Ion channel
drugs

Ion channels represent one of the largest drug target class. Nearly 18% of all existing drugs exert their therapeutic activity through ion channels. Our database contains > 170 marketed ion channel drugs and > 80 ion channel drug candidates in preclinical development and clinical trials.

Ion channel drugs on the market

NameBrand namesMechanism of actionIndicationTypeYear of ApprovalCompany
AmlodipineNorvasc, AforbesCav1.x inhibitorHypertension, vasospastic angina, angina pectoris Small molecule1992Pfizer
AjmalineNav1.5 inhibitorArrhythmiaSmall Molecule
AlosetronLotronex5HT3A antagonistIrritable bowel syndrome with diarrheaSmall molecule2002 FDA
AlprazolamXanaxGABA-A positive modulatorAnxietySmall molecule1981 FDAUpjohn
AmantadineSymadine, OsmolexGluN inhibitorParkinson's diseaseSmall molecule
AmifampridineFirdapseKv blockerLambert-Eaton myasthenic syndromeSmall molecule2009BioMarin
AmilorideMidamorENaC inhibitorHypertensive disorder, edema, hypokalemiaSmall molecule1981
AmiodaroneCordaroneKv11.1 blockerVentricular fibrillation, life-threatening ventricular tachycardia Small molecule1961
AtracuriumChrn abd antagonistGeneral anaesthesia, muscle relaxationSmall Molecule1983 FDA
AzelnidipineCalBlock Cav1.x blockerHypertensionSmall MoleculeDaiichi-Sankyo
BenzocaineAnacaine, DermoplastNav blockerLocal anesthesia Small Molecule
Bioallethrin Sodium channel (Pediculus humanus) modulatorLice and scabies infestationSmall Molecule
BrexanoloneZulressoGABA-A positive modulatorPostpartum depressionSmall Molecule2019Sage Therapeutics
BupivacaineMarcaineNav inhibitorLocal anesthesiaSmall molecule1972 FDAHospira
ButalbitalSandoptal GABA-A potentiatorTension-type headacheSmall Molecule1976Actavis Labs
CapsaicinZostrix, QutenzaTRPV1 activatorNeuralgia, postherpetic neuralgia, backache, arthritic painSmall molecule2009 FDAAcorda Therapeutics
CarbamazepineActebral, TegretolNav1.5 blockerEpilepsy, Lennox-Gastaut syndrome, bipolar disorderSmall molecule1968Novartis
CarbutamideGlucidoralKir6.2 inhibitorDiabetes mellitus type 2Small molecule1956Servier
ChlordiazepoxideRisolidGABAA positive modulatorAnxiety, alcohol withdrawal syndromeSmall molecule1960 FDAValeant
ChloroprocaineNesacaineNav1.8 inhibitorLocal anesthesia Small Molecule
ChlorpropamideKir6.2 inhibitorDiabetes mellitus type 2Small molecule1958Pfizer
ChlorzoxazoneParafon, ParaflexKCa activatorSpasticity, muscle spasm with painSmall molecule1958Janssen
CilnidipineAtelec, CilogardCav1.x blocker, Cav2.2 blockerHypertensionSmall Molecule1995Fuji Viscera, Ajinomoto
CinchocaineDibucaine, NupercainalNav blockerLocal anesthesia Small Molecule
CinnarizineStugeron, CinazynCav inhibitorVertigo, motion sickness, nauseaSmall molecule1955Jansen Pharmaceutica
CisatracuriumNimbexChrn a1b1d inhibitorGeneral anaesthesia, muscle relaxationSmall molecule1995 FDA
ClevidipineCleviprexCav1.x blockerHypertensionSmall molecule2008The Medicines Company
ClobazamFrisium, Urbanol, Onfi, TapclobGABAA partial agonistEpilepsy, anxietySmall molecule2011Lundbeck
ClonazepamClonapam, RivotrilGABAA positive modulatorMyoclonic, atonic and absence seizures; Lennox-Gastaut syndromeSmall molecule1975Roche
ClorazepateTranxeneGABAA positive modulatorAnxiety, alcohol withdrawal syndrome, partial epilepsy Small molecule1972
ClotiazepamClozan GABA-A potentiatorAnxiety disordersSmall Molecule
CrofelemerMytesi, FulyzaqCFTR inhibitor, ANO1 inhibitorNon-infectious diarrheaSmall Molecule2012Salix Pharmaceuticals
CyclandelateCyclospasmol Cav alpha-2/delta-1 modulatorArteriosclerosis, Raynaud's diseaseSmall Molecule
DalfampridineAmpyra, FampyraKv blockerMultiple sclerosisSmall molecule2010Acorda Therapeutics
DantroleneDantriumRyR1 inhibitorSpasticity, malignant hyperthermia Small molecule1974Par Pharmaceutical
DesfluraneSupraneGABA-A agonist, GluA1 inhibitor, GLYRA1 agonistGeneral anestesiaSmall Molecule1992Baxter
DextromethorphanGluN3A antagonistCough, rhinitis, sneezingSmall Molecule1957ANI Pharmaceuticals
DiazepamValium, Diastat GABA-A potentiatorAnxiety, alcohol withdrawal syndrome, spasticity, epilepsySmall molecule1963 FDARoche
DiazoxideProglycemKir6.2 activatorHypertensive emergencies, hyperinsulinismSmall molecule1973
