Novel long-acting opthamology drugs

PASylation® in Ophthalmology

Back of the eye disorders are not accessible by systemic drugs and require intravitreal (IVT) injection. Drugs directly injected into the eye often suffer from a fast clearance and require frequent injection, which is a burden to patients and physicians. While a correlation between in intravitreal half-life and macromolecular size has been shown with PEGylated proteins, PEG is also known to activate the complement in the eye.

PASylation®, a biological alternative to PEGylation, is a superior technology to design intravitreal long-acting drugs to treat back of the eye diseases and to improve patient’s quality of life. The hydrated, disordered PAS polypeptide chain adopts an expanded hydrodynamic volume and strongly increases the intraviteal half-life of the therapeutic. There is no need for a potential inflammatory Fc-part. Furthermore, PAS fusion proteins can be produced in a cheap way, at high yield using industry-leading expression technology platforms. In addition, PAS can be can be utilized as a linker to generate innovative 3rd generation biologics with bi- or multispecificity.

Together with our partners, among Akari Therapeutics, we meanwhile developed 3 different PASylated ophthalmology drugs to prevent and treat the leading causes of blindness.

  • Expanded hydrodynamic volume

    • Slow vitreal clearance
    • Reduced injection frequencies
  • No Fc region, no PEG

    • No inflammatory mediator
    • No complement activation
    • Excellent patient compliance
  • Genetic PAS fusion enables:

    • Creation of bi-/multispecifics
    • Cheap manufacturing
    • Homogenous product

Akari’s CEO talks about PASylated Nomacopan:

  • Related publications & press releases

    Eskandarpour M., Chen Y.H., Nunn M.A., Coupland S.E., Weston-Davies W., Calder V.L. (2021) Leukotriene B 4 and Its Receptor in Experimental Autoimmune Uveitis and in Human Retinal Tissues: Clinical Severity and LTB 4 Dependence of Retinal Th17 Cells. Am. J. Pathol. 191, 320-334.

  • Eskandarpour M., Nunn M.A., Weston-Davies W., Calder V.L. (2021) Immune-Mediated Retinal Vasculitis in Posterior Uveitis and Experimental Models: The Leukotriene (LT)B4-VEGF Axis
    Cells 10, 396.

  • NEW YORK and LONDON, Feb. 25, 2021 (GLOBE NEWSWIRE): Akari Therapeutics Presents New Preclinical Data Highlighting Potential of Long-Acting PASylated Nomacopan to Treat Retinal Diseases, Including Age-Related Macular Degeneration (AMD) and Uveitis