TG100801 a prodrug version of TG100572, is administered noninvasively as an eye drop and is designed to suppress VEGF mediated leakage and additionally the kinase targets associated with inflammation, edema, and angiogenesis which are the pathological hallmarks of AMD and of other back of the eye diseases including diabetic macular oedema and proliferative diabetic retinopathy⁽²⁵⁾.

It is synthesized at TargeGen (TargeGen inc San Diego).

Topical administration of TG100801 suppressed CNV in mice and reduced the retinal oedema induced by retinal vein occlusion in rats, without observable safety issues.

Data have suggested that the delivery of these agents occur by local penetration through sclera rather than by systemic absorption as neither compound was detectable in the plasma⁽²⁴⁾.

Therefore, TG100801 may offer equal efficacy to injectable agents, while offering the convenience and potential safety advantages due to a non-invasive route of delivery and eye penetration.

Currently a multicentric, open-label, randomized, phase II study is evaluating the effects of 30 days of dosing with two dose levels of TG100801, instilled twice a day, on central retinal/lesion thickness, as measured by optical coherence tomography (OCT).

The safety of TG100801 in patients with AMD will also be evaluated in this trial⁽²⁶⁾.