Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DM1IS6U)

Drug Name

Tenofovir Drug Info

Synonyms

Apropovir; PMPA; TFV; Tenefovir; GS 1275; GS 1278; GS1278; GNA & Tenofovir; HHA & Tenofovir; KS-5021; Viread (TN); Viread, Tenofovir; D,L-Tenofovir; PMPA-(R); Phosphonic acid, [[2-(6-amino-9H-purin-9; [(2R)-1-(6-aminopurin-9-yl)propan-2-yl]oxymethylphosphonic acid; Phosphonic acid, [[(1R)-2-(6-amino-9H-purin-9-yl)-1-methylethoxy]methyl]-(9CI); Phosphonic acid, [[(1R)-2-(6-amino-9H-purin-9-yl)-1-methylethoxy]methyl]-& Galanthus nivalis agglutinin (GNA); Phosphonic acid, [[(1R)-2-(6-amino-9H-purin-9-yl)-1-methylethoxy]methyl]-& Hippeastrum hybrid agglutinin(HHA); (R)-9-(2-Phosphonomethoxypropyl)adenine; (R)-9-(2-Phosphonylmethoxypropyl)adenine; (R)-PMPA

Indication

Disease Entry	ICD 11	Status	REF
Chronic hepatitis B virus infection		Approved	[1]
Hepatitis B virus infection	1E51.0	Approved	[1]
Human immunodeficiency virus infection	1C62	Approved	[2]

Therapeutic Class

Anti-HIV Agents

Cross-matching ID

PubChem CID: 464205
ChEBI ID: CHEBI:63625
CAS Number: CAS 147127-20-6
TTD Drug ID: DM1IS6U
VARIDT Drug ID: DR00174

Molecule-Related Drug Atlas

Molecule Type:

DTT

DTP

Drug Status:

Approved Drug(s)

