CS-7017 + erlotinib

CS-7017 + erlotinib is an investigational **oral combination therapy** for advanced non-small cell lung cancer (NSCLC) and potentially other advanced malignancies. CS-7017 (also known as efatutazone) is a novel, third-generation thiazolidinedione (TZD) and a potent peroxisome proliferator-activated receptor gamma (PPARγ) agonist, showing approximately 50-500 times higher potency than older TZDs. Erlotinib is a small molecule tyrosine kinase inhibitor targeting the epidermal growth factor receptor (EGFR). The combination is based on the rationale that simultaneous modulation of PPARγ and inhibition of EGFR signaling can provide synergistic antitumor effects, including overcoming resistance to EGFR-TKI monotherapy (except in cases with EGFR T790M mutation). Clinical studies have demonstrated evidence of tolerability and preliminary antitumor activity in advanced or refractory NSCLC, with the most common adverse effects being edema, weight gain (attributed mainly to CS-7017), and rash or diarrhea (attributed mainly to erlotinib). Clinical trials have assessed oral efatutazone (CS-7017) at 0.25 to 0.5 mg BID with erlotinib 150 mg QD, demonstrating acceptable safety and partial responses in some patients[3][4][5][7].

Other names

efatutazone + erlotinib