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dasolampanel etibutil
- Development stage
- Phase 2
- Lead developer
- Amgen
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Dasolampanel etibutil is an orally available small molecule competitive antagonist of the AMPA and kainate subtypes of ionotropic glutamate receptors. It was developed as a follow-on compound to tezampanel, with improved oral bioavailability, for the treatment of chronic pain conditions including neuropathic pain and migraine. The drug originated at Eli Lilly and Horizon Pharma, and was later developed by Raptor Pharmaceuticals/Torrey Pines Therapeutics. Dasolampanel etibutil demonstrated efficacy in reducing capsaicin-induced pain and hyperalgesia in human volunteers but failed to achieve positive results in phase 2 clinical trials for osteoarthritis knee pain and diabetic peripheral neuropathic pain. Its mechanism involves blocking excitatory neurotransmission mediated by AMPA (GRIA) and kainate (GRIK) receptors[1][2][3][4][6].
- Other names
- dasolampanel etibutil tosylate
02
Targets
AMPAR (AMPA receptor)Kainate-type ionotropic glutamate receptor
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