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KRAS G12C inhibitor

ADAGRASIB (brand name KRAZATI) is a prescription medicine used to treat adults with certain types of lung or colorectal cancer that have a specific KRAS G12C mutation. It works by blocking the protein that helps cancer cells grow.

How it worksADAGRASIB is a KRas inhibitor. It works by sticking to the mutated KRAS G12C protein and locking it in an 'off' position, which stops the signal that tells cancer cells to grow.

Brand names:KRAZATI

Used for
Non-small cell lung cancer (NSCLC) in adults with a KRAS G12C mutation who have had at least one previous systemic therapy.Colorectal cancer (CRC) in adults with a KRAS G12C mutation when used with cetuximab, after treatment with certain types of chemotherapy.
Conditions
Non-small cell lung cancer (NSCLC)Colorectal cancer (CRC)
Class
Small moleculeKRas inhibitorKRAS G12C inhibitorRespiratoryGastrointestinalHepaticCardiovascular

How to take

Forms200 mg tablets
RoutesOral

The standard dose is 600 mg taken orally twice daily. Tablets should be swallowed whole; do not chew, crush, or split them.

You can take KRAZATI with or without food, but try to take it at the same time every day. If you vomit after taking a dose, do not take an extra one; just wait until your next scheduled dose.

Missed dose: If a dose is missed by more than 4 hours, it should be skipped. Do not take an extra dose if you vomit.

Key warnings

  • ·Monitor for stomach problems like diarrhea, nausea, and vomiting.
  • ·Be aware of potential heart rhythm changes; avoid taking KRAZATI with other drugs known to affect heart rhythm.
  • ·Regular liver function tests are needed.
  • ·Watch for new or worsening breathing issues, which could indicate lung inflammation.

Do not use if

  • ·None listed

Side effects

Common

NauseaDiarrheaVomitingFatigueMusculoskeletal painDecreased appetiteHeadacheDry skinAbdominal painRash

Serious

  • ·Severe stomach issues like bleeding or blockage
  • ·Heart rhythm changes (QTc prolongation)
  • ·Liver problems (hepatotoxicity)
  • ·Lung inflammation (interstitial lung disease or pneumonitis)

Seek help if

  • ·Severe gastrointestinal reactions
  • ·Heart palpitations or rhythm changes
  • ·Yellowing of eyes or skin (liver issues)
  • ·New or worsening shortness of breath

Interactions

  • ·Avoid using KRAZATI with strong CYP3A4 inducers.
  • ·Avoid using KRAZATI with strong CYP3A4 inhibitors until the drug reaches a steady state in your body.
  • ·Avoid using KRAZATI with drugs that can affect heart rhythm (QT interval prolongers).
  • ·Avoid using KRAZATI with certain sensitive substrates of CYP3A4, CYP2C9, CYP2D6, or P-gp.
FoodFood does not significantly change how the body absorbs KRAZATI.

Special populations

PregnancyThere is no data on how KRAZATI affects pregnant women. Animal studies showed some risks to developing embryos, so use with caution.

PediatricThe safety and effectiveness of KRAZATI have not been tested in children.

GeriatricNo significant differences in safety or effectiveness were found in older patients compared to younger patients in clinical studies.

Talk to your doctor

Monitor

  • ·Diarrhea, nausea, and vomiting
  • ·Heart rhythm (QTc interval)
  • ·Liver function (laboratory tests)
  • ·Respiratory symptoms (breathing changes)

Questions to ask

  • ·What kind of testing do I need to confirm my KRAS G12C mutation?
  • ·How often will my liver and heart be monitored while on KRZATI?
  • ·What should I do if I experience new breathing problems?
  • ·Are there any specific medications I must avoid while taking this?

Pharmacokinetics

OnsetSteady state reached within 8 days
MetabolismCYP3A4 substrate

Practical

StorageStore tablets at room temperature between 20°C to 25°C (68°F to 77°F).

Ingredients

Inactive

colloidal silicon dioxidecrospovidonemagnesium stearate (vegetable sourced)mannitolmicrocrystalline cellulosehypromellosemaltodextrinmedium chain triglycerides (vegetable sourced)polydextrosetalctitanium dioxide

Educational summary derived from FDA labeling, AI-assisted. Not medical advice — consult a healthcare professional. Updated 2026-04-25.