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

Ion channel drug candidates in preclinical development and clinical trials

Ion channel drugs on the WHO List of Essential Medicines 2019

Withdrawn/Discontinued ion channel drugs

Ion channel drugs on the market

Name	Brand names	Mechanism of action	Indication	Type	Year of Approval	Company
Amlodipine	Norvasc, Aforbes	Cav1.x inhibitor	Hypertension, vasospastic angina, angina pectoris	Small molecule	1992	Pfizer
Ajmaline		Nav1.5 inhibitor	Arrhythmia	Small Molecule
Alosetron	Lotronex	5HT3A antagonist	Irritable bowel syndrome with diarrhea	Small molecule	2002 FDA
Alprazolam	Xanax	GABA-A positive modulator	Anxiety	Small molecule	1981 FDA	Upjohn
Amantadine	Symadine, Osmolex	GluN inhibitor	Parkinson's disease	Small molecule
Amifampridine	Firdapse	Kv blocker	Lambert-Eaton myasthenic syndrome	Small molecule	2009	BioMarin
Amiloride	Midamor	ENaC inhibitor	Hypertensive disorder, edema, hypokalemia	Small molecule	1981
Amiodarone	Cordarone	Kv11.1 blocker	Ventricular fibrillation, life-threatening ventricular tachycardia	Small molecule	1961
Atracurium		Chrn abd antagonist	General anaesthesia, muscle relaxation	Small Molecule	1983 FDA
Azelnidipine	CalBlock	Cav1.x blocker	Hypertension	Small Molecule		Daiichi-Sankyo
Benzocaine	Anacaine, Dermoplast	Nav blocker	Local anesthesia	Small Molecule
Bioallethrin		Sodium channel (Pediculus humanus) modulator	Lice and scabies infestation	Small Molecule
Brexanolone	Zulresso	GABA-A positive modulator	Postpartum depression	Small Molecule	2019	Sage Therapeutics
Bupivacaine	Marcaine	Nav inhibitor	Local anesthesia	Small molecule	1972 FDA	Hospira
Butalbital	Sandoptal	GABA-A potentiator	Tension-type headache	Small Molecule	1976	Actavis Labs
Capsaicin	Zostrix, Qutenza	TRPV1 activator	Neuralgia, postherpetic neuralgia, backache, arthritic pain	Small molecule	2009 FDA	Acorda Therapeutics
Carbamazepine	Actebral, Tegretol	Nav1.5 blocker	Epilepsy, Lennox-Gastaut syndrome, bipolar disorder	Small molecule	1968	Novartis
Carbutamide	Glucidoral	Kir6.2 inhibitor	Diabetes mellitus type 2	Small molecule	1956	Servier
Chlordiazepoxide	Risolid	GABAA positive modulator	Anxiety, alcohol withdrawal syndrome	Small molecule	1960 FDA	Valeant
Chloroprocaine	Nesacaine	Nav1.8 inhibitor	Local anesthesia	Small Molecule
Chlorpropamide		Kir6.2 inhibitor	Diabetes mellitus type 2	Small molecule	1958	Pfizer
Chlorzoxazone	Parafon, Paraflex	KCa activator	Spasticity, muscle spasm with pain	Small molecule	1958	Janssen
Cilnidipine	Atelec, Cilogard	Cav1.x blocker, Cav2.2 blocker	Hypertension	Small Molecule	1995	Fuji Viscera, Ajinomoto
Cinchocaine	Dibucaine, Nupercainal	Nav blocker	Local anesthesia	Small Molecule
Cinnarizine	Stugeron, Cinazyn	Cav inhibitor	Vertigo, motion sickness, nausea	Small molecule	1955	Jansen Pharmaceutica
Cisatracurium	Nimbex	Chrn a1b1d inhibitor	General anaesthesia, muscle relaxation	Small molecule	1995 FDA
Clevidipine	Cleviprex	Cav1.x blocker	Hypertension	Small molecule	2008	The Medicines Company
Clobazam	Frisium, Urbanol, Onfi, Tapclob	GABAA partial agonist	Epilepsy, anxiety	Small molecule	2011	Lundbeck
Clonazepam	Clonapam, Rivotril	GABAA positive modulator	Myoclonic, atonic and absence seizures; Lennox-Gastaut syndrome	Small molecule	1975	Roche
Clorazepate	Tranxene	GABAA positive modulator	Anxiety, alcohol withdrawal syndrome, partial epilepsy	Small molecule	1972
Clotiazepam	Clozan	GABA-A potentiator	Anxiety disorders	Small Molecule
Crofelemer	Mytesi, Fulyzaq	CFTR inhibitor, ANO1 inhibitor	Non-infectious diarrhea	Small Molecule	2012	Salix Pharmaceuticals
