Tafluprost: A Comprehensive Pharmacological and Clinical Review

1. Introduction and Drug Identity

1.1. Overview

Tafluprost is a synthetic, fluorinated analog of prostaglandin F_2α, employed as an ophthalmic agent to reduce elevated intraocular pressure (IOP).[1] It is indicated for patients with open-angle glaucoma or ocular hypertension, conditions that can lead to progressive vision loss if untreated.[1] Tafluprost is administered topically as eye drops and functions as an ester prodrug; it is hydrolyzed in vivo within the eye to its pharmacologically active metabolite, tafluprost acid.[1] The primary therapeutic objective of tafluprost is to control the progression of glaucoma and manage ocular hypertension by effectively lowering IOP.[3]

1.2. Chemical Identity

A precise understanding of tafluprost's chemical nature is fundamental to comprehending its pharmacological behavior and formulation characteristics.

• Chemical Name: The International Union of Pure and Applied Chemistry (IUPAC) name for tafluprost is 1-methylethyl (5Z)-7-{(1R,2R,3R,5S)-2-[(1E)-3,3-difluoro-4-phenoxy-1-butenyl]-3,5-dihydroxycyclopentyl}-5-heptenoate.[2] This systematic name meticulously describes the molecule's complex structure, including the specific stereochemistry at its chiral centers and the geometry of its double bonds, which are crucial for its interaction with biological targets.
• Synonyms: Tafluprost is also identified by the developmental codes AFP-168 and MK-2452.[1] These synonyms are valuable for comprehensive literature searches and for tracking the compound through its various stages of research and development.
• CAS Number: The Chemical Abstracts Service (CAS) registry number for tafluprost is 209860-87-7.[6] This unique numerical identifier ensures unambiguous identification of the chemical substance across global databases and scientific publications.
• DrugBank ID: Tafluprost is assigned the DrugBank