PF-06264490

PF-06264490 is the released payload (active moiety) of antibody-drug conjugates using a non-cleavable maleimidocaproyl (mc) linker conjugated to monomethylauristatin F (MMAF). It is formed intracellularly during the catabolism of the antibody-drug conjugate (such as PF-06263507) and is responsible for the cytotoxic effect. MMAF is a fully synthetic auristatin that inhibits tubulin polymerization, leading to G2/M phase cell cycle arrest and cell death at picomolar concentrations. PF-06264490 is active in vitro and in vivo (as part of an ADC), showing equivalent activity to MMAF in tubulin polymerization inhibition assays. It is being explored as a component of ADCs designed to treat solid tumors expressing specific tumor-associated antigens such as 5T4[1].

Other names

Cys–mcMMAF