General Information of DTP (ID: DTFI42L)

DTP Name Multidrug resistance-associated protein 2 (ABCC2) DTP Info
Gene Name MRP2

Molecule-Related Drug & Molecule List

Molecule-Related Drug List
Molecule Type:
DTT
DTP
DME
Drug Status:
Approved Drug(s)
Discontinued Drug(s)
Clinical Trial Drug(s)
Preclinical Drug(s)
Investigative Drug(s)
74 Approved Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [1]
Aciclovir DMYLOVR Genital herpes 1A94 Approved [2]
Adefovir DMM278X N. A. N. A. Approved [3]
Ampicillin DMHWE7P Acute epiglottitis Approved [4]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [5]
Carbamazepine DMZOLBI Epilepsy 8A60-8A68 Approved [6]
Cefadroxil DMMC345 Bacterial infection 1A00-1C4Z Approved [7]
Cefodizime DMORSGU N. A. N. A. Approved [4]
Ceftriaxone DMCEW64 Acute gonococcal cervicitis Approved [4]
Cerivastatin DMXCM7H Hyperlipidaemia 5C80 Approved [8]
Cholic Acid DM7OKQV Cholelithiasis DC11 Approved [9]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [10]
Cidofovir DMA13GD Cytomegalovirus infection 1D82 Approved [4]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [11]
Dehydroepiandrosterone sulfate DM4Q80H N. A. N. A. Approved [12]
Dinoprostone DMTYOPD Medical abortion JA00.1Z Approved [13]
Docetaxel DMDI269 Advanced cancer 2A00-2F9Z Approved [14]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [15]
Enalapril DMNFUZR Congestive heart failure BD10 Approved [16]
Epirubicin DMPDW6T Solid tumour/cancer 2A00-2F9Z Approved [4]
Erythromycin DM4K7GQ Acne vulgaris ED80 Approved [17]
Estrone sulfate DMVBIZL Atrophic vaginitis GA30.2 Approved [18]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [19]
Ezetimibe DM7A8TW Atherosclerosis BD40 Approved [20]
FLUORESCEIN DMQTFAO Ocular disease 1F00.1Z Approved [21]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [22]
Folic Acid DMEMBJC Colorectal carcinoma Approved [23]
Gadobenate Dimeglumine DM4VAOG Schizophrenia 6A20 Approved [24]
Gatifloxacin DMSL679 Acute gonococcal cervicitis Approved [25]
Gemifloxacin DMHT34O Bacterial infection 1A00-1C4Z Approved [26]
Glutathione DMAHMT9 Human immunodeficiency virus infection 1C62 Approved [27]
Grepafloxacin DMGLX0T Chronic bronchitis CA20.1 Approved [28]
Indinavir DM0T3YH Human immunodeficiency virus infection 1C62 Approved [29]
Irinotecan DMP6SC2 Adenocarcinoma 2D40 Approved [30]
Leucovorin DMUAZWG Colon adenocarcinoma Approved [31]
Lopinavir DMITQS0 Human immunodeficiency virus infection 1C62 Approved [32]
Mesalazine DMOL5IU Diverticulitis Approved [33]
Methotrexate DM2TEOL Anterior urethra cancer Approved [34]
Mitoxantrone DMM39BF Acute myelogenous leukaemia 2A41 Approved [4]
Mycophenolate mofetil DMPQAGE Hepatosplenic T-cell lymphoma Approved [35]
Mycophenolic acid DMRBMAU Crohn disease DD70 Approved [36]
Nilotinib DM7HXWT Chronic myelogenous leukaemia 2A20.0 Approved [37]
Octreotide DMHIDCJ Acromegaly 5A60.0 Approved [38]
Olamufloxacin DMQ4PKA N. A. N. A. Approved [39]
Olmesartan medoxomil DMWBHRY High blood pressure BA00 Approved [40]
Oxaliplatin DMQNWRD Adenocarcinoma 2D40 Approved [41]
Paclitaxel DMLB81S Breast carcinoma Approved [42]
Pemetrexed DMMX2E6 Central nervous system lymphoma 2B33.5 Approved [39]
