RO6839921

RO6839921 is an inactive pegylated prodrug of the oral MDM2 antagonist idasanutlin. It was developed to allow intravenous administration by improving solubility and pharmacokinetic properties compared to oral idasanutlin. Upon IV administration, esterases in the blood cleave the pegylated tail of RO6839921, releasing active idasanutlin. The drug acts as an antagonist of MDM2 (mouse double minute-2 homolog), thereby inhibiting the interaction between MDM2 and p53 tumor suppressor protein. This leads to activation of p53-dependent pathways including cell cycle arrest and apoptosis in cancer cells with wild-type TP53. RO6839921 was evaluated primarily for acute myeloid leukemia (AML) in phase 1 clinical trials[1][7][4][2].

Other names

idasanutlin