Cyclandelate	Cyclospasmol	Cav alpha-2/delta-1 modulator	Arteriosclerosis, Raynaud's disease	Small Molecule
Dalfampridine	Ampyra, Fampyra	Kv blocker	Multiple sclerosis	Small molecule	2010	Acorda Therapeutics
Dantrolene	Dantrium	RyR1 inhibitor	Spasticity, malignant hyperthermia	Small molecule	1974	Par Pharmaceutical
Desflurane	Suprane	GABA-A agonist, GluA1 inhibitor, GLYRA1 agonist	General anestesia	Small Molecule	1992	Baxter
Dextromethorphan		GluN3A antagonist	Cough, rhinitis, sneezing	Small Molecule	1957	ANI Pharmaceuticals
Diazepam	Valium, Diastat	GABA-A potentiator	Anxiety, alcohol withdrawal syndrome, spasticity, epilepsy	Small molecule	1963 FDA	Roche
Diazoxide	Proglycem	Kir6.2 activator	Hypertensive emergencies, hyperinsulinism	Small molecule	1973
Diltiazem	Cardizem, Tiazac	Cav1.x inhibitor	Hypertension, angina pectoris	Small molecule	1982
Disopyramide	Norpace, Ritmodan, Dicorantil	Nav1.5 inhibitor	Ventricular arrhythmia	Small molecule	1977	G.D. Searle LLC
Dofetilide	Tikosyn	Kir2.2, Kv10.1, Kv11.1 inhibitor	Atrial fibrillation, atrial flutter	Small molecule	1999	Pfizer
Dronedarone	Multaq	Multichannel blocker	Atrial fibrillation	Small molecule	2009 FDA	Sanofi-Aventis
Efonidipine	Landel	Cav1.x inhibitor, Cav3.x inhibitor	Hypertension	Small molecule	1995
Enflurane	Ethrane, Alyrane	GABA-A agonist, GluA1 inhibitor, GLYRA1 agonist	General anestesia	Small Molecule	1972	Baxter
Eslicarbazepine	Aptiom, Zebinix, Exalief	Nav inhibitor	Partial seizures	Small molecule	2009 EMA 2013 FDA	Bial
Estazolam	Prosom, Eurodin, Nuctalon	GABAA potentiator	Severe Insomnia	Small molecule	1990	Abbott
Eszopiclone	Lunesta	GABA-A potentiator	Insomnia	Small molecule	2004	Sunovion
Ethosuximide	Zarontin	Cav3.1 inhibitor	Absence seizures	Small molecule	1960	Parke Davis
Etidocaine	Duranest	Nav inhibitor	Local anesthesia	Small molecule	1976 FDA
Felbamate	Felbatol	GluN antagonist	Epilepsy, Lennox-Gastaut syndrome	Small molecule	1993 FDA
Felodipine	Plendil	Cav1.x blocker, Cav3.x blocker	Hypertension, Angina pectoris prophylaxis	Small molecule	1991	AstraZeneca
Flecainide	Tambocor	Nav1.4 and Nav1.5 blocker	Atrial fibrillation, atrial flutter, life-threatening ventricular tachycardia	Small molecule	1985
Flumazenil	Anexate, Romazicon	GABA-A antagonist	Benzodiazepine induced sedation or toxicity	Small molecule	1991 FDA	Hoffman La Roche
Flunarizine	Sibelium	Cav3.x inhibitor	Migraine, epilepsy, vertigo	Small molecule	1968	Jansen Pharmaceutica
Flunitrazepam	Hypnodorm	GABA-A potentiator	Severe insomnia, anxiety	Small Molecule	1976
Flupirtine	Katadolon	Kv7.2-Kv7.5 activator	Acute and chronic pain	Small molecule	1984	Asta-Medica
Flurazepam	Dalmadorm, Dalmane	GABAA activator	Insomnia	Small molecule	1970
Fluspirilene	Redeptin, Imap	Cav inhibitor	Schizophrenia	Small molecule	1963	Jansen Pharmaceutica
Fosphenytoin	Cerebyx	Nav1.5 blocker	Epilepsy	Small molecule	1996	Parke-Davis
Funapide	TV-45070, XEN402	Nav1.7 and Nav1.8 blocker	Chronic pain	Small Molecule		Xenon Pharmaceuticals
Gabapentin	Neurontin	Cav alpha-2/delta inhibitor, GluN inhibitor	Postherpetic neuralgia, partial seizures	Small molecule	1993	Pfizer
Glibenclamide	Diabeta, Glyburide	Kir6.2 inhibitor	Diabetes mellitus type 2	Small molecule	1984	Sanofi Aventis
Glibornuride	Glutril	Kir6.2 inhibitor	Diabetes mellitus type 2	Small molecule	1969/
Gliclazide	Diamicron	Kir6.2 inhibitor	Diabetes mellitus type 2	Small molecule	1972
Glimepiride	Amaryl	Kir6.2 inhibitor	Diabetes mellitus type 2	Small molecule	1995	Sanofi Aventis