Pemirolast DML97WV Allergic conjunctivitis 9A60.02 Approved [39]
Phenobarbital DMXZOCG Cluster headache 8A81.0 Approved [43]
Phenytoin DMNOKBV Epilepsy 8A60-8A68 Approved [44]
Pitavastatin DMJH792 Hypercholesterolaemia 5C80.0 Approved [45]
PITAVASTATIN CALCIUM DM1UJO0 Dyslipidemia 5C80-5C81 Approved [4]
Pravastatin DM6A0X7 Adult acute monocytic leukemia Approved [46]
Probenecid DMMFWOJ Acute gonococcal cervicitis Approved [47]
Raltitrexed DMT9K8G Rectal adenocarcinoma 2B92 Approved [48]
Regorafenib DMHSY1I Gastrointestinal stromal tumour 2B5B Approved [49]
Rifampin DMA8J1G Tuberculosis 1B10-1B1Z Approved [50]
Ritonavir DMU764S Human immunodeficiency virus infection 1C62 Approved [29]
Rosuvastatin DMMIQ7G Arteriosclerosis BD40 Approved [51]
Saquinavir DMG814N Human immunodeficiency virus infection 1C62 Approved [52]
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [53]
Succimer DME81IY Metal intoxication NE60 Approved [54]
Sulfasalazine DMICA9H Irritable bowel syndrome DD91.0 Approved [55]
Sulfinpyrazone DMEV954 Gout FA25 Approved [56]
Technetium (99MTC) mebrofenin DMUEWM3 N. A. N. A. Approved [4]
Telithromycin DMZ4P3A Bacterial infection 1A00-1C4Z Approved [15]
Temocaprilate DMNX2QI N. A. N. A. Approved [4]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [3]
Valsartan DMREUQ6 Chronic heart failure BD1Z Approved [57]
Vasopressin DMQ2FPC Diabetes insipidus 5A61.5 Approved [58]
Vinblastine DM5TVS3 Advanced cancer 2A00-2F9Z Approved [59]
Vincristine DMINOX3 Acute lymphoblastic leukaemia 2A85 Approved [4]
VRX496 DMIO4V5 Acquired immune deficiency syndrome 1C62.3 Approved [4]
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⏷ Show the Full List of 74 Approved Drug(s)
9 Clinical Trial Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Camptothecin DM6CHNJ Solid tumour/cancer 2A00-2F9Z Phase 3 [3]
GLYCYRRHIZIN DM8M2N3 Influenza virus infection 1E30-1E32 Phase 3 [39]
BQ-123 DM0MO8I Pulmonary arterial hypertension BB01.0 Phase 2 [39]
CKD602 DMW9F1G Solid tumour/cancer 2A00-2F9Z Phase 2 [39]
Glutathione-S-S-glutathione DMJ85FS N. A. N. A. Phase 2 [60]
LE-SN38 DMW50NF Colorectal cancer 2B91.Z Phase 2 [61]
PEITC DMOMN31 Prostate cancer 2C82.0 Phase 2 [62]
EPICATECHIN DMN0EMP Duchenne dystrophy 8C70 Phase 1/2 [63]
Sodium taurocholate DM3GO0J Type-2 diabetes 5A11 Phase 1/2 [64]
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⏷ Show the Full List of 9 Clinical Trial Drug(s)
2 Discontinued Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Phenolphthalein DM5SICT Constipation DD91.1 Withdrawn from market [65]
Rhodamine-123 DMQAK6T Prostate cancer 2C82.0 Discontinued in Phase 1 [66]
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3 Preclinical Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Alpha-Zearalenol DMQMAWK N. A. N. A. Preclinical [67]
Scutellarin DMJT1E5 N. A. N. A. Preclinical [68]
Taxifolin DMQJSF9 N. A. N. A. Preclinical [69]
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11 Investigative Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
AMINOHIPPURIC ACID DMUN54G Discovery agent N.A. Investigative [70]
bilirubin DMI0V4O Discovery agent N.A. Investigative [71]
