What kind of drug is bimatoprost?

Bimatoprost is in a class of medications called prostaglandin analogues.

Bimatoprost, a synthetic analogue of endogenous prostamides, is in development as a topical ocular hypotensive agent for treating glaucoma and ocular hypertension. Prostamides are a newly discovered class of compounds with potent ocular hypotensive activity in the laboratory. Bimatoprost is a highly efficacious ocular hypotensive in glaucomatous patients, and the evidence suggests that it is the most efficacious agent currently available for treating glaucoma[1].

Bimatoprost mimics the endogenous prostamides by lowering intraocular pressure (IOP). Bimatoprost provides outstanding control of IOP throughout the day, and a high percentage of patients receiving bimatoprost achieve the low target pressures important for clinical success. The difference in absolute mm Hg is only about 0.5–1, but when intraocular pressure approaches the normal range, each mm Hg of additional ocular hypotensive effect is of significant value in preventing visual field loss. Bimatoprost efficacy may be related to a dual mechanism of action on aqueous humor outflow that involves both uveoscleral and trabecular meshwork/Schlemm's canal pathways. Effects on uveoscleral outflow measured directly in monkeys correlate with morphological changes in the anterior portion of the ciliary body. Bimatoprost results in a controlled remodeling of the anterior third of the ciliary body, resulting in new, organized drainage channels partially lined with endothelial cells. At the gene regulation level, Cyr 61 upregulation appears to provide a common upstream event for prostamides, FP agonists, and EP2 agonists. Studies in human models of the trabecular meshwork/Schlemm's canal outflow pathways have demonstrated that bimatoprost produces increased hydraulic conductivity, which is prostamide receptor-mediated[2].

In controlled clinical trials, bimatoprost 0.03% given once daily has displayed efficacy superior to timolol 0.5% given twice daily, the current standard for therapy. Analysis of pooled six-month data from two large Phase III trials demonstrated that mean IOP was consistently 2 - 3 mmHg lower with bimatoprost q.d. than with timolol b.i.d. Bimatoprost 0.03% q.d. has also been shown to provide significantly better diurnal IOP control than latanoprost 0.005% q.d., probably the most efficacious topical medication currently available. Patients receiving bimatoprost q.d. were more likely to achieve low target pressures than timolol or latanoprost patients. In all clinical evaluations, bimatoprost q.d. has been demonstrated to be safe and well-tolerated.

References

[1] D.F. Woodward . “The pharmacology and therapeutic relevance of endocannabinoid derived cyclo-oxygenase (COX)-2 products.” Pharmacology & Therapeutics 120 1 (2008): Pages 71-80.

[2] Cantor, L B. “Bimatoprost: a member of a new class of agents, the prostamides, for glaucoma management.” Expert opinion on investigational drugs vol. 10,4 (2001): 721-31. doi:10.1517/13543784.10.4.721

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