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Drug(s) Targeting Human immunodeficiency virus Reverse transcriptase (HIV RT)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Zidovudine	DM4KI7O	Human immunodeficiency virus infection	1C62	Approved	[3]
Nevirapine	DM6HX9B	Human immunodeficiency virus infection	1C62	Approved	[11]
Zalcitabine	DMH7MUV	Human immunodeficiency virus infection	1C62	Approved	[12]
Lamivudine	DMI347A	Chronic HBV infection	1E51.0Z	Approved	[13]
Abacavir	DMMN36E	Human immunodeficiency virus infection	1C62	Approved	[14]
Delavirdine	DM3NF5G	Human immunodeficiency virus infection	1C62	Approved	[13]
Efavirenz	DMC0GSJ	Human immunodeficiency virus infection	1C62	Approved	[13]
Rilpivirine	DMJ0QOW	Human immunodeficiency virus infection	1C62	Approved	[15]
Etravirine	DMGV8QU	Human immunodeficiency virus-1 infection	1C62	Approved	[16]
MK-1439	DM215WE	Human immunodeficiency virus infection	1C62	Approved	[17]
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Drug(s) Transported By P-glycoprotein 1 (ABCB1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Amoxicillin	DMUYNEI	Acute otitis media	AB00	Approved	[18]
Doxorubicin	DMVP5YE	Acute myelogenous leukaemia	2A41	Approved	[19]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[20]
Folic Acid	DMEMBJC	Colorectal carcinoma		Approved	[21]
Fluorouracil	DMUM7HZ	Adenocarcinoma	2D40	Approved	[20]
Cisplatin	DMRHGI9	Adenocarcinoma	2D40	Approved	[20]
Progesterone	DMUY35B	Amenorrhea	GA20.0	Approved	[22]
Tamoxifen	DMLB0EZ	Breast cancer	2C60-2C65	Approved	[20]
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[23]
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[24]
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Drug(s) Transported By Breast cancer resistance protein (ABCG2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Doxorubicin	DMVP5YE	Acute myelogenous leukaemia	2A41	Approved	[25]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[26]
Folic Acid	DMEMBJC	Colorectal carcinoma		Approved	[27]
Fluorouracil	DMUM7HZ	Adenocarcinoma	2D40	Approved	[28]
Cisplatin	DMRHGI9	Adenocarcinoma	2D40	Approved	[29]
Progesterone	DMUY35B	Amenorrhea	GA20.0	Approved	[30]
Tamoxifen	DMLB0EZ	Breast cancer	2C60-2C65	Approved	[31]
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[30]
Sulfasalazine	DMICA9H	Irritable bowel syndrome	DD91.0	Approved	[32]
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[33]
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Drug(s) Transported By Multidrug resistance-associated protein 4 (ABCC4)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[34]
Folic Acid	DMEMBJC	Colorectal carcinoma		Approved	[35]
Fluorouracil	DMUM7HZ	Adenocarcinoma	2D40	Approved	[36]
Dinoprostone	DMTYOPD	Medical abortion	JA00.1Z	Approved	[37]
Zidovudine	DM4KI7O	Human immunodeficiency virus infection	1C62	Approved	[18]
Prasterone	DM67VKL	Chronic obstructive pulmonary disease	CA22	Approved	[38]
Irinotecan	DMP6SC2	Adenocarcinoma	2D40	Approved	[39]
Mercaptopurine	DMTM2IK	Acute lymphoblastic leukaemia	2A85	Approved	[40]
Glutathione	DMAHMT9	Human immunodeficiency virus infection	1C62	Approved	[41]
Ganciclovir	DM1MBYQ	Cytomegalovirus infection	1D82	Approved	[18]
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Drug(s) Transported By Organic anion transporter 1 (SLC22A6)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Amoxicillin	DMUYNEI	Acute otitis media	AB00	Approved	[42]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[43]
Dinoprostone	DMTYOPD	Medical abortion	JA00.1Z	Approved	[44]
Zidovudine	DM4KI7O	Human immunodeficiency virus infection	1C62	Approved	[45]
Aciclovir	DMYLOVR	Genital herpes	1A94	Approved	[45]
Ganciclovir	DM1MBYQ	Cytomegalovirus infection	1D82	Approved	[45]
Cefazolin	DMPDYFR	Bacteremia	1A73	Approved	[46]
Olmesartan medoxomil	DMWBHRY	High blood pressure	BA00	Approved	[47]
Zalcitabine	DMH7MUV	Human immunodeficiency virus infection	1C62	Approved	[48]
FLUORESCEIN	DMQTFAO	Ocular disease	1F00.1Z	Approved	[49]
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Drug(s) Transported By Organic anion transporter 3 (SLC22A8)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[50]
Dinoprostone	DMTYOPD	Medical abortion	JA00.1Z	Approved	[44]
Zidovudine	DM4KI7O	Human immunodeficiency virus infection	1C62	Approved	[45]
Prasterone	DM67VKL	Chronic obstructive pulmonary disease	CA22	Approved	[51]
Pravastatin	DM6A0X7	Adult acute monocytic leukemia		Approved	[52]
L-Tryptophan	DMIBH7M	Depression	6A70-6A7Z	Approved	[53]
Mercaptopurine	DMTM2IK	Acute lymphoblastic leukaemia	2A85	Approved	[54]
PITAVASTATIN CALCIUM	DM1UJO0	Dyslipidemia	5C80-5C81	Approved	[55]
Rosuvastatin	DMMIQ7G	Arteriosclerosis	BD40	Approved	[56]
Cilostazol	DMZMSCT	Intermittent claudication	BD40.00	Approved	[57]
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Drug(s) Transported By Multidrug resistance-associated protein 7 (ABCC10)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Tamoxifen	DMLB0EZ	Breast cancer	2C60-2C65	Approved	[58]
Docetaxel	DMDI269	Advanced cancer	2A00-2F9Z	Approved	[58]
Paclitaxel	DMLB81S	Breast carcinoma		Approved	[58]
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Drug(s) Transported By Multidrug resistance-associated protein 8 (ABCC11)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[59]
Prasterone	DM67VKL	Chronic obstructive pulmonary disease	CA22	Approved	[60]
Zalcitabine	DMH7MUV	Human immunodeficiency virus infection	1C62	Approved	[61]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Download the Complete Interaction Atlas for Visualization in Cytoscape

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Human immunodeficiency virus Reverse transcriptase (HIV RT)	TT84ETX	POL_HV1B1	Inhibitor	[3]

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Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	MOA	REF
Multidrug resistance-associated protein 7 (ABCC10)	DTPS120	MRP7_HUMAN	Substrate	[4]
Multidrug resistance-associated protein 8 (ABCC11)	DTWN7FC	ABCCB_HUMAN	Substrate	[5]
Multidrug resistance-associated protein 4 (ABCC4)	DTCSGPB	MRP4_HUMAN	Substrate	[6]
Breast cancer resistance protein (ABCG2)	DTI7UX6	ABCG2_HUMAN	Substrate	[7]
Organic anion transporter 1 (SLC22A6)	DTQ23VB	S22A6_HUMAN	Substrate	[8]
Organic anion transporter 3 (SLC22A8)	DTVP67E	S22A8_HUMAN	Substrate	[9]
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Substrate	[10]

