Examples of drugs in development that remain viable candidates for future therapeutic interventions
| Drug | Target | Comments |
|---|---|---|
| Mg2+ | NMDA receptors | Some positive results reported in the clinic (Pickering et al., 2011) |
| Cobazam | α2 subunit of GABAA receptor | Encouraging results in preliminary clinical trials (Besson et al., 2015) |
| N-desmethyl clobazam | α2 subunit of GABAA receptor | Parent compound for development of new drugs (Ralvenius et al., 2016) |
| µ-TRTX-Hhn1b | Nav1.7 | Liu et al., 2014 |
| μ-SLPTX-Ssm6a | Nav1.7 | Yang et al., 2013 |
| Monoclonal antibody | Voltage sensor paddle domain of Nav1.7 | Lee et al., 2014 |
| ΟΒ−1 | STOML-3 and Piezo2 mechanoreceptor channels | Wetzel et al., 2017 |
| CLP-257 | KCC2 (K+/Cl− cotransporter) | Gagnon et al., 2013 |
| KYS05090S or ABT-639. . | Small-molecule T-channel blockers | Jarvis et al., 2014; Zhang et al., 2015a; M’Dahoma et al., 2016 |
| N-((1-(2-(tertbutylamino)-2-oxoethyl)piperidin-4-yl)methyl)-9-pentyl-9Hcarbazole-3-carboxamide | CB2 agonist that targets Cav3.2 T-type channels | Berger et al., 2014; Bladen et al., 2015; Snutch and Zamponi, 2017 |
| A-1264087 | State-dependent Cav2 blockers | Oral administration of all of these drugs displays antiallodynic efficacy in rodent models (Patel et al., 2017) |
| TROX-1 | ||
| ZC88. | ||
| Clobezam | α2 subunit of GABAA | (Besson et al., 2013) Encouraging results in preliminary trials (Besson et al., 2015) |
| GCD-0276 | Nav1.7 | Under development (Bagal et al., 2014, 2015; Yekkirala et al., 2017) |
| GCD-0310 | ||
| PF-05089771 | ||
| BIIB074 | Nav1.7 | In phase 2a clinical trials (Zakrzewska et al., 2017) |
| M4 | Broad-spectrum dihydropyridine-related Ca2+ channel blocker blocks Cav 1.2 (L-type), Cav 2.2 (N-type), and Cav 3.2 and 3.3 (T-type channels) | Under development (Gadotti et al., 2015; Zamponi et al., 2015). |
| EMA401 | AT2 (angiotensin) receptor antagonist | Produces antinociception in mouse neuropathic pain models and inhibits capsaicin-induced calcium fluxes in human and DRGs |
| IB-MECA | Adenosine A3 receptor | Efficacy of A3 receptor agonists in relief of allodynia in rodent models has been convincingly demonstrated (Ford et al., 2015; Little et al., 2015) |
| MRS5698 | ||
| ICA-27243 | KCNQ/Kv7.2/7.3 channel opener | Effective in animal models of inflammatory pain (Hayashi et al., 2014) |
KCNQ, M-type potassium channel comprising Kv7.2 and Kv7.3 subunits.