Details of the Drug Combination

General Information of Drug Combination (ID: DCE88RB)

Drug Combination Name
Entecavir Adefovir
Indication
Disease Entry Status REF
Hepatitis B, Chronic Phase 4 [1]
Component Drugs Entecavir   DM7VTQO Adefovir   DMM278X
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 Entecavir
Disease Entry ICD 11 Status REF
Hepatitis B virus infection 1E51.0 Approved [2]
Entecavir Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Hepatitis B virus Reverse transcriptase (HBV RT) TTS5K1M DPOL_HBVA3 Modulator [3]
------------------------------------------------------------------------------------
Entecavir Interacts with 9 DTP Molecule(s)
DTP Name DTP ID UniProt ID Mode of Action REF
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [4]
Organic anion transporter 2 (SLC22A7) DT0OC1Q S22A7_HUMAN Substrate [5]
Organic cation transporter 3 (SLC22A3) DT6201N S22A3_HUMAN Substrate [4]
Peptide transporter 2 (SLC15A2) DT8QKNP S15A2_HUMAN Substrate [6]
Organic cation/carnitine transporter 2 (SLC22A5) DT3HUVD S22A5_HUMAN Substrate [4]
Concentrative nucleoside transporter 2 (SLC28A2) DT82KPY S28A2_HUMAN Substrate [4]
Concentrative Na(+)-nucleoside cotransporter 3 (SLC28A3) DT4YL5R S28A3_HUMAN Substrate [4]
Equilibrative nucleoside transporter 1 (SLC29A1) DTXD1TQ S29A1_HUMAN Substrate [4]
Equilibrative nucleoside transporter 2 (SLC29A2) DTW78DQ S29A2_HUMAN Substrate [4]
------------------------------------------------------------------------------------
⏷ Show the Full List of 9 DTP(s)
Adefovir Interacts with 6 DTP Molecule(s)
DTP Name DTP ID UniProt ID Mode of Action REF
Multidrug resistance-associated protein 1 (ABCC1) DTSYQGK MRP1_HUMAN Substrate [7]
Multidrug resistance-associated protein 2 (ABCC2) DTFI42L MRP2_HUMAN Substrate [8]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [9]
Multidrug resistance-associated protein 4 (ABCC4) DTCSGPB MRP4_HUMAN Substrate [10]
Organic anion transporter 1 (SLC22A6) DTQ23VB S22A6_HUMAN Substrate [11]
Organic anion transporter 3 (SLC22A8) DTVP67E S22A8_HUMAN Substrate [12]
------------------------------------------------------------------------------------
⏷ Show the Full List of 6 DTP(s)
Adefovir Interacts with 1 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Band 3 anion transport protein (SLC4A1) OT3EFUK8 B3AT_HUMAN Increases ADR [13]
------------------------------------------------------------------------------------

Test Results of This Drug Combination in Other Disease Systems

Indication DrugCom ID Cell Line Status REF
Hepatitis B, Chronic DC5MTN9 N. A. Phase 1 [14]
------------------------------------------------------------------------------------

References

1 ClinicalTrials.gov (NCT02482272) Compare Continuing Lamivudine Plus Adefovir or Adefovir Versus Switching to Entecavir Plus Adefovir in Patients With LAM-resistant Chronic Hepatitis B
2 Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77.
3 Effect of hepatitis B virus reverse transcriptase variations on entecavir treatment response. J Infect Dis. 2014 Sep 1;210(5):701-7.
4 Multiple SLC and ABC Transporters Contribute to the Placental Transfer of Entecavir. Drug Metab Dispos. 2017 Mar;45(3):269-278.
5 Human organic anion transporter 2 is an entecavir, but not tenofovir, transporter. Drug Metab Pharmacokinet. 2017 Feb;32(1):116-119.
6 The oligopeptide transporter 2-mediated reabsorption of entecavir in rat kidney. Eur J Pharm Sci. 2014 Feb 14;52:41-7.
7 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
8 Pharmacogenetics of membrane transporters: an update on current approaches. Mol Biotechnol. 2010 Feb;44(2):152-67.
9 ABC transporters and their role in nucleoside and nucleotide drug resistance. Biochem Pharmacol. 2012 Apr 15;83(8):1073-83.
10 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.
11 Cytotoxicity of antiviral nucleotides adefovir and cidofovir is induced by the expression of human renal organic anion transporter 1. J Am Soc Nephrol. 2000 Mar;11(3):383-93.
12 FDA Drug Development and Drug Interactions
13 ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
14 ClinicalTrials.gov (NCT00410202) Entecavir Plus Adefovir Combination Therapy Versus Entecavir Monotherapy vs Therapy With Adefovir Plus Lamivudine for Chronic Hepatitis B Infected Subjects With Lamivudine-resistant Virus