| Name | Brand names | Mechanism of action | Indication | Type | Status | Year of Approval/Withdrawal | Company | Notes |
|---|---|---|---|---|---|---|---|---|
| Acetohexamide | Dymelor | Kir6.2 inhibitor | Diabetes mellitus type 2 | Small molecule | Withdrawn in the US | 1964/ | Lilly | |
| Alpidem | GABA-A agonist | Anxiety | Small molecule | Withdrawn | 1991 (France)/1994 | Synthélabo | ||
| Bepridil | Vascor | Cav1.x blocker | Hypertension, chronic stable angina | Small molecule | Withdrawn | 1990/2004 | ||
| Butamben | Alvogil | Cav inhibitor | Skin irritation, chronic pain | Small molecule | Withdrawn | |||
| Cronidipine | Cav blocker | Hypertension | Small molecule | Discontinued | Groupe Fournier | |||
| Encainide | Enkaid | Nav blocker | Ventricular premature beats | Small molecule | Withdrawn | /1991 | ||
| Gaboxadol | GABA-A antagonist | Insomnia | Small Molecule | Discontinued | Lundbeck and Merck | |||
| Halazepam | Paxipam, Alapryl, Pacinone | GABAA potentiator | Anxiety | Small molecule | Withdrawn in the US | 1981/2009 | Schering-Plough | |
| Lindane | Scabene | GABA-A (Sarcoptes scabiei) negative modulator | Infestation by Sarcoptes scabiei, Pediculosis | Small molecule | Withdrawn | 1974/ | ||
| Linopirdine | KCNQ blockers | Alzheimer's disease | Small molecule | Discontinued | ||||
| Mephenytoin | Mesantoin | Nav blocker | Epilepsy | Small molecule | Withdrawn | 1946/ | Novartis | |
| Mibefradil | Posicor | Cav1.x inhibitor, Cav3.x inhibitor | Hypertension, angina | Small molecule | Withdrawn | 1997/1998 | Roche | |
| Moracizine | Ethmozine | Nav1.5 blocker | Ventricular arrhythmia | Small molecule | Withdrawn | 1990 FDA/2007 | ||
| PF-05089771 | Nav1.7 inhibitor | Painful diabetic peripheral neuropathy | Small Molecule | Discontinued | 2015 | Pfizer | Failed phase II | |
| Retigabine | Trobalt, Potiga | Kv7.2-Kv7.5 activator | Epilepsy | Small molecule | Discontinued | 2011/2017 | GSK | |
| RG-6029 | GDC-0310 | Nav1.7 inhibitor | Pain | Small Molecule | Discontinued | 2018 | Roche/Genentech/Xenon | |
| Senicapoc | KCa3.1 (Gardos channel) blocker | Hereditary xerocytosis | Small Molecule | SpringWorks Therapeutics | Repurposed | |||
| Senicapoc | KCa3.1 (Gardos channel) blocker | Sickle cell disease and asthma | Small Molecule | Discontinued | Icagen | |||
| Triazolam | Halcion | GABA-A positive modulator | Insomnia | Small molecule | Withdrawn in the UK | 1982/ | ||
| Unoprostone | Rescula | BK and CLC-2 activator | Ocular hypertension, open-angle glaucoma | Small Molecule | Discontinued in the US | 2000 FDA/ 2015 | Sucampo Pharmaceuticals | |
| TV-45070 | Nav1.7 inhibitor | Post-herpetic neuralgia | Small Molecule | Discontinued | 2017 | Teva/Xenon | Failed phase II | |
| Vixotrigine | BIIB074 | Nav1.7 inhibitor | Painful lumbosacral radiculopathy | Small Molecule | Discontinued | 2018 | Biogen | Failed phase II |
| Z160 | MK-6721, NMED-160 | Cav2.2 antagonist | Chronic pain | Small molecule | Discontinued | Neuromed, Zalicus | ||
| Zoxazolamine | Zoxine | KCa activator | Spasm | Small molecule | Withdrawn | 1955/1961 | ||
| VX-128 | NaV1.8 inhibitor | Pain | Small molecule | Discontinued | 2018 | Vertex Pharmaceuticals | ||
| VX-961 | NaV1.8 inhibitor | Pain | Small molecule | Discontinued | 2020 | Vertex Pharmaceuticals |