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imagabalin + metformin
- Development stage
- Preclinical
- 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
ND1 (Mitochondrial electron transport chain complex I)COXGPD2 (Glycerol-3-phosphate dehydrogenase 2)GSEC (Gamma-Secretase Complex)v-ATPase-Ragulator-AXIN-LKB1-AMPK (Vacuolar H+-ATPase-Ragulator-AXIN-LKB1-AMPK complex)CACNA2D1 (Voltage-gated calcium channel subunit alpha2/delta-1)CACNA2D2 (α2δ-2)AMPK (Adenosine monophosphate–activated protein kinase)G6PC1 (Glucose 6-phosphatase alpha)α2δ (Voltage-gated calcium channel alpha-2-delta subunit)
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