General Information of Drug Combination (ID: DC8OI8E)

Drug Combination Name
Dolutegravir GSK1265744
Indication
Disease Entry Status REF
HIV Infections Phase 1 [1]
Component Drugs Dolutegravir   DMCZGRE GSK1265744   DMT8J0I
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 Dolutegravir
Disease Entry ICD 11 Status REF
Human immunodeficiency virus infection 1C62 Approved [2]
Dolutegravir Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Human immunodeficiency virus Integrase (HIV IN) TT5FH9Y POL_HV1B1 Modulator [4]
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Dolutegravir Interacts with 1 DTP Molecule(s)
DTP Name DTP ID UniProt ID Mode of Action REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [5]
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Dolutegravir Interacts with 2 DME Molecule(s)
DME Name DME ID UniProt ID Mode of Action REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Metabolism [6]
UDP-glucuronosyltransferase 1A1 (UGT1A1) DEYGVN4 UD11_HUMAN Metabolism [6]
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Dolutegravir Interacts with 5 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Cytochrome P450 26A1 (CYP26A1) OTL1DFWV CP26A_HUMAN Decreases Expression [7]
T-box transcription factor TBX6 (TBX6) OTW1Q8RM TBX6_HUMAN Increases Expression [7]
Homeobox protein Hox-B1 (HOXB1) OTGC0EKI HXB1_HUMAN Increases Expression [7]
Fibroblast growth factor 8 (FGF8) OTFU0IUW FGF8_HUMAN Increases Expression [7]
Homeobox protein MIXL1 (MIXL1) OT584VOQ MIXL1_HUMAN Increases Expression [7]
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Indication(s) of GSK1265744
Disease Entry ICD 11 Status REF
Human immunodeficiency virus infection 1C62 Phase 3 [3]
GSK1265744 Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Human immunodeficiency virus Integrase (HIV IN) TT5FH9Y POL_HV1B1 Inhibitor [8]
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GSK1265744 Interacts with 2 DME Molecule(s)
DME Name DME ID UniProt ID Mode of Action REF
UDP-glucuronosyltransferase 1A1 (UGT1A1) DEYGVN4 UD11_HUMAN Metabolism [9]
UDP-glucuronosyltransferase 1A9 (UGT1A9) DE85D2P UD19_HUMAN Metabolism [9]
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References

1 ClinicalTrials.gov (NCT04484337) Study to Evaluate Pharmacokinetic (PK), Safety and Tolerability of Cabotegravir (CAB) 400 Milligrams Per Milliliter (mg/mL) Formulation in Healthy Adult Participants
2 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7365).
3 ClinicalTrials.gov (NCT02951052) Study Evaluating the Efficacy, Safety, and Tolerability of Switching to Long-acting Cabotegravir Plus Long-acting Rilpivirine From Current Antiretroviral Regimen in Virologically Suppressed HIV-1-infected Adults. U.S. National Institutes of Health.
4 Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.
5 Tarascon Pocket Pharmacopoeia 2018 Classic Shirt-Pocket Edition.
6 Mechanisms of action, pharmacology and interactions of dolutegravir. Enferm Infecc Microbiol Clin. 2015 Mar;33 Suppl 1:2-8.
7 Dolutegravir Impairs Stem Cell-Based 3D Morphogenesis Models in a Manner Dependent on Dose and Timing of Exposure: An Implication for Its Developmental Toxicity. Toxicol Sci. 2021 Nov 24;184(2):191-203. doi: 10.1093/toxsci/kfab112.
8 Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
9 Disposition and metabolism of cabotegravir: a comparison of biotransformation and excretion between different species and routes of administration in humans. Xenobiotica. 2016;46(2):147-62.