Drug intelligence / Profile preview

dolastatin 10

Development stage
Phase 2
Lead developer
Arizona State University
Modality
Peptides, Small Molecules
Administration
Intravenous
01

Overview

Dolastatin 10 is a highly potent antineoplastic pentapeptide originally isolated from the marine mollusk Dolabella auricularia. It acts as a microtubule inhibitor by binding to tubulin, inhibiting microtubule assembly, and causing the formation of tubulin aggregates, which leads to mitotic arrest and apoptosis in cancer cells. Dolastatin 10 exhibits strong cytotoxicity at nanomolar concentrations against various tumor cell lines, including lymphoma and other cancers. Although it showed promising preclinical activity, clinical trials were limited by toxicity and lack of efficacy separation; however, its structure has served as the basis for several approved antibody-drug conjugates (ADCs) such as monomethyl auristatin E (MMAE) payloads[1][2][4][6].

Other names
dolastatin 10dolastatin10dolastatin-10
02

Targets

TUBB (Tubulin (alpha and beta subunits))

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