DiltiazemCardizem, TiazacCav1.x inhibitorHypertension, angina pectorisSmall molecule1982
DisopyramideNorpace, Ritmodan, DicorantilNav1.5 inhibitorVentricular arrhythmiaSmall molecule1977G.D. Searle LLC
DofetilideTikosynKir2.2, Kv10.1, Kv11.1 inhibitor Atrial fibrillation, atrial flutter Small molecule1999Pfizer
DronedaroneMultaqMultichannel blockerAtrial fibrillationSmall molecule2009 FDASanofi-Aventis
EfonidipineLandelCav1.x inhibitor, Cav3.x inhibitor HypertensionSmall molecule1995
EnfluraneEthrane, Alyrane GABA-A agonist, GluA1 inhibitor, GLYRA1 agonistGeneral anestesiaSmall Molecule1972Baxter
EslicarbazepineAptiom, Zebinix, ExaliefNav inhibitorPartial seizuresSmall molecule2009 EMA 2013 FDABial
EstazolamProsom, Eurodin, NuctalonGABAA potentiatorSevere InsomniaSmall molecule1990Abbott
EszopicloneLunestaGABA-A potentiatorInsomniaSmall molecule2004Sunovion
EthosuximideZarontinCav3.1 inhibitorAbsence seizuresSmall molecule1960Parke Davis
EtidocaineDuranestNav inhibitorLocal anesthesiaSmall molecule1976 FDA
FelbamateFelbatolGluN antagonistEpilepsy, Lennox-Gastaut syndromeSmall molecule1993 FDA
FelodipinePlendilCav1.x blocker, Cav3.x blockerHypertension, Angina pectoris prophylaxisSmall molecule1991AstraZeneca
FlecainideTambocorNav1.4 and Nav1.5 blockerAtrial fibrillation, atrial flutter, life-threatening ventricular tachycardiaSmall molecule1985
FlumazenilAnexate, RomaziconGABA-A antagonistBenzodiazepine induced sedation or toxicitySmall molecule1991 FDAHoffman La Roche
FlunarizineSibeliumCav3.x inhibitorMigraine, epilepsy, vertigoSmall molecule1968Jansen Pharmaceutica
FlunitrazepamHypnodorm GABA-A potentiatorSevere insomnia, anxietySmall Molecule1976
FlupirtineKatadolon Kv7.2-Kv7.5 activatorAcute and chronic painSmall molecule1984Asta-Medica
FlurazepamDalmadorm, DalmaneGABAA activatorInsomniaSmall molecule1970
FluspirileneRedeptin, ImapCav inhibitorSchizophreniaSmall molecule1963Jansen Pharmaceutica
FosphenytoinCerebyxNav1.5 blockerEpilepsySmall molecule1996Parke-Davis
FunapideTV-45070, XEN402Nav1.7 and Nav1.8 blockerChronic painSmall MoleculeXenon Pharmaceuticals
GabapentinNeurontinCav alpha-2/delta inhibitor, GluN inhibitorPostherpetic neuralgia, partial seizures Small molecule1993Pfizer
GlibenclamideDiabeta, GlyburideKir6.2 inhibitorDiabetes mellitus type 2Small molecule1984Sanofi Aventis
GlibornurideGlutrilKir6.2 inhibitorDiabetes mellitus type 2Small molecule1969/
GliclazideDiamicronKir6.2 inhibitorDiabetes mellitus type 2Small molecule1972
GlimepirideAmarylKir6.2 inhibitorDiabetes mellitus type 2Small molecule1995Sanofi Aventis
GlipizideGlucotrolKir6.2 inhibitorDiabetes mellitus type 2Small molecule1984Pfizer
GliquidoneGlurenormKir6.2 blockerDiabetes mellitus type 2Small Molecule
GlisoxepideKir6.x inhibitorDiabetes mellitus type 2Small molecule
GlyclopyramideDeamelinKir6.x inhibitorDiabetes mellitus type 2Small molecule1965
GlymidineGlycanol Kir inhibitorDiabetes mellitus type 2Small Molecule
GranisetronKytril5HT3A antagonist Therapy-induced nausea and vomitingSmall molecule1993 FDA
HalothaneGABA-A agonist, GluA1 inhibitor, GLYRA1 agonistGeneral anesthesiaSmall Molecule1958 FDA
HexylcaineCyclaineNav blockerLocal anesthesiaSmall MoleculeMerck
IbutilideCorvertKv11.1 blockerAtrial fibrillation, atrial flutterSmall Molecule1995
IsofluraneIsorane, AerraneGABA-A agonist, GluA1 inhibitor, GLYRA1 agonistGeneral anestesiaSmall Molecule1979Baxter
IsradipineDynaCirc, Prescal, Clivoten, Esradin, Lomir Cav1.x blockerHypertensionSmall molecule1989Sandoz (now division of Novartis)
IvabradineCorlanor, CorlentorHCN inhibitorChronic heart failure, angina pectorisSmall molecule2005 EMA 2015 FDAServier, Amgen
IvacaftorKalydecoCFTR potentiatorCystic fibrosisSmall molecule2012Vertex Pharmaceuticals
KetamineKetalarGluN antagonistGeneral and local anaesthesiaSmall molecule1970 FDA
KetazolamLoftran, Anseren GABA-A potentiatorAnxietySmall Molecule
LacidipineLacipil, MotensCav1.x blockerHypertensionSmall Molecule
LacosamideVimpatNav inhibitorPartial epilepsySmall molecule2008 FDA 2008 EMAUCB
LamotrigineLamictalNav inhibitorTonic-clonic seizures, epilepsy, Lennox-Gastaut syndrome Small molecule1994GSK
LeconotideCav2.2 blockerPainPeptide
