ATP-Dependent Translocase ABCB1, EC:, EC, Phospholipid Transporter ABCB1, P-Glycoprotein 1, PGY1, Doxorubicin Resistance, P Glycoprotein, CD243 Antigen, EC, ABC20, CD243, GP170, P-GP, CLCS, ATP Binding Cassette Transporter, Subfamily B, Member 1, Multidrug resistance protein 1, EC 3.6.3, EC, EC:, MDR1, ABCB1, ATP-binding cassette sub-family B member 1, ATP Binding Cassette Subfamily B Member 1, ATP-Binding Cassette, Sub-Family B (MDR/TAP), Member 1, Colchicin Sensitivity


P-glycoprotein 1 (permeability glycoprotein, abbreviated as P-gp or Pgp) also known as multidrug resistance protein 1 (MDR1) or ATP-binding cassette sub-family B member 1 (ABCB1) or cluster of differentiation 243 (CD243) is an important protein of the cell membrane that pumps many foreign substances out of cells. Translocates drugs and phospholipids across the membrane . Catalyzes the flop of phospholipids from the cytoplasmic to the exoplasmic leaflet of the apical membrane. Participates mainly to the flop of phosphatidylcholine, phosphatidylethanolamine, beta-D-glucosylceramides and sphingomyelins . Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.

KO Status

F2 (-/-)

Drug Information

Launched drugs: 6
Drugs in clinical trials: 12
Latest Research Phase: Approved

Drug Name





Clinical Trials

Dapagliflozin Propanediol Monohydrate

HGP-1812, BMS-512148, BMS-512148-05, HGP-1602, ATB-1012


Bristol-Myers Squibb Company

Diabetes Mellitus, Type 1, Diabetes Mellitus, Type 2, Heart Failure, Hyperuricemia, Myocardial Infarction, Kidney Diseases, Hyperglycemia, Hypertension, Cardiovascular Diseases, Renal Insufficiency, Chronic, Diabetes Mellitus

Paclitaxel/Encequidar mesylate


Hanmi Pharmaceutical Co Ltd

Solid tumours, Hemangiosarcoma, Breast Neoplasms, Adenocarcinoma



VX-661/VX-770, VX-770/VX-661


Vertex Pharmaceuticals Incorporated

Cystic Fibrosis



Vertex Pharmaceuticals Incorporated

Cystic Fibrosis




Vertex Pharmaceuticals Incorporated

Ciliary Motility Disorders, Cystic Fibrosis, Hepatic Insufficiency




Vertex Pharmaceuticals Incorporated

Cystic Fibrosis



Cadila Pharmaceuticals

Tuberculosis, Pulmonary


d-DM, AVP-786, CTP-786, d6-DM/Q

Phase 3 Clinical

Concert Pharmaceuticals

Solid tumours, Carcinoma, Renal Cell, Schizophrenia, Mitochondrial Diseases, Alzheimer Disease, Disruptive, Impulse Control, and Conduct Disorders, Melanoma


HE-10, HU-004

Phase 3 Clinical


Dry Eye Syndromes, Xerophthalmia





Initial characterization of the human central proteome

Burkard T.R., Planyavsky M., Kaupe I., Breitwieser F.P., Buerckstuemmer T., Bennett K.L., Superti-Furga G., Colinge J.,

BMC Syst. Biol. 5:17-17(2011)

Protein phosphatase complex PP5/PPP2R3C dephosphorylates P-glycoprotein/ABCB1 and down-regulates the expression and function

Katayama K., Yamaguchi M., Noguchi K., Sugimoto Y.,

Cancer Lett. 345:124-131(2014)

An altered pattern of cross-resistance in multidrug-resistant human cells results from spontaneous mutations in the mdr1 (P-glycoprotein) gene

Choi K.H., Chen C.-J., Kriegler M., Roninson I.B.,

Cell 53:519-529(1988)

Genetic polymorphism in MDR-1: a tool for examining allelic expression in normal cells, unselected and drug-selected cell lines, and human tumors

Mickley L.A., Lee J.-S., Weng Z., Zhan Z., Alvarez M., Wilson W., Bates S.E., Fojo T.,

Blood 91:1749-1756(1998)

A new polymorphism (N21D) in the exon 2 of the human MDR1 gene encoding the P-glycoprotein

Decleves X., Chevillard S., Charpentier C., Vielh P., Laplanche J.-L.,

Hum. Mutat. 15:486-486(2000)

Functional polymorphisms of the human multidrug-resistance gene: multiple sequence variations and correlation of one allele with P-glycoprotein expression and activity in vivo

Hoffmeyer S., Burk O., von Richter O., Arnold H.P., Brockmoeller J., Johne A., Cascorbi I., Gerloff T., Roots I., Eichelbaum M., Brinkmann U.,

Proc. Natl. Acad. Sci. U.S.A. 97:3473-3478(2000)

Frequency of single nucleotide polymorphisms in the P-glycoprotein drug transporter MDR1 gene in white subjects

Cascorbi I., Gerloff T., Johne A., Meisel C., Hoffmeyer S., Schwab M., Schaeffeler E., Eichelbaum M., Brinkmann U., Roots I.,

Clin. Pharmacol. Ther. 69:169-174(2001)

Polymorphism of MDR1 gene in healthy Japanese subjects: a novel SNP with an amino acid substitution (Glu108Lys)

Honda T., Dan Y., Koyabu N., Ieiri I., Otsubo K., Higuchi S., Ohtani H., Sawada J.,

Drug Metab. Pharmacokinet. 17:479-481(2002)

Twelve novel single nucleotide polymorphisms in ABCB1/MDR1 among Japanese patients with ventricular tachycardia who were administered amiodarone

Itoda M., Saito Y., Komamura K., Ueno K., Kamakura S., Ozawa S., Sawada J.,

Drug Metab. Pharmacokinet. 17:566-571(2002)

Three hundred twenty-six genetic variations in genes encoding nine members of ATP-binding cassette, subfamily B (ABCB/MDR/TAP), in the Japanese population

Saito S., Iida A., Sekine A., Miura Y., Ogawa C., Kawauchi S., Higuchi S., Nakamura Y.,

J. Hum. Genet. 47:38-50(2002)