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Anticonvulsants and neurological agents

148 articles

Donepezil

Donepezil, sold as Aricept, is a reversible acetylcholinesterase inhibitor used to treat dementia in mild, moderate, and severe Alzheimer's disease. Developed by Eisai and approved in 1996, it eases symptoms but does not slow the disease.

Dronabinol

Dronabinol, marketed as Marinol, is a synthetic version of THC, the main psychoactive compound in cannabis, approved in 1985 for chemotherapy nausea and in 1992 for AIDS-related weight loss.

Edaravone and dexborneol concentrated solution for injection

Edaravone dexborneol concentrated solution for injection (依达拉奉右莰醇注射用浓溶液, Xianbixin) is a Simcere 4:1 edaravone/(+)-dexborneol neuroprotectant, 37.5 mg twice daily for 10-14 days, approved in China for acute ischemic stroke; TASTE and TASTE-2 trials support functional benefit.

Elenbecestat

Elenbecestat (E2609) is a discontinued oral BACE1 inhibitor (IC50 7 nM) developed by Eisai and Biogen for early Alzheimer's disease; its Phase 3 MISSION AD1/AD2 trials ended in 2019 for unfavorable risk-benefit with no cognitive benefit.

Emestedastat (Xanamem)

Emestedastat (Xanamem, UE2343) is Actinogen Medical's oral brain-penetrant 11β-HSD1 inhibitor lowering brain cortisol, in Phase 2b/3 trials for Alzheimer's disease (XanaMIA, topline November 2026) and depression; not approved anywhere.

Encenicline

Encenicline (EVP-6124, MT-4666) is a discontinued selective α7 nicotinic acetylcholine receptor partial agonist developed by Forum Pharmaceuticals for cognitive impairment in schizophrenia and Alzheimer's disease; Phase 2 trials were positive, but Phase 3 schizophrenia trials failed and FDA placed Alzheimer's trials on clinical hold over GI safety events.

Entacapone

Entacapone (Comtan) is a reversible peripheral COMT inhibitor taken with levodopa/carbidopa to treat wearing-off motor fluctuations in Parkinson's disease; approved 1998 (EMA) and 1999 (FDA), 200 mg tablets, up to 10 daily.

Eslicarbazepine

Eslicarbazepine, also known as S-licarbazepine, is the active metabolite of eslicarbazepine acetate, a once-daily antiseizure medication for focal (partial-onset) seizures marketed as Aptiom in the United States and Zebinix in Europe.

Ethopropazine

Ethopropazine (profenamine; Parsidol, Parsitan) is a phenothiazine-derived antimuscarinic drug for Parkinson's disease and drug-induced extrapyramidal symptoms; discontinued in the US, still marketed in Canada.

Exifone

Exifone (Adlone, NSC 680919), a hexahydroxybenzophenone nootropic, antioxidant and HDAC1 activator trialed at 600-1200 mg/d for cognitive deficits in Parkinson's disease and cerebral senescence.

Ezogabine

Ezogabine (retigabine; Potiga, Trobalt), a Kv7 potassium channel opener anticonvulsant, was approved in 2011 for adjunctive treatment of adult partial-onset seizures and discontinued in 2017 over blue skin discoloration and retinal pigment changes.

Felbamate

Felbamate (Felbatol), a second-generation antiepileptic drug approved by the FDA in 1993 for Lennox-Gastaut syndrome and partial seizures, acts on NMDA and GABA receptors but is restricted by boxed warnings for aplastic anemia and hepatic failure.

Fenebrutinib

Fenebrutinib (GDC-0853, RG7845) is Roche/Genentech's oral, non-covalent, reversible BTK inhibitor in Phase III for relapsing and primary progressive MS; FDA NDA accepted under priority review 30 September 2026; also trialed in rheumatoid arthritis and lupus.

Fipexide

Fipexide (Vigilor, Attentil) is a withdrawn piperazine nootropic, ATC N06BX05, approved 1983 and withdrawn 1991 for hepatic safety; studied at 600 mg/day for cognitive disorders.

Flindokalner

Flindokalner (BMS-204352, MaxiPost), a fluoro-oxindole potassium channel opener by Bristol-Myers Squibb; BK and Kv7.2-7.5 activator that failed phase III trials for acute ischemic stroke.

