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

Approval Year

Substance Class Protein
Created
by admin
on Fri Jun 25 21:45:15 UTC 2021
Edited
by admin
on Fri Jun 25 21:45:15 UTC 2021
Protein Type TRANSPORTER
Protein Sub Type Other|ABC
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
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 Fri Jun 25 21:45:16 UTC 2021 , Edited by admin on Fri Jun 25 21:45:16 UTC 2021
EC (ENZYME CLASS) EC 3.6.3.44
Created by admin on Fri Jun 25 21:45:16 UTC 2021 , Edited by admin on Fri Jun 25 21:45:16 UTC 2021
Code System Code Type Description
CAS
1646537-23-6
Created by admin on Fri Jun 25 21:45:16 UTC 2021 , Edited by admin on Fri Jun 25 21:45:16 UTC 2021
PRIMARY
UNIPROT
P08183
Created by admin on Fri Jun 25 21:45:16 UTC 2021 , Edited by admin on Fri Jun 25 21:45:16 UTC 2021
PRIMARY
FDA UNII
22ES734693
Created by admin on Fri Jun 25 21:45:16 UTC 2021 , Edited by admin on Fri Jun 25 21:45:16 UTC 2021
PRIMARY
Glycosylation Type HUMAN
Glycosylation Link Type Site
N 1_91
N 1_94
N 1_99
Related Record Type Details
INHIBITOR -> TRANSPORTER
Regorafenib inhibits Pgp and BCRP in vitro.
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
NON-SUBSTRATE -> TRANSPORTER
NON-SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
In vitro investigations indicated that indacaterol is a low affinity substrate for the efflux pump P-gp.
SUBSTRATE -> TRANSPORTER
COADMINSTERED WITH RITONAVIR TO INCREASE BIOAVAILABILITY
SUBSTRATE -> TRANSPORTER
NON-SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
IC50
SUBSTRATE -> TRANSPORTER
IN VITRO
WEAK
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
Niraparib is a substrate of P-gp and BCRP in vitro.
SUBSTRATE -> TRANSPORTER
IN VITRO
SUBSTRATE -> TRANSPORTER
Drugs that induce or inhibit CYP3A, P-gp, and BCRP may affect temsavir plasma concentrations.
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
NON-INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
NON-SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
NON-SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
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.
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TARGET
SUBSTRATE -> TRANSPORTER
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.
SUBSTRATE -> TRANSPORTER
INDUCER -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
WEAK
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
WEAK
IC50
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
The in vitro study result indicated that alpelisib is a weak P-gp inhibitor with a Ki of 98.6 ?M (R0900459).
Ki
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TARGET
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
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%).
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TARGET
IC50
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
IC50
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.
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
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
IC50
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
WEAK
IC50
SUBSTRATE -> TRANSPORTER
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
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
NON-SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
IC50
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
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.
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR
IC50
INHIBITOR -> TRANSPORTER
INDUCER -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
NON-SUBSTRATE -> TRANSPORTER
INDUCER -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
IC50
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR
IC50
SUBSTRATE -> TRANSPORTER
However, because of low oral bioavailability, inhibition of P-gp is unlikely to have an impact on the overall bioavailability of vilanterol.
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
NON-SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
WEAK
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
Abiraterone acetate inhibits Pgp significantly, with an IC50 of 10.8 ?M in vitro.
IC50
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
Based on in vitro results
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
NON-SUBSTRATE -> TRANSPORTER
INDUCER -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
In overexpressing BCRP and P-gp cell line, the estimate Km for both transporters is >300 ?M. 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.
SUBSTRATE -> TRANSPORTER
INHIBITOR -> METABOLIC ENZYME
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
TRANSPORTER
IC50
NON-SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
Lasmiditan is an in-vitro inhibitor of P-gp and BCRP.
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
clinical studies indicate that voclosporin is a weak inhibitor of P-gp
WEAK
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
IC50
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
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.
INDUCER -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
IC50
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
Lonafarnib is likely a marginal substrate of P-gp.
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
LDV is a substrate for P-gp and BCRP in vitro (AD-256-2144 and AD-256-2150).
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TARGET
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
IC50
INHIBITOR -> TRANSPORTER
WEAK
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
WEAK
SUBSTRATE -> TRANSPORTER
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
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INDUCER -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INDUCER -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
NON-SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
Crizotinib is a substrate for P-glycoprotein in vitro.
TISSUE EXPRESSION->TRANSPORTER
EFFLUX
APICAL
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
NON-INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
MAJOR
SUBSTRATE -> TRANSPORTER
Veliparib was a weak P-glycoprotein (P-gp) substrate.
INHIBITOR -> TRANSPORTER
NON-INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
NON-SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
WEAK
SUBSTRATE -> TRANSPORTER
However, because of low oral bioavailability, inhibition of P-gp is unlikely to have an impact on the overall bioavailability of UMEC.
NON-SUBSTRATE -> TRANSPORTER
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.
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
INHIBITOR -> TARGET
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
IC50
INHIBITOR -> TRANSPORTER
WEAK
SUBSTRATE -> TRANSPORTER
PARENT->INNOVATOR
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
IC50
INDUCER -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
Name Property Type Amount Referenced Substance Defining Parameters References
Molecular Formula CHEMICAL
MOL_WEIGHT:NUMBER(CALCULATED) CHEMICAL