Instituut voor Neuropathische Pijn
English articles Research & Development NMDA receptor: target for new developments in neuropathic pain
| NMDA receptor: target for new developments in neuropathic pain |
The NMDA receptor (NMDAR) received a new wave of attention as a target receptor for the development of new drugs for the treatment of neuropathic pain. A substantial body of data supports the expectation that a safe, potent, N-methyl-D-aspartate receptor (NMDAR) blockers would offer symptomatic relief from neuropathic pain. NMDAR stimulation is linked to sensitization of dorsal horn neurons and thus has a direct link to pain and hyperalgesia. Here some of these new R&D activities related to NMDAR ligands.
Anavir PharmaceuticalsAnavir focuses on the NMDA receptor as a prime target for the control of neuropathic pain. The company is developing Neurodex, dextromethorphan in combination with an enzyme inhibitor to block the rapid metabolism of dextromethorphan and maintain elevated blood levels. Dextromethorphan is a potent antagonist of the NMDA receptor. The use of low dose quindine sulfate blocks enzyme activity responsible for the rapid degradation of dextromethorphan and Neurodex currently is being tested for the indication of neuropathic pain. Avanir has completed a Phase II trial in patients with diabetic neuropathy. Treatment was well-tolerated and significantly decreased pain intensity, according to the company. Evotec Neurosciences GmbHEvotec is developing an NMDA receptor NR2B subtype selective antagonist for neuropathic pain. Older compounds emerged as less selective NMDA antagonists with drawbacks such as a narrow therapeutic index and too much side effects. VistaGen Therapeutics, Inc.VistaGen is developing a drug for neuropathic pain and its lead drug candidate AV-101 is entering clinical development. AV-101, L-4-chlorokynurenine, is a novel orally available prodrug (7-chlorokynurenic acid) and a potent glycine receptor antagonist. GB Therapeutics Ltd.GB Therapeutics is also targeting the NMDA glutamate receptor recognized for its role in pain. The glutamate antagonist GT 3381 showed good pain relief and safety in first humans.Defined as a third-generation oral NMDA modulator, GT 3381 currently is in Phase II clinical trials as a first-line therapy for neuropathic pain. March 2010, Jan M. Keppel Hesselink, MD. PhD Gerelateerde artikelen |