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References

1	Tenofovir FDA Label
2	Anti-hepatitis B virus activity in vitro of combinations of tenofovir with nucleoside/nucleotide analogues. Antivir Chem Chemother. 2009;19(4):165-76.
3	Antiviral drugs in current clinical use. J Clin Virol. 2004 Jun;30(2):115-33.
4	Genetic variants of ABCC10, a novel tenofovir transporter, are associated with kidney tubular dysfunction. J Infect Dis. 2011 Jul 1;204(1):145-53.
5	Tenofovir Disoproxil Fumarate Is a New Substrate of ATP-Binding Cassette Subfamily C Member 11. Antimicrob Agents Chemother. 2017 Mar 24;61(4). pii: e01725-16.
6	Functional involvement of multidrug resistance-associated protein 4 (MRP4/ABCC4) in the renal elimination of the antiviral drugs adefovir and tenofovir. Mol Pharmacol. 2007 Feb;71(2):619-27.
7	KEGG: new perspectives on genomes, pathways, diseases and drugs. Nucleic Acids Res. 2017 Jan 4;45(D1):D353-D361. (dg:DG01913)
8	Human renal organic anion transporter 1 (hOAT1) and its role in the nephrotoxicity of antiviral nucleotide analogs. Nucleosides Nucleotides Nucleic Acids. 2001 Apr-Jul;20(4-7):641-8.
9	Tenofovir alafenamide is not a substrate for renal organic anion transporters (OATs) and does not exhibit OAT-dependent cytotoxicity. Antivir Ther. 2014;19(7):687-92.
10	KEGG: new perspectives on genomes, pathways, diseases and drugs. Nucleic Acids Res. 2017 Jan 4;45(D1):D353-D361. (dg:DG01665)
11	HIV-1 reverse transcriptase complex with DNA and nevirapine reveals non-nucleoside inhibition mechanism.Nat Struct Mol Biol.2012 Jan 22;19(2):253-9.
12	A peptide inhibitor of HIV-1 reverse transcriptase using alpha,beta-dehydro residues: a structure-based computer model. J Biomol Struct Dyn. 1998 Oct;16(2):347-54.
13	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
14	Quadruple nucleos(t)ide reverse transcriptase inhibitors-only regimen of tenofovir plus zidovudine/lamivudine/abacavir in heavily pre-treated HIV-1 infected patients: salvage therapy or backbone only Curr HIV Res. 2009 May;7(3):320-6.
15	Emerging antiviral drugs. Expert Opin Emerg Drugs. 2008 Sep;13(3):393-416.
16	2008 FDA drug approvals. Nat Rev Drug Discov. 2009 Feb;8(2):93-6.
17	2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
18	Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
19	MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
20	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.
21	Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
22	Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
23	Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
24	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.
25	Doxorubicin transport by RALBP1 and ABCG2 in lung and breast cancer. Int J Oncol. 2007 Mar;30(3):717-25.
26	Wild-type breast cancer resistance protein (BCRP/ABCG2) is a methotrexate polyglutamate transporter. Cancer Res. 2003 Sep 1;63(17):5538-43.
27	The effect of low pH on breast cancer resistance protein (ABCG2)-mediated transport of methotrexate, 7-hydroxymethotrexate, methotrexate diglutamate, folic acid, mitoxantrone, topotecan, and resveratrol in in vitro drug transport models. Mol Pharmacol. 2007 Jan;71(1):240-9.
28	Role of BCRP as a biomarker for predicting resistance to 5-fluorouracil in breast cancer. Cancer Chemother Pharmacol. 2009 May;63(6):1103-10.
29	Inhibiting the function of ABCB1 and ABCG2 by the EGFR tyrosine kinase inhibitor AG1478. Biochem Pharmacol. 2009 Mar 1;77(5):781-93.
30	Sterol transport by the human breast cancer resistance protein (ABCG2) expressed in Lactococcus lactis. J Biol Chem. 2003 Jun 6;278(23):20645-51.
31	The phytoestrogen genistein enhances multidrug resistance in breast cancer cell lines by translational regulation of ABC transporters. Cancer Lett. 2016 Jun 28;376(1):165-72.
32	Curcumin inhibits the activity of ABCG2/BCRP1, a multidrug resistance-linked ABC drug transporter in mice. Pharm Res. 2009 Feb;26(2):480-7.
33	Imatinib mesylate (STI571) is a substrate for the breast cancer resistance protein (BCRP)/ABCG2 drug pump. Blood. 2004 Nov 1;104(9):2940-2.
34	Interaction of nonsteroidal anti-inflammatory drugs with multidrug resistance protein (MRP) 2/ABCC2- and MRP4/ABCC4-mediated methotrexate transport. J Pharmacol Exp Ther. 2007 Jan;320(1):229-35.
35	Analysis of methotrexate and folate transport by multidrug resistance protein 4 (ABCC4): MRP4 is a component of the methotrexate efflux system. Cancer Res. 2002 Jun 1;62(11):3144-50.
