laigubicin

Laigubicin (also known as legubicin or QHL-108) is a tumor-microenvironment-activated prodrug of doxorubicin developed by Shanghai Affinity Biopharmaceutical. It is designed using the company's proprietary Tumor Microenvironment Activation (TMEA) platform as a peptide-drug conjugate (or small molecule drug conjugate). Laigubicin consists of doxorubicin conjugated to a legumain-cleavable tetrapeptide linker (Ala-Ala-Asn-Leu). In the bloodstream, it binds to albumin, which shields its systemic toxicity. Upon reaching the tumor microenvironment, where the cysteine protease legumain (asparaginyl endopeptidase) is highly expressed by tumor cells and tumor-associated macrophages, the linker is cleaved to selectively release active doxorubicin. This targeted activation significantly reduces systemic toxicities, particularly the dose-limiting cardiotoxicity and hematological toxicity associated with conventional doxorubicin, while enhancing antitumor efficacy. It has completed Phase III clinical trials for advanced soft tissue sarcoma.

Other names

legubicin莱古比星Doxorubicin-LNAA-Boc