LercanidipineZanidipCav1.x inhibitorHypertensionSmall molecule1997
LevamlodipineAsomex, Espin Cav1.x blockerHypertension, anginaSmall Molecule
LevobupivacaineChirocaineNav inhibitorLocal anesthesiaSmall molecule1999 FDAPurdue pharma
Levomenthol MentholTRPM8 agonistMinor irritation, pain, sore mouth, sore throat, itching, local anesthesiaSmall Molecule
LidocaineXylocaineNav blockerLocal anaesthesia, neuralgia, itching, pediculosis, ventricular arrhythmiaSmall molecule1948Fresenius Kabi
LorazepamAtivanGABAA activatorAnxiety, Myoclonic seizure, Atonic seizure, Status epilepticusSmall molecule1977 FDAWyeth Pharmaceuticals
LormetazepamGABA-A potentiatorShort-term insomniaSmall Molecule
LubiprostoneAmitizaCLC-2 activatorChronic idiopathic constipationSmall Molecule2006Sucampo Pharmaceuticals
LumacaftorOrkambi (a combination of ivacaftor and lumacaftor)CFTR modulatorCystic fibrosisSmall molecule2015Vertex Pharmaceuticals
ManidipineCalslot, ManyperCav1.x and Cav3.x blockerHypertensionSmall Molecule
MavatrepTRPV1 antagonistPainSmall MoleculeJanssen
MemantineAxura, NamendaGluN antagonistModerate to severe Alzheimer's type dementiaSmall molecule2003Forest labs
MepivacaineCarbocaineNav inhibitorLocal anesthesiaSmall molecule1960 FDAHospira, Inc., Pfizer
MethoxyfluranePenthroxGABA-A activator, GluA1 inhibitor, GLYRA1 agonistGeneral anestesiaSmall MoleculeAbbott
MethsuximidePetinutinCav3.x blockerAbsence seizures, epilepsy Small Molecule1957Parke Davis
MexiletineMexitilNav inhibitorVentricular arrhythmiaSmall molecule1985
MidazolamBuccolam, VersedGABA-A activatorAnxiety, Anesthesia, Status epilepticusSmall molecule1985
MinoxidilLonitenKir6.2 activatorHypertension, alopecia Small molecule1979 FDA
MirogabalinTarligeCav ?2? modulatorPeripheral neuropathic painDaiichi Sankyo
NateglinideStarlixKir6.2 blockerDiabetes mellitus type 2Small molecule2000 FDANovartis
NicardipineCardeneCav1.x inhibitorHypertension, angina pectorisSmall molecule1988
NicorandilIkorel, DancorKir6.2 activatorAngina pectorisSmall molecule1984
NicotineNicorette, NicotrolChrn agonistSmoking cessation, nicotine dependence Small molecule
NifedipineAdalat, Procardia, Afeditab, Nifediac Cav1.x blockerHypertension, vasospastic angina, premature laborSmall molecule1981Pfizer
NilvadipineEscor, Escor forte, Naftdil, Nilvadipine, Nivadil, Towajilcalcium channel blockerhypertension, vasospastic angina, chronic stable anginaSmall MoleculeAstellas Pharma, Archer Pharmaceuticals
NimodipineNimotop, NymalizeCav1.x blockerSubarachnoid hemorrhage, hypertensionSmall molecule1988
NisoldipineSularCav1.x blockerHypertensionSmall Molecule1995Shionogi
NitrazepamMogadon, Alodorm, NitrazadonGABA-A potentiatorInsomniaSmall molecule1965
NitrendipineBaypress, Nidrel Cav1.x blockerHypertensionSmall Molecule1985
OndansetronZophren5HT3A antagonist Therapy-induced nausea and vomitingSmall molecule1991 FDAGSK
OxazepamNovoxapam, Alepam GABA-A potentiatorAnxiety, alcohol withdrawal deliriumSmall molecule1965
OxcarbazepineTrileptalNav1.5 blockerEpilepsySmall molecule1990
OxybuprocaineNovesine, NovesinNav inhibitorLocal anesthesia Small Molecule
PalonosetronAloxi5HT3A antagonistChemotherapy-induced nausea and vomitingSmall molecule2003 FDA 2009 EMAHelsinn Healthcare
PentoliniumNACHR antagonistHypertensionSmall MoleculeWyeth Pharmaceuticals
PerampanelFycompaGluA1-4 antagonistPartial seizuresSmall molecule2012 FDAEisai
PermethrinElimiteSodium channel (Sarcoptes scabiei) inhibitorInfestation by Sarcoptes scabiei, PediculosisSmall Molecule1986
PhenobarbitalLuminalGABA-A potentiatorEpilepsy, Lennox-Gastaut syndrome, migraineSmall molecule1912
PhensuximideMilontinCav inhibitor Nav inhibitorEpilepsy, absence seizuresSmall moleculeFDAParke Davis
PhenytoinDilantinNav inhibitorEpilepsySmall molecule1953Parke Davis
PinacidilPindac Kir6.2 activatorHypertensionSmall molecule1989 FDALeo Pharma
PinaveriumDicetelCav1.x antagonistIrritable bowel syndrome Small molecule1975 Solvay Pharmaceuticals
PregabalinLyricaCav alpha-2/delta modulatorDiabetic peripheral neuropathy, postherpetic neuralgiaSmall molecule2004
PrilocaineCitanest, Xylonest Nav inhibitorLocal anaesthesia, premature ejaculationSmall molecule1965
