Chemical formula: C₃₂H₃₅ClFN₇O₂ Molecular mass: 604.119 g/mol PubChem compound: 138611145
Adagrasib is a selective, irreversible inhibitor of KRAS (Kirsten rat sarcoma viral oncogene homolog) G12C that covalently binds to the mutant cysteine in KRAS G12C and locks the mutant KRAS protein in its inactive, GDP-bound conformation, which prevents KRAS-dependent downstream signalling. Adagrasib inhibits tumour cell growth and viability in cells harbouring KRAS G12C mutations and results in regression in KRAS G12C-positive nonclinical tumour models with minimal off-target activity.
This medicinal substance has been classified in the anatomical therapeutic chemical (ATC) classification according to its main therapeutic use as follows:
ATC code | Group title | Classification |
---|---|---|
L01XX77 | L Antineoplastic and immunomodulating agents → L01 Antineoplastic agents → L01X Other antineoplastic agents → L01XX Other antineoplastic agents | |
Competent medicine agencies globally have authorized commercialization of this active ingredient according to these medication package inserts (MPIs):
Title | Information Source | Document Type | |
---|---|---|---|
KRAZATI Film-coated tablet | European Medicines Agency (EU) | MPI, EU: SmPC |
Adagrasib is an active ingredient of these brands:
United States (US)Austria (AT)Croatia (HR)Estonia (EE)Lithuania (LT)Note the following: The list of brand names is continuously updated, and thus does not include the total of products circulating worldwide. |
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