Tafluprost

Tafluprost acid, a prostaglandin analog is a selective FP prostanoid receptor agonist which is believed to reduce intraocular pressure by increasing uveoscleral outflow. The exact mechanism of action is unknown at this time.

• Tafluprost ophthalmic solution, 0.0015% is indicated for reducing elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension. Tafluprost ophthalmic solution, 0.0015% is a prostaglandin analog indicated for reducing elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension.ICD-10: H40.059, H40.9

• None. None.contraindicated

The recommended dose is one drop of tafluprost ophthalmic solution in the conjunctival sac of the affected eye(s) once daily in the evening. The dose should not exceed once daily since it has been shown that more frequent administration of prostaglandin analogs may lessen the intraocular pressure lowering effect. Reduction of the intraocular pressure starts approximately 2 to 4 hours after the first administration with the maximum effect reached after 12 hours. Tafluprost ophthalmic solution may be used concomitantly with other topical ophthalmic drug products to lower intraocular pressure. If more than one topical ophthalmic product is being used, each one should be administered at least 5 minutes apart. The solution from one individual unit is to be used immediately after opening for administration to one or both eyes. Since sterility cannot be maintained after the individual unit is opened, the remaining contents should be discarded immediately after administration. One drop in the affected eye(s) once daily in the evening. ( 2 )

Pigmentation Pigmentation of the iris, periorbital tissue (eyelid) and eyelashes can occur. Iris pigmentation is likely to be permanent. ( 5.1 ) Eyelash Changes Gradual changes to eyelashes including increased length, thickness and number of lashes. Usually reversible. ( 5.2 ) 5.1 Pigmentation Tafluprost ophthalmic solution has been reported to cause changes to pigmented tissues. The most frequently reported changes have been increased pigmentation of the iris, periorbital tissue (eyelid) and eyelashes. Pigmentation is expected to increase as long as tafluprost is administered. The pigmentation change is due to increased melanin content in the melanocytes rather than to an increase in the number of melanocytes. After discontinuation of tafluprost, pigmentation of the iris is likely to be permanent, while pigmentation of the periorbital tissue and eyelash changes have been reported to be reversible in some patients. Patients who receive treatment should be informed of the possibility of increased pigmentation. The long term effects of increased pigmentation are not known. Iris color change may not be noticeable for several months to years. Typically, the brown pigmentation around the pupil spreads concentrically towards the periphery of the iris and the entire iris or parts of the iris become more brownish. Neither nevi nor freckles of the iris appear to be affected by treatment. While treatment with tafluprost ophthalmic solution can be continued in patients who develop noticeably increased iris pigmentation, these patients should be examined regularly.

Most common ocular adverse reaction is conjunctival hyperemia (range 4% – 20%). ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Ingenus Pharmaceuticals, LLC at 1-877-748-1970 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Studies Experience Because clinical studies are conducted under widely varying conditions, adverse reaction rates observed in the clinical studies of a drug cannot be directly compared to rates in the clinical studies of another drug and may not reflect the rates observed in practice. Preservative-containing or preservative-free tafluprost 0.0015% was evaluated in 905 patients in five controlled clinical studies of up to 24-months duration. The most common adverse reaction observed in patients treated with tafluprost was conjunctival hyperemia which was reported in a range of 4% to 20% of patients. Approximately 1% of patients discontinued therapy due to ocular adverse reactions. Ocular adverse reactions reported at an incidence of ≥ 2% in these clinical studies included ocular stinging/irritation (7%), ocular pruritus including allergic conjunctivitis (5%), cataract (3%), dry eye (3%), ocular pain (3%), eyelash darkening (2%), growth of eyelashes (2%) and vision blurred (2%). Nonocular adverse reactions reported at an incidence of 2% to 6% in these clinical studies in patients treated with tafluprost 0.0015% were headache (6%), common cold (4%), cough (3%) and urinary tract infection (2%). 6.2 Postmarketing Experience The following adverse reactions have been identified during postapproval use of tafluprost.

Use in pediatric patients is not recommended because of potential safety concerns related to increased pigmentation following long-term chronic use. ( 8.4 ) 8.1 Pregnancy Pregnancy Category C. Teratogenic effects: In embryo-fetal development studies in rats and rabbits, tafluprost administered intravenously was teratogenic. Tafluprost caused increases in post-implantation losses in rats and rabbits and reductions in fetal body weights in rats. Tafluprost also increased the incidence of vertebral skeletal abnormalities in rats and the incidence of skull, brain and spine malformations in rabbits. In rats, there were no adverse effects on embryo-fetal development at a dose of 3 mcg/kg/day corresponding to maternal plasma levels of tafluprost acid that were 343 times the maximum clinical exposure based on C max . In rabbits, effects were seen at a tafluprost dose of 0.03 mcg/kg/day corresponding to maternal plasma levels of tafluprost acid during organogenesis that were approximately 5 times higher than the clinical exposure based on C max . At the no-effect dose in rabbits (0.01 mcg/kg/day), maternal plasma levels of tafluprost acid were below the lower level of quantification (20 pg/mL). In a pre- and postnatal development study in rats, increased mortality of newborns, decreased body weights and delayed pinna unfolding were observed in offsprings.

