gabapentin enacarbil immediate release

Gabapentin enacarbil immediate release (GE-IR) is an oral immediate-release formulation of gabapentin enacarbil, a prodrug of the neuromodulator gabapentin. Developed by Arbor Pharmaceuticals, GE-IR was specifically utilized in clinical studies to evaluate the pharmacokinetics and human abuse potential of the prodrug, comparing it to both placebo and active controls like oxycodone. Unlike the commercially available extended-release formulation (Horizant), GE-IR provides a rapid release of the active moiety. Gabapentin enacarbil is designed to overcome the saturable absorption limitations of gabapentin by utilizing high-capacity transporters (MCT1 and SMVT) in the intestine. Once absorbed, it is rapidly hydrolyzed to gabapentin, which then binds to the α2δ-1 subunit of voltage-gated calcium channels in the central nervous system, reducing the release of excitatory neurotransmitters.

Other names

gabapentin enacarbil IRgabapentin enacarbil immediate release capsules