Pronunciation:

pral-SE-ti-nib

Brand Names:

• Gavreto

Dosage Forms:

• Capsule

Classifications:

Therapeutic—

Antineoplastic Agent

Pharmacologic—

Tyrosine Kinase Inhibitor

Uses of This Medicine:

Pralsetinib is used to treat metastatic (cancer that has already spread) non-small cell lung cancer (NSCLC) and in patients whose tumors have RET fusion-positive genes. Your doctor will perform a test to check for the RET gene fusion before you use this medicine.

Pralsetinib is also used to treat advanced or metastatic (cancer that has already spread) medullary thyroid cancer (MTC) in patients whose tumors have abnormal RET (RET-mutant) genes. Your doctor will perform a test to check for the abnormal RET gene before you use this medicine. It is used in patients who needs a medicine by mouth or injection.

Pralsetinib is also used to treat advanced or metastatic (cancer that has already spread) thyroid cancer in patients whose tumors have RET fusion-positive genes. Your doctor will perform a test to check for the RET gene fusion before you use this medicine. It is used in patients who needs a medicine by mouth or injection and have received radioactive iodine but did not work.

Pralsetinib belongs to the group of medicines called antineoplastics (cancer medicines). It works by interfering with the growth of cancer cells, which are eventually destroyed.

This medicine is available only with your doctor's prescription.

Before Using This Medicine:

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Allergies—

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Children—

Appropriate studies have not been performed on the relationship of age to the effects of pralsetinib to treat non-small cell lung cancer in the pediatric population. Safety and efficacy have not been established.

Appropriate studies performed to date have not demonstrated pediatric-specific problems that would limit the usefulness of pralsetinib to treat medullary thyroid cancer and thyroid cancer in children 12 years of age and older. Safety and efficacy have not been established in children younger than 12 years of age.

Older adults—

Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of pralsetinib in the elderly.

Breast-feeding—

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Other medicines—

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Amiodarone
• Amprenavir
• Apalutamide
• Aprepitant
• Atazanavir
• Berotralstat
• Boceprevir
• Bosentan
• Carbamazepine
• Carvedilol
• Cenobamate
• Ceritinib
• Cimetidine
• Ciprofloxacin
• Clarithromycin
• Clofazimine
• Cobicistat
• Conivaptan
• Crizotinib
• Cyclosporine
• Dabrafenib
• Darunavir
• Diltiazem
• Dipyrone
• Dronedarone
• Duvelisib
• Efavirenz
• Elagolix
• Enzalutamide
• Erythromycin
• Etravirine
• Flibanserin
• Fluconazole
• Fluvoxamine
• Fosamprenavir
• Fosnetupitant
• Fosphenytoin
• Idelalisib
• Imatinib
• Indinavir
• Itraconazole
• Ivosidenib
• Josamycin
• Ketoconazole
• Lapatinib
• Lesinurad
• Letermovir
• Lonafarnib
• Lopinavir
• Lorlatinib
• Lumacaftor
• Mibefradil
• Mifepristone
• Mitotane
• Modafinil
• Nafcillin
• Nefazodone
• Nelfinavir
• Netupitant
• Nilotinib
• Phenobarbital
• Phenytoin
• Posaconazole
• Primidone
• Quinidine
• Ranolazine
• Ribociclib
• Rifabutin
• Rifampin
• Rifapentine
• Ritonavir
• Saquinavir
• Schisandra sphenanthera
• St John's Wort
• Telaprevir
• Telithromycin
• Telotristat Ethyl
• Thioridazine
• Treosulfan
• Troleandomycin
• Tucatinib
• Vemurafenib
• Verapamil
• Voriconazole
• Voxelotor

Other interactions—

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following is usually not recommended, but may be unavoidable in some cases. If used together, your doctor may change the dose or how often you use this medicine, or give you special instructions about the use of food, alcohol, or tobacco.

• Grapefruit Juice

Other medical problems—

The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:

• Bleeding problems or
• Kidney disease or
• Liver disease or
• Lung problems (eg, interstitial lung disease, pneumonitis)—Use with caution. May make these conditions worse.

• Hypertension (high blood pressure), uncontrolled or—This condition must be corrected first before using and during treatment with this medicine.

• Surgery, recent—Use with caution. May cause side effects to become worse.

Proper Use of This Medicine:

Medicines used to treat cancer are very strong and can have many side effects. Before receiving this medicine, make sure you understand all the risks and benefits. It is important for you to work closely with your doctor during your treatment.

Take this medicine exactly as directed by your doctor. Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered. To do so may increase the chance of side effects.

This medicine comes with a patient information leaflet. It is very important that you read and understand this information. Be sure to ask your doctor about anything you do not understand.

