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**Locnartecan (PEN-866)** is an investigational miniature drug conjugate designed for cancer therapy, consisting of the irinotecan metabolite **SN-38** (7-ethyl-10-hydroxycamptothecin) linked via a cleavable linker to an **HSP90** chaperone protein ligand. Developed by **Tarveda Therapeutics**, it selectively targets **HSP90**, which is upregulated in tumor cells, enabling tumor-specific accumulation, sustained **SN-38** release, and inhibition of **topoisomerase I** to induce DNA damage and apoptosis. It is being evaluated in clinical trials for various solid tumors, offering improved efficacy and reduced toxicity compared to free SN-38 due to preferential tumor retention.
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