esperamicin

Esperamicin is a highly potent enediyne antitumor antibiotic being developed by Shanghai Hisun Pharmaceutical Technology as a small molecule payload for antibody-drug conjugates (ADCs). Like other enediynes such as calicheamicin, esperamicin exerts its cytotoxic effect by binding to the minor groove of DNA and undergoing a Bergman cyclization to generate a highly reactive benzenoid diradical. This diradical abstracts hydrogen atoms from the deoxyribose backbone, resulting in site-specific DNA double-strand breaks and subsequent apoptosis. Due to its extreme systemic toxicity as a free agent, it is intended for targeted delivery as an ADC warhead in oncology applications. Shanghai Hisun is currently in the manufacturing development phase, progressing through bench and pilot scales for this compound.

Other names

埃斯培拉霉素esperamicin A1