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legusitaxel
- Development stage
- Unknown
- Lead developer
- Shanghai Affinity Biopharmaceutical
- Modality
- Peptide-Drug Conjugates → Peptide Conjugates → Peptides, Small Molecules
- Administration
- Intravesical, Intravenous
01
Overview
Legusitaxel (also known as legutaxel or QHL-236) is a tumor microenvironment-activated small molecule-drug conjugate (SMDC) developed by Shanghai Affinity Biopharmaceutical. It consists of the microtubule-stabilizing agent paclitaxel conjugated to a legumain-cleavable peptide linker (Ala-Ala-Asn). Legumain (asparaginyl endopeptidase) is an enzyme highly expressed in the tumor microenvironment of various solid tumors, including bladder cancer. By utilizing this tumor-specific enzyme, legusitaxel remains inactive in systemic circulation, thereby reducing the systemic toxicities typically associated with paclitaxel (such as myelosuppression and peripheral neuropathy). Upon reaching the tumor microenvironment, legusitaxel is cleaved by legumain to release active paclitaxel locally, enhancing therapeutic efficacy and expanding the safety window. Legusitaxel is being evaluated in clinical trials for the treatment of non-muscle-invasive bladder cancer (via intravesical instillation) and other solid tumors.
- Other names
- legufaniblegutaxel注射用莱古杉醇莱古杉醇
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