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CS-7017 + FOLFIRI is a combination therapy developed by Daiichi Sankyo for the treatment of metastatic colorectal cancer (mCRC). The combination consists of efatutazone (CS-7017), a novel, third-generation oral small molecule agonist of the peroxisome proliferator-activated receptor gamma (PPARγ), and the standard chemotherapy regimen FOLFIRI. FOLFIRI is a combination of irinotecan (a topoisomerase I inhibitor), 5-fluorouracil (a thymidylate synthase inhibitor), and leucovorin (a biochemical modulator of 5-fluorouracil). Efatutazone works by binding to PPARγ, a nuclear receptor that regulates gene expression involved in cell differentiation, growth, and apoptosis, thereby exerting anti-cancer effects. This combination was evaluated in a Phase 2 clinical trial (NCT00967616) in patients with mCRC who had failed first-line therapy, but development for this indication was subsequently discontinued.
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