Avapritinib

What is Avapritinib?

• Avapritinib (Ayvakit) is a kinase