First-in-Human Phase I/IB Dose-Finding Study of Adagrasib (MRTX849) in Patients With Advanced KRAS^G12C Solid Tumors (KRYSTAL-1).

ABSTRACT:

Purpose

Adagrasib (MRTX849) is an oral, highly selective, small-molecule, covalent inhibitor of KRAS^G12C. We report results from a phase I/IB study of adagrasib in non-small-cell lung cancer, colorectal cancer, and other solid tumors harboring the KRAS^G12C mutation.

Materials and methods

Patients with advanced KRAS^G12C-mutant solid tumors were treated with adagrasib 150 mg orally once daily, 300 mg once daily, 600 mg once daily, 1,200 mg once daily, or 600 mg orally twice a day using an accelerated titration design, which transitioned to a modified toxicity probability interval design when a predefined degree of toxicity was observed or target adagrasib exposure was achieved. Safety, pharmacokinetics, and clinical

SUBMITTER: Ou SI 

PROVIDER: S-EPMC9362872 | biostudies-literature | 2022 Aug

REPOSITORIES: biostudies-literature