ProLynx extends lead in half-life extension platform technology – Shows primary deuterium kinetic isotope effects prolong drug release and polymer biodegradation in a drug delivery system

SAN FRANCISCO, April 03, 2018 -- ProLynx announced today the publication of a paper demonstrating its leading capabilities to exploit primary deuterium kinetic isotope effects (1°DKIEs) for prolonging in vivo drug release and polymer degradation.  In contrast to studies of 1°DKIEs that modify in vivo properties of individual drugs, ProLynx is the first to exploit their use in a platform technology that is generally applicable in modifying the pharmacokinetic behavior of multiple drugs.  Published in the Journal of Controlled Release, the paper describes methods to prepare deuterated linkers, assessment of the in vitro primary deuterium kinetic isotope effects that occur upon β-elimination and provides examples of such isotope effect for extending in vivo drug release and polymer degradation.

Daniel Santi, cofounder, stated, “We continue to push for simple and durable ways to more effectively deliver native drug through our half-life extension platform technology.  The addition of deuterated linkers to our system enables a nearly 3-fold increase on the already long half-lives we can deliver.”  Santi added, “we’re excited about the flexibility this gives us to fine-tune rates at which drug is released while dialing in the desired biodegradation rate of the drug’s hydrogel carrier.”

Previous work suggested that the rate determining step of the β-elimination involved cleavage of the carbon-hydrogen bond (C-H) and indicated that the electron withdrawing group modifies the kinetic controlled acidity of the C-H bond.  This led ProLynx to expect a 1°DKIE in the β-elimination, and by incorporating deuterium atoms in the α-carbon of its linkers, a simple process to attenuate the rate of drug release or hydrogel degradation has been achieved both in vitro and in vivo. 

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~SN38, in Phase 1 clinical trials.  Further information about the company may be found at www.ProLynxllc.com.

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