Glipizide	Glucotrol	Kir6.2 inhibitor	Diabetes mellitus type 2	Small molecule	1984	Pfizer
Gliquidone	Glurenorm	Kir6.2 blocker	Diabetes mellitus type 2	Small Molecule
Glisoxepide		Kir6.x inhibitor	Diabetes mellitus type 2	Small molecule
Glyclopyramide	Deamelin	Kir6.x inhibitor	Diabetes mellitus type 2	Small molecule	1965
Glymidine	Glycanol	Kir inhibitor	Diabetes mellitus type 2	Small Molecule
Granisetron	Kytril	5HT3A antagonist	Therapy-induced nausea and vomiting	Small molecule	1993 FDA
Halothane		GABA-A agonist, GluA1 inhibitor, GLYRA1 agonist	General anesthesia	Small Molecule	1958 FDA
Hexylcaine	Cyclaine	Nav blocker	Local anesthesia	Small Molecule		Merck
Ibutilide	Corvert	Kv11.1 blocker	Atrial fibrillation, atrial flutter	Small Molecule	1995
Isoflurane	Isorane, Aerrane	GABA-A agonist, GluA1 inhibitor, GLYRA1 agonist	General anestesia	Small Molecule	1979	Baxter
Isradipine	DynaCirc, Prescal, Clivoten, Esradin, Lomir	Cav1.x blocker	Hypertension	Small molecule	1989	Sandoz (now division of Novartis)
Ivabradine	Corlanor, Corlentor	HCN inhibitor	Chronic heart failure, angina pectoris	Small molecule	2005 EMA 2015 FDA	Servier, Amgen
Ivacaftor	Kalydeco	CFTR potentiator	Cystic fibrosis	Small molecule	2012	Vertex Pharmaceuticals
Ketamine	Ketalar	GluN antagonist	General and local anaesthesia	Small molecule	1970 FDA
Ketazolam	Loftran, Anseren	GABA-A potentiator	Anxiety	Small Molecule
Lacidipine	Lacipil, Motens	Cav1.x blocker	Hypertension	Small Molecule
Lacosamide	Vimpat	Nav inhibitor	Partial epilepsy	Small molecule	2008 FDA 2008 EMA	UCB
Lamotrigine	Lamictal	Nav inhibitor	Tonic-clonic seizures, epilepsy, Lennox-Gastaut syndrome	Small molecule	1994	GSK
Leconotide		Cav2.2 blocker	Pain	Peptide
Lercanidipine	Zanidip	Cav1.x inhibitor	Hypertension	Small molecule	1997
Levamlodipine	Asomex, Espin	Cav1.x blocker	Hypertension, angina	Small Molecule
Levobupivacaine	Chirocaine	Nav inhibitor	Local anesthesia	Small molecule	1999 FDA	Purdue pharma
Levomenthol	Menthol	TRPM8 agonist	Minor irritation, pain, sore mouth, sore throat, itching, local anesthesia	Small Molecule
Lidocaine	Xylocaine	Nav blocker	Local anaesthesia, neuralgia, itching, pediculosis, ventricular arrhythmia	Small molecule	1948	Fresenius Kabi
Lorazepam	Ativan	GABAA activator	Anxiety, Myoclonic seizure, Atonic seizure, Status epilepticus	Small molecule	1977 FDA	Wyeth Pharmaceuticals
Lormetazepam		GABA-A potentiator	Short-term insomnia	Small Molecule
Lubiprostone	Amitiza	CLC-2 activator	Chronic idiopathic constipation	Small Molecule	2006	Sucampo Pharmaceuticals
Lumacaftor	Orkambi (a combination of ivacaftor and lumacaftor)	CFTR modulator	Cystic fibrosis	Small molecule	2015	Vertex Pharmaceuticals
Manidipine	Calslot, Manyper	Cav1.x and Cav3.x blocker	Hypertension	Small Molecule
Mavatrep		TRPV1 antagonist	Pain	Small Molecule		Janssen
Memantine	Axura, Namenda	GluN antagonist	Moderate to severe Alzheimer's type dementia	Small molecule	2003	Forest labs
Mepivacaine	Carbocaine	Nav inhibitor	Local anesthesia	Small molecule	1960 FDA	Hospira, Inc., Pfizer
Methoxyflurane	Penthrox	GABA-A activator, GluA1 inhibitor, GLYRA1 agonist	General anestesia	Small Molecule		Abbott
Methsuximide	Petinutin	Cav3.x blocker	Absence seizures, epilepsy	Small Molecule	1957	Parke Davis
Mexiletine	Mexitil	Nav inhibitor	Ventricular arrhythmia	Small molecule	1985
Midazolam	Buccolam, Versed	GABA-A activator	Anxiety, Anesthesia, Status epilepticus	Small molecule	1985
Minoxidil	Loniten	Kir6.2 activator	Hypertension, alopecia	Small molecule	1979 FDA
