Evidence map›Paper›PMID 41987023›Full record

ArticleInternational journal of retina and vitreous2026

Ocular pharmacokinetics of tivozanib eye drops in patients with neovascular age-related macular degeneration: comparison with phase 1 trials of oral tivozanib in solid tumors.

Shinya Horita, Mayumi Saki, Sotaro Takigawa, Yasumasa Kanai, Kenta Murotani, Fumi Gomi

Abstract readLetter
In one paragraph

Article in International journal of retina and vitreous, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

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1 · What the graph read from it

What it found

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2 · The registry

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3 · Its place in the literature

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4 · The record

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5 · Who and what money

Authors and funding

6 authors.

Shinya HoritaDevelopment Division, Kyowa Kirin Co., Ltd., Tokyo, Japan.
Mayumi SakiMedical Affairs Division, Kyowa Kirin Co., Ltd., Tokyo, Japan. mayumi.saki.sm@kyowakirin.com.
Sotaro TakigawaDevelopment Division, Kyowa Kirin Co., Ltd., Tokyo, Japan.
Yasumasa KanaiMedical Affairs Division, Kyowa Kirin Co., Ltd., Tokyo, Japan.
Kenta MurotaniSchool of Medical Technology, Kurume University, Kurume-shi, Fukuoka, Japan.
Fumi GomiDepartment of Ophthalmology, Hyogo Medical University, Nishinomiya-shi, Hyogo, Japan.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Intravitreal anti-vascular endothelial growth factor (VEGF) therapy is the standard treatment for neovascular age-related macular degeneration (nAMD) but is invasive and burdensome for patients. To overcome these obstacles, tivozanib, a pan-VEGF receptor inhibitor approved for renal cell carcinoma, is in development as eye drops. The phase 1 study of a 3-week administration of tivozanib eye drops showed a preferable safety profile and exploratory efficacy signs in Japanese patients with nAMD. During eye drop administration, two drug delivery pathways affect ocular pharmacokinetics, either directly through the ocular tissues or through systemic circulation. To assess the ocular pharmacokinetics of tivozanib eye drops, we conducted an integrated analysis of systemic adverse event occurrence and systemic exposure in patients with nAMD treated with tivozanib eye drops and in patients with cancer treated with oral tivozanib, using previous phase 1 study results. Systemic exposure was significantly lower with tivozanib eye drops versus oral tivozanib, with no drug-related hypertension due to the systemic pan-VEGF receptor inhibition observed, suggesting systemic VEGF receptors are not fully inhibited by tivozanib. Exploratory efficacy signs in patients with nAMD after short-term use of tivozanib eye drops also suggest tivozanib might reach the retina and inhibit VEGF receptors, although further long-term efficacy studies are warranted. Given the integrated analysis, we hypothesize that tivozanib eye drops could predominantly be delivered to the posterior eye segment through the ocular tissues, with limited contribution by the systemic drug delivery pathway. This hypothesis provides meaningful insights into the ocular pharmacokinetics of tivozanib eye drops.

Indexed as

ChoroidDrug deliveryEye dropsHypertensionNeovascular age-related macular degenerationPharmacokineticsPosterior eye tissuesReceptors, vascular endothelial growth factorRetinaTivozanib

Identifiers

PMID41987023
PMCPMC13085304

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