Investigational Drug Details

Drug ID: D382
Drug Name: Vigabatrin
Synonyms: 4-Amino-5-hexenoic acid; Gamma vinyl GABA; gamma-Vinyl GABA; gamma-Vinyl-gamma-aminobutyric acid; GVG; Vigabatrin; Vinyl gamma-aminobutyric acid
Type: Chemical drug
DrugBank ID: DB01080
DrugBank Description: Vigabatrin is an analog of gamma-aminobutyric acid (), the main inhibitory neurotransmitter in the central nervous system, used in the treatment of refractory seizures and infantile spasms. It irreversibly inhibits the enzyme responsible for GABA metabolism, thereby increasing levels of circulating GABA. Although administered as a racemic mixture, only the S(+) enantiomer is pharmacologically active. It was first introduced as an antiepileptic agent in the United Kingdom in 1989 and was used extensively until 1997, when an association with vision loss became apparent. Its use is now generally reserved for patients who have failed alternative therapies, and its US approval by the FDA in 2009 mandated the creation of a drug registry to monitor patients for visual deficits.
PubChem ID: 5665
CasNo: 68506-86-5
Repositioning for NAFLD: Yes
SMILES: C(CCC(=O)O)(C=C)N
Structure:
InChiKey: PJDFLNIOAUIZSL-UHFFFAOYSA-N
Molecular Weight: 129.159
DrugBank Targets: 4-aminobutyrate aminotransferase, mitochondrial inhibitor
DrugBank MoA: Gamma-aminobutyric acid (GABA) is the major inhibitory transmitter throughout the central nervous system, and the potentiation of GABAergic neurotransmission is therefore a crucial mechanism through which antiepileptic agents may combat the pathologic excitatory neurotransmission seen in epilepsy. Vigabatrin increases concentrations of GABA in the central nervous system by irreversibly inhibiting the enzymes responsible for its metabolism to succinic semialdehyde: gamma-aminobutyric acid transaminase (GABA-T).
DrugBank Pharmacology: Vigabatrin is an antiepileptic agent chemically unrelated to other anticonvulsants. Vigabatrin prevents the metabolism of GABA by irreversibly inhibiting GABA transaminase (GABA-T). As vigabatrin is an irreversible inhibitor of gamma-aminobutyric acid transaminase (GABA-T), its duration of effect is thought to be dependent on the rate of GABA-T re-synthesis rather than on the rate of drug elimination.
DrugBank Indication: Vigabatrin is indicated as adjunctive therapy in the treatment of refractory complex partial seizures in patients 2 years of age and older who have had inadequate responses to multiple previous treatments (i.e. not to be used for first-line therapy). It is also indicated as monotherapy in the treatment of infantile spasms in patients between 1 month and 2 years of age for whom the potential benefits outweigh the risk of vision loss.
Targets: GABBR1 agonist; ABAT inhibitor
Therapeutic Category: Antiepileptic drug
Clinical Trial Progress: Phase 2 on-going (NCT04321395)
Latest Progress: Under clinical trials