CCK-8 DMN0J4W N. A. N. A. Investigative [18]
chelerythrine DMCP1G9 Discovery agent N.A. Investigative [39]
Genistein-7-glucoside DMMLNTW N. A. N. A. Investigative [4]
glycocholic acid DM0SXNM Discovery agent N.A. Investigative [72]
N5-methylfolate DML0R9M Discovery agent N.A. Investigative [39]
Phlorizin DMNARGO Discovery agent N.A. Investigative [4]
talinolol DMRTD16 Discovery agent N.A. Investigative [73]
tauroursodeoxycholic acid DMFKRQE Discovery agent N.A. Investigative [74]
[3H]estradiol-17beta-glucuronide DM3KJ45 Discovery agent N.A. Investigative [75]
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⏷ Show the Full List of 11 Investigative Drug(s)
Molecule Interaction Atlas

References

1 Effect of acetaminophen on expression and activity of rat liver multidrug resistance-associated protein 2 and P-glycoprotein. Biochem Pharmacol. 2004 Aug 15;68(4):791-8.
2 Gene expression in the human intestine and correlation with oral valacyclovir pharmacokinetic parameters. J Pharmacol Exp Ther. 2003 Aug;306(2):778-86.
3 Pharmacogenetics of membrane transporters: an update on current approaches. Mol Biotechnol. 2010 Feb;44(2):152-67.
4 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.
5 MRP2 and acquired tolerance to inorganic arsenic in the kidney of killifish (Fundulus heteroclitus). Toxicol Sci. 2007 May;97(1):103-10.
6 A nonsynonymous variation in MRP2/ABCC2 is associated with neurological adverse drug reactions of carbamazepine in patients with epilepsy. Pharmacogenet Genomics. 2010 Apr;20(4):249-56.
7 Oral availability of cefadroxil depends on ABCC3 and ABCC4. Drug Metab Dispos. 2012 Mar;40(3):515-21.
8 Identification of the hepatic efflux transporters of organic anions using double-transfected Madin-Darby canine kidney II cells expressing human organic anion-transporting polypeptide 1B1 (OATP1B1)/multidrug resistance-associated protein 2, OATP1B1/multidrug resistance 1, and OATP1B1/breast cancer resistance protein. J Pharmacol Exp Ther. 2005 Sep;314(3):1059-67.
9 Multiple pathways for fluoroquinolone secretion by human intestinal epithelial (Caco-2) cells. Br J Pharmacol. 2002 Mar;135(5):1263-75.
10 Is cyclosporine A transport inhibited by pravastatin via multidrug resistant protein 2? Eur J Clin Pharmacol. 2010 Feb;66(2):153-8.
11 Lentivirus-mediated RNAi silencing targeting ABCC2 increasing the sensitivity of a human nasopharyngeal carcinoma cell line against cisplatin. J Transl Med. 2008 Oct 4;6:55.
12 Directional trans-epithelial transport of organic anions in porcine LLC-PK1 cells that co-express human OATP1B1 (OATP-C) and MRP2. Biochem Pharmacol. 2005 Feb 1;69(3):415-23.
13 Multidrug resistance associated protein 2 mediates transport of prostaglandin E2. Liver Int. 2006 Apr;26(3):362-8.
14 Transport of diclofenac by breast cancer resistance protein (ABCG2) and stimulation of multidrug resistance protein 2 (ABCC2)-mediated drug transport by diclofenac and benzbromarone. Drug Metab Dispos. 2009 Jan;37(1):129-36.
15 Involvement of the drug transporters p glycoprotein and multidrug resistance-associated protein Mrp2 in telithromycin transport. Antimicrob Agents Chemother. 2006 Jan;50(1):80-7.
