Adagrasib (1 brand name, 1 dosage form, 1 route)
Available dosage forms: TABLET.
Routes of administration: ORAL.
Brand Names
- KRAZATI
Contraindications
None.
Adverse Reactions
The following clinically significant adverse reactions are described elsewhere in the labeling: •Gastrointestinal Adverse Reactions [see Warnings and Precautions (5.1)] •QTc Interval Prolongation [see Warnings and Precautions (5.2)] •Hepatotoxicity [see Warnings and Precautions (5.3)] •Interstitial Lung Disease (ILD)/Pneumonitis [see Warnings and Precautions (5.4)]
Mechanism of Action
Adagrasib is an irreversible inhibitor of KRAS G12C that covalently binds to the mutant cysteine in KRAS G12C and locks the mutant KRAS protein in its inactive state that prevents downstream signaling without affecting wild-type KRAS protein. Adagrasib inhibited tumor cell growth and viability in cells harboring KRAS G12C mutations and resulted in tumor regression in KRAS G12C-mutated tumor xenograft models with minimal off-target activity. Adagrasib in combination with cetuximab had increased antitumor activity in some cell line-derived and patient-derived KRAS G12C-mutant CRC tumor xenograft models compared to adagrasib or cetuximab alone.