRANSPORTER
a high-fat meal increased bosutinib AUC 1.7-fold and Cmax 1.8-fold compared with bosutinib administration under fasting conditions
MAJOR
Structure of GALLOPAMIL
INHIBITOR -> TRANSPORTER
Structure of EMOPAMIL
INHIBITOR -> TRANSPORTER
Structure of Nirmatrelvir
INHIBITOR -> TRANSPORTER
IC50
Structure of VEMURAFENIB
INHIBITOR -> TRANSPORTER
Structure of RIFAMYCIN
INHIBITOR -> TRANSPORTER
IC50
Structure of RANOLAZINE
SUBSTRATE -> TRANSPORTER
Structure of RISPERIDONE
SUBSTRATE -> TRANSPORTER
INHIBITOR
IC50
Structure of VILANTEROL
SUBSTRATE -> TRANSPORTER
However, because of low oral bioavailability, inhibition of P-gp is unlikely to have an impact on the overall bioavailability of vilanterol.
Structure of BT-070
INHIBITOR -> TRANSPORTER
Structure of AVATROMBOPAG
SUBSTRATE -> TRANSPORTER
Structure of ENASIDENIB
NON-SUBSTRATE -> TRANSPORTER
Structure of Fluometacyl
INHIBITOR -> TRANSPORTER
WEAK
Structure of BISANTRENE
SUBSTRATE -> TRANSPORTER
Structure of ATRASENTAN
INHIBITOR -> TRANSPORTER
Moderately inhibited P-gp in P388/dx cells.
IC50
Structure of VALSPODAR
INHIBITOR -> TRANSPORTER
Structure of PONATINIB
INHIBITOR -> TRANSPORTER
Structure of OMADACYCLINE
SUBSTRATE -> TRANSPORTER
Structure of ABIRATERONE ACETATE
INHIBITOR -> TRANSPORTER
Abiraterone acetate inhibits Pgp significantly, with an IC50 of 10.8 μM in vitro.
IC50
Structure of LOMITAPIDE
INHIBITOR -> TRANSPORTER
Structure of ATRASENTAN
SUBSTRATE -> TRANSPORTER
Structure of METHYLPREDNISOLONE
SUBSTRATE -> TRANSPORTER
Structure of ELEXACAFTOR
SUBSTRATE -> TRANSPORTER
Based on in vitro results
Structure of ACT-777991
SUBSTRATE -> TRANSPORTER
Structure of TICAGRELOR
INHIBITOR -> TRANSPORTER
IVERMECTIN
SUBSTRATE -> TRANSPORTER
Structure of PROPANAMIDE, N-(5-(2-(2-METHOXY-3-PYRIDINYL)-7-METHYLIMIDAZO(1,2-A)PYRIDIN-3-YL)-6-(2-(1-METHYL-6-ISOQUINOLINYL)ETHYNYL)-2-PYRIDINYL)-2-(METHYLAMINO)-, (2S)-
INHIBITOR -> TRANSPORTER
Structure of DOLUTEGRAVIR
SUBSTRATE -> TRANSPORTER
Structure of SPARFLOXACIN
SUBSTRATE -> TRANSPORTER
Structure of WILFORINE
INHIBITOR -> TRANSPORTER
Structure of ONT-093
INHIBITOR -> TRANSPORTER
Structure of FEXOFENADINE
SUBSTRATE -> TRANSPORTER
Structure of PF-06282999
SUBSTRATE -> TRANSPORTER
Structure of DELAFLOXACIN
SUBSTRATE -> TRANSPORTER
Structure of NORTRIPTYLINE
SUBSTRATE -> TRANSPORTER
Structure of GNE-0877
NON-SUBSTRATE -> TRANSPORTER
Structure of NOBILETIN
INHIBITOR -> TRANSPORTER
Decreased the IC50 value of paclitaxel by 15.92-fold. Restored the sensitivity of paclitaxel, doxorubicin, docetaxel, and daunorubicin in ABCB1, overexpressing A2780/T and A549/T cells.
