The pharmacology of bimatoprost (Lumigan™)

Bimatoprost (Lumigan (TM)) is a pharmalogically unique and highly efficacious ocular hypotensive agent. It appeal's to mimic the activity of a newly discovered family of fatty acid amides, termed prostamides. Our biosynthetic route to the prostamides involves anandamide as the precursor. Bimatoprost pharmacology has been extensively characterised by binding and functional studies at more than 100 drug targets, which comprise a diverse variety of receptors, ion channels, and transporters. Bimatoprost exhibited no meaningful activity at receptors known to include antiglaucoma drug targets as follows: adenosine (A(1-3)), adrenergic (alpha (1), alpha (2), beta (1), beta (2)), cannabinoid (CB1, CB2), dopamine (D1-5). muscarinic (M1-5), prostanoid (DP, EP1-4, FP, IF, TP), and serotonin (5HT(1-7)). Bimatoprost does, here ever, exhibit potent inherent pharmacological activity in the feline iris sphincter preparation, which is prostamide-sensitive. Bimatoprost also resembles the prostamides ill that it is a potent and highly efficacious ocular hypotensive agent. A single dose of bimatoprost markedly reduces intraocular pressure in dogs and laser-induced ocular hypertensive monkeys. Decreases in intraocular pressure are well maintained for at least 24 h post-dose. Human studies have demonstrated that systemic exposure to bimatoprost is low and that accumulation does not occur. The sclera is the preferred route of accession to the eye. The high scleral permeability coefficient Papp is a likely contributing factor to the rapid onset and long-acting ocular hypotensive profile of bimatoprost.