General Information of Drug Combination (ID: DC21DGG)

Drug Combination Name
Tenofovir Emtricitabine
Indication
Disease Entry Status REF
HIV/AIDS Phase 1 [1]
Component Drugs Tenofovir   DM1IS6U Emtricitabine   DMBMUWZ
Small molecular drug Small molecular drug
2D MOL 2D MOL
3D MOL 3D MOL

Molecular Interaction Atlas of This Drug Combination

Molecular Interaction Atlas (MIA)
Indication(s) of Tenofovir
Disease Entry ICD 11 Status REF
Chronic hepatitis B virus infection N.A. Approved [2]
Hepatitis B virus infection 1E51.0 Approved [2]
Human immunodeficiency virus infection 1C62 Approved [3]
Tenofovir Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Human immunodeficiency virus Reverse transcriptase (HIV RT) TT84ETX POL_HV1B1 Inhibitor [6]
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Tenofovir Interacts with 7 DTP Molecule(s)
DTP Name DTP ID UniProt ID Mode of Action REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [7]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [8]
Multidrug resistance-associated protein 4 (ABCC4) DTCSGPB MRP4_HUMAN Substrate [9]
Organic anion transporter 1 (SLC22A6) DTQ23VB S22A6_HUMAN Substrate [10]
Organic anion transporter 3 (SLC22A8) DTVP67E S22A8_HUMAN Substrate [11]
Multidrug resistance-associated protein 7 (ABCC10) DTPS120 MRP7_HUMAN Substrate [12]
Multidrug resistance-associated protein 8 (ABCC11) DTWN7FC ABCCB_HUMAN Substrate [13]
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⏷ Show the Full List of 7 DTP(s)
Indication(s) of Emtricitabine
Disease Entry ICD 11 Status REF
Hepatitis virus infection 1E50-1E51 Approved [4]
Human immunodeficiency virus infection 1C62 Approved [4]
Hepatitis B virus infection 1E51.0 Phase 3 [5]
Emtricitabine Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Human immunodeficiency virus Reverse transcriptase (HIV RT) TT84ETX POL_HV1B1 Modulator [4]
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Emtricitabine Interacts with 1 DTP Molecule(s)
DTP Name DTP ID UniProt ID Mode of Action REF
Multidrug and toxin extrusion protein 1 (SLC47A1) DTZGT0P S47A1_HUMAN Substrate [14]
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Emtricitabine Interacts with 3 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
E3 ubiquitin-protein ligase parkin (PRKN) OTJBN41W PRKN_HUMAN Decreases Expression [15]
Albumin (ALB) OTVMM513 ALBU_HUMAN Affects Binding [16]
Deoxycytidine kinase (DCK) OTW8HLZC DCK_HUMAN Affects Binding [17]
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Test Results of This Drug Combination in Other Disease Systems

Indication DrugCom ID Cell Line Status REF
HIV-1-infection DC0E91Q N. A. Phase 4 [18]
HIV DCSIUUP N. A. Phase 4 [19]
Infection, Human Immunodeficiency Virus DC2KNZU N. A. Phase 2 [20]
Acute HIV Infection DC4VA0W N. A. Phase 1 [21]
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References

1 ClinicalTrials.gov (NCT03917420) Quantification of Estradiol's Impact on Nucleotides in Cellular Populations of the Lower GI Tract
2 Tenofovir FDA Label
3 Anti-hepatitis B virus activity in vitro of combinations of tenofovir with nucleoside/nucleotide analogues. Antivir Chem Chemother. 2009;19(4):165-76.
4 Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
5 Clinical pipeline report, company report or official report of Gilead (2011).
6 Antiviral drugs in current clinical use. J Clin Virol. 2004 Jun;30(2):115-33.
7 KEGG: new perspectives on genomes, pathways, diseases and drugs. Nucleic Acids Res. 2017 Jan 4;45(D1):D353-D361. (dg:DG01665)
8 KEGG: new perspectives on genomes, pathways, diseases and drugs. Nucleic Acids Res. 2017 Jan 4;45(D1):D353-D361. (dg:DG01913)
9 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.
10 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.
11 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.
12 Genetic variants of ABCC10, a novel tenofovir transporter, are associated with kidney tubular dysfunction. J Infect Dis. 2011 Jul 1;204(1):145-53.
13 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.
14 Emtricitabine is a substrate of MATE1 but not of OCT1, OCT2, P-gp, BCRP or MRP2 transporters. Xenobiotica. 2017 Jan;47(1):77-85.
15 Chronic Nucleoside Reverse Transcriptase Inhibitors Disrupt Mitochondrial Homeostasis and Promote Premature Endothelial Senescence. Toxicol Sci. 2019 Dec 1;172(2):445-456. doi: 10.1093/toxsci/kfz203.
16 Binding of anti-HIV drugs to human serum albumin. IUBMB Life. 2004 Oct;56(10):609-14. doi: 10.1080/15216540400016286.
17 Nonenantioselectivity property of human deoxycytidine kinase explained by structures of the enzyme in complex with L- and D-nucleosides. J Med Chem. 2007 Jun 28;50(13):3004-14. doi: 10.1021/jm0700215. Epub 2007 May 27.
18 ClinicalTrials.gov (NCT03360682) Clinical Trial to Evaluate the Efficacy, Pharmacokinetics (PK) Interactions and Safety of Dolutegravir Plus 2 Nucleoside Reverse Transcriptase Inhibitors (NRTIs) in HIV-1-Infected Solid Organ Transplant Patients
19 ClinicalTrials.gov (NCT01335620) The Safety, Pharmacokinetic Profile and Efficacy of Raltegravir in HIV-infected Patients at Least 60 Years of Age
20 ClinicalTrials.gov (NCT01803074) Study to Evaluate a HIV Drug for the Treatment of HIV Infection
21 ClinicalTrials.gov (NCT02475915) Efficacy of VHM After Treatment Interruption in Subjects Initiating ART During Acute HIV Infection