2. Academic Validation
  3. AZD4625 is a Potent and Selective Inhibitor of KRASG12C

AZD4625 is a Potent and Selective Inhibitor of KRASG12C

  • Mol Cancer Ther. 2022 Oct 7;21(10):1535-1546. doi: 10.1158/1535-7163.MCT-22-0241.
Atanu Chakraborty # 1,  Lyndsey Hanson # 1,  David Robinson # 1,  Hilary Lewis 1,  Sue Bickerton 1,  Michael Davies 1,  Radoslaw Polanski 1,  Rebecca Whiteley 1,  Alex Koers 1,  James Atkinson 1,  Tamara Baker 1,  Ivan Del Barco Barrantes 1,  Giovanni Ciotta 1,  Jason G Kettle 1,  Lukasz Magiera 1,  Carla P Martins 1,  Alison Peter 1,  Eleanor Wigmore 1,  Zoe Underwood 1,  Sabina Cosulich 1,  Michael Niedbala 2,  Sarah Ross 1
Affiliations

Affiliations

  • 1 AstraZeneca, Cambridge, United Kingdom.
  • 2 AstraZeneca, Waltham, Massachusetts.
  • # Contributed equally.
PMID: 35930755 DOI: 10.1158/1535-7163.MCT-22-0241
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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