36	ATP-binding cassette C transporters in human pancreatic carcinoma cell lines. Upregulation in 5-fluorouracil-resistant cells. Pancreatology. 2009;9(1-2):136-44.
37	The human multidrug resistance protein MRP4 functions as a prostaglandin efflux transporter and is inhibited by nonsteroidal antiinflammatory drugs. Proc Natl Acad Sci U S A. 2003 Aug 5;100(16):9244-9.
38	Steroid and bile acid conjugates are substrates of human multidrug-resistance protein (MRP) 4 (ATP-binding cassette C4). Biochem J. 2003 Apr 15;371(Pt 2):361-7.
39	P-glycoprotein, but not multidrug resistance protein 4, plays a role in the systemic clearance of irinotecan and SN-38 in mice. Drug Metab Lett. 2010 Dec;4(4):195-201.
40	Polymorphisms in multidrug resistance-associated protein gene 4 is associated with outcome in childhood acute lymphoblastic leukemia. Blood. 2009 Aug 13;114(7):1383-6.
41	Role of glutathione in the multidrug resistance protein 4 (MRP4/ABCC4)-mediated efflux of cAMP and resistance to purine analogues. Biochem J. 2002 Feb 1;361(Pt 3):497-503.
42	The anti-influenza drug oseltamivir exhibits low potential to induce pharmacokinetic drug interactions via renal secretion-correlation of in vivo and in vitro studies. Drug Metab Dispos. 2002 Jan;30(1):13-9.
43	Transport of aminopterin by human organic anion transporters hOAT1 and hOAT3: Comparison with methotrexate. Drug Metab Pharmacokinet. 2010;25(2):163-9.
44	Human organic anion transporters and human organic cation transporters mediate renal transport of prostaglandins. J Pharmacol Exp Ther. 2002 Apr;301(1):293-8.
45	Human organic anion transporters and human organic cation transporters mediate renal antiviral transport. J Pharmacol Exp Ther. 2002 Mar;300(3):918-24.
46	Expression levels of renal organic anion transporters (OATs) and their correlation with anionic drug excretion in patients with renal diseases. Pharm Res. 2004 Jan;21(1):61-7.
47	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.
48	Interaction of zalcitabine with human organic anion transporter 1. Pharmazie. 2006 May;61(5):491-2.
49	Apical expression or expression in a non polarized cell of hOAT1 inverses regulation by epidermal growth factor (EGF) as compared to basolateral hOAT1. Cell Physiol Biochem. 2004;14(3):177-86.
50	Methotrexate-loxoprofen interaction: involvement of human organic anion transporters hOAT1 and hOAT3. Drug Metab Pharmacokinet. 2004 Oct;19(5):369-74.
51	Identification and characterization of human organic anion transporter 3 expressing predominantly in the kidney. Mol Pharmacol. 2001 May;59(5):1277-86.
52	Prediction of the overall renal tubular secretion and hepatic clearance of anionic drugs and a renal drug-drug interaction involving organic anion transporter 3 in humans by in vitro uptake experiments. Drug Metab Dispos. 2011 Jun;39(6):1031-8.
53	Murine renal organic anion transporters mOAT1 and mOAT3 facilitate the transport of neuroactive tryptophan metabolites. Am J Physiol Cell Physiol. 2005 Nov;289(5):C1075-84.
54	Organic anion transporter 3 is involved in the brain-to-blood efflux transport of thiopurine nucleobase analogs. J Neurochem. 2004 Aug;90(4):931-41.
55	Transporter-mediated influx and efflux mechanisms of pitavastatin, a new inhibitor of HMG-CoA reductase. J Pharm Pharmacol. 2005 Oct;57(10):1305-11.
56	The contribution of organic anion transporters OAT1 and OAT3 to the renal uptake of rosuvastatin. J Pharmacol Exp Ther. 2007 Sep;322(3):1221-7.
57	Aspirin and probenecid inhibit organic anion transporter 3-mediated renal uptake of cilostazol and probenecid induces metabolism of cilostazol in the rat. Drug Metab Dispos. 2014 Jun;42(6):996-1007.
58	Modulation of the ATPase and transport activities of broad-acting multidrug resistance factor ABCC10 (MRP7). Cancer Res. 2012 Dec 15;72(24):6457-67.
59	ABCC11/MRP8 confers pemetrexed resistance in lung cancer. Cancer Sci. 2010 Nov;101(11):2404-10.
60	Human multidrug resistance protein 8 (MRP8/ABCC11), an apical efflux pump for steroid sulfates, is an axonal protein of the CNS and peripheral nervous system. Neuroscience. 2006;137(4):1247-57.
61	MRP8, ATP-binding cassette C11 (ABCC11), is a cyclic nucleotide efflux pump and a resistance factor for fluoropyrimidines 2',3'-dideoxycytidine and 9'-(2'-phosphonylmethoxyethyl)adenine. J Biol Chem. 2003 Aug 8;278(32):29509-14.