Drug intelligence / Profile preview

imagabalin + cimetidine

Development stage
Discontinued
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

**imagabalin + cimetidine** is a theoretical or investigational combination of two agents: **imagabalin** (a gabapentinoid, chemically related to gabapentin and pregabalin, under development for neuropathic pain and other indications) and **cimetidine** (a well-established histamine H2 receptor antagonist primarily used to treat gastric acid disorders). Imagabalin functions primarily as a ligand of the α2δ subunit of voltage-gated calcium channels in the central nervous system, inhibiting excitatory neurotransmitter release. Cimetidine inhibits gastric acid secretion via antagonism of the histamine H2 receptor and also acts as an inhibitor of organic cation transporters (OCT2, MATE1/2-K), affecting renal elimination of certain drugs. No evidence supports the existence of a fixed-dose combination product or specific brand, and no clinical development status for the direct combination has been identified. However, pharmacokinetic drug–drug interaction studies with mirogabalin (a related gabapentinoid) and cimetidine have shown that coadministration increases exposure to mirogabalin (and likely imagabalin) due to reduced renal clearance, mediated by inhibition of renal transporters by cimetidine. No clinically significant safety concerns or need for dose adjustment have been reported for similar combinations.

02

Targets

HRH2 (Histamine H2 Receptor)OCT (Organic cation transporter family)α2δ (Voltage-gated calcium channel alpha-2-delta subunit)SLC47A1 (Multidrug and toxin extrusion transporter 1)MATE2-K (Multidrug and toxin extrusion protein 2)OCT2 (Organic cation transporter 2)CACNA2D1 (Voltage-gated calcium channel subunit alpha2/delta-1)

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