Prodrug strategies have been widely used to modify distribution and improve the delivery of active pharmacological agents to the cancerous target tissues. Researchers from Johns Hopkins Medicine have discovered a prodrug called DRP-104 (sirpiglenastat), which has shown that augmented drugs preferentially eliminate cancer cells without harming the healthy cells. The research aimed to modify an old cancer drug that had shown efficacy but was toxic in the gut. The study team utilized a novel chemistry design (adding promoieties) to create a prodrug that was bioactivated in cancer cells while simultaneously being inactivated in healthy tissues like the gut.
Researchers gave the original DON (6-Diazo-5-Oxo-L-norleucine) drug and DRP-104 drug to mice implanted with tumors . The mice receiving DRP-104 reported 11 times more active drug in the tumor than in the gut. Both DON and DRP-104…
