General Information of Drug Combination (ID: DCGL2JR)

Drug Combination Name
Famotidine Raltegravir
Indication
Disease Entry Status REF
HIV-1 Infection Phase 1 [1]
Component Drugs Famotidine   DMRL3AB Raltegravir   DMYURI6
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 Famotidine
Disease Entry ICD 11 Status REF
Gastric ulcer DA60 Approved [2]
Gastrinoma 2C10.1 Approved [2]
Peptic esophagitis N.A. Approved [2]
Peptic ulcer DA61 Approved [3]
Coronavirus Disease 2019 (COVID-19) 1D6Y Phase 3 [4]
Famotidine Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Histamine H2 receptor (H2R) TTQHJ1K HRH2_HUMAN Antagonist [6]
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Famotidine Interacts with 3 DTP Molecule(s)
DTP Name DTP ID UniProt ID Mode of Action REF
Organic cation transporter 2 (SLC22A2) DT9IDPW S22A2_HUMAN Substrate [7]
Organic anion transporter 1 (SLC22A6) DTQ23VB S22A6_HUMAN Substrate [8]
Organic anion transporter 3 (SLC22A8) DTVP67E S22A8_HUMAN Substrate [7]
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Famotidine Interacts with 1 DME Molecule(s)
DME Name DME ID UniProt ID Mode of Action REF
Mephenytoin 4-hydroxylase (CYP2C19) DEGTFWK CP2CJ_HUMAN Metabolism [9]
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Famotidine Interacts with 16 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Solute carrier family 22 member 2 (SLC22A2) OTGFK1AL S22A2_HUMAN Increases Uptake [7]
Organic anion transporter 3 (SLC22A8) OT8BY933 S22A8_HUMAN Increases Uptake [8]
Solute carrier family 22 member 3 (SLC22A3) OTQYGVXX S22A3_HUMAN Decreases Activity [10]
Transmembrane protease serine 2 (TMPRSS2) OTN44YQ5 TMPS2_HUMAN Increases Expression [11]
Prolactin (PRL) OTWFQGX7 PRL_HUMAN Increases Expression [12]
Gastrin (GAST) OTD0IP9N GAST_HUMAN Affects Expression [13]
HLA class I histocompatibility antigen, alpha chain E (HLA-E) OTX1CTFB HLAE_HUMAN Affects Expression [14]
Serine/threonine-protein kinase B-raf (BRAF) OT7S81XQ BRAF_HUMAN Decreases Activity [15]
HLA class II histocompatibility antigen, DM beta chain (HLA-DMB) OT17HGXJ DMB_HUMAN Affects Expression [14]
Catenin beta-1 (CTNNB1) OTZ932A3 CTNB1_HUMAN Increases Expression [16]
Fibroblast growth factor 21 (FGF21) OT3RXVRD FGF21_HUMAN Increases Expression [17]
Interleukin-3 (IL3) OT0CQ35N IL3_HUMAN Increases ADR [18]
Granulocyte-macrophage colony-stimulating factor (CSF2) OT1M7D28 CSF2_HUMAN Increases ADR [18]
Solute carrier family 22 member 1 (SLC22A1) OT7817I4 S22A1_HUMAN Affects Transport [10]
Thiamine transporter 2 (SLC19A3) OTOWP1CT S19A3_HUMAN Increases Uptake [19]
Granulocyte colony-stimulating factor receptor (CSF3R) OTXRAY6X CSF3R_HUMAN Increases ADR [18]
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⏷ Show the Full List of 16 DOT(s)
Indication(s) of Raltegravir
Disease Entry ICD 11 Status REF
Human immunodeficiency virus infection 1C62 Approved [5]
Raltegravir 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 [5]
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Raltegravir Interacts with 2 DME Molecule(s)
DME Name DME ID UniProt ID Mode of Action REF
UDP-glucuronosyltransferase 1A1 (UGT1A1) DEYGVN4 UD11_HUMAN Metabolism [21]
Cytochrome P450 1A1 (CYP1A1) DE6OQ3W CP1A1_HUMAN Metabolism [22]
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References

1 ClinicalTrials.gov (NCT01000818) A Study to Evaluate the Effect of Famotidine and Omeprazole on MK0518 (Raltegravir) Pharmacokinetics in Human Immunodeficiency Virus (HIV)-Infected Patients (0518-054)
2 Famotidine FDA Label
3 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: 7074).