PrimidoneMysolineGABA-A positive modulatorEpilepsy, Lennox-Gastaut syndromeSmall molecule1954 FDAValeant
ProcainamidePronestyl, Procan-SR, ProcanbidNav inhibitor, Kv11.1 inhibitorLife-threatening ventricular tachycardiaSmall molecule1950Bristol-Meyers Squibb
ProcaineNovocaineNav1.8 blockerLocal anesthesia Small Molecule1954
PropafenoneRythmolNav1.5 blockerAtrial fibrillation, atrial flutter, life-threatening ventricular tachycardiaSmall molecule1989GSK
ProparacaineAlcaine, OphtheticNav blockerLocal anesthesiaSmall Molecule1953
PropofolDiprivanGABA-A potentiatorGeneral anaesthesiaSmall molecule1989 FDAFresenius Kabi
QuazepamDoral, DormalinGABA-A potentiatorInsomniaSmall molecule1985Sciencure Pharma
QuinidineCardioquin, QuinidexNav inhibitorAtrial fibrillation, malaria, life-threatening ventricular tachycardiaSmall Molecule1950Lilly
RanolazineRanexaNav inhibitorAngina pectorisSmall molecule2006Gilead
RepaglinideGluconorm, Prandin, Novonorm Kir6.2 blockerDiabetes mellitus type 2Small molecule1997Novo Nordisk
RiluzoleRilutekKCa2.3 activator, Nav1.5 inhibitor Amyotrophic lateral sclerosisSmall molecule1995 FDA
RocuroniumZemuron, EsmeronChrn a1b1d/g antagonistGeneral anaesthesia, muscle relaxationSmall molecule1994 FDA
RopivacaineNaropinNav blockerLocal anaesthesiaSmall molecule1996Fresenius Kabi
RufinamideBanzelNav modulatorLennox-Gastaut syndromeSmall Molecule2007 EMA 2008 FDANovartis
SafinamideXadagoNav and Cav inhibitorParkinson’s diseaseSmall Molecule2015 EMA 2017 FDANewron Pharmaceuticals
SevofluraneUltane, SojournGABA-A activator, GLYRA1 agonistGeneral anestesiaSmall Molecule1995Abbvie
SotalolBiosotal, SotalexKv11.1 blockerAtrial fibrillation, life-threatening ventricular tachycardia Small molecule1974
StiripentolDiacomitGABA-A positive modulatorMyoclonic seizuresSmall Molecule2007 EMA 2018 FDABiocodex
SuccinylcholineAnectineChrn a1b1deg agonistGeneral anaesthesia, muscle relaxationSmall molecule1952 FDASandoz
TemazepamRestorilGABA-A potentiatorInsomniaSmall molecule1981Mallinckrodt Pharmaceuticals
TetracainePontocaineNav inhibitorLocal anesthesiaSmall molecule1941
TezacaftorCFTR activatorCystic fibrosisSmall Molecule2018Vertex Pharmaceuticals
TocainideTonocard Nav blockerVentricular arrhythmiaSmall Molecule1984
TolazamideTolinase, Norglycin Kir6.2 inhibitorDiabetes mellitus type 2Small molecule1966
TolbutamideKir6.2 inhibitorDiabetes mellitus type 2Small molecule1961 FDA
TopiramateTopamaxGABA-A positive modulator, Nav blocker, GluA antagonistEpilepsy, migraine, Lennox-Gastaut syndrome Small Molecule
TriamtereneDyreniumENaC inhibitorHypertensive disorder, edemaSmall molecule1964Smith Kline & French
TriazolamHalcionGABA-A positive modulator InsomniaSmall molecule 1982 (withdrawn in the UK)Pharmacia and Upjohn
TrimebutineTrimebutineCav1.x inhibitor, KCa inhibitorIrritable bowel syndrome, postoperative paralytic ileusSmall Molecule
TrimethadioneTridioneCav3.1 inhibitorAbsence seizures, epilepsy Small Molecule1946Abbvie
UnoprostoneResculaBK and CLC-2 activatorOcular hypertension, open-angle glaucomaSmall Molecule2000 FDA (discontinued in the US)Sucampo Pharmaceuticals
Valproic acidConvulex, Depakene, ValcoteNav inhibitor, GABAA modulator Epilepsy, absence seizures, bipolar disorder, migraine Small molecule
VareniclineChantix, ChampixChrn a4b2 agonistSmoking cessationSmall molecule2006 FDAPfizer
VerapamilCalan, VerelanCav1.x inhibitorHypertension, angina, supraventricular tachycardia, migraine, cluster headacheSmall molecule1981
VernakalantBrinavessNav1.5, Kv1.5, Kv4.3 blockerAtrial fibrillationSmall Molecule2010, EMACardiome Pharma
XEP-018NaV1.4 blockerSkin wrinklesSynthetic peptideActiven
ZaleplonSonataGABA-A agonistInsomniaSmall Molecule1999Meda Ab, Pfizer
ZiconotidePrialtCav2.2 blockerSevere and chronic painSynthetic peptide2004Elan Pharmaceuticals
ZolpidemAmbienGABA-A agonistInsomniaSmall molecule1992Sanofi Aventis
ZonisamideZonegranNav blocker, Cav3.x blockerPartial epilepsySmall Molecule2000Eisai
ZopicloneImovane, ZimovaneGABA-A potentiatorInsomniaSmall molecule1986Rhône-Poulenc
ZucapsaicinZuactaTRPV1 agonistSevere pain associated with osteoarthritis of the knee, neuropathic painSmall MoleculeSanofi Aventis

