Adagrasib
Adagrasib is a targeted cancer therapy that specifically inhibits the KRAS G12C mutant protein, which is implicated in tumor growth and progression. It is indicated for the treatment of adults with KRAS G12C-mutated locally advanced or metastatic non-small cell lung cancer who have received at least one prior systemic therapy.
Adagrasib is a KRAS G12C inhibitor used to treat KRAS G12C-mutated non-small cell lung cancer by irreversibly binding to and inactivating the mutant KRAS protein.
Key facts at a glance
- ATC
- L01XX77
- RxNorm
- 2625882
- Generic
- Adagrasib
- Class
- atc-l01
- Brands
- Krazati
- Availability
- rx
- Lactation
- unknown
- Routes
- oral
- Forms
- tablet
- Regions
- US, EU, CN, JP
- Monitoring
- —
This page is for informational purposes only.
Do not use this information to diagnose yourself or to replace a physician's advice. Always consult a qualified healthcare provider before starting, stopping, or changing any medication. If you believe you are experiencing a medical emergency, call your local emergency number immediately.
Dosage and administration
- Usual dose
- 600mg once daily
- Maximum
- consult physician
- Frequency
- once daily
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
Overdose information
Special Populations
12 groupspregnancy
first trimesteravoid if possible
avoid use during pregnancy unless benefits outweigh risks to the fetus
regular fetal monitoring and ultrasound assessments
Use of this medication in this population requires careful consideration of risks and benefits.
pregnancy
second trimesteravoid if possible
avoid use during pregnancy unless benefits outweigh risks
regular fetal monitoring
Use of this medication in this population requires careful consideration of risks and benefits.
pregnancy
third trimesteravoid if possible
avoid use during pregnancy unless benefits outweigh risks
regular fetal monitoring and assessment of fetal well-being
Use of this medication in this population requires careful consideration of risks and benefits.
lactation
breastfeedingcontraindicated
discontinue breastfeeding during treatment and for at least 1 week after last dose
not applicable
Use of this medication in this population requires careful consideration of risks and benefits.
geriatric
elderly over 65no initial dose adjustment required
use standard dosing; monitor for adverse reactions including nausea, diarrhea, and fatigue
regular monitoring of renal and hepatic function
Use with caution and monitor for adverse effects.
pediatric_age
children under 18not established
not approved for use in pediatric patients; safety and efficacy not established
not applicable
renal_impairment
mildno dose adjustment recommended
no dose adjustment needed for mild renal impairment (CrCl 60-89 mL/min)
routine renal function monitoring
renal_impairment
moderateconsider close monitoring
use with caution in moderate renal impairment (CrCl 30-59 mL/min); monitor for increased adverse effects
regular monitoring of renal function and adverse effects
Use with caution and monitor for adverse effects.
renal_impairment
severenot studied
use with caution; no dosing recommendations available for severe renal impairment (CrCl <30 mL/min)
frequent renal function monitoring and adverse event assessment
Use with caution and monitor for adverse effects.
hepatic_impairment
mildno dose adjustment recommended
no dose adjustment needed for mild hepatic impairment (Child-Pugh A)
routine liver function monitoring
Use with caution and monitor for adverse effects.
hepatic_impairment
moderateconsider dose reduction
use with caution in moderate hepatic impairment (Child-Pugh B); consider dose reduction
regular monitoring of liver function tests
Use with caution and monitor for adverse effects.
hepatic_impairment
severenot recommended
not recommended for use in severe hepatic impairment (Child-Pugh C)
not applicable
Use of this medication in this population requires careful consideration of risks and benefits.
Statistics and clinical data
Drug class
Targeted therapy for KRAS G12C mutated cancers
FDA approval date
Initial FDA approval for Adagrasib
Approved indication
Therapeutic indication for adult patients
Brand name
Commercial brand name for Adagrasib
Treatment of adults with KRAS G12C-mutated locally advanced or metastatic non-small cell lung cancer (NSCLC) who have received at least one prior systemic therapy.
Adagrasib is an irreversible (covalent) inhibitor that binds specifically to the mutant cysteine residue in KRAS G12C, locking the protein in its inactive GDP-bound state and preventing downstream oncogenic signaling pathways, without affecting normal wild-type KRAS function.
Adagrasib may cause serious adverse effects including hepatotoxicity, gastrointestinal toxicity (diarrhea, nausea, vomiting), and QT prolongation. Patients should be monitored for these toxicities. Drug interactions may occur with CYP3A4 substrates and other QT-prolonging agents. Efficacy depends on confirmed KRAS G12C mutation status prior to treatment initiation.
Contraindications
Conditions and patient states where this medication should be avoided or used with caution.
Do not use (1)
Known allergy to this medication or its components
Use caution (1)
Consult healthcare provider for benefits vs risks assessment
Official drug label
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This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment.
This content is for general informational and educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the guidance of a qualified healthcare provider with any questions you have about a medical condition, and never disregard professional medical advice or delay seeking it because of something you read here.
If you think you may have a medical emergency, call your local emergency number or go to the nearest emergency department immediately.
Medically reviewed by WellAlly Editorial Team Last reviewed July 26, 2026. · Read our editorial policy