cyclosporine + irinotecan

Cyclosporine + irinotecan is an investigational combination therapy involving the immunosuppressant cyclosporine and the topoisomerase I inhibitor irinotecan. This combination has been studied primarily in patients with metastatic colorectal cancer, particularly those refractory to fluorouracil-based regimens. The rationale for combining these agents is based on pharmacokinetic modulation; cyclosporine inhibits certain drug transporters (notably ABC transporters such as P-glycoprotein) and enzymes (such as UGT1A1), which can increase systemic exposure to irinotecan and its active metabolite SN-38, potentially enhancing antitumor activity but also altering toxicity profiles[1][3][5]. Irinotecan acts by inhibiting DNA topoisomerase I, leading to DNA damage in rapidly dividing tumor cells[4]. Cyclosporine is a calcineurin inhibitor that suppresses T-cell activation by blocking IL-2 transcription[7]. Clinical studies have explored this combination to improve therapeutic index or overcome resistance mechanisms in colorectal cancer[3][6].

Other names

cyclosporine/irinotecan