News Article

ProLynx and Daiichi Sankyo announce the development of technology for half-life extension of small molecules in the eye
Date: Aug 29, 2018
Source: GlobeNewswire ( click here to go to the source)

Featured firm in this article: Prolynx LLC of San Francisco, CA

DaiSAN FRANCISCO, Aug. 29, 2018 (GLOBE NEWSWIRE) -- ProLynx and Daiichi Sankyo Company, Limited, announced today the publication of a paper in the journal TVST entitled "A controlled release system for long-acting intravitreal delivery of small molecules". In this work, they described a technology to extend the intravitreal half-life of small molecule drugs to rival the intravitreal half-lives of macromolecules such as antibodies and PEGylated aptamers.

Intravitreal (IVT) injection is an important drug delivery modality for many diseases of the eye. IVT injection minimizes systemic exposure and allows intraocular drug exposures not otherwise achievable. However, because IVT therapy is an invasive procedure that often requires long-term serial injections, IVT drugs require long IVT half-lives and dosing intervals.

In the past, IVT injections of small molecule therapeutics have been impractical for treatment of chronic eye diseases because they have short half-lives in the vitreous and require frequent injections. In the present work a small molecule drug was attached to a nanomolecular 40kDa PEG via a cleavable linker. The large nanomolecule maintains the small molecule in the vitreous for long periods, and the attached drug is slowly released by a self-cleaving linker. Using this approach, the half-life of a small molecule complement factor D inhibitor in the rabbit eye was prolonged 10-fold. It was posited that the technology could maintain a small molecule drug in the human vitreous for periods comparable to macromolecular drugs, requiring intravitreal injections at about one month intervals.

Daniel Santi, co-founder and President of ProLynx, stated "This study reports an entirely new approach for increasing the intravitreal half-lives of small molecule therapeutics; a potent small molecule with an appropriate therapeutic window should be administrable by intravitreal injections in the human at once-monthly intervals."

About ProLynx: ProLynx LLC is a privately held biotechnology company located in San Francisco, CA, developing proprietary controlled release systems for long-acting delivery of small molecules, peptides and proteins. The company applies its technology to extend half-lives and improve properties of the drug candidates of pharmaceutical companies as well as to enhance properties of off-patent therapeutics. ProLynx has a monthly GLP-1 receptor agonist and a subcutaneous long-acting octreotide in its pre-clinical portfolio, and a DNA-damage response enhancer, PEG~SN-38, in Phase 1 clinical trials. For more information, please visit:

About Daiichi Sankyo: Daiichi Sankyo is dedicated to the creation and supply of innovative pharmaceutical products to address unmet medical needs of patients. With over 100 years of scientific expertise and a presence in more than 20 countries, Daiichi Sankyo draws upon a rich legacy of innovation and a robust pipeline of new medicines. In addition to a strong portfolio of medicines for hypertension and thrombotic disorders, Daiichi Sankyo research and development is focused on bringing forth novel therapies in oncology, and new horizon areas such as pain management, neurodegenerative diseases, heart and kidney diseases, and rare diseases. For more information, please visit: or 805-558-0361