Drug intelligence / Profile preview

adagrasib

Development stage
Approved
Lead developer
Bristol Myers Squibb
Modality
Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral
01

Overview

Adagrasib is an oral small molecule antineoplastic drug that acts as a covalent, irreversible inhibitor of the KRAS G12C mutant protein. By binding specifically to the mutant cysteine in KRAS G12C, adagrasib locks the protein in its inactive GDP-bound state and prevents downstream signaling that drives cancer cell proliferation. This selectivity spares wild-type KRAS and minimizes off-target effects. Adagrasib is primarily indicated for adults with locally advanced or metastatic non-small cell lung cancer (NSCLC) harboring a KRAS G12C mutation who have received at least one prior systemic therapy. It is also approved in combination with cetuximab for metastatic colorectal cancer (CRC) with a KRAS G12C mutation after prior treatment[1][2][4][5][6][7]. The drug was developed by Mirati Therapeutics.

Brand names
Krazati
Other names
compound 20compound20compound-20
02

Targets

KRASG12C (Kirsten rat sarcoma viral oncogene homolog G12C)

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