Examples of drugs in development that remain viable candidates for future therapeutic interventions

Mg2+NMDA receptorsSome positive results reported in the clinic (Pickering et al., 2011)
Cobazamα2 subunit of GABAA receptorEncouraging results in preliminary clinical trials (Besson et al., 2015)
N-desmethyl clobazamα2 subunit of GABAA receptorParent compound for development of new drugs (Ralvenius et al., 2016)
µ-TRTX-Hhn1bNav1.7Liu et al., 2014
μ-SLPTX-Ssm6aNav1.7Yang et al., 2013
Monoclonal antibodyVoltage sensor paddle domain of Nav1.7Lee et al., 2014
ΟΒ−1STOML-3 and Piezo2 mechanoreceptor channelsWetzel et al., 2017
CLP-257KCC2 (K+/Cl cotransporter)Gagnon et al., 2013
KYS05090S or ABT-639. .Small-molecule T-channel blockersJarvis 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-carboxamideCB2 agonist that targets Cav3.2 T-type channelsBerger et al., 2014; Bladen et al., 2015; Snutch and Zamponi, 2017
A-1264087State-dependent Cav2 blockersOral administration of all of these drugs displays antiallodynic efficacy in rodent models (Patel et al., 2017)
Clobezamα2 subunit of GABAA(Besson et al., 2013) Encouraging results in preliminary trials (Besson et al., 2015)
GCD-0276Nav1.7Under development (Bagal et al., 2014, 2015; Yekkirala et al., 2017)
BIIB074Nav1.7In phase 2a clinical trials (Zakrzewska et al., 2017)
M4Broad-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).
EMA401AT2 (angiotensin) receptor antagonistProduces antinociception in mouse neuropathic pain models and inhibits capsaicin-induced calcium fluxes in human and DRGs
IB-MECAAdenosine A3 receptorEfficacy of A3 receptor agonists in relief of allodynia in rodent models has been convincingly demonstrated (Ford et al., 2015; Little et al., 2015)
ICA-27243KCNQ/Kv7.2/7.3 channel openerEffective in animal models of inflammatory pain (Hayashi et al., 2014)
  • KCNQ, M-type potassium channel comprising Kv7.2 and Kv7.3 subunits.