Mirogabalin	Tarlige	Cav ?2? modulator	Peripheral neuropathic pain			Daiichi Sankyo
Nateglinide	Starlix	Kir6.2 blocker	Diabetes mellitus type 2	Small molecule	2000 FDA	Novartis
Nicardipine	Cardene	Cav1.x inhibitor	Hypertension, angina pectoris	Small molecule	1988
Nicorandil	Ikorel, Dancor	Kir6.2 activator	Angina pectoris	Small molecule	1984
Nicotine	Nicorette, Nicotrol	Chrn agonist	Smoking cessation, nicotine dependence	Small molecule
Nifedipine	Adalat, Procardia, Afeditab, Nifediac	Cav1.x blocker	Hypertension, vasospastic angina, premature labor	Small molecule	1981	Pfizer
Nilvadipine	Escor, Escor forte, Naftdil, Nilvadipine, Nivadil, Towajil	calcium channel blocker	hypertension, vasospastic angina, chronic stable angina	Small Molecule		Astellas Pharma, Archer Pharmaceuticals
Nimodipine	Nimotop, Nymalize	Cav1.x blocker	Subarachnoid hemorrhage, hypertension	Small molecule	1988
Nisoldipine	Sular	Cav1.x blocker	Hypertension	Small Molecule	1995	Shionogi
Nitrazepam	Mogadon, Alodorm, Nitrazadon	GABA-A potentiator	Insomnia	Small molecule	1965
Nitrendipine	Baypress, Nidrel	Cav1.x blocker	Hypertension	Small Molecule	1985
Ondansetron	Zophren	5HT3A antagonist	Therapy-induced nausea and vomiting	Small molecule	1991 FDA	GSK
Oxazepam	Novoxapam, Alepam	GABA-A potentiator	Anxiety, alcohol withdrawal delirium	Small molecule	1965
Oxcarbazepine	Trileptal	Nav1.5 blocker	Epilepsy	Small molecule	1990
Oxybuprocaine	Novesine, Novesin	Nav inhibitor	Local anesthesia	Small Molecule
Palonosetron	Aloxi	5HT3A antagonist	Chemotherapy-induced nausea and vomiting	Small molecule	2003 FDA 2009 EMA	Helsinn Healthcare
Pentolinium		NACHR antagonist	Hypertension	Small Molecule		Wyeth Pharmaceuticals
Perampanel	Fycompa	GluA1-4 antagonist	Partial seizures	Small molecule	2012 FDA	Eisai
Permethrin	Elimite	Sodium channel (Sarcoptes scabiei) inhibitor	Infestation by Sarcoptes scabiei, Pediculosis	Small Molecule	1986
Phenobarbital	Luminal	GABA-A potentiator	Epilepsy, Lennox-Gastaut syndrome, migraine	Small molecule	1912
Phensuximide	Milontin	Cav inhibitor Nav inhibitor	Epilepsy, absence seizures	Small molecule	FDA	Parke Davis
Phenytoin	Dilantin	Nav inhibitor	Epilepsy	Small molecule	1953	Parke Davis
Pinacidil	Pindac	Kir6.2 activator	Hypertension	Small molecule	1989 FDA	Leo Pharma
Pinaverium	Dicetel	Cav1.x antagonist	Irritable bowel syndrome	Small molecule	1975	Solvay Pharmaceuticals
Pregabalin	Lyrica	Cav alpha-2/delta modulator	Diabetic peripheral neuropathy, postherpetic neuralgia	Small molecule	2004
Prilocaine	Citanest, Xylonest	Nav inhibitor	Local anaesthesia, premature ejaculation	Small molecule	1965
Primidone	Mysoline	GABA-A positive modulator	Epilepsy, Lennox-Gastaut syndrome	Small molecule	1954 FDA	Valeant
Procainamide	Pronestyl, Procan-SR, Procanbid	Nav inhibitor, Kv11.1 inhibitor	Life-threatening ventricular tachycardia	Small molecule	1950	Bristol-Meyers Squibb
Procaine	Novocaine	Nav1.8 blocker	Local anesthesia	Small Molecule	1954
Propafenone	Rythmol	Nav1.5 blocker	Atrial fibrillation, atrial flutter, life-threatening ventricular tachycardia	Small molecule	1989	GSK
Proparacaine	Alcaine, Ophthetic	Nav blocker	Local anesthesia	Small Molecule	1953
Propofol	Diprivan	GABA-A potentiator	General anaesthesia	Small molecule	1989 FDA	Fresenius Kabi
Quazepam	Doral, Dormalin	GABA-A potentiator	Insomnia	Small molecule	1985	Sciencure Pharma
Quinidine	Cardioquin, Quinidex	Nav inhibitor	Atrial fibrillation, malaria, life-threatening ventricular tachycardia	Small Molecule	1950	Lilly
