Table 2.
Voltage-gated sodium channel inhibitors in current study.
| Company | Code | Selectivity | Clinical phase | Indications | Results | Observations | Identifiers |
|---|---|---|---|---|---|---|---|
| Pfizer | PF-05089771 | Nav1.7 | II | Postoperative dental pain | None reported | NCT01529346 | |
| I | OA | None reported | NCT01529671 | ||||
| II | DPN and painful | None reported | NCT02215252 | ||||
| II | IEM | None reported | NCT01769274 | ||||
| Convergence Pharmaceuticals | CNV-1014802 or GSK-1014802 (Raxatrigine) |
Nav1.7 | II | Trigeminal neuralgia | Well tolerated, no major side effects [25], reduced pain severity and the number of paroxysms in all primary and secondary outcomes [26] | Orphan-drug designation by the FDA.[27] Phase III preparation [28] | NCT01540630 |
| II | NP (lumbosacral radiculopathy) | Reduced pain [26] | NCT01561027 | ||||
| CNV-1061436 | Nav blocker | Pain | None reported | Ready for phase I [28,29] | Not applicable | ||
| CNV-3000223 | Nav1.7 | None reported | Undergoing preclinical studies [28,30] | Not applicable | |||
| CNV-3000164 | Nav1.7 | None reported | Undergoing preclinical studies [28] | Not applicable | |||
| Xenon/Teva | XEN-402 (or TV-45070) |
Nav1.7 | I II |
Primary erythermalgiaIEM | Reduced pain, well tolerated [31] | NCT01486446 | |
| II | Post herpetic neuralgia | Reduced of pain, well tolerated, improvements in sleep [31] | NCT01195636 | ||||
| Inflammatory pain [32] | None reported | Not applicable | |||||
| Xenon/Genentech | GDC-0276 or RG7893 | Nav1.7 | I | Pain | None reported | Not disclosed [33] | |
| Xenon/Genentech | GDC-0310 | Nav1.7 | I | Pain | None reported | Not disclosed [34] | |
| Sumitomo Dainippon Pharma | DSP-2230 | Nav1.7/ Nav1.8 | I | NP | None reported | Antiallodynic effect in animal models of neuropathic pain [35] | ISRCTN07951717 |
| Necktar Therapeutics | NKTR-171 | Peripheral Nav | I | NP | Preclinical studies in rodents demonstrate that NKTR-171 has a superior therapeutic index (efficacy over CNS side effects) compared to pregabalin and clinically used Na+ channel blockers [36] | Not disclosed | |
| WEX Pharmaceuticals | TTX | Nav TTX-s | III | Moderate to severe inadequately controlled cancer-related pain | None reported | NCT00725114 | |
| II | Pain, peripheral neuropathy, NP | None reported | NCT01655823 | ||||
| Astellas Pharma Inc. /Chromocell Corp. | CC8464 | Nav1.7 | Expected to begin phase I in 2016 [37] | OA, DPN, NP | None reported | Preclinical trials in neuropathic pain in USA (PO) before September 2015 | Not applicable |
OA: osteoarthritis; DPN: diabetic peripheral neuropathy; IEM: inherited erythromelalgia; NP: neuropathic pain; CNS: central nervous system; TTX-s: tetrodotoxin-sensitive.[25–38], https://patents.google.com.