Flunarizine

Flunarizine, a selective calcium-entry blocker related to cinnarizine, is a once-daily 5–10 mg migraine prophylactic with level A evidence, also used for vertigo and refractory epilepsy; not marketed in the US, limited by somnolence, weight gain, depression, and parkinsonism.

Foslevodopa

Foslevodopa (levodopa-4'-monophosphate, ABBV-951 with foscarbidopa; Vyalev, Produodopa) is a phosphate prodrug of levodopa given by continuous subcutaneous infusion for motor fluctuations in advanced Parkinson's disease.

Fosmetpantotenate

Fosmetpantotenate (RE-024) is a discontinued Retrophin phosphopantothenate prodrug for pantothenate kinase-associated neurodegeneration (PKAN); safe in the phase 3 FORT trial but failed to improve PKAN-ADL function.

Fosphenytoin

Fosphenytoin (Cerebyx) is a water-soluble phosphate ester prodrug of phenytoin, dosed in phenytoin sodium equivalents, FDA-approved in 1996 for status epilepticus and neurosurgical seizures.

Gabapentin

Gabapentin (Neurontin), a gabapentinoid GABA analog, binds the alpha2delta-1 calcium channel subunit; FDA-approved 1993 for partial seizures and 2002 for postherpetic neuralgia, widely prescribed off-label for neuropathic pain, with known misuse and overdose risks.

Gabapentin enacarbil

Gabapentin enacarbil (Horizant, Regnite, XP13512) is an extended-release prodrug of gabapentin approved for moderate-to-severe primary restless legs syndrome and postherpetic neuralgia, dosed 600 mg daily for RLS, with somnolence and dizziness as common adverse effects.

Galantamine

Galantamine (galanthamine), a plant-derived acetylcholinesterase inhibitor from snowdrop (Galanthus), treats mild to moderate Alzheimer's symptoms; FDA-approved 2001 as Razadyne, formerly Nivalin and Reminyl.

Ganaxolone

Ganaxolone, sold as Ztalmy, is a synthetic neuroactive steroid that modulates GABA receptors and is used as an antiseizure medication, approved in 2022 as the first treatment for seizures in CDKL5 deficiency disorder.

Guanfacine

Guanfacine (Tenex IR, Intuniv ER) is a selective alpha-2A-adrenergic receptor agonist; a nonstimulant second-line ADHD medication for children and adolescents, also used adjunctively with stimulants and for tics, with somnolence and hypotension as key effects.

Hydromethylthionine

Hydromethylthionine (leucomethylene blue, LMTM, TRx0237) is the reduced form of methylene blue, an oral tau aggregation inhibitor developed by TauRx for Alzheimer's disease and frontotemporal dementia; investigational, MHRA review expected 2026.

Ibudilast

Ibudilast (MN-166, AV411, Ketas) is an oral nonselective PDE inhibitor (PDE-3/4/10/11) also inhibiting MIF and TLR-4; approved in Japan since 1989 for asthma and post-stroke dizziness, in trials for progressive MS and ALS.

Idalopirdine

Idalopirdine (Lu AE58054, SGS518, LY483518) is a selective 5-HT6 receptor antagonist developed by Lundbeck with Otsuka for Alzheimer's disease; positive phase 2 but failed phase 3 STAR trials, rights licensed to Denovo Biopharma in 2021.

Imagabalin

Imagabalin (PD-0332334, PF-00195889) is Pfizer's discontinued oral α2δ calcium-channel ligand, a gabapentinoid β-amino acid tested in Phase 3 for generalized anxiety disorder; development ended in 2009 for lack of benefit over standard care, never approved.

Intepirdine

Intepirdine (RVT-101, SB-742457), a selective 5-HT6 receptor antagonist developed by GSK and Axovant for Alzheimer's and Lewy body dementia; failed phase 3 MINDSET and phase 2b HEADWAY-DLB trials.

Isaxonine

Isaxonine (2-(isopropylamino)pyrimidine, Nerfactor) is a withdrawn French neurotrophic drug for peripheral neuropathy, marketed 1981 as the phosphate salt and withdrawn in 1983-1984 for toxic hepatitis.