16 Vectorial transport of enalapril by Oatp1a1/Mrp2 and OATP1B1 and OATP1B3/MRP2 in rat and human livers. J Pharmacol Exp Ther. 2006 Jul;318(1):395-402.
17 Effect of ABCC2 (MRP2) transport function on erythromycin metabolism. Clin Pharmacol Ther. 2011 May;89(5):693-701.
18 Human hepatobiliary transport of organic anions analyzed by quadruple-transfected cells. Mol Pharmacol. 2005 Oct;68(4):1031-8.
19 Delineating the contribution of secretory transporters in the efflux of etoposide using Madin-Darby canine kidney (MDCK) cells overexpressing P-glycoprotein (Pgp), multidrug resistance-associated protein (MRP1), and canalicular multispecific organic anion transporter (cMOAT). Drug Metab Dispos. 2002 Apr;30(4):457-63.
20 Intestinal expression of P-glycoprotein (ABCB1), multidrug resistance associated protein 2 (ABCC2), and uridine diphosphate-glucuronosyltransferase 1A1 predicts the disposition and modulates the effects of the cholesterol absorption inhibitor ezetimibe in humans. Clin Pharmacol Ther. 2006 Mar;79(3):206-17.
21 Phosphoinositide 3-kinase/protein kinase B signaling pathway is involved in estradiol 17-D-glucuronide-induced cholestasis: complementarity with classical protein kinase C. Hepatology. 2010 Oct;52(4):1465-76.
22 Enhancing chemosensitivity in oral squamous cell carcinoma by lentivirus vector-mediated RNA interference targeting EGFR and MRP2. Oncol Lett. 2016 Sep;12(3):2107-2114.
23 Mammalian multidrug-resistance proteins (MRPs). Essays Biochem. 2011 Sep 7;50(1):179-207.
24 Liver Perfusion Modifies Gd-DTPA and Gd-BOPTA Hepatocyte Concentrations Through Transfer Clearances Across Sinusoidal Membranes. Eur J Drug Metab Pharmacokinet. 2017 Aug;42(4):657-667.
25 Uptake and intracellular release kinetics of liposome formulations in glioma cells. Int J Pharm. 2010 Aug 16;395(1-2):251-9.
26 Differential effect of P-gp and MRP2 on cellular translocation of gemifloxacin. Int J Pharm. 2011 Nov 25;420(1):26-33.
27 Oxidative and electrophilic stress induces multidrug resistance-associated protein transporters via the nuclear factor-E2-related factor-2 transcriptional pathway. Hepatology. 2007 Nov;46(5):1597-610.
28 Fluoroquinolone efflux mediated by ABC transporters. J Pharm Sci. 2008 Sep;97(9):3483-93.
29 Interaction of eight HIV protease inhibitors with the canalicular efflux transporter ABCC2 (MRP2) in sandwich-cultured rat and human hepatocytes. Biopharm Drug Dispos. 2010 Mar;31(2-3):178-88.
30 Intestinal transport of irinotecan in Caco-2 cells and MDCK II cells overexpressing efflux transporters Pgp, cMOAT, and MRP1. Drug Metab Dispos. 2002 Jul;30(7):763-70.
31 Transport of methotrexate, methotrexate polyglutamates, and 17beta-estradiol 17-(beta-D-glucuronide) by ABCG2: effects of acquired mutations at R482 on methotrexate transport. Cancer Res. 2003 Jul 15;63(14):4048-54.
32 Effects of cytochrome P450 3A (CYP3A) and the drug transporters P-glycoprotein (MDR1/ABCB1) and MRP2 (ABCC2) on the pharmacokinetics of lopinavir. Br J Pharmacol. 2010 Jul;160(5):1224-33.
