Drug intelligence / Profile preview

isofludelone

Development stage
Phase 1
Lead developer
Memorial Sloan Kettering Cancer Center
Modality
Small Molecules
Administration
Intravenous
01

Overview

Isofludelone is a synthetic third-generation epothilone drug discovered at Memorial Sloan Kettering Cancer Center. It functions as a tubulin inhibitor, promoting microtubule polymerization and stabilizing microtubules against depolymerization. This action disrupts normal cell division, leading to G2/M arrest and inducing apoptosis in cancer cells. Isofludelone exhibits potential anti-mitotic and antineoplastic activities. Compared to earlier epothilones, it offers increased stability, water solubility, potency, duration of action, and tumor penetration, alongside reduced toxicity. Notably, it is not a substrate for P-glycoprotein (P-gp), which helps in overcoming multidrug resistance. It is primarily indicated for the treatment of neoplasms, specifically advanced solid tumors.

Other names
iso-fludelone
02

Targets

TUBB (Tubulin (alpha and beta subunits))

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