IC50
Structure of RITONAVIR
INDUCER -> TRANSPORTER
Structure of LAROTRECTINIB
SUBSTRATE -> TRANSPORTER
In overexpressing BCRP and P-gp cell line, the estimate Km for both transporters is >300 μM. Coadministration of larotrectinib with a single dose of a P-gp inhibitor (rifampin), increased the AUCinf of larotrectinib by 1.7-fold and the Cmax by 1.8-fold as compared to larotrectinib administered alone.
Structure of Ertugliflozin
SUBSTRATE -> TRANSPORTER
Structure of FOSTAMATINIB
INHIBITOR -> METABOLIC ENZYME
Structure of IDELALISIB
INHIBITOR -> TRANSPORTER
Structure of VENETOCLAX
SUBSTRATE -> TRANSPORTER
Structure of AMISULPRIDE
SUBSTRATE -> TRANSPORTER
Structure of MITOXANTRONE
SUBSTRATE -> TRANSPORTER
Structure of DUVELISIB
SUBSTRATE -> TRANSPORTER
Structure of METHADONE
SUBSTRATE -> TRANSPORTER
Structure of ELACRIDAR
INHIBITOR -> TARGET
Structure of TALINOLOL
SUBSTRATE -> TRANSPORTER
Structure of RETAPAMULIN
SUBSTRATE -> TRANSPORTER
Structure of GLECAPREVIR
SUBSTRATE -> TRANSPORTER
Structure of DOFEQUIDAR
INHIBITOR -> TARGET
Structure of UMBRALISIB
INHIBITOR -> TRANSPORTER
Structure of VELPATASVIR
SUBSTRATE -> TRANSPORTER
Structure of PALIPERIDONE
SUBSTRATE -> TRANSPORTER
TRANSPORTER
IC50
Structure of CETIRIZINE
SUBSTRATE -> TRANSPORTER
Structure of Belumosudil
SUBSTRATE -> TRANSPORTER
Structure of TAZEMETOSTAT
SUBSTRATE -> TRANSPORTER
Structure of FLUOROURACIL
SUBSTRATE -> TRANSPORTER
Structure of (3-(((7R)-4-(5-CHLORO-1,3-BENZOXAZOL-2-YL)-7-METHYL-1,4-DIAZEPAN-1-YL)CARBONYL)-4-(2H-1,2,3-TRIAZOL-2-YL)PHENYL)METHANOL
SUBSTRATE -> TRANSPORTER
Structure of ADAGRASIB
INHIBITOR -> TRANSPORTER
Reverses the multidrug resistance mediated by ABCB1 inhibits efflux.
Structure of TETRANDRINE, (+)-
INHIBITOR -> TRANSPORTER
Structure of NELFINAVIR
SUBSTRATE -> TRANSPORTER
Structure of Crizotinib
INHIBITOR -> TRANSPORTER
Structure of RIMEGEPANT
SUBSTRATE -> TRANSPORTER
Structure of SILDENAFIL
INHIBITOR -> TRANSPORTER
Structure of RELUGOLIX
INHIBITOR -> TRANSPORTER
Structure of LOSARTAN
SUBSTRATE -> TRANSPORTER
Structure of NILOTINIB
SUBSTRATE -> TRANSPORTER
Structure of LASMIDITAN
INHIBITOR -> TRANSPORTER
Lasmiditan is an in-vitro inhibitor of P-gp and BCRP.
Structure of GLASDEGIB
SUBSTRATE -> TRANSPORTER
Structure of ELAGOLIX
INHIBITOR -> TRANSPORTER
Structure of VOCLOSPORIN
INHIBITOR -> TRANSPORTER
clinical studies indicate that voclosporin is a weak inhibitor of P-gp
WEAK
Structure of PROPANAMIDE, N-(5-(2-(2-METHOXY-3-PYRIDINYL)-7-METHYLIMIDAZO(1,2-A)PYRIDIN-3-YL)-6-(2-(1-METHYL-6-ISOQUINOLINYL)ETHYNYL)-2-PYRIDINYL)-2-(METHYLAMINO)-, (2S)-
NON-SUBSTRATE -> TRANSPORTER
Structure of BAZEDOXIFENE
SUBSTRATE -> TRANSPORTER
Structure of RHINACANTHIN C
INHIBITOR -> TRANSPORTER
IC50
Structure of MITAPIVAT
INHIBITOR -> TRANSPORTER
P-gp–mediated transport of digoxin across Caco-2 cells
IC50
Structure of AMITRIPTYLINE
SUBSTRATE -> TRANSPORTER
Structure of ISOTENULIN
INHIBITOR -> TRANSPORTER
Inhibited the P-gp efflux function by stimulating P-gp ATPase activity. T
Structure of TUCATINIB
SUBSTRATE -> TRANSPORTER
Structure of RHODAMINE 123
SUBSTRATE -> TRANSPORTER
Structure of RESVERATROL
INHIBITOR -> TRANSPORTER
inhibited MTX efflux transport in MDR1-MDCK and MRP2-MDCK cellmonolayers, suggesting that the target of drug interaction wasMDR1 andMRP2 in the intestine duringthe absorption process.