Ion channel drug candidates in preclinical development and clinical trials

NameOther namesMechanism of actionIndicationTypeStatusCompany
ACP-044CT-044
Reactive species decomposition accelerant preventing hyper-activation of TRPA1
Acute post-operative, chronic neuropathic pain
Phase I
ACADIA Pharmaceuticals
AM-6120, AM-8145, AM-0422Nav1.7 inhibitorPeptideDiscoveryAmgen
AP30663KCa inhibitorAtrial fibrillationPhase I/IIAcesion Pharma
AP-325
Positive allosteric modulator of GABA-A
Neuropathic pain
Small Molecule
Phase IIa
Algiax Pharmaceuticals
ARO-ENaC
ENAC downregulation
Cystic fibrosis
RNAi therapeutic
Phase I/IIa
Arrowhead Pharmaceuticals
ASN008Na+ channel blockerPruritus, atopic dermatitis, painPhase IIaAsana BioSciences
ASN009P2X3 antagonistCoughPreclinicalAsana BioSciences
ASP-0819KCa3.1 activatorFibromyalgiaPhase IIAstellas Pharma
AUT00201Modulator of Kv3 channelsSchizophrenia, hearing disordersPhase IAutifony Therapeutics
AuxoraCM4620-IECRAC inhibitorSevere COVID-19 pneumonia, Viral pneumonia, Acute pancreatitisSmall MoleculePhase IICalciMedica
AV-1014-Cl-KYN
NMDAR antagonist
CNS disorders
Preclinical
VistaGen Therapeutics
AXS-05
NMDAR antagonist
Major Depressive Disorder, Alzheimer’s Disease agitation, and Smoking Cessation
Small Molecule
Phase III
Axsome Therapeutics
BAY-1817080P2X3 inhibitorEndometriosis and persistent
chronic cough
Phase IBayer
BAY-1902607P2X3 inhibitorPersistent chronic coughPhase IIBayer
BAY-2253651TASK inhibitorObstructive sleep apnoeaPhase IIBayer
BIIB093SUR1-TRPM4 blockerBrain ContusionSmall MoleculePhase IIBiogen
BIIB095Nav1.7 inhibitorNeuropathic painSmall MoleculePhase IBiogen
BIIB104PF-04958242AMPAR activatorCognitive impairment associated
with schizophrenia
Phase IIaBiogen
BIL010tnfP2X7Skin cancerAntibodyPhase IBiosceptre
BIL06vnfP2X7Skin cancerPeptide vaccinePhase IBiosceptre
BLU-5937P2X3 antagonistRefractory chronic coughPhase IIbBELLUS Health
BNC-210alpha7 nAChRs antagonistAgitation, post-traumatic stress disorder, generalised anxiety disorder Phase IIBionomics
CAD-1883KCa activatorAtaxia or essential tremorsPhase I/IICadent Therapeutics
CAD-9303
NMDAR positive allosteric modulator
Schizophrenia
Phase I
Cadent Therapeutics
CC 8464ASP 1807Nav1.7 antagonistNeuropathic and inflammatory painSmall MoleculePhase IChromocell/Astellas Pharma
CVL-865Positive allosteric modulator of alpha-2/3/5 subunits of the GABA-ADrug-resistant focal onset epilepsyPhase I/IICerevel Therapeutics
CVL-865Positive allosteric modulator of alpha-2/3/5 subunits of the GABA-AAcute anxietyPhase ICerevel Therapeutics
CX-8998 T-type calcium channel modulatorAbsence epilepsy, essential tremorPhase IICavion 
DalazatideShK-186Kv1.3 inhibitorMyositis, Psoriasis Synthetic peptidePhase IIKv1.3 Therapeutics
DSP-2230NaV1.7 and NaV1.8 inhibitorNeuropathic painSmall MoleculePhase IAlphaNavi Pharma
DSP-3905NaV1.7 inhibitorNeuropathic painSmall MoleculePhase ISunovion Pharmaceuticals
ENX-101sub-type selective GABA-A modulatorDiseases of the nervous systemPreclinicalEngrail Therapeutics
ETD001ENaC blockerRespiratory diseasesPreclinicalEnterprise Therapeutics
ETD002TMEM16A potentiatorCystic fibrosisPhase IEnterprise Therapeutics
EvenamideNav blockerSchizophreniaPhase IINewron Pharmaceuticals
Evt201GABAA receptor PAMInsomniaPhase IIEvotec
FX301FunapideNav1.7 inhibitorAcute post-operative painPreclinicalFlexion
GalicaftorABBV-2222CFTRCystic fibrosisPhase IIAbbVie
GFB-887TRPC5 inhibitorFocal segmental glomerulosclerosis, diabetic nephropathyPhase I/IIGoldfinch Bio
Granexin gelalphaCT1, a peptide mimetic of the Cx43 carboxyl terminusCutaneous
radiation injury, Diabetic foot and venous leg ulcers
Synthetic peptidePhase IIIFirstString Research
GRC 17536TRPA1 antagonistPainful diabetic neuropathyPhase IIGlenmark 
GSK-2798745TRPV4 inhibitorHeart failurePhase IIGlaxoSmithKline
HalneuronTetrodotoxinNav blockerSevere neuropathic pain, cancer related painSmall MoleculePhase IIIWex Pharmaceuticals
HBI-3000Multi-channel inhibitorAtrial fibrillationPhase IHUYA Bioscience International