33 Transport studies with 5-aminosalicylate. Eur J Clin Pharmacol. 2006 Oct;62(10):871-5.
34 Dose-dependent disposition of methotrexate in Abcc2 and Abcc3 gene knockout murine models. Drug Metab Dispos. 2011 Nov;39(11):2155-61.
35 Influence of SLCO1B1, 1B3, 2B1 and ABCC2 genetic polymorphisms on mycophenolic acid pharmacokinetics in Japanese renal transplant recipients. Eur J Clin Pharmacol. 2007 Dec;63(12):1161-9.
36 C-440T/T-331C polymorphisms in the UGT1A9 gene affect the pharmacokinetics of mycophenolic acid in kidney transplantation. Pharmacogenomics. 2007 Sep;8(9):1127-41.
37 Interaction of nilotinib, dasatinib and bosutinib with ABCB1 and ABCG2: implications for altered anti-cancer effects and pharmacological properties. Br J Pharmacol. 2009 Oct;158(4):1153-64.
38 P-glycoprotein- and mrp2-mediated octreotide transport in renal proximal tubule. Br J Pharmacol. 2000 Jan;129(2):251-6.
39 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
40 Multiple human isoforms of drug transporters contribute to the hepatic and renal transport of olmesartan, a selective antagonist of the angiotensin II AT1-receptor. Drug Metab Dispos. 2007 Dec;35(12):2166-76.
41 Multidrug Resistance-Associated Protein 2 (MRP2) Mediated Transport of Oxaliplatin-Derived Platinum in Membrane Vesicles. PLoS One. 2015 Jul 1;10(7):e0130727.
42 Multidrug resistance protein 2 is an important determinant of paclitaxel pharmacokinetics. Clin Cancer Res. 2006 Oct 15;12(20 Pt 1):6125-32.
43 Regulation of multidrug resistance-associated protein 2 (ABCC2) by the nuclear receptors pregnane X receptor, farnesoid X-activated receptor, and constitutive androstane receptor. J Biol Chem. 2002 Jan 25;277(4):2908-15.
44 Upregulation of brain expression of P-glycoprotein in MRP2-deficient TR(-) rats resembles seizure-induced up-regulation of this drug efflux transporter in normal rats. Epilepsia. 2007 Apr;48(4):631-45.
45 Involvement of BCRP (ABCG2) in the biliary excretion of pitavastatin. Mol Pharmacol. 2005 Sep;68(3):800-7.
46 Role of transporters in the tissue-selective distribution and elimination of drugs: transporters in the liver, small intestine, brain and kidney. J Control Release. 2002 Jan 17;78(1-3):43-54.
47 MRP2 (ABCC2) transports taxanes and confers paclitaxel resistance and both processes are stimulated by probenecid. Int J Cancer. 2005 Sep 20;116(5):824-9.
48 Antifolate resistance mediated by the multidrug resistance proteins MRP1 and MRP2. Cancer Res. 1999 Jun 1;59(11):2532-5.
49 Regorafenib is transported by the organic anion transporter 1B1 and the multidrug resistance protein 2. Biol Pharm Bull. 2015;38(4):582-6.
50 Expression and distribution of CYP3A genes, CYP2B22, and MDR1, MRP1, MRP2, LRP efflux transporters in brain of control and rifampicin-treated pigs. Mol Cell Biochem. 2010 Apr;337(1-2):133-43.
51 Involvement of multiple transporters in the hepatobiliary transport of rosuvastatin. Drug Metab Dispos. 2008 Oct;36(10):2014-23.
52 Evidence for two interacting ligand binding sites in human multidrug resistance protein 2 (ATP binding cassette C2). J Biol Chem. 2003 Jun 27;278(26):23538-44.
53 Multidrug resistance protein 2 implicates anticancer drug-resistance to sorafenib. Biol Pharm Bull. 2011;34(3):433-5.
54 MRP2 involvement in renal proximal tubular elimination of methylmercury mediated by DMPS or DMSA. Toxicol Appl Pharmacol. 2009 Feb 15;235(1):10-7.