Ranolazine	Ranexa	Nav inhibitor	Angina pectoris	Small molecule	2006	Gilead
Repaglinide	Gluconorm, Prandin, Novonorm	Kir6.2 blocker	Diabetes mellitus type 2	Small molecule	1997	Novo Nordisk
Riluzole	Rilutek	KCa2.3 activator, Nav1.5 inhibitor	Amyotrophic lateral sclerosis	Small molecule	1995 FDA
Rocuronium	Zemuron, Esmeron	Chrn a1b1d/g antagonist	General anaesthesia, muscle relaxation	Small molecule	1994 FDA
Ropivacaine	Naropin	Nav blocker	Local anaesthesia	Small molecule	1996	Fresenius Kabi
Rufinamide	Banzel	Nav modulator	Lennox-Gastaut syndrome	Small Molecule	2007 EMA 2008 FDA	Novartis
Safinamide	Xadago	Nav and Cav inhibitor	Parkinsons disease	Small Molecule	2015 EMA 2017 FDA	Newron Pharmaceuticals
Sevoflurane	Ultane, Sojourn	GABA-A activator, GLYRA1 agonist	General anestesia	Small Molecule	1995	Abbvie
Sotalol	Biosotal, Sotalex	Kv11.1 blocker	Atrial fibrillation, life-threatening ventricular tachycardia	Small molecule	1974
Stiripentol	Diacomit	GABA-A positive modulator	Myoclonic seizures	Small Molecule	2007 EMA 2018 FDA	Biocodex
Succinylcholine	Anectine	Chrn a1b1deg agonist	General anaesthesia, muscle relaxation	Small molecule	1952 FDA	Sandoz
Temazepam	Restoril	GABA-A potentiator	Insomnia	Small molecule	1981	Mallinckrodt Pharmaceuticals
Tetracaine	Pontocaine	Nav inhibitor	Local anesthesia	Small molecule	1941
Tezacaftor		CFTR activator	Cystic fibrosis	Small Molecule	2018	Vertex Pharmaceuticals
Tocainide	Tonocard	Nav blocker	Ventricular arrhythmia	Small Molecule	1984
Tolazamide	Tolinase, Norglycin	Kir6.2 inhibitor	Diabetes mellitus type 2	Small molecule	1966
Tolbutamide		Kir6.2 inhibitor	Diabetes mellitus type 2	Small molecule	1961 FDA
Topiramate	Topamax	GABA-A positive modulator, Nav blocker, GluA antagonist	Epilepsy, migraine, Lennox-Gastaut syndrome	Small Molecule
Triamterene	Dyrenium	ENaC inhibitor	Hypertensive disorder, edema	Small molecule	1964	Smith Kline & French
Triazolam	Halcion	GABA-A positive modulator	Insomnia	Small molecule	1982 (withdrawn in the UK)	Pharmacia and Upjohn
Trimebutine	Trimebutine	Cav1.x inhibitor, KCa inhibitor	Irritable bowel syndrome, postoperative paralytic ileus	Small Molecule
Trimethadione	Tridione	Cav3.1 inhibitor	Absence seizures, epilepsy	Small Molecule	1946	Abbvie
Unoprostone	Rescula	BK and CLC-2 activator	Ocular hypertension, open-angle glaucoma	Small Molecule	2000 FDA (discontinued in the US)	Sucampo Pharmaceuticals
Valproic acid	Convulex, Depakene, Valcote	Nav inhibitor, GABAA modulator	Epilepsy, absence seizures, bipolar disorder, migraine	Small molecule
Varenicline	Chantix, Champix	Chrn a4b2 agonist	Smoking cessation	Small molecule	2006 FDA	Pfizer
Verapamil	Calan, Verelan	Cav1.x inhibitor	Hypertension, angina, supraventricular tachycardia, migraine, cluster headache	Small molecule	1981
Vernakalant	Brinavess	Nav1.5, Kv1.5, Kv4.3 blocker	Atrial fibrillation	Small Molecule	2010, EMA	Cardiome Pharma
XEP-018		NaV1.4 blocker	Skin wrinkles	Synthetic peptide		Activen
Zaleplon	Sonata	GABA-A agonist	Insomnia	Small Molecule	1999	Meda Ab, Pfizer
Ziconotide	Prialt	Cav2.2 blocker	Severe and chronic pain	Synthetic peptide	2004	Elan Pharmaceuticals
Zolpidem	Ambien	GABA-A agonist	Insomnia	Small molecule	1992	Sanofi Aventis
Zonisamide	Zonegran	Nav blocker, Cav3.x blocker	Partial epilepsy	Small Molecule	2000	Eisai
Zopiclone	Imovane, Zimovane	GABA-A potentiator	Insomnia	Small molecule	1986	Rhône-Poulenc
Zucapsaicin	Zuacta	TRPV1 agonist	Severe pain associated with osteoarthritis of the knee, neuropathic pain	Small Molecule		Sanofi Aventis

