RS-0139

RS-0139 is a tumor-targeted docetaxel-releasing prodrug developed using the Sagitta™ platform technology. It consists of docetaxel (DTX) covalently bound to a water-soluble polymeric carrier backbone via a short peptide, which releases only upon entry to the cell via endocytosis. The carrier is equipped with a targeting peptide showing high affinity to αvβ3, αvβ5, and αvβ6 integrin receptors that are highly expressed on tumor cells. This targeted delivery approach aims to reduce toxicity while maximizing efficacy compared to conventional docetaxel. RS-0139 demonstrates enhanced aqueous solubility, improved pharmacokinetic profile with a 5-fold increase in half-life, and superior tolerability in preclinical studies.