4 ClinicalTrials.gov (NCT04370262) Multi-site Adaptive Trials Using Hydroxycholoroquine for COVID-19. U.S. National Institutes of Health.
5 2007 FDA drug approvals: a year of flux. Nat Rev Drug Discov. 2008 Feb;7(2):107-9.
6 Histamine H1 and H2 receptor antagonists accelerate skin barrier repair and prevent epidermal hyperplasia induced by barrier disruption in a dry environment. J Invest Dermatol. 2001 Feb;116(2):261-5.
7 A species difference in the transport activities of H2 receptor antagonists by rat and human renal organic anion and cation transporters. J Pharmacol Exp Ther. 2005 Oct;315(1):337-45.
8 Different transport properties between famotidine and cimetidine by human renal organic ion transporters (SLC22A). Eur J Pharmacol. 2004 Oct 25;503(1-3):25-30.
9 Initial 48-hour acid inhibition by intravenous infusion of omeprazole, famotidine, or both in relation to cytochrome P450 2C19 genotype status. Clin Pharmacol Ther. 2006 Nov;80(5):539-48.
10 Differential substrate and inhibitory activities of ranitidine and famotidine toward human organic cation transporter 1 (hOCT1; SLC22A1), hOCT2 (SLC22A2), and hOCT3 (SLC22A3). J Pharmacol Exp Ther. 2005 Dec;315(3):1288-97.
11 Effect of common medications on the expression of SARS-CoV-2 entry receptors in liver tissue. Arch Toxicol. 2020 Dec;94(12):4037-4041. doi: 10.1007/s00204-020-02869-1. Epub 2020 Aug 17.
12 Hyperprolactinaemia during famotidine therapy. Lancet. 1993 Oct 2;342(8875):868. doi: 10.1016/0140-6736(93)92729-d.
13 Effects of three H2-receptor antagonists (cimetidine, famotidine, ranitidine) on serum gastrin level. Int J Clin Pharmacol Res. 2002;22(2):29-35.
14 Systems pharmacological analysis of drugs inducing stevens-johnson syndrome and toxic epidermal necrolysis. Chem Res Toxicol. 2015 May 18;28(5):927-34. doi: 10.1021/tx5005248. Epub 2015 Apr 3.
15 Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma. Nature. 2010 Sep 30;467(7315):596-9. doi: 10.1038/nature09454.
16 Famotidine has a neuroprotective effect on MK-801 induced toxicity via the Akt/GSK-3/-catenin signaling pathway in the SH-SY5Y cell line. Chem Biol Interact. 2019 Dec 1;314:108823. doi: 10.1016/j.cbi.2019.108823. Epub 2019 Sep 26.
17 Increased immunoreactivity and concentration of basic fibroblast growth factor in lansoprazole-treated gastric mucosa. J Clin Gastroenterol. 1995;21 Suppl 1:S24-9.
18 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.
19 Metformin Is a Substrate and Inhibitor of the Human Thiamine Transporter, THTR-2 (SLC19A3). Mol Pharm. 2015 Dec 7;12(12):4301-10.
20 Population pharmacokinetic analysis and pharmacogenetics of raltegravir in HIV-positive and healthy individuals. Antimicrob Agents Chemother. 2012 Jun;56(6):2959-66. doi: 10.1128/AAC.05424-11. Epub 2012 Feb 27.
21 Successful tacrolimus treatment following renal transplant in a HIV-infected patient with raltegravir previously treated with a protease inhibitor based regimen. Drug Metabol Drug Interact. 2011;26(3):139-41.
22 Exposure-related effects of atazanavir on the pharmacokinetics of raltegravir in HIV-1-infected patients. Ther Drug Monit. 2010 Dec;32(6):782-6.