Structure of TIPRANAVIR
INDUCER -> TRANSPORTER
Structure of LANIQUIDAR
INHIBITOR -> TARGET
Structure of CEP-33779
INHIBITOR -> TRANSPORTER
Seems to be more potent than verapamil.
Structure of CIMETIDINE
SUBSTRATE -> TRANSPORTER
Structure of ERDAFITINIB
SUBSTRATE -> TRANSPORTER
Structure of SOTORASIB
INHIBITOR -> TRANSPORTER
IC50
Structure of ONDANSETRON
SUBSTRATE -> TRANSPORTER
Structure of PRALSETINIB
SUBSTRATE -> TRANSPORTER
Structure of ELBASVIR
INHIBITOR -> TRANSPORTER
IC50
Structure of Binimetinib
SUBSTRATE -> TRANSPORTER
Structure of DEXAMETHASONE
SUBSTRATE -> TRANSPORTER
Structure of LONAFARNIB
SUBSTRATE -> TRANSPORTER
Lonafarnib is likely a marginal substrate of P-gp.
Structure of POSACONAZOLE
SUBSTRATE -> TRANSPORTER
Structure of VARDENAFIL
INHIBITOR -> TRANSPORTER
Structure of AMBRISENTAN
SUBSTRATE -> TRANSPORTER
Structure of CLOBAZAM
SUBSTRATE -> TRANSPORTER
Structure of VERAPAMIL
INHIBITOR -> TRANSPORTER
Structure of LEDIPASVIR
SUBSTRATE -> TRANSPORTER
LDV is a substrate for P-gp and BCRP in vitro (AD-256-2144 and AD-256-2150).
Structure of NERATINIB
INHIBITOR -> TRANSPORTER
Structure of TRIAMCINOLONE
SUBSTRATE -> TRANSPORTER
Structure of TAMOXIFEN
SUBSTRATE -> TARGET
Structure of QUINIDINE
SUBSTRATE -> TRANSPORTER
Structure of ENCORAFENIB
INHIBITOR -> TRANSPORTER
IC50
Structure of CARFILZOMIB
INHIBITOR -> TRANSPORTER
WEAK
Structure of MW-150
NON-SUBSTRATE -> TRANSPORTER
Structure of CANERTINIB
INHIBITOR -> TRANSPORTER
Structure of CAPMATINIB
SUBSTRATE -> TRANSPORTER
Structure of ABAMETAPIR CARBOXYL
INHIBITOR -> TRANSPORTER
Structure of CYCLOSPORINE
SUBSTRATE -> TRANSPORTER
Structure of Eribulin
SUBSTRATE -> TRANSPORTER
WEAK
Structure of NINGETINIB
SUBSTRATE -> TRANSPORTER
Structure of UBROGEPANT
SUBSTRATE -> TRANSPORTER
Structure of IMATINIB
INHIBITOR -> TRANSPORTER
Gao et al. reported that in vitro, imatinib (1 M) increases the intracellular concentration of vincristine and mitoxantrone in cells overexpressing ABCB1 and ABCG2, respectively.
