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Drug intelligence / Profile preview
cys-monomethyl auristatin F
- Development stage
- Unknown
- Lead developer
- Skagen
- Modality
- Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Intravenous, Intramuscular, Intradermal, Intraperitoneal, Subcutaneous
01
Overview
cys-monomethyl auristatin F is a synthetic antineoplastic agent and a potent inhibitor of tubulin polymerization, leading to cell cycle arrest and apoptosis. It is derived from dolastatin 10. Due to its high toxicity, it cannot be used as a standalone drug and is primarily employed as a cytotoxic payload within Antibody-Drug Conjugates (ADCs). The "cys" prefix indicates a cysteine-linked form, often through a maleimidocaproyl (mc) linker, which is the active species released from certain ADCs upon internalization into cancer cells.
- Other names
- Monomethylauristatin Fcysteine maleimidocaproyl monomethyl auristatin F
02
Targets
TUBB (Tubulin (alpha and beta subunits))
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