Pronunciation: gav-REH-toh
Generic name: pralsetinib
Dosage form: oral capsule
Drug class: Multikinase inhibitors

Medically reviewed by Carmen Pope, BPharm. Last updated on Aug 22, 2024.

What is Gavreto?

Gavreto (pralsetinib) is an oral prescription medicine that may be used to treat the following cancers caused by abnormal RET (rearranged during transfection) genes that have spread (metastasized):

• non-small cell lung cancer (NSCLC) in adults
• advanced thyroid cancer or thyroid cancer in adults and children 12 years of age and older who require a medicine by mouth or injection (systemic therapy) and who have received radioactive iodine and it did not work or is no longer working.

Your healthcare provider will perform a test to make sure that Gavreto is right for you.

Gavreto is a targeted cancer treatment that works by blocking the activity of a specific protein called RET, which is involved in the growth and development of certain cancers. Gavreto's mechanism of action means it effectively targets RET-driven cancers, including those with specific mutations or fusions.

Gavreto gained FDA approval initially under the accelerated designation for metastatic RET fusion-positive NSCLC on September 4, 2020, which was upgraded to full approval on August 9, 2023.

• FDA approval for metastatic RET fusion-positive thyroid cancer for Gavreto is still under the accelerated approval designation. Continued approval may be dependent on favorable clinical trials.

Gavreto side effects

The most common side effects of Gavreto are:

• muscle or joint pain
• constipation or diarrhea
• high blood pressure
• low blood cell counts or other abnormal laboratory tests
• feeling tired
• swelling of your face, arms, legs, hands, and feet (edema)
• fever
• cough
• low sodium levels and other electrolyte changes.

The most common severe abnormal blood test results with Gavreto include:

• decreased white blood cell, red blood cell, and platelet counts
• decreased levels of phosphate, body salt (sodium), calcium, and potassium in the blood
• abnormal liver function blood tests
• increased levels of an enzyme called alkaline phosphatase in the blood (this is a test for liver or bone problems)
• increased levels of potassium in the blood.

Serious side effects and warnings

Gavreto may cause the following serious side effects.

Lung problems. Gavreto may cause severe or life-threatening inflammation of the lungs during treatment,
which can lead to death. Tell your healthcare provider right away if you have any new or worsening
symptoms, including:

• shortness of breath
• cough
• fever.

High blood pressure (hypertension). High blood pressure is common with Gavreto and may sometimes
be severe. You should check your blood pressure regularly during treatment. Tell your healthcare provider if you have increased blood pressure readings or get any symptoms of high blood pressure, including:

• confusion
• headaches
• shortness of breath
• dizziness
• chest pain.

Liver problems. Liver problems (showing as increased liver function blood test results) can happen during treatment with Gavreto and may sometimes be serious. Your healthcare provider will do blood tests before and
during treatment to check you for liver problems. Tell your healthcare provider right away if you get any signs or symptoms of liver problems during treatment, including:

• yellowing of your skin or the white part of your eyes (jaundice)
• dark “tea-colored” urine
• sleepiness
• bleeding or bruising
• loss of appetite
• nausea or vomiting
• pain on the upper right side of your stomach area.

Bleeding problems. Gavreto can cause bleeding which can be serious and cause death. Tell your
healthcare provider if you have any signs or symptoms of bleeding during treatment, including:

• vomiting blood or if your vomit looks like coffee grounds
• pink or brown urine
• red or black (looks like tar) stools
• coughing up blood or blood clots
• unusual bleeding or bruising of your skin
• menstrual bleeding that is heavier than normal
• unusual vaginal bleeding
• nose bleeds that happen often
• drowsiness or difficulty being awakened
• confusion
• headache
• change in speech.

Tumor lysis syndrome (TLS). TLS is caused by a fast breakdown of cancer cells. TLS can cause you to
have kidney failure and the need for dialysis treatment, an abnormal heartbeat, and may sometimes lead
to hospitalization. Your healthcare provider may do blood tests to check you for TLS. You should stay well
hydrated during treatment with Gavreto. Call your healthcare provider or get emergency medical help
right away if you develop any of these symptoms during treatment:

• nausea
• vomiting
• weakness
• swelling
• shortness of breath
• muscle cramps
• seizures.

Risk of wound healing problems. Wounds may not heal properly during treatment with Gavreto. Tell your
healthcare provider if you plan to have any surgery before or during treatment.

• You should not take Gavreto for at least 5 days before surgery.
• Your healthcare provider should tell you when you may start taking Gavreto again after surgery

Gavreto may affect fertility in males and females, which may affect your ability to have children. Talk to your
healthcare provider if this is a concern for you.

Allergic reactions. Gavreto may cause hypersensitivity reactions. Get emergency medical help if you have signs of an allergic reaction to Gavreto such as hives; difficulty breathing; or swelling of your face, lips, tongue, or throat.

Gavreto may affect the growth plates of growing children.

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.

Related/similar drugs

Before taking

Before taking Gavreto, tell your healthcare provider about all of your medical conditions, including if you:

• have lung or breathing problems other than lung cancer
• have high blood pressure
• have bleeding problems
• have liver problems
• plan to have surgery. You should stop taking Gavreto at least 5 days before your planned surgery
• are pregnant or plan to become pregnant
• are breastfeeding or plan to breastfeed.