Swallow the capsule whole. Do not crush, open, or chew it.

It is best to take this medicine on an empty stomach. Do not eat for at least 2 hours before and 1 hour after taking this medicine.

Dosing—

The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

• For oral dosage form (capsules):
  • For non-small cell lung cancer (NSCLC), medullary thyroid cancer (MTC), and thyroid cancer:
    • Adults—400 milligrams (mg) once a day. Your doctor may adjust your dose as needed and tolerated.
    • Children—Use and dose must be determined by your doctor.

Missed dose—

If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

If you vomit after taking a dose of this medicine, do not take an extra dose. Take your next dose at your regular time the next day.

Storage—

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Precautions While Using This Medicine:

It is very important that your doctor check your progress at regular visits to make sure that this medicine is working properly. Blood tests may be needed to check for unwanted effects.

Using this medicine while you are pregnant can harm your unborn baby. If you are a woman who can bear children, your doctor may give you a pregnancy test before you start using this medicine to make sure you are not pregnant. Use an effective form of birth control during treatment and for at least 2 weeks after the last dose. Males with female partners who are able to become pregnant should use an effective form of birth control during treatment and for at least 1 week after the last dose. If you think you have become pregnant, tell your doctor right away.

This medicine may cause swelling of the lungs (pneumonitis) or interstitial lung disease. These are life-threatening conditions and require immediate medical attention. The symptoms may be similar to the symptoms from lung cancer. Check with your doctor right away if you have new or worsening cough, fever, or trouble breathing.

Check with your doctor right away if you have blurred vision, dizziness, nervousness, headache, pounding in the ears, or slow or fast heartbeat occurs during or after treatment with this medicine. These can be symptoms of hypertension (high blood pressure).

Check with your doctor right away if you have pain or tenderness in the upper stomach, pale stools, dark urine, loss of appetite, nausea, vomiting, unusual tiredness or weakness, or yellow eyes or skin. These could be symptoms of a serious liver problem.

This medicine can cause serious bleeding problems that may be life-threatening. Check with your doctor right away if you have coughing up blood, increased menstrual flow or vaginal bleeding, nosebleeds, red or black, tarry stools, red or dark brown urine, vomiting of blood or material that looks like coffee grounds, or any unusual bleeding or bruising.

This medicine may cause a serious type of reaction called tumor lysis syndrome. Your doctor may give you medicine to help prevent this. Call your doctor right away if you have a decrease or change in the amount of urine, joint pain, stiffness, or swelling, lower back, side, or stomach pain, a rapid weight gain, swelling of the feet or lower legs, or unusual tiredness or weakness.

This medicine may affect the way your body heals from cuts and wounds. Make sure any doctor who treats you knows that you are using this medicine. You may need to stop using this medicine several days before and after having surgery.

Talk with your doctor before using this medicine if you plan to have children. Some men and women using this medicine have become infertile (unable to have children).

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal or vitamin supplements.

Side Effects of This Medicine:

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

More common

Bleeding gums

blurred vision

chest pain

chills

cough

coughing up blood

dark urine

decrease or change in the amount of urine

difficulty in breathing or swallowing

dizziness

fainting

fast or slow heartbeat

fever

general feeling of discomfort or illness

headache

increased menstrual flow or vaginal bleeding

irregular pulse

joint pain, stiffness, or swelling

loss of appetite

lower back, side, or stomach pain

nausea

nervousness

nosebleeds

paralysis

pounding in the ears

prolonged bleeding from cuts

rapid weight gain

red or black, tarry stools

red or dark brown urine

slow or fast heartbeat

stomach pain, severe

swelling around the eye

swelling of the eyelids

swelling of the feet or lower legs

swelling or puffiness of the face

thickening of bronchial secretions

unusual tiredness or weakness

vomiting

yellow eyes or skin

Less common

Black, tarry stools

bladder pain

bloody or cloudy urine

chest pain or tightness

confusion

difficult, burning, or painful urination

frequent urge to urinate

lightheadedness

lower back or side pain

pale skin

sneezing

sore throat

sores, ulcers, or white spots on the lips or in the mouth

swollen glands

unusual bleeding or bruising

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

Bone pain

burning, numbness, tingling, or painful sensations

change in taste

constipation

decreased appetite

difficulty in moving

dry mouth

joint pain

lack or loss of strength

loss of taste

muscle aching or cramping

muscle pains or stiffness

neck pain

pain, swelling, or redness in the joints

swelling or inflammation of the mouth

tenderness

unsteadiness or awkwardness

watery or bloody diarrhea

weakness in the arms, hands, legs, or feet

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.