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MMAF is a highly potent antimitotic agent [1].

MMAF is an auristatin F (AF) derivative and is used as an antimitotic drug in the form of antibody drug conjugates (ADCs). It is reported that both the N-terminal monomethylvaline and the C-terminal carboxyl group of MMAF can be attached to the linker. Dipeptide linkers used for the attachment of MMAF to mAbs result in conjugates pronounced and potent activities against an array of tumor types. In the in vitro cytotoxicity assays, the ADC generated by attaching MMAF to the 1F6 mAb shows a potent inhibition to the cell viability with IC50 values of 10ng/ml, 8ng/ml, and 123ng/ml in 786-O, Caki-1 and L428 cell lines, respectively. Moreover, it is reported that the dipeptide linker attached to MMAF with C-terminal amino acids could modulate the efficacy, potency, and tolerability. The manipulation of the C-terminal peptide sequence leads to the improved potency, specificity and therapeutic windows of the conjugates [1].

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