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BST-605 is an investigational small molecule prodrug of the chemotherapy agent etoposide, originally developed by Biosight Ltd (now part of Ayala Pharmaceuticals). It is engineered as a stable, water-soluble derivative designed to undergo controlled enzymatic conversion to release active etoposide in the systemic circulation. This controlled-release mechanism is intended to mitigate the high peak plasma concentrations (Cmax) associated with conventional etoposide formulations, which are frequently linked to severe dose-limiting toxicities such as myelosuppression, mucositis, and alopecia. As a topoisomerase II inhibitor, the released etoposide stabilizes the transient covalent complex between the enzyme and DNA, preventing the religation of DNA strands and inducing lethal double-strand breaks. This mechanism triggers cell cycle arrest in the S and G2 phases and subsequent apoptosis in rapidly dividing malignant cells. BST-605 is being evaluated for its potential in treating various hematological malignancies and solid tumors where the therapeutic index of standard etoposide is limited.
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