Mirogabalin besylate Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
Mirogabalin besylate (mirogabalin, Tarlige) is a gabapentinoid therapy developed by Daiichi Sankyo, which is approved in Japan for the treatment of postherpetic neuralgia and painful diabetic peripheral neuropathy. Mirogabalin has a potent pain-modulating effect with a unique high affinity and prolonged dissociation rate for the a2delta-1 subunit of voltage-gated calcium (Ca2+) channels (VGCCs) on the dorsal root ganglion resulting in more sustained analgesia compared with traditional gabapentinoids[1].
Verwenden
Mirogabalin besylate is an oral gabapentin analogue for the treatment of peripheral neuralgia (PNP), including diabetic PNP and postherpetic neuralgia. The drug has been approved in Japan for the treatment of PNP and has not yet received FDA approval.
Synthese
Synthesis of Mirogabalin besylate
Stoffwechsel
Mirogabalin is rapidly absorbed, and clearance is through renal excretion (approximately 80%) with approximately 20% being metabolized. Metabolism is primarily to the biologically inactive14 lactam form (A204-4455) and involves various uridine 5′-diphospho-glucuronosyltransferase (UGT) isoforms acting at the carboxylic acid moiety to produce mirogabalin acylglucuronide, which is then nonenzymatically converted to A204-4455.
Mirogabalin besylate Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
