Developing next generation treatments to preserve vision for patients with diseases affecting the back of the eye

Oxurion NV - Journal of Pharmacokinetics and Pharmacodynamics highlights desirable PK/PD profiles of THR-687 and THR-149

THR-149 and THR-687 show targeted activity in the eye following intravitreal injection with low systemic exposure Novel pharmacokinetic models developed by Oxurion may have broad utility to analyze systemic exposure of a wide variety of drugs delivered
16 Aug 2021

Leuven, BE, Boston, MA, US – August 16, 2021 – 8.00 AM CET – Oxurion NV (Euronext Brussels: OXUR), a biopharmaceutical company developing next generation standard of care therapies for retinal vascular disorders, announces the publication of two related papers in the Journal of Pharmacokinetics and Pharmacodynamics entitled“Systemic exposure following intravitreal administration of therapeutic agents: an integrated pharmacokinetic approach.”

These papers describe the pharmacokinetic properties of THR-149 and THR-687 following intravitreal (IVT) injection in animals and utilize novel pharmacokinetic models developed by Oxurion to accurately assess the systemic levels of these exciting novel drug candidates, which are both in clinical development for diabetic macular edema (DME).

THR-149 is a plasma kallikrein inhibitor being developed as a potential new standard of care for the 40-50% of DME patients showing suboptimal response to anti-VEGF therapy. With that, THR-149 holds potential to grow the existing $4.5B DME market.

THR-687 is a pan-RGD integrin antagonist initially being developed as a potential first line therapy for treatment of DME patients. In addition, Oxurion believes that THR-687 could deliver improved clinical outcomes to the large number of patients with wet age macular degeneration (AMD) and retinal vein occlusion (RVO) which together with DME represents a >$12B market opportunity.

IVT injection remains the preferred route of administration for pharmacological agents intended for the treatment of back of the eye diseases such as diabetic macular edema (DME) and neovascular age-related macular degeneration (wet AMD).  The procedure enables drugs to be delivered locally at high concentrations whilst limiting systemic exposure and associated risk of systemic adverse events.

Intravitreally-delivered drugs do, however, enter the general circulation and achieving an accurate understanding of systemic exposure as enabled by these new pharmacokinetic models is pivotal for the evaluation and development of drugs administered in the eye. 

Prof Alan Stitt, Ph.D., Chief Scientific Officer (CSO) of Oxurion, said, “These publications in the Journal of Pharmacokinetics and Pharmacodynamics underline the highly attractive clinical profiles of both THR-149 and THR-687. Both compounds show a short intravitreal half-life but sustained biological activity with low systemic exposure due to their rapid clearance. This enables targeted activity in the eye combined with minimal risk of systemic side effects. The animal models and analytical techniques that we have developed have proven accurate in predicting circulating plasma levels of these novel drug candidates following intravitreal injection, and potentially have broad predictive value for a variety of therapeutics administered by IVT. These publications reflect the calibre and thought leadership of the high-quality science that we are generating at Oxurion.”

Articles can be accessed at:

https://link.springer.com/article/10.1007/s10928-021-09773-w

https://link.springer.com/article/10.1007/s10928-021-09774-9