Drug intelligence / Profile preview

auristatin F

Development stage
Preclinical
Lead developer
Pfizer
Modality
Small Molecules
Administration
Intravenous
01

Overview

Auristatin F is a potent synthetic cytotoxic small molecule and a member of the auristatin family, derived from the natural product dolastatin 10. It acts as a microtubule inhibitor by binding to tubulin and inhibiting its polymerization, which leads to cell cycle arrest and apoptosis. Structurally, it is closely related to monomethyl auristatin F (MMAF) but features two methyl substituents on the N-terminal amino group. In addition to its antimitotic effects, auristatin F functions as a vascular damaging agent (VDA). Due to its extreme systemic toxicity, auristatin F is primarily utilized as a cytotoxic payload in the development of antibody-drug conjugates (ADCs) for targeted cancer therapy, where it is linked to monoclonal antibodies to ensure selective delivery to malignant cells.

Other names
CAS 163768-50-1CAS163768-50-1CAS-163768-50-1
02

Targets

TUBB (Tubulin (alpha and beta subunits))

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