Drug intelligence / Profile preview

auristatin E

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

Overview

Auristatin E is a potent cytotoxic tubulin modifier and a synthetic analog of the marine natural product dolastatin 10. It exerts its antitumor activity by binding to tubulin and inhibiting its polymerization, which disrupts the formation of the mitotic spindle during cell division. This leads to cell cycle arrest in the G2/M phase and subsequent apoptosis. Because of its high systemic toxicity, auristatin E is primarily utilized as a cytotoxic payload in the design of antibody-drug conjugates (ADCs) rather than as a standalone therapeutic. It is a linear peptide consisting of four amino acids and has been extensively studied for its efficacy against various cancers, including B-cell malignancies.

Other names
AECAS 160800-57-7CAS160800-57-7CAS-160800-57-7
02

Targets

TUBB (Tubulin (alpha and beta subunits))

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