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.CRLX101 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. 


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