Ion channel drug candidates in preclinical development and clinical trials

Name	Other names	Mechanism of action	Indication	Type	Status	Company
ACP-044	CT-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-0422		Nav1.7 inhibitor		Peptide	Discovery	Amgen
AP30663		KCa inhibitor	Atrial fibrillation		Phase I/II	Acesion 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
ASN008		Na+ channel blocker	Pruritus, atopic dermatitis, pain		Phase IIa	Asana BioSciences
ASN009		P2X3 antagonist	Cough		Preclinical	Asana BioSciences
ASP-0819		KCa3.1 activator	Fibromyalgia		Phase II	Astellas Pharma
AUT00201		Modulator of Kv3 channels	Schizophrenia, hearing disorders		Phase I	Autifony Therapeutics
Auxora	CM4620-IE	CRAC inhibitor	Severe COVID-19 pneumonia, Viral pneumonia, Acute pancreatitis	Small Molecule	Phase II	CalciMedica
AV-101	4-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-1817080		P2X3 inhibitor	Endometriosis and persistent chronic cough		Phase I	Bayer
BAY-1902607		P2X3 inhibitor	Persistent chronic cough		Phase II	Bayer
BAY-2253651		TASK inhibitor	Obstructive sleep apnoea		Phase II	Bayer
BIIB093		SUR1-TRPM4 blocker	Brain Contusion	Small Molecule	Phase II	Biogen
BIIB095		Nav1.7 inhibitor	Neuropathic pain	Small Molecule	Phase I	Biogen
BIIB104	PF-04958242	AMPAR activator	Cognitive impairment associated with schizophrenia		Phase IIa	Biogen
BIL010t		nfP2X7	Skin cancer	Antibody	Phase I	Biosceptre
BIL06v		nfP2X7	Skin cancer	Peptide vaccine	Phase I	Biosceptre
BLU-5937		P2X3 antagonist	Refractory chronic cough		Phase IIb	BELLUS Health
BNC-210		alpha7 nAChRs antagonist	Agitation, post-traumatic stress disorder, generalised anxiety disorder		Phase II	Bionomics
CAD-1883		KCa activator	Ataxia or essential tremors		Phase I/II	Cadent Therapeutics
CAD-9303		NMDAR positive allosteric modulator	Schizophrenia		Phase I	Cadent Therapeutics
CC 8464	ASP 1807	Nav1.7 antagonist	Neuropathic and inflammatory pain	Small Molecule	Phase I	Chromocell/Astellas Pharma
CVL-865		Positive allosteric modulator of alpha-2/3/5 subunits of the GABA-A	Drug-resistant focal onset epilepsy		Phase I/II	Cerevel Therapeutics
CVL-865		Positive allosteric modulator of alpha-2/3/5 subunits of the GABA-A	Acute anxiety		Phase I	Cerevel Therapeutics
CX-8998		T-type calcium channel modulator	Absence epilepsy, essential tremor		Phase II	Cavion
Dalazatide	ShK-186	Kv1.3 inhibitor	Myositis, Psoriasis	Synthetic peptide	Phase II	Kv1.3 Therapeutics
DSP-2230		NaV1.7 and NaV1.8 inhibitor	Neuropathic pain	Small Molecule	Phase I	AlphaNavi Pharma
DSP-3905		NaV1.7 inhibitor	Neuropathic pain	Small Molecule	Phase I	Sunovion Pharmaceuticals
ENX-101		sub-type selective GABA-A modulator	Diseases of the nervous system		Preclinical	Engrail Therapeutics
ETD001		ENaC blocker	Respiratory diseases		Preclinical	Enterprise Therapeutics
ETD002		TMEM16A potentiator	Cystic fibrosis		Phase I	Enterprise Therapeutics
Evenamide		Nav blocker	Schizophrenia		Phase II	Newron Pharmaceuticals
Evt201		GABAA receptor PAM	Insomnia		Phase II	Evotec
FX301	Funapide	Nav1.7 inhibitor	Acute post-operative pain		Preclinical	Flexion
Galicaftor	ABBV-2222	CFTR	Cystic fibrosis		Phase II	AbbVie
GFB-887		TRPC5 inhibitor	Focal segmental glomerulosclerosis, diabetic nephropathy		Phase I/II	Goldfinch Bio
Granexin gel		alphaCT1, a peptide mimetic of the Cx43 carboxyl terminus	Cutaneous radiation injury, Diabetic foot and venous leg ulcers	Synthetic peptide	Phase III	FirstString Research
GRC 17536		TRPA1 antagonist	Painful diabetic neuropathy		Phase II	Glenmark
GSK-2798745		TRPV4 inhibitor	Heart failure		Phase II	GlaxoSmithKline
Halneuron	Tetrodotoxin	Nav blocker	Severe neuropathic pain, cancer related pain	Small Molecule	Phase III	Wex Pharmaceuticals
HBI-3000		Multi-channel inhibitor	Atrial fibrillation		Phase I	HUYA Bioscience International
JNJ-55308942		P2X7 inhibitor	Neuroinflammation and anhedonia		Phase I	Johnson & Johnson
KB-3061		Kv7 modulator	KCNQ2 epileptic encephalopathy		Preclinical	Knopp Biosciences
