Mirogabalin Besylate

Mirogabalin belongs to the class of gamma amino acids and their derivatives. It binds selectively to the α2δ subunits of voltage-gated calcium channels (VGCCs). This reduces calcium (Ca2+) influx and neurotransmission, which in turn inhibits the release of neurotransmitters at the presynaptic nerve endings. With less neurotransmitter released, the hyper-excitability of central nervous system (CNS) neurons decreases.

After oral administration, mirogabalin is absorbed rapidly, and the median time to maximum plasma concentration is 0.5 to 1.5 h. Plasma protein binding is low, at approximately 25%. The mean apparent volume of distribution is 64 to 88 L after single or multiple doses. Most of the drug is cleared unchanged (61 to 72%) through the kidneys, by filtration and active secretion. A slight fraction (13 to 20%) is metabolized by hepatic uridine 5'-diphospho-glucuronosyltransferase isoforms. The mean elimination half-life of mirogabalin was observed to be 2 to 4.9 h. About 99% of the drug is excreted through the kidneys, and only 1% of the dose goes out through the feces.