Details of the Drug Combination

General Information of Drug Combination (ID: DC93237)

Drug Combination Name
Gabapentin Duloxetine
Indication
Disease Entry Status REF
Diabetic Neuropathic Pain Phase 1 [1]
Component Drugs Gabapentin   DM6T924 Duloxetine   DM9BI7M
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 Gabapentin
Disease Entry ICD 11 Status REF
Complex partial seizure 8A68.0 Approved [2]
Postherpetic neuralgia 1E91.5 Approved [3]
Solid tumour/cancer 2A00-2F9Z Phase 3 [2]
Gabapentin Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Gamma-aminobutyric acid B receptor (GABBR) TTDCVZW GABR1_HUMAN; GABR2_HUMAN Antagonist [6]
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Gabapentin 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 cation/carnitine transporter 1 (SLC22A4) DT2EG60 S22A4_HUMAN Substrate [8]
L-type amino acid transporter 1 (SLC7A5) DT48T0N LAT1_HUMAN Substrate [9]
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Gabapentin Interacts with 11 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
D(1A) dopamine receptor (DRD1) OTLZPBT7 DRD1_HUMAN Increases ADR [10]
5-hydroxytryptamine receptor 3A (HTR3A) OTAIV1AK 5HT3A_HUMAN Increases ADR [10]
5-hydroxytryptamine receptor 2B (HTR2B) OTM1AD9J 5HT2B_HUMAN Increases ADR [10]
Alpha-1A adrenergic receptor (ADRA1A) OTUIWCL5 ADA1A_HUMAN Increases ADR [10]
5-hydroxytryptamine receptor 2A (HTR2A) OTWXJX0M 5HT2A_HUMAN Increases ADR [10]
Glutamine--fructose-6-phosphate aminotransferase 1 (GFPT1) OTQBDO45 GFPT1_HUMAN Increases ADR [10]
Transforming growth factor beta-1 proprotein (TGFB1) OTV5XHVH TGFB1_HUMAN Increases ADR [10]
ATP-dependent translocase ABCB1 (ABCB1) OTEJROBO MDR1_HUMAN Decreases Activity [11]
Sodium-dependent serotonin transporter (SLC6A4) OT6FGDLW SC6A4_HUMAN Decreases Expression [12]
Voltage-dependent calcium channel subunit alpha-2/delta-2 (CACNA2D2) OTFJXVQQ CA2D2_HUMAN Affects Binding [13]
SH3 and multiple ankyrin repeat domains protein 2 (SHANK2) OTSQTPFQ SHAN2_HUMAN Decreases Expression [12]
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⏷ Show the Full List of 11 DOT(s)
Indication(s) of Duloxetine
Disease Entry ICD 11 Status REF
Depression 6A70-6A7Z Approved [4]
Major depressive disorder 6A70.3 Approved [5]
Stress urinary incontinence MF50.20 Approved [5]
Traumatic brain injury NA07.Z Approved [5]
Duloxetine Interacts with 2 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Norepinephrine transporter (NET) TTAWNKZ SC6A2_HUMAN Inhibitor [14]
Serotonin transporter (SERT) TT3ROYC SC6A4_HUMAN Inhibitor [14]
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Duloxetine Interacts with 3 DME Molecule(s)
DME Name DME ID UniProt ID Mode of Action REF
Cytochrome P450 1A2 (CYP1A2) DEJGDUW CP1A2_HUMAN Metabolism [15]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Metabolism [15]
Cytochrome P450 2C9 (CYP2C9) DE5IED8 CP2C9_HUMAN Metabolism [15]
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References

1 ClinicalTrials.gov (NCT00619983) Three Way Interaction Between Gabapentin, Duloxetine, and Donepezil in Patients With Diabetic Neuropathy
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: 5483).
3 Gabapentin FDA Label
4 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: 202).
5 Duloxetine FDA Label
6 Gabapentin increases a tonic inhibitory conductance in hippocampal pyramidal neurons. Anesthesiology. 2006 Aug;105(2):325-33.
7 Clinical pharmacokinetic drug interaction studies of gabapentin enacarbil, a novel transported prodrug of gabapentin, with naproxen and cimetidine. Br J Clin Pharmacol. 2010 May;69(5):498-507.
8 Effects of genetic variation in the novel organic cation transporter, OCTN1, on the renal clearance of gabapentin. Clin Pharmacol Ther. 2008 Mar;83(3):416-21.
9 Transport of gabapentin by LAT1 (SLC7A5). Biochem Pharmacol. 2013 Jun 1;85(11):1672-83.
10 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.
11 Functional evaluation of polymorphisms in the human ABCB1 gene and the impact on clinical responses of antiepileptic drugs. Pharmacogenet Genomics. 2008 May;18(5):390-402. doi: 10.1097/FPC.0b013e3282f85e36.
12 Establishment of a 13 genes-based molecular prediction score model to discriminate the neurotoxic potential of food relevant-chemicals. Toxicol Lett. 2022 Feb 1;355:1-18. doi: 10.1016/j.toxlet.2021.10.013. Epub 2021 Nov 5.
13 Tissue-specific expression and gabapentin-binding properties of calcium channel alpha2delta subunit subtypes. J Membr Biol. 2001 Nov 1;184(1):35-43. doi: 10.1007/s00232-001-0072-7.
14 Multi-target therapeutics: when the whole is greater than the sum of the parts. Drug Discov Today. 2007 Jan;12(1-2):34-42.
15 Duloxetine: clinical pharmacokinetics and drug interactions. Clin Pharmacokinet. 2011 May;50(5):281-94.