KCP-506		alpha9alpha10 nAChR antagonist	Chronic pain		Phase I	Kineta
Kv7 modulator		Kv7 modulator	Neuropathic pain, hearing disorders, ALS		Discovery	Knopp Biosciences
LUNAR-CF		CFTR upregulation	Cystic fibrosis	mRNA therapeutic	Preclinical	Arcturus Therapeutics
MIJ821	CAD-9271	NMDAR negative allosteric modulator	Depression		Phase II	Novartis
MK-7264	Gefapixant	P2X3 antagonist	Chronic cough	Small Molecule	Phase III	Merck, Roche
MRT5005		CFTR upregulation	Cystic fibrosis	mRNA therapeutic	Phase I/II	Translate Bio
NBI-1065845	TAK-653	AMPAR activator	Depression		Phase II	Neurocrine Biosciences, Takeda
NBI-827104	ACT-709478	T-type calcium channel blocker	Pediatric epilepsy		Phase I/II	Neurocrine Biosciences, Idorsia
NBI-921352	XEN901	Nav1.6 inhibitor	Epilepsy	Small Molecule	Phase I/II	Neurocrine Biosciences, Xenon
NMD670		Skeletal muscle specific inhibitor of ClC-1	Myasthenia gravis	Small Molecule	Phase I/IIa	NMD Pharma
NOC-100	NTX-1175	Charged sodium channel blocker	Chronic and acute cough	Small Molecule	Phase I	Nocion Therapeutics
OV101	Gaboxadol	GABA-A agonist	Fragile X syndrome, Angelman syndrome	Small Molecule	Phase II-III	Ovid Therapeutics
P-1037	VX-371	ENaC inhibitor	Pulmonary diseases		Phase II	Parion Sciences, Vertex Pharmaceuticals
P-1055	VX-551	ENaC inhibitor	Pulmonary diseases		Preclinical	Parion Sciences, Vertex Pharmaceuticals
P-321		ENaC inhibitor	Dry eye disease		Phase II	Parion Sciences, Takeda
P2X4 inhibitor		P2X4 inhibitor	Endometriosis		Phase I	Bayer
P2X7 MAB		P2X7 monoclonal antibody	Autoimmune disorders	Antibody	Preclinical	Integral Molecular
PRAX-114		GABA-A positive allosteric modulator	Major depressive disorder, perimenopausal depression	Small Molecule	Phase II	Praxis Precision Medicines
PRAX-944		T-type calcium channel blocker	Essential tremor	Small Molecule	Phase II	Praxis Precision Medicines
PRAX-562			Pediatric epilepsy, adult cephalgia	Small Molecule	Phase I	Praxis Precision Medicines
PRAX-020/021			Genetic epilepsies		Preclinical	Praxis Precision Medicines
PRAX-222			Genetic epilepsies		Preclinical	Praxis Precision Medicines
Ralfinamide		Nav blocker, Cav2.2 blocker	Neuropathic pain		Phase II	Newron Pharmaceuticals
Resiniferatoxin		TRPV1 agonist	Cancer pain	Small Molecule	Phase I	Sorrento Therapeutics
RG-7816		GABA-A receptor alpha5 subunit-targeting NAM	Autism spectrum disorder		Phase I	Roche
S-600918		P2X3 antagonist	Refractory chronic cough		Phase IIb	Shionogi
SAN711		GABAA alpha3 modulator	Neuropathic pain disorders		Preclinical	Saniona
SAN903		KCa3.1 inhibitor	Rare inflammatory/fibrotic diseases, hereditary xerocytosis		Preclinical	Saniona
SAGE-217	Zuranolon, S-812217	GABA-A positive allosteric modulator	Major depression	Small Molecule	Phase II	Sage Therapeutics, Shionogi
SAGE-324		GABA-A receptor PAM	Essential tremor and Parkinson disease		Phase I	Sage Therapeutics
SAGE-689		GABA-A modulator	GABA hypofunction		Preclinical	Sage Therapeutics
SAGE-718		NMDAR activator	NMDAR hypofunction		Phase I	Sage Therapeutics
SAGE-904		NMDAR modulator	NMDAR hypofunction		Preclinical	Sage Therapeutics
Senicapoc		KCa3.1 inhibitor	Hereditary xerocytosis and Alzheimer disease		Phase I	SpringWorks Therapeutics/ University of California, Davis
SOR-C13		TRPV6 inhibitor	Solid tumor cancer	Synthetic peptide	Phase Ib	Soricimed Biopharma
ST-2427		Nav1.7 inhibitor	Post-operative pain	Small Molecule	IND	SiteOne Therapeutics
STK-001		Upregulates Nav1.1 protein expression	Dravet syndrome	Antisense oligonucleotide	Phase I/IIa	Stoke Therapeutics
TRPC4 and TRPC5 inhibitor		TRPC4 and TRPC5 inhibitor	Anxiety disorder and depression		Phase I	Hydra/Boehringer Ingelheim
VX-150		Nav1.8 inhibitor	Acute and neuropathic pain	Small Molecule	Phase II	Vertex Pharmaceuticals
XEN007	Flunarizine	Cav2.1 modulator	Migraine and other neurological disorders	Small Molecule	Phase I	Xenon
XEN1101		Kv7 modulator	Epilepsy		Phase II	Xenon
XEN496	Retigabine	Kv7 modulator	KCNQ2 and pediatric epilepsy		Phase II	Xenon
XEN-D0501		TRPV1 antagonist	Type 2 diabetes		Phase II	Pila Pharma

