AZD5213 + pregabalin

AZD5213 + pregabalin is a combination of two investigational and approved drugs evaluated for the treatment of painful diabetic neuropathy. AZD5213 is a potent, competitive, rapidly reversible functional antagonist (inverse agonist) at the human histamine H3 receptor. It increases the release of neurotransmitters such as histamine, acetylcholine, dopamine, and norepinephrine in preclinical models and has shown activity in reversing neuropathic pain in rodents[1][5]. Pregabalin is an approved gabapentinoid that binds to the α2δ subunit of voltage-gated calcium channels in the central nervous system, reducing excitatory neurotransmitter release and providing antinociceptive (pain-reducing) and anticonvulsant effects[6][8]. The combination was studied by AstraZeneca for efficacy in treating painful diabetic neuropathy but did not demonstrate clinical benefit over placebo or monotherapy with pregabalin[4][5][7].

Other names

AZD5213 + Lyrica