indisulam + irinotecan

**Indisulam + irinotecan** is an investigational combination of two small molecule chemotherapeutic agents. **Indisulam** (E7070) is a sulfonamide cell cycle inhibitor that selectively targets the RNA splicing factor RBM39 for proteasomal degradation through interaction with the DCAF15-E3 ubiquitin ligase[5][6]. This leads to widespread splicing errors, cell cycle arrest, and apoptosis. **Irinotecan** (CPT-11) is a topoisomerase I inhibitor that, after conversion to its active metabolite SN-38, prevents DNA religation during replication, inducing cytotoxic DNA damage. Co-administration of indisulam and irinotecan has demonstrated synergistic antitumor effects in preclinical human colorectal cancer models, with indisulam suppressing SN-38-induced upregulation of topoisomerase IIα, thereby enhancing irinotecan cytotoxicity[1]. This combination’s mechanism represents a dual attack: indisulam impairs cell cycle and splicing, while irinotecan causes DNA damage in dividing cells. The combination has been advanced to clinical evaluation for solid tumors, particularly colorectal cancer[1].

Brand names

CamptosarOnivydeCampto

Other names

indisulam + irinotecan