INHIBITOR
CLINICALLY SIGNIFICANT
Structure of 21-DESACETYLDEFLAZACORT
SUBSTRATE -> TRANSPORTER
Structure of SIMEPREVIR
SUBSTRATE -> TRANSPORTER
Structure of VANDETANIB
INHIBITOR -> TRANSPORTER
Structure of ACALABRUTINIB
SUBSTRATE -> TRANSPORTER
Structure of ERVOGASTAT
INHIBITOR -> TRANSPORTER
Structure of TIPRANAVIR
SUBSTRATE -> TRANSPORTER
COADMINSTERED WITH RITONAVIR TO INCREASE BIOAVAILABILITY
Structure of LOPINAVIR
SUBSTRATE -> TRANSPORTER
Structure of LETERMOVIR
SUBSTRATE -> TRANSPORTER
Structure of PRALSETINIB
INHIBITOR -> TRANSPORTER
Structure of 5H-BENZO(B)CARBAZOLE-3-CARBONITRILE, 9-ETHYL-6,11-DIHYDRO-8-(4-((2-HYDROXYETHYL)AMINO)-1-PIPERIDINYL)-6,6-DIMETHYL-11-OXO-
SUBSTRATE -> TRANSPORTER
Structure of CABAZITAXEL
SUBSTRATE -> TRANSPORTER
Structure of OLACAFTOR
SUBSTRATE -> TRANSPORTER
Structure of NERATINIB
SUBSTRATE -> TRANSPORTER
Structure of LOPINAVIR
INHIBITOR -> TRANSPORTER
ST. JOHN'S WORT
INDUCER -> TRANSPORTER
Structure of ENZALUTAMIDE
INHIBITOR -> TRANSPORTER
Structure of LINAGLIPTIN
INHIBITOR -> TRANSPORTER
Structure of LENVATINIB
SUBSTRATE -> TRANSPORTER
Structure of SIROLIMUS
SUBSTRATE -> TRANSPORTER
Structure of LURBINECTEDIN
SUBSTRATE -> TRANSPORTER
Structure of AMPRENAVIR
SUBSTRATE -> TRANSPORTER
Structure of GILTERITINIB
SUBSTRATE -> TRANSPORTER
Structure of CELIPROLOL
SUBSTRATE -> TRANSPORTER
Structure of GLECAPREVIR
INHIBITOR -> TRANSPORTER
Structure of Crizotinib
SUBSTRATE -> TRANSPORTER
Crizotinib is a substrate for P-glycoprotein in vitro.
Structure of FELODIPINE
INHIBITOR -> TRANSPORTER
Structure of PHENYTOIN
INDUCER -> TRANSPORTER
Structure of Tildacerfont
NON-SUBSTRATE -> TRANSPORTER
Structure of RALTEGRAVIR
SUBSTRATE -> TRANSPORTER
HUMAN PLACENTAL TISSUE
TISSUE EXPRESSION->TRANSPORTER
EFFLUX
APICAL
Structure of TEZACAFTOR
SUBSTRATE -> TRANSPORTER
IVERMECTIN
INHIBITOR -> TRANSPORTER
Structure of PACLITAXEL
SUBSTRATE -> TRANSPORTER
Structure of DABRAFENIB
NON-INHIBITOR -> TRANSPORTER
Structure of PHENYTOIN
SUBSTRATE -> TRANSPORTER
Structure of ABEMACICLIB
SUBSTRATE -> TRANSPORTER
Structure of ITRACONAZOLE
SUBSTRATE -> TRANSPORTER
Structure of CURCUMIN
INHIBITOR -> TRANSPORTER
Structure of HERNANDEZINE
INHIBITOR -> TRANSPORTER
Structure of VUTIGLABRIDIN
NON-SUBSTRATE -> TRANSPORTER
Structure of ETRAVIRINE
SUBSTRATE -> TRANSPORTER
Structure of BMS-986224
SUBSTRATE -> TRANSPORTER
Structure of MORPHINE
SUBSTRATE -> TRANSPORTER
Structure of DAROLUTAMIDE
SUBSTRATE -> TRANSPORTER
MAJOR
Structure of VELIPARIB
SUBSTRATE -> TRANSPORTER
Veliparib was a weak P-glycoprotein (P-gp) substrate.
Structure of JERVINE
INHIBITOR -> TRANSPORTER
Showed a concentration-dependent manner, stimulation of ABCB1-ATPase activity, and had a weaker effect than the verapamil.