JNJ-55308942P2X7 inhibitorNeuroinflammation and anhedoniaPhase IJohnson & Johnson
KB-3061Kv7 modulatorKCNQ2 epileptic encephalopathyPreclinicalKnopp Biosciences
KCP-506alpha9alpha10 nAChR antagonistChronic painPhase IKineta 
Kv7 modulatorKv7 modulatorNeuropathic pain, hearing disorders, ALSDiscoveryKnopp Biosciences
LUNAR-CF
CFTR upregulation
Cystic fibrosis
mRNA therapeutic
Preclinical
Arcturus Therapeutics
MIJ821
CAD-9271
NMDAR negative allosteric modulator
Depression
Phase II
Novartis
MK-7264GefapixantP2X3 antagonistChronic coughSmall MoleculePhase IIIMerck, Roche
MRT5005
CFTR upregulation
Cystic fibrosis
mRNA therapeutic
Phase I/II
Translate Bio
NBI-1065845TAK-653AMPAR activatorDepressionPhase IINeurocrine Biosciences, Takeda
NBI-827104ACT-709478T-type calcium channel blockerPediatric epilepsyPhase I/IINeurocrine Biosciences, Idorsia
NBI-921352XEN901Nav1.6 inhibitorEpilepsySmall MoleculePhase I/IINeurocrine Biosciences, Xenon
NMD670Skeletal muscle specific inhibitor of ClC-1Myasthenia gravisSmall MoleculePhase I/IIaNMD Pharma
NOC-100
NTX-1175
Charged sodium channel blocker
Chronic and acute cough
Small Molecule
Phase I
Nocion Therapeutics
OV101GaboxadolGABA-A agonistFragile X syndrome, Angelman syndromeSmall MoleculePhase II-IIIOvid Therapeutics
P-1037VX-371ENaC inhibitorPulmonary diseasesPhase IIParion Sciences, Vertex Pharmaceuticals 
P-1055VX-551ENaC inhibitorPulmonary diseasesPreclinicalParion Sciences, Vertex Pharmaceuticals 
P-321ENaC inhibitorDry eye diseasePhase IIParion Sciences, Takeda
P2X4 inhibitorP2X4 inhibitorEndometriosisPhase IBayer
P2X7 MABP2X7 monoclonal antibodyAutoimmune disordersAntibodyPreclinicalIntegral Molecular
PRAX-114GABA-A positive allosteric modulatorMajor depressive disorder, perimenopausal depressionSmall MoleculePhase IIPraxis Precision Medicines
PRAX-944T-type calcium channel blockerEssential tremorSmall MoleculePhase IIPraxis Precision Medicines
PRAX-562Pediatric epilepsy, adult cephalgiaSmall MoleculePhase IPraxis Precision Medicines
PRAX-020/021Genetic epilepsiesPreclinicalPraxis Precision Medicines
PRAX-222Genetic epilepsiesPreclinicalPraxis Precision Medicines
RalfinamideNav blocker, Cav2.2 blockerNeuropathic painPhase IINewron Pharmaceuticals
ResiniferatoxinTRPV1 agonistCancer painSmall MoleculePhase ISorrento Therapeutics
RG-7816GABA-A receptor alpha5
subunit-targeting NAM
Autism spectrum disorderPhase IRoche
S-600918P2X3 antagonistRefractory chronic coughPhase IIbShionogi
SAN711GABAA alpha3 modulatorNeuropathic pain disordersPreclinicalSaniona
SAN903KCa3.1 inhibitorRare inflammatory/fibrotic diseases, hereditary xerocytosis PreclinicalSaniona
SAGE-217Zuranolon, S-812217GABA-A positive allosteric modulatorMajor depressionSmall MoleculePhase IISage Therapeutics, Shionogi
SAGE-324GABA-A receptor PAMEssential tremor and Parkinson
disease
Phase ISage Therapeutics
SAGE-689GABA-A modulatorGABA hypofunctionPreclinicalSage Therapeutics
SAGE-718NMDAR activatorNMDAR hypofunctionPhase ISage Therapeutics
SAGE-904NMDAR modulatorNMDAR hypofunctionPreclinicalSage Therapeutics
SenicapocKCa3.1 inhibitorHereditary xerocytosis and
Alzheimer disease
Phase ISpringWorks Therapeutics/
University of California, Davis
SOR-C13TRPV6 inhibitorSolid tumor cancerSynthetic peptidePhase IbSoricimed Biopharma
ST-2427Nav1.7 inhibitorPost-operative painSmall MoleculeINDSiteOne Therapeutics
STK-001Upregulates Nav1.1 protein expressionDravet syndromeAntisense oligonucleotidePhase I/IIaStoke Therapeutics
TRPC4 and TRPC5 inhibitorTRPC4 and TRPC5 inhibitorAnxiety disorder and depressionPhase IHydra/Boehringer Ingelheim
VX-150Nav1.8 inhibitorAcute and neuropathic painSmall MoleculePhase IIVertex Pharmaceuticals 
XEN007FlunarizineCav2.1 modulatorMigraine and other neurological disordersSmall MoleculePhase IXenon
XEN1101Kv7 modulatorEpilepsyPhase IIXenon
XEN496Retigabine Kv7 modulatorKCNQ2 and pediatric epilepsyPhase IIXenon
XEN-D0501TRPV1 antagonist Type 2 diabetesPhase IIPila Pharma

