Drug intelligence / Profile preview

BST-605

Development stage
Preclinical
Lead developer
Ayala Pharmaceuticals
Modality
Small Molecules
Administration
Intravenous
01

Overview

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.

Other names
etoposide prodrug
02

Targets

TOP2A (DNA topoisomerase II)

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