Structure of VALSPODAR
INHIBITOR -> TARGET
Structure of DRONEDARONE
INHIBITOR -> TRANSPORTER
Structure of ZOLPIDEM
NON-INHIBITOR -> TRANSPORTER
Structure of CONIVAPTAN
INHIBITOR -> TRANSPORTER
Structure of PIBRENTASVIR
SUBSTRATE -> TRANSPORTER
Structure of EPIGALLOCATECHIN GALLATE
INHIBITOR -> TRANSPORTER
Structure of LESINURAD
NON-SUBSTRATE -> TRANSPORTER
Structure of BMS-690514
SUBSTRATE -> TRANSPORTER
Structure of AZELAPRAG
SUBSTRATE -> TRANSPORTER
Structure of PARITAPREVIR
SUBSTRATE -> TRANSPORTER
Structure of Digoxin
SUBSTRATE -> TRANSPORTER
Structure of CANAGLIFLOZIN ANHYDROUS
SUBSTRATE -> TRANSPORTER
Structure of TELAPREVIR
SUBSTRATE -> TRANSPORTER
Structure of TAPRIZOSIN
SUBSTRATE -> TRANSPORTER
WEAK
Structure of UMECLIDINIUM
SUBSTRATE -> TRANSPORTER
However, because of low oral bioavailability, inhibition of P-gp is unlikely to have an impact on the overall bioavailability of UMEC.
Structure of Olaparib
SUBSTRATE -> TRANSPORTER
Structure of LASMIDITAN
SUBSTRATE -> TRANSPORTER
In vitro studies showed that lasmiditan is a substrate of P-gp. However, lasmiditan is a BCS Class I drug and is unlikely to be affected by P-gp inhibitors.
Structure of ROLAPITANT
INHIBITOR -> TRANSPORTER
[I]/IC50 value for p-gp inhibition was estimated to be 0.23. Based on [I]/IC50 > 0.1 a potential in-vivo drug interaction via inhibition of p-gp cannot be ruled out.
INHIBITOR
IC50
Structure of ENCEQUIDAR
INHIBITOR -> TARGET
Structure of RIOCIGUAT
SUBSTRATE -> TRANSPORTER
Structure of FEDRATINIB
SUBSTRATE -> TRANSPORTER
Structure of BIRICODAR
INHIBITOR -> TRANSPORTER
Structure of Maraviroc
SUBSTRATE -> TRANSPORTER
Structure of ELETRIPTAN
SUBSTRATE -> TRANSPORTER
EFFLUX RATIO
Structure of VELPATASVIR
INHIBITOR -> TRANSPORTER
IC50
Structure of ABIRATERONE
INHIBITOR -> TRANSPORTER
WEAK
Structure of DARUNAVIR
SUBSTRATE -> TRANSPORTER
Structure of VERICIGUAT
SUBSTRATE -> TRANSPORTER
Structure of CHLORAMBUCIL
SUBSTRATE -> TRANSPORTER
Structure of SARECYCLINE
INHIBITOR -> TRANSPORTER
IC50
Structure of CARBAMAZEPINE
INDUCER -> TRANSPORTER
Structure of GRAZOPREVIR ANHYDROUS
SUBSTRATE -> TRANSPORTER
Structure of SELUMETINIB
SUBSTRATE -> TRANSPORTER
Structure of FEVIPIPRANT
SUBSTRATE -> TRANSPORTER
Structure of CYCLOSPORINE
INHIBITOR -> TRANSPORTER
Structure of REVEFENACIN
SUBSTRATE -> TRANSPORTER
Structure of IMATINIB
SUBSTRATE -> TRANSPORTER
Structure of ALISKIREN
SUBSTRATE -> TRANSPORTER
Structure of HYDROCORTISONE
SUBSTRATE -> TRANSPORTER
Structure of OPICAPONE
SUBSTRATE -> TRANSPORTER
Structure of ERLOTINIB
INHIBITOR -> TRANSPORTER
Structure of METHOTREXATE
SUBSTRATE -> TRANSPORTER
Structure of RITONAVIR
INHIBITOR -> TRANSPORTER
Structure of VERAPAMIL
SUBSTRATE -> TRANSPORTER
Name Property Type Amount Referenced Substance Defining Parameters References
MOL_WEIGHT:NUMBER(CALCULATED) CHEMICAL
Molecular Formula CHEMICAL
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