Drug intelligence / Profile preview

ketoprofen lysine salt + gabapentin

Development stage
Preclinical
Lead developer
Dompé
Modality
Small Molecules
Administration
Oral
01

Overview

Ketoprofen lysine salt + gabapentin is a fixed-dose combination of two active pharmaceutical ingredients used for the management of pain, particularly chronic and neuropathic pain. Ketoprofen lysine salt is a nonsteroidal anti-inflammatory drug (NSAID) that works primarily by inhibiting cyclooxygenase enzymes (COX-1 and COX-2), thereby reducing prostaglandin synthesis involved in inflammation, pain, and fever. Gabapentin is an anticonvulsant that acts mainly by binding to the α2δ-1 subunit of voltage-gated calcium channels in the central nervous system, which inhibits excitatory neurotransmitter release and reduces neuronal hyperexcitability associated with neuropathic pain. The combination aims to provide synergistic analgesic effects through multimodal mechanisms—anti-inflammatory action from ketoprofen and modulation of neuropathic pathways from gabapentin[1][4]. This co-crystal or fixed-dose formulation has been investigated for enhanced efficacy and bioavailability compared to individual components.

Other names
ketoprofen lysine salt + gabapentin
02

Targets

CACNA2D1 (Voltage-gated calcium channel subunit alpha2/delta-1)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)PGHS-1 (Prostaglandin G/H Synthase 1)

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