Cerulean’s lead candidate, CRLX101, appears to have overcome the liabilities of its payload, camptothecin, a highly potent anti-cancer agent that was discovered in the 1960s, but was not tolerable enough to be developed past Phase 1 clinical trials. Two less potent derivatives of camptothecin—irinotecan and topotecan—were subsequently developed, approved, and commercialized. But the original, most-potent member of the class remained undeveloped until it was incorporated into a nanopharmaceutical to create CRLX101.COMBINATION THERAPIESCRLX101 is designed to be a dual inhibitor of topoisomerase 1 and hypoxia-inducible factor-1 alpha (commonly referred to as HIF-1α). We are evaluating CRLX101 in clinical trials in multiple tumor types and believe that exploration of additional tumor types is warranted given CRLX101’s pan-tumor relevance.

HIF snip 3.17.14

Clinical development program

CRLX101 is being studied in combination with other cancer therapies. 

CRLX101 Snip 3.31.14

For more information about Cerulean’s ongoing clinical trials, please visit