- AZD4625 is a Potent and Selective Inhibitor of KRASG12C.
AZD4625 is a Potent and Selective Inhibitor of KRASG12C.
Molecular cancer therapeutics (2022-08-06)
Atanu Chakraborty, Lyndsey Hanson, David Robinson, Hilary Lewis, Sue Bickerton, Michael Davies, Radoslaw Polanski, Rebecca Whiteley, Alex Koers, James Atkinson, Tamara Baker, Ivan Del Barco Barrantes, Giovanni Ciotta, Jason G Kettle, Lukasz Magiera, Carla P Martins, Alison Peter, Eleanor Wigmore, Zoe Underwood, Sabina Cosulich, Michael Niedbala, Sarah Ross
PMID35930755
ABSTRACT
AZD4625 is a potent, selective, and orally bioavailable inhibitor of oncogenic KRASG12C as demonstrated in cellular assays and in vivo in preclinical cell line-derived and patient-derived xenograft models. In vitro and cellular assays have shown selective binding and inhibition of the KRASG12C mutant isoform, which carries a glycine to cysteine mutation at residue 12, with no binding and inhibition of wild-type RAS or isoforms carrying non-KRASG12C mutations. The pharmacology of AZD4625 shows that it has the potential to provide therapeutic benefit to patients with KRASG12C mutant cancer as either a monotherapy treatment or in combination with other targeted drug agents.
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