Ion channel drugs on the WHO List of Essential Medicines

NameMechanism of actionIndicationYear of ApprovalType of medicineSubtype of medicineNote
AmilorideENaC inhibitorHypertensive disorder, edema, hypokalemia1981Diuretics
AmiodaroneKv11.1 blockerVentricular fibrillation, life-threatening ventricular tachycardia 1961Cardiovascular medicinesAntiarrhythmic medicinesComplementary List
AmlodipineCav1.x inhibitorHypertension, vasospastic angina, angina pectoris 1992Cardiovascular medicinesAntihypertensive medicines
AtracuriumChrn abd antagonistGeneral anaesthesia, muscle relaxation1983 FDAMucsle relaxants (peripherally acting) and cholinesterase inhibitors
BupivacaineNav inhibitorLocal anesthesia1972 FDAAnaesthetics, preoperative medicines and medical gasesLocal anaesthetics
CarbamazepineNav1.5 blockerEpilepsy, Lennox-Gastaut syndrome, bipolar disorder1968Anticonvulsants/Antiepileptics

Medicines for mental and behavioural disorders
Medicines used in bipolar disorders
DiazepamGABA-A potentiatorAnxiety, alcohol withdrawal syndrome, spasticity, epilepsy1963 FDAMedicines for pain and paliative care

Anticonvulsants/Antiepileptics

Medicines for mental and behavioural disorders
Medicines for other common symptoms in palliative care

Medicines for anxiety disorders
DiazoxideKir6.2 activatorHypertensive emergencies, hyperinsulinism1973Medicines for endocrine disordersMedicines for hypoglycaemiaComplementary List
EthosuximideCav3.1 inhibitorAbsence seizures1960Anticonvulsants/AntiepilepticsComplementary List
GliclazideKir6.2 inhibitorDiabetes mellitus type 21972Medicines for endocrine disordersMedicines for diabetesOral hypoglycaemic agents
HalothaneGABA-A agonist, GluA1 inhibitor, GLYRA1 agonistGeneral anesthesia1958 FDAAnaesthetics, preoperative medicines and medical gasesGeneral anaesthetics and oxygenInhalational medicines
IsofluraneGABA-A agonist, GluA1 inhibitor, GLYRA1 agonistGeneral anestesia1979Anaesthetics, preoperative medicines and medical gasesGeneral anaesthetics and oxygenInhalational medicines
KetamineGluN antagonistGeneral and local anaesthesia1970 FDAAnaesthetics, preoperative medicines and medical gasesGeneral anaesthetics and oxygenInjectable medicines
LamotrigineNav inhibitorTonic-clonic seizures, epilepsy, Lennox-Gastaut syndrome 1994Anticonvulsants/Antiepileptics
LidocaineNav blockerLocal anaesthesia, neuralgia, itching, pediculosis, ventricular arrhythmia1948Anaesthetics, preoperative medicines and medical gases

Cardiovascular medicines
Local anaesthetics

Antiarrhythmic medicines
LorazepamGABAA activatorAnxiety, Myoclonic seizure, Atonic seizure, Status epilepticus1977Anticonvulsants/Antiepileptics
MidazolamGABA-A activatorAnxiety, Anesthesia, Status epilepticus1985Anaesthetics, preoperative medicines and medical gases

Medicines for pain and paliative care

Anticonvulsants/Antiepileptics
Preoperative medication and sedation for short-term procedures

