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
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 |
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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 |