Ion channel drugs on the WHO List of Essential Medicines

Name	Mechanism of action	Indication	Year of Approval	Type of medicine	Subtype of medicine	Note
Amiloride	ENaC inhibitor	Hypertensive disorder, edema, hypokalemia	1981	Diuretics
Amiodarone	Kv11.1 blocker	Ventricular fibrillation, life-threatening ventricular tachycardia	1961	Cardiovascular medicines	Antiarrhythmic medicines	Complementary List
Amlodipine	Cav1.x inhibitor	Hypertension, vasospastic angina, angina pectoris	1992	Cardiovascular medicines	Antihypertensive medicines
Atracurium	Chrn abd antagonist	General anaesthesia, muscle relaxation	1983 FDA	Mucsle relaxants (peripherally acting) and cholinesterase inhibitors
Bupivacaine	Nav inhibitor	Local anesthesia	1972 FDA	Anaesthetics, preoperative medicines and medical gases	Local anaesthetics
Carbamazepine	Nav1.5 blocker	Epilepsy, Lennox-Gastaut syndrome, bipolar disorder	1968	Anticonvulsants/Antiepileptics Medicines for mental and behavioural disorders	Medicines used in bipolar disorders
Diazepam	GABA-A potentiator	Anxiety, alcohol withdrawal syndrome, spasticity, epilepsy	1963 FDA	Medicines 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
Diazoxide	Kir6.2 activator	Hypertensive emergencies, hyperinsulinism	1973	Medicines for endocrine disorders	Medicines for hypoglycaemia	Complementary List
Ethosuximide	Cav3.1 inhibitor	Absence seizures	1960	Anticonvulsants/Antiepileptics		Complementary List
Gliclazide	Kir6.2 inhibitor	Diabetes mellitus type 2	1972	Medicines for endocrine disorders	Medicines for diabetes	Oral hypoglycaemic agents
Halothane	GABA-A agonist, GluA1 inhibitor, GLYRA1 agonist	General anesthesia	1958 FDA	Anaesthetics, preoperative medicines and medical gases	General anaesthetics and oxygen	Inhalational medicines
Isoflurane	GABA-A agonist, GluA1 inhibitor, GLYRA1 agonist	General anestesia	1979	Anaesthetics, preoperative medicines and medical gases	General anaesthetics and oxygen	Inhalational medicines
Ketamine	GluN antagonist	General and local anaesthesia	1970 FDA	Anaesthetics, preoperative medicines and medical gases	General anaesthetics and oxygen	Injectable medicines
Lamotrigine	Nav inhibitor	Tonic-clonic seizures, epilepsy, Lennox-Gastaut syndrome	1994	Anticonvulsants/Antiepileptics
Lidocaine	Nav blocker	Local anaesthesia, neuralgia, itching, pediculosis, ventricular arrhythmia	1948	Anaesthetics, preoperative medicines and medical gases Cardiovascular medicines	Local anaesthetics Antiarrhythmic medicines
Lorazepam	GABAA activator	Anxiety, Myoclonic seizure, Atonic seizure, Status epilepticus	1977	Anticonvulsants/Antiepileptics
Midazolam	GABA-A activator	Anxiety, Anesthesia, Status epilepticus	1985	Anaesthetics, 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
Nicotine	Chrn agonist	Smoking cessation, nicotine dependence		Medicines for mental and behavioural disorders	Medicines for disorders due to psychoactive substance use	Nicotine replacement therapy
Nifedipine	Cav1.x blocker	Hypertension, vasospastic angina, premature labor	1981	Medicines for reproductive health and perinatal care	Antioxytocics (tocolytics)
Ondansetron	5HT3A antagonist	Therapy-induced nausea and vomiting	1991 FDA	Medicines for pain and paliative care Gastrointestinal medicines	Medicines for other common symptoms in palliative care Antiemetic medicines
Permethrin	Sodium channel (Sarcoptes scabiei) inhibitor	Infestation by Sarcoptes scabiei, Pediculosis	1986	Dermatological medicines (topical)	Scabicides and pediculicides
Phenobarbital	GABA-A potentiator	Epilepsy, Lennox-Gastaut syndrome, migraine	1912	Anticonvulsants/Antiepileptics
Phenytoin	Nav inhibitor	Epilepsy	1953	Anticonvulsants/Antiepileptics
Propofol	GABA-A potentiator	General anaesthesia	1989 FDA	Anaesthetics, preoperative medicines and medical gases	General anaesthetics and oxygen	Injectable medicines
Tetracaine	Nav inhibitor	Local anesthesia	1941	Ophtalmological preparations	Local anaesthetics
Valproic acid	Nav inhibitor, GABAA modulator	Epilepsy, absence seizures, bipolar disorder, migraine		Anticonvulsants/Antiepileptics Medicines for mental and behavioural disorders	Medicines used in bipolar disorders
Verapamil	Cav1.x inhibitor	Hypertension, angina, supraventricular tachycardia, migraine, cluster headache	1981	Cardiovascular medicines	Antianginal medicines Antiarrhythmic medicines

Withdrawn/Discontinued ion channel drugs

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

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

Ion channel drug candidates in preclinical development and clinical trials

Ion channel drugs on the WHO List of Essential Medicines 2019

Withdrawn/Discontinued ion channel drugs

Ion channel drugs on the market

Ion channel drug candidates in preclinical development and clinical trials

Ion channel drugs on the WHO List of Essential Medicines

Withdrawn/Discontinued ion channel drugs

Ion Channel library

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