monomethyl auristatin F

Monomethyl auristatin F is a **synthetic antineoplastic drug** that acts as a highly potent antimitotic agent by inhibiting tubulin polymerization, thereby preventing cell division[1][2][3][4][7][10]. It is a derivative of dolastatin 10, with the N-terminal amino group containing a single methyl substituent and a charged C-terminal phenylalanine group, reducing cytotoxicity and membrane permeability compared to its uncharged analogue, monomethyl auristatin E[2][4][7][9]. Due to extreme toxicity, MMAF is not used as a standalone pharmaceutical but rather as a **cytotoxic payload** in several antibody-drug conjugates (ADCs) for targeted cancer therapy; in these constructs, MMAF is conjugated to monoclonal antibodies via stable, mostly non-cleavable maleimidocaproyl linkers, which are then cleaved intracellularly to release the payload and induce cell death in tumor cells expressing the target antigen[2][3][4][7][9][10]. MMAF-containing ADCs are undergoing extensive clinical evaluation for indications including multiple myeloma (in belantamab mafodotin), non-Hodgkin’s lymphoma, renal cell carcinoma, glioblastoma, and other solid and hematologic malignancies[4][10].

Other names

auristatin Fdesmethyl-auristatin F