GP-2250 + gemcitabine

GP-2250 + gemcitabine is an investigational combination therapy under clinical evaluation for advanced pancreatic cancer. GP-2250 is a small molecule analog of taurultam developed as a selective anti-neoplastic agent that disrupts cancer cell energy metabolism by inhibiting hexokinase 2 (HK2) and glyceraldehyde-3-phosphate dehydrogenase (GAPDH), reducing ATP production and inducing oxidative, metabolic, and hypoxic stress exclusively in cancer cells[1][3][5]. GP-2250 also inhibits transcription factor NF-κB, downregulating cell proliferation genes and inducing apoptosis. Gemcitabine is a nucleoside analog and DNA synthesis inhibitor, and the combination exploits synergy to enhance cytotoxicity and overcome tumor resistance to gemcitabine. This combination is being evaluated in phase I clinical trials for subjects with advanced pancreatic cancer, particularly after prior 5-fluorouracil-based chemotherapy[3][7]. The anticipated mechanism brings together GP-2250’s metabolic and transcriptional disruption with gemcitabine’s cytotoxic effect[1][3][7].

Other names

misetionamide + gemcitabine