Gavreto may impair fertility. Talk to your healthcare provider if this is a concern for you.

It is not known if Gavreto is safe and effective when used to treat cancers caused by abnormal RET genes:

• in children for the treatment of NSCLC
• in children younger than 12 years of age for the treatment of thyroid cancer.

Pregnancy

Gavreto can harm an unborn baby. If you are a female who can become pregnant your healthcare provider will do a pregnancy test before you start treatment with Gavreto. You should use an effective form of non-hormonal birth control (contraception) during treatment and for 2 weeks after your last dose of Gavreto.

Birth control methods that contain hormones (such as birth control pills, injections, or transdermal system
patches) may not work as well during treatment with Gavreto. To prevent pregnancy while using Gavreto, use a barrier form of birth control: condom, diaphragm, cervical cap, or contraceptive sponge. Talk to your healthcare provider about birth control methods that may be right for you during this time.

Tell your healthcare provider right away if you become pregnant or think you might be pregnant during
treatment with Gavreto.

Males with female partners who can become pregnant should use effective birth control (contraception) during treatment with Gavreto and for 1 week after their last dose.

Breastfeeding

It is not known if Gavreto passes into your breast milk. Do not breastfeed during treatment and for 1 week after your last dose of Gavreto.

How should I take Gavreto?

Take Gavreto exactly as your healthcare provider tells you to take it. Do not change your dose or stop using the medicine without your doctor's advice.

• Take Gavreto 1 time each day.
• Gavreto should be taken on an empty stomach at least 1 hour before or 2 hours after a meal.

Your healthcare provider may change your dose, temporarily stop, or permanently stop treatment with Gavreto if you develop side effects.

• If you vomit after taking a dose of Gavreto, do not take an extra dose. Take your next dose of Gavreto at your regular time the next day.
• Your blood pressure will need to be checked often and you will need frequent blood tests.
• Your doctor will monitor your liver function (specifically ALT and AST enzymes) before initiating Gavreto, then every 2 weeks for the first 3 weeks, then monthly thereafter.
• If you need surgery, tell your surgeon you currently use this medicine. You may need to stop for a short time.

Gavreto dosing information

Gavreto dosage for adults and children 12 and over: Gavreto 400 mg orally 1 time a day.

• Each Gavreto capsule is 100 mg, which means you will take 4 capsules of Gavreto.
• Gavreto should be taken on an empty stomach, at least 1 hour before or 2 hours after a meal.
• If you vomit shortly after taking Gavreto, do not take another dose. Wait until your next scheduled dose time to take the medicine again.

What happens if I miss a dose?

If you miss a dose of Gavreto, take it as soon as possible on the same day. Then take your next dose of
Gavreto at your regular time the next day. Skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

What to avoid

Gavreto can delay wound healing. Do not take Gavreto for at least 5 days before surgery. Your healthcare provider should tell you when you may start taking Gavreto again after surgery

What other drugs will affect Gavreto?

Sometimes it is not safe to use certain medications at the same time. Some drugs can affect your blood levels of other drugs you take, which may increase side effects or make the medications less effective. Tell your doctor about all your current medicines including prescription medicines, over-the-counter drugs, vitamins, and herbal products. Many drugs can interact with Gavreto, especially:

• some antibiotic or antifungal medicines
• antiviral medications used to treat HIV or hepatitis C
• some cancer medications
• certain cholesterol medications
• seizure medications.

Avoid administering Gavreto with strong or moderate CYP3A inhibitors and/or P-gp inhibitors such as clarithromycin, erythromycin, diltiazem, itraconazole, ketoconazole, ritonavir, verapamil, goldenseal, and grapefruit. Your doctor may reduce the dosage of Gavreto if coadministration is unavoidable.

Avoid administering Gavreto with strong or moderate CYP3A inducers such as phenobarbital, phenytoin, rifampicin, St. John's Wort, and glucocorticoids. Your doctor may increase the dosage of Gavreto if coadministration is unavoidable.

This list is not complete and many other drugs may interact with pralsetinib. This includes prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible drug interactions are listed here. See the Gavreto Prescribing Information for a complete list.

Storage

Store Gavreto 100 mg capsules at room temperature between 68°F to 77°F (20°C to 25°C) away from moisture and heat.

Keep out of the reach of children.

Gavreto ingredients

Active ingredient: pralsetinib 100 mg.

Inactive ingredients: citric acid, hydroxypropyl methylcellulose (HPMC), magnesium stearate, microcrystalline cellulose (MCC), pregelatinized starch, and sodium bicarbonate.

Capsule shell: FD&C Blue #1 (Brilliant Blue FCF), hypromellose, and titanium dioxide.

White printing ink: butyl alcohol, dehydrated alcohol, isopropyl alcohol, potassium hydroxide, propylene glycol, purified water, shellac, strong ammonia solution, and titanium dioxide.

Gavreto 100 mg capsules are available in bottles of 60, 90, and 120 capsules.

Who makes Gavreto?

Rigel Pharmaceuticals, Inc. manufactures Gavreto.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

Medical Disclaimer