Metabolism

Absorption Following instillation, tafluprost is absorbed through the cornea and is hydrolyzed to the biologically active acid metabolite, tafluprost acid. Following instillation of one drop of the 0.0015% solution once daily into each eye of healthy volunteers, the plasma concentrations of tafluprost acid peaked at a median time of 10 minutes on both Days 1 and 8.

• Feb 10, 2012NDANDA202514Thea Pharma
• Aug 19, 2019ANDAANDA209051Micro Labs
• Jan 28, 2022ANDAANDA209040Sandoz
• Apr 5, 2024ANDAANDA218002Ingenus Pharms Llc

1. 1Ocular Hyperaemia46316%
2. 2Eye Irritation42215%
3. 3Eye Pain29310%
4. 4Eye Pruritus2287.9%
5. 5Drug Ineffective2087.2%
6. 6Death1986.9%
7. 7Vision Blurred1695.9%
8. 8Headache1655.7%
9. 9Eye Swelling1224.2%
10. 10Dry Eye1093.8%
11. 11Intraocular Pressure Increased963.3%
12. 12Photophobia863.0%
13. 13Lacrimation Increased742.6%
14. 14Dizziness722.5%
15. 15Dyspnoea692.4%

The 10 most recently updated of 37 ClinicalTrials.gov registrations naming Tafluprost as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Retinal Ganglion Cell Neuroprotection Under Prostaglandin Analogues
  Not yet recruiting · Observational · 1,500 enrolled · Association for Innovation and Biomedical Research on Light and Image
  NCT07074782updated 2026-05-06
• Inflammatory Biomarkers in Ocular Surface in Primary Open Angle Glaucoma or Ocular Hypertension Under Topical Prostaglandins
  Recruiting · Observational · 40 enrolled · Instituto Universitario de Oftalmobiología Aplicada (Institute of Applied Ophthalmobiology) - IOBA
  NCT05039684updated 2024-10-31
• A Study of DE-111A on the Treatment of Open Angle Glaucoma or Ocular Hypertension
  Completed · Phase 3 · Interventional · 219 enrolled · Santen Pharmaceutical Co., Ltd.
  NCT03822559updated 2023-07-14
• Preservative-free Fixed-dose Combination of Tafluprost 0.0015% / Timolol 0.5% in Patients With Open-angle Glaucoma or Ocular Hypertension: Clinical Effectiveness, Tolerability and Safety in a Real World Setting
  Completed · Observational · 50 enrolled · Santen Pharmaceutical (Taiwan) Co., LTD
  NCT04828057updated 2022-10-31
• From Preserved, to Preservative-free Cyclosporine 0.1% Enhanced Triple Glaucoma Therapy
  Completed · Interventional · 42 enrolled · Aristotle University Of Thessaloniki
  NCT04673604updated 2022-07-20
• Alleviating Effects Against High Intraocular Pressure by Oral Intake of Cordyceps Cicadae Mycelia
  Completed · Interventional · 46 enrolled · Han-Hsin Chang
  NCT05304299updated 2022-03-31
• 24-hour Efficacy and Tolerability of the Tafluprost-timolol Fixed Association Without Preservatives in Glaucomatous or Ocular Hypertensive Patients Already Treated With Latanoprost Preserved With BAK. A Prospective, Open Study of 3 Months Duration.
  Unknown · Phase 4 · Interventional · 43 enrolled · Fondazione G.B. Bietti, IRCCS
  NCT05299593updated 2022-03-29
• Prospective, Single Center Switching Study of 0.0015% Tafluprost Ophthalmic Solution in Primary Open-angle Glaucoma and Ocular Hypertension Patients With Corneal Disorders (Switching From 0.005% Latanoprost Ophthalmic Solution)
  Completed · Interventional · 1 enrolled · Santen Pharmaceutical (Taiwan) Co., LTD
  NCT04737928updated 2021-02-04
• Preservative-free Tafluprost/Timolol Fixed Combination: Morning vs Evening Dosing
  Completed · Phase 4 · Interventional · 42 enrolled · Aristotle University Of Thessaloniki
  NCT03612817updated 2020-12-17
• 24-hour Efficacy and Ocular Surface With Talfuprost and Triple Combined Therapy
  Completed · Phase 4 · Interventional · 43 enrolled · Aristotle University Of Thessaloniki
  NCT02802137updated 2020-12-17

Frequently asked questions

How does Tafluprost work?

Tafluprost acid, a prostaglandin analog is a selective FP prostanoid receptor agonist which is believed to reduce intraocular pressure by increasing uveoscleral outflow. The exact mechanism of action is unknown at this time.

What is Tafluprost used for?

According to FDA labeling, Tafluprost carries indications including: Tafluprost ophthalmic solution, 0.0015% is indicated for reducing elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension. Tafluprost ophthalmic solution, 0.0015% is a prostaglandin analog indicated for reducing elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Tafluprost?

Tafluprost is classified as Prostaglandin analogues, Prostaglandin Analog, Prostaglandin Receptor Agonists, Decreased Intraocular Fluid Pressure, Increased Prostaglandin Activity.

What are the brand names for Tafluprost?

Tafluprost is marketed under brand names including Zioptan.

What are the contraindications for Tafluprost?

Tafluprost labeling lists contraindications including: None. None.. Always consult the full prescribing information and a clinician.