Medicines for other common symptoms in palliative care
NicotineChrn agonistSmoking cessation, nicotine dependence Medicines for mental and behavioural disordersMedicines for disorders due to psychoactive substance useNicotine replacement therapy
NifedipineCav1.x blockerHypertension, vasospastic angina, premature labor1981Medicines for reproductive health and perinatal careAntioxytocics (tocolytics)
Ondansetron5HT3A antagonist Therapy-induced nausea and vomiting1991 FDAMedicines for pain and paliative care

Gastrointestinal medicines
Medicines for other common symptoms in palliative care

Antiemetic medicines
PermethrinSodium channel (Sarcoptes scabiei) inhibitorInfestation by Sarcoptes scabiei, Pediculosis1986Dermatological medicines (topical)Scabicides and pediculicides
PhenobarbitalGABA-A potentiatorEpilepsy, Lennox-Gastaut syndrome, migraine1912Anticonvulsants/Antiepileptics
PhenytoinNav inhibitorEpilepsy1953Anticonvulsants/Antiepileptics
PropofolGABA-A potentiatorGeneral anaesthesia1989 FDAAnaesthetics, preoperative medicines and medical gasesGeneral anaesthetics and oxygenInjectable medicines
TetracaineNav inhibitorLocal anesthesia1941Ophtalmological preparationsLocal anaesthetics
Valproic acidNav inhibitor, GABAA modulator Epilepsy, absence seizures, bipolar disorder, migraine Anticonvulsants/Antiepileptics

Medicines for mental and behavioural disorders
Medicines used in bipolar disorders
VerapamilCav1.x inhibitorHypertension, angina, supraventricular tachycardia, migraine, cluster headache1981Cardiovascular medicinesAntianginal medicines
Antiarrhythmic medicines

Withdrawn/Discontinued ion channel drugs

NameBrand namesMechanism of actionIndicationTypeStatusYear of Approval/WithdrawalCompanyNotes
AcetohexamideDymelorKir6.2 inhibitorDiabetes mellitus type 2 Small moleculeWithdrawn in the US1964/Lilly
AlpidemGABA-A agonistAnxietySmall moleculeWithdrawn1991 (France)/1994Synthélabo
BepridilVascorCav1.x blockerHypertension, chronic stable anginaSmall moleculeWithdrawn1990/2004
ButambenAlvogil Cav inhibitorSkin irritation, chronic painSmall moleculeWithdrawn
CronidipineCav blockerHypertensionSmall moleculeDiscontinuedGroupe Fournier
EncainideEnkaidNav blockerVentricular premature beatsSmall moleculeWithdrawn/1991
GaboxadolGABA-A antagonistInsomniaSmall MoleculeDiscontinuedLundbeck and Merck
HalazepamPaxipam, Alapryl, PacinoneGABAA potentiatorAnxietySmall moleculeWithdrawn in the US1981/2009Schering-Plough
LindaneScabeneGABA-A (Sarcoptes scabiei) negative modulatorInfestation by Sarcoptes scabiei, PediculosisSmall moleculeWithdrawn1974/
LinopirdineKCNQ blockersAlzheimer's diseaseSmall moleculeDiscontinued
MephenytoinMesantoinNav blockerEpilepsySmall moleculeWithdrawn1946/Novartis
MibefradilPosicorCav1.x inhibitor, Cav3.x inhibitor Hypertension, angina Small moleculeWithdrawn1997/1998Roche
MoracizineEthmozineNav1.5 blockerVentricular arrhythmiaSmall moleculeWithdrawn1990 FDA/2007
PF-05089771Nav1.7 inhibitorPainful diabetic peripheral neuropathySmall MoleculeDiscontinued2015PfizerFailed phase II
RetigabineTrobalt, PotigaKv7.2-Kv7.5 activatorEpilepsySmall moleculeDiscontinued2011/2017GSK
RG-6029GDC-0310Nav1.7 inhibitorPainSmall MoleculeDiscontinued2018Roche/Genentech/Xenon
SenicapocKCa3.1 (Gardos channel) blockerHereditary xerocytosisSmall MoleculeSpringWorks TherapeuticsRepurposed
SenicapocKCa3.1 (Gardos channel) blockerSickle cell disease and asthmaSmall MoleculeDiscontinuedIcagen
TriazolamHalcionGABA-A positive modulatorInsomniaSmall moleculeWithdrawn in the UK1982/
UnoprostoneResculaBK and CLC-2 activatorOcular hypertension, open-angle glaucomaSmall MoleculeDiscontinued in the US2000 FDA/ 2015 Sucampo Pharmaceuticals
TV-45070Nav1.7 inhibitorPost-herpetic neuralgiaSmall MoleculeDiscontinued2017Teva/XenonFailed phase II
VixotrigineBIIB074Nav1.7 inhibitorPainful lumbosacral radiculopathy Small MoleculeDiscontinued2018BiogenFailed phase II
Z160MK-6721, NMED-160Cav2.2 antagonistChronic painSmall moleculeDiscontinuedNeuromed, Zalicus
ZoxazolamineZoxineKCa activatorSpasmSmall moleculeWithdrawn1955/1961
VX-128
NaV1.8 inhibitor
Pain
Small moleculeDiscontinued2018Vertex Pharmaceuticals
VX-961
NaV1.8 inhibitor
Pain
Small moleculeDiscontinued2020Vertex Pharmaceuticals