55 Small intestinal efflux mediated by MRP2 and BCRP shifts sulfasalazine intestinal permeability from high to low, enabling its colonic targeting. Am J Physiol Gastrointest Liver Physiol. 2009 Aug;297(2):G371-7.
56 Vinblastine and sulfinpyrazone export by the multidrug resistance protein MRP2 is associated with glutathione export. Br J Cancer. 2000 Aug;83(3):375-83.
57 Involvement of transporters in the hepatic uptake and biliary excretion of valsartan, a selective antagonist of the angiotensin II AT1-receptor, in humans. Drug Metab Dispos. 2006 Jul;34(7):1247-54.
58 Transport function and hepatocellular localization of mrp6 in rat liver. Mol Pharmacol. 2000 Mar;57(3):634-41.
59 Severe hypokalemia due to a possible drug-drug interaction between vinblastine and antiretrovirals in a HIV-infected patient with Hodgkin's lymphoma. Int J STD AIDS. 2017 Oct;28(12):1259-1262.
60 Purification of the human apical conjugate export pump MRP2 reconstitution and functional characterization as substrate-stimulated ATPase. Eur J Biochem. 1999 Oct 1;265(1):281-9.
61 Biliary excretion mechanism of CPT-11 and its metabolites in humans: involvement of primary active transporters. Cancer Res. 1998 Nov 15;58(22):5137-43.
62 Transport of dietary phenethyl isothiocyanate is mediated by multidrug resistance protein 2 but not P-glycoprotein. Biochem Pharmacol. 2005 Aug 15;70(4):640-7.
63 Transport and metabolism of the tea flavonoid (-)-epicatechin by the human intestinal cell line Caco-2. Pharm Res. 2001 Oct;18(10):1420-5.
64 Functional analysis of ABCA8, a new drug transporter. Biochem Biophys Res Commun. 2002 Oct 18;298(1):41-5.
65 Biliary excretion of phenolphthalein sulfate in rats. Pharmacology. 2003 Aug;68(4):177-82.
66 Characterization of rhodamine-123, calcein and 5(6)-carboxy-2',7'-dichlorofluorescein (CDCF) export via MRP2 (ABCC2) in MES-SA and A549 cells. Eur J Pharm Sci. 2011 Aug 17;43(5):359-69.
67 ABCC1, ABCC2 and ABCC3 are implicated in the transepithelial transport of the myco-estrogen zearalenone and its major metabolites. Toxicol Lett. 2009 Oct 28;190(2):215-23.
68 Mechanistic studies on the absorption and disposition of scutellarin in humans: selective OATP2B1-mediated hepatic uptake is a likely key determinant for its unique pharmacokinetic characteristics. Drug Metab Dispos. 2012 Oct;40(10):2009-20.
69 Permeation of astilbin and taxifolin in Caco-2 cell and their effects on the P-gp. Int J Pharm. 2009 Aug 13;378(1-2):1-8.
70 ATP-dependent para-aminohippurate transport by apical multidrug resistance protein MRP2. Kidney Int. 2000 Apr;57(4):1636-42.
71 Transport of monoglucuronosyl and bisglucuronosyl bilirubin by recombinant human and rat multidrug resistance protein 2. Hepatology. 1999 Aug;30(2):485-90.
72 Differential modulation of the human liver conjugate transporters MRP2 and MRP3 by bile acids and organic anions. J Biol Chem. 2003 Jun 27;278(26):23529-37.
73 FDA Drug Development and Drug Interactions
74 Human multidrug resistance protein 2 transports the therapeutic bile salt tauroursodeoxycholate. J Pharmacol Exp Ther. 2007 Feb;320(2):893-9.
75 Drug resistance and ATP-dependent conjugate transport mediated by the apical multidrug resistance protein, MRP2, permanently expressed in human and canine cells. Mol Pharmacol. 1999 May;55(5):929-37.