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New research · Ophthalmology
Investigative ophthalmology & visual science · 5d
Animal / preclinicalInvestigative ophthalmology & visual science · 2026

Preclinical Ocular Pharmacokinetics and Efficacy of Novel Tivozanib Eye Drops for Neovascular Age-Related Macular Degeneration.

Kyosuke Satake, Shoko Koshiba, Hiroki Haniuda … Shinya Horita
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OphthalmologyAnimal / preclinical

Nanocrystallized tivozanib eye drops deliver far more drug to the retina in rabbits.

Preclinical Ocular Pharmacokinetics and Efficacy of Novel Tivozanib Eye Drops for Neovascular Age-Related Macular Degeneration.

Kyosuke Satake … Shinya Horita
Investigative ophthalmology & visual science · 2026
Background

In neovascular age-related macular degeneration (nAMD), invasive intravitreal injection of anti-vascular endothelial growth factor (VEGF) drugs is the current standard of care, highlighting the need for noninvasive eye drop formulations.

Purpose

We aimed to assess the ocular pharmacokinetics and anti-angiogenic efficacy of nanocrystallized tivozanib (nTivo) eye drops in rabbits and monkeys.

Methods

We investigated the ocular distribution of nTivo eye drops and conventional microcrystallized tivozanib eye drops in albino and pigmented rabbits.

Results

far more tivozanib drug reached the retina than with older formulation

247.5hours
Retina/choroid t1/2
49.7hours
Serum t1/2
More results

Additionally, accumulation of the ocular exposure was observed with the repeated instillation of nTivo eye drops, and the elimination half-life (t1/2) of tivozanib was longer in the retina/choroid (247.5 hours) than in serum (49.7 hours).

More results

In comparison to albino rabbits, pigmented rabbits showed higher exposure (3.2-fold) and longer t1/2 (5.7-fold) in the retina/choroid, suggesting that the melanin binding properties of tivozanib potentially contribute to its accumulation and prolonged retention in the retina and choroid.

“
Conclusion

The nTivo eye drop formulation may be a potential new treatment option for nAMD due to its preferable ocular pharmacokinetic and anti-angiogenic profiles based on potential contributions of nanocrystallization and the melanin binding properties of tivozanib.

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