Krazati

Krazati is a targeted therapy used to treat non-small cell lung cancer (NSCLC) that has an abnormal KRAS G12C gene. Krazati slows tumor growth by locking the KRAS protein so that it stays inactive. Krazati tablets are taken twice daily.

The KRAS gene makes a protein that works like an on and off switch to control how cells grow and die. An abnormal KRAS G12C gene can keep this switch turned on, which may cause cancer cells to grow and spread in the body. Krazati works by blocking the KRAS G12C protein to help stop tumor growth.

Krazati received FDA approval on December 12, 2022, for certain adults with non-small cell lung cancer. It is approved under the FDA accelerated approval pathway, which is based on early measures of how well a cancer responds to treatment while longer-term studies continue.

Krazati was previously approved in June 2024, in combination with Erbitux (cetuximab), for certain adults with KRAS G12C-mutated colorectal cancer. In 2026, this colorectal cancer approval was voluntarily withdrawn after a confirmatory clinical trial did not confirm a clinical benefit. Krazati is no longer approved to treat colorectal cancer.

Krazati is FDA-approved to treat adults with KRAS G12C-mutated locally advanced or metastatic NSCLC, as determined by an FDA-approved test, who have received at least one prior systemic therapy. Krazati is used on its own (as a single agent) for this cancer.

• Take Krazati twice a day, with or without food, at the same times each day.
• Swallow the tablets whole. Do not crush, chew, or break them.
• If you vomit shortly after taking a dose, do not take another dose. Take your next dose as scheduled.
• If you miss a dose, take it as soon as you remember. If it has been more than 4 hours, skip it. Take your next dose at the usual time. Do not take 2 doses at once to make up for a missed dose.
• This medicine can affect the results of certain medical tests. Tell any doctor who treats you that you are using it.
• You will need medical tests before and during treatment with this medicine.
• If you develop certain side effects, your healthcare provider may change your dose or temporarily or permanently stop treatment.

Gastrointestinal side effects. This medicine may cause diarrhea, nausea, and vomiting. Seek medical advice. Depending on how severe your symptoms are, your dose may be reduced or permanently stopped.

QTc interval prolongation. This medicine should not be used with other products known to prolong the QTc interval. If you are at risk or take medicines known to prolong the QT interval, your heart rhythm (ECG) will be monitored, along with your electrolytes, particularly potassium and magnesium. Your healthcare provider will correct any electrolyte abnormalities.

Liver problems. Your healthcare provider will check liver laboratory tests before you start this medicine, monthly for the first 3 months, and as needed after that.

Lung problems. Your healthcare provider will monitor you for new or worsening breathing symptoms.

Before you start treatment, tell your healthcare provider about all of your medical conditions, including if you:

• have any heart problems, including heart failure and congenital long QT syndrome.
• have liver problems.

Pregnancy

This medicine may harm an unborn baby. Tell your doctor or healthcare provider if you are pregnant.

This medicine may affect fertility in men and women. Pregnancy could be harder to achieve while either parent is using this medicine.

Breastfeeding

Tell your doctor or healthcare provider if you are breastfeeding or plan to breastfeed. It is not known if this medicine passes into your breast milk. Do not breastfeed during treatment or for one week after your last dose.

Common Krazati side effects

The most common Krazati side effects, which occurred in 25% or more of patients treated for non-small cell lung cancer, include:

• nausea
• diarrhea
• vomiting
• tiredness (fatigue)
• muscle and bone pain
• liver problems
• reduced kidney function
• swelling (edema)
• shortness of breath
• loss of appetite.

Changes in laboratory blood tests may also occur.

Serious Krazati side effects

Get emergency medical help if you have signs of an allergic reaction, such as hives, difficulty breathing, or swelling of your face, lips, tongue, or throat.

Krazati may cause other serious side effects. Call your doctor at once if you have:

• nausea, diarrhea, or vomiting;
• shortness of breath, cough, or fever;
• fast or pounding heartbeats, fluttering in your chest, and sudden dizziness (like you might pass out);
• stomach bleeding, such as bloody or tarry stools, coughing up blood, or vomit that looks like coffee grounds;
• liver problems, such as loss of appetite, stomach pain (upper right side), tiredness, itching, dark urine, clay-colored stools, or jaundice (yellowing of the skin or eyes).

This is not a complete list of side effects, and others may occur. Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

Usual adult Krazati dose for non-small cell lung cancer:

Recommended dosage: 600 mg orally twice daily, continued until the cancer progresses or side effects become unacceptable.

This indication is approved under accelerated approval based on objective response rate (ORR) and duration of response (DOR). Continued approval may be contingent upon verifying and describing a clinical benefit in a confirmatory trial.

Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. Krazati can affect the way other medicines work, and other medicines can affect how Krazati works.

Medicines that can interact with Krazati include:

• Strong CYP3A4 inducers: avoid use with Krazati.
• Strong CYP3A4 inhibitors: avoid use with Krazati until Krazati levels have reached a steady state (after about 8 days).
• Sensitive CYP3A4 substrates: avoid use with Krazati.
• Sensitive CYP2C9 or CYP2D6 substrates, or P-gp substrates: avoid use with Krazati when small changes in their levels could lead to serious side effects.
• Drugs that prolong the QT interval: avoid use with Krazati.

This is not a complete list of interactions. To check for interactions, click the link below.

• Store at room temperature between 68 degrees F and 77 degrees F (20 degrees C to 25 degrees C).
• The tablets come in a child-resistant container.
• The container has a desiccant (drying agent) to keep the medicine dry. Do not remove the desiccant from the container after opening. Do not eat or swallow the desiccant.

Review the Krazati package insert for more detailed information about this medicine. Discuss any medical questions with your doctor or other healthcare provider. This is not all the information you need to know about this medicine for safe and effective use, and it does not take the place of talking to your doctor about your treatment.

Active ingredient: adagrasib

Inactive ingredients: colloidal silicon dioxide, crospovidone, magnesium stearate (vegetable sourced), mannitol, and microcrystalline cellulose. The tablet film coating contains hypromellose, maltodextrin, medium-chain triglycerides (vegetable sourced), polydextrose, talc, and titanium dioxide.