Kyowa Kirin Tivozanib ophthalmic formulation Phase 2 trial preview

Research evidence excerpt

Kyowa Kirin Tivozanib ophthalmic formulation Phase 2 trial preview

safety and pharmacokinetics. From a safety perspective, no serious adverse events were

observed; reversible punctate keratitis was the main adverse event, and given that

tivozanib is already approved, safety concerns appear limited.

From a market perspective, the AMD market is larger than the DME market, and there is

potential for market expansion through ophthalmic formulations. Based on market

reports, the total AMD market is estimated at approximately $18.5bn in 2025, of which

wet AMD accounts for around $11.1bn, while the DME treatment market is estimated

at approximately $4.6bn in 2025. The overall anti-VEGF ophthalmology market is

estimated at approximately $18.2bn in 2025, with Eylea (Regeneron/Bayer) and

Vabysmo (Roche) as the main products.

Why can eye drops reach the retina and choroid?

What is critical for tivozanib is not that nanocrystal particles physically pass through to

the retina intact, but rather that, after instillation, tivozanib gradually dissolves on the

ocular surface and conjunctival side, maintaining a high local concentration of dissolved

molecules and creating a concentration gradient toward the posterior segment as a

drug delivery system (DDS).

Figure 1: Mechanism by which crystal particles increase local dissolved drug

concentration

Mecha nism by w hich crystal pa rticles increase local dissolved

drug con

centration

Source: UBS.

Patent WO2018052053A1 defines the invention as an ophthalmic therapeutic agent

containing a VEGF receptor inhibitor or EGF receptor inhibitor in nanoparticle form that

has the property of remaining in posterior ocular tissues when systemically administered.

Posterior ocular tissues here include the choroid, retina, sclera, and optic nerve,