Drug intelligence / Profile preview

imagabalin + metformin

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

Overview

**imagabalin + metformin** is a combination of two pharmaceutical agents: *imagabalin*, a small molecule that acts as a selective ligand of the calcium channel α2δ subunit (structurally related to gabapentin/pregabalin, developed for neuropathic pain), and *metformin*, a small molecule antihyperglycemic agent widely used in the treatment of type 2 diabetes. Imagabalin is primarily investigated for neuropathic pain management, while metformin is indicated for glycemic control in patients with type 2 diabetes. Combination therapy could hypothetically benefit diabetic patients suffering from neuropathic pain, improving pain control without significantly affecting the pharmacokinetics or safety of metformin (based on evidence for the similar agent mirogabalin)[1]. Mechanistically, imagabalin modulates neuronal calcium channels to reduce excitatory neurotransmitter release, while metformin decreases hepatic glucose production, improves peripheral glucose uptake, and exhibits anti-inflammatory activity.

02

Targets

v-ATPase-Ragulator-AXIN-LKB1-AMPK (Vacuolar H+-ATPase-Ragulator-AXIN-LKB1-AMPK complex)ND1 (Mitochondrial electron transport chain complex I)CACNA2D2 (α2δ-2)GSEC (Gamma-Secretase Complex)GPD2 (Glycerol-3-phosphate dehydrogenase 2)CACNA2D1 (Voltage-gated calcium channel subunit alpha2/delta-1)COX

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