technologies > prodrug technologies

Prodrug Technologies

TSRL's proprietary prodrug technology enables the development of unique orally available prodrugs for individual therapeutic candidates. Prodrugs are optimized for oral bioavailability by utilizing intestinal carrier proteins, such as the dipeptide transporter (hPEPT1), as a shuttle. Drug candidates that are inherently not capable of crossing intestinal membranes to any appreciable extent can thereby reach oral bioavailability levels of 20-50%. This opens up a large market for the convenient oral delivery of potent therapeutics which currently have to be administered parenterally. This strategy also functions as an effective means of lifecycle extension through creation of novel chemical matter patents.

We use our understanding of intestinal physiology and associated molecular biology to enable identification of prodrug moieties that will uniquely benefit an individual drug candidate. Prodrug synthesis is based on well established chemical synthesis processes and projected costs of goods are low. Also, since the drug candidates may already be marketed as a parenteral product, the development program of the prodrug may rely to some extent on existing toxicology information. Safety profiles can therefore be projected based on pharmacokinetic comparisons with the existing parenteral formulations, which will allow for a shorter and more focused toxicology strategy.