Tafluprost

CAS No:
209860-87-7

Molecular Formula：

C25H34F2O5

Molecular Weight：

452.53

Storage:

Store in a tightly closed container in a cool, dry，Protect from moisture and direct sunlight.

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Technical Data

Appearance	pale yellow to colorless Oil
Identification	NMR HPLC
Optical Rotation(C=0.5 ethanol)	+19.0° ~ +23°
Water	≤ 1.0%
Related substances	Tafluprost acid≤ 0.3% 5,6-trans isomer ≤ 0.5 % Any unspecified impurity:≤0.1 % Total impurities：≤2.0 %
Residue Solvent	n-Hexane：≤0.029% Isopropanol：≤0.5% Methyl tert-butyl ether：≤0.5% N,N-Dimethylformamide≤ 0.088%
Purity by HPLC	≥98%

Description

Tafluprost (MK2452, AFP-168) is a selective prostaglandin F (FP) receptor agonist that effectively lowers intraocular pressure (IOP) in preclinical models. In studies using normotensive and glaucomatous rabbits and monkeys, topical administration of tafluprost reduced IOP by 25–35%, demonstrating dose-dependent ocular hypotensive activity. It enhanced uveoscleral outflow with high receptor selectivity and minimal off-target effects, while showing efficient corneal penetration and sustained ocular residence. Pharmacokinetic analyses indicated low systemic exposure, reducing potential side effects. These findings support tafluprost’s potential as a safe and effective therapy for glaucoma and ocular hypertension, providing sustained IOP reduction and protection against optic nerve damage.

Tafluprost (AFP-168) is an anti-glaucoma prostaglandin (PG) analog. Tafluprost can inhibit the apoptosis of retinal ganglion cells (RGCs) and rat RGCs cells. Tafluprost promotes axon regeneration by regulating Zn²⁺-mTOR pathway, inhibits intracellular lipid accumulation in human preorbital adipocytes. Tafluprost can be used in the study of optic nerve injury in glaucoma.

Safety Information

GHS

Pictogram:

GHS08

Signal Word:

Warning

Hazard Statements:

H361 Suspected of damaging fertility or the unborn child.

Precautionary Statements:

P201 Obtain special instructions before use.
P202 Do not handle until all safety precautions have been read and understood.
P280 Wear protective gloves/ protective clothing/ eye protection/ face protection.
P308 + P313 IF exposed or concerned: Get medical advice/ attention.
P405 Store locked up.
P501 Dispose of contents/ container to an approved waste disposal plant.

References

[1]. Kuwayama, Y. and A. Nomura, Prospective observational post-marketing study of tafluprost for glaucoma and ocular hypertension: short-term efficacy and safety. Adv Ther, 2014. 31(4): p. 461-71.

[2]. Kanamori A, et al. Tafluprost protects rat retinal ganglion cells from apoptosis in vitro and in vivo. Graefes Arch Clin Exp Ophthalmol. 2009 Oct;247(10):1353-60.

[3]. Ota T, et al. The IOP-lowering effects and mechanism of action of tafluprost in prostanoid receptor-deficient mice. Br J Ophthalmol. 2007 May;91(5):673-6.

[4]. Kumagami, T., et al., Comparison of corneal safety and intraocular pressure-lowering effect of tafluprost ophthalmic solution with other prostaglandin ophthalmic solutions. J Ocul Pharmacol Ther, 2014. 30(4): p. 340-5.

[5]. Inoue, K., A. Tanaka, and G. Tomita, Effects of tafluprost treatment for 3 years in patients with normal-tension glaucoma. Clin Ophthalmol, 2013. 7: p. 1411-6.

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