KRASG12D Inhibitor

MRTX1133

MRTX1133 is an investigational, highly selective and potent small molecule inhibitor of KRASG12D designed to treat patients with high unmet need.

MRTX1133

MRTX1133 is an investigational, highly selective and potent small molecule inhibitor of KRASG12D designed to treat patients with high unmet need.

Mechanism of Action

Mirati is developing investigational drug candidate, MRTX1133, which is optimized to inhibit KRASG12D and has the potential to be a first-in-class therapeutic.

In preclinical studies, MRTX1133 exhibited an ability to bind the KRAS G12D protein in both active and inactive states, and selectively inhibit KRASG12D mutant, but not KRAS wild-type, tumor cells.

Preclinical studies of MRTX1133 demonstrated key characteristics including:

Potent

Low nanomolar potency across multiple cellular models of KRASG12D13

Long half-life

Predicted ~ 50-hour half-life13

Highly selective

1,000+ fold selective for mutant KRASG12D vs wild-type KRAS13

MRTX1133 demonstrates dose-dependent inhibition of the KRAS pathway tumor regression in G12D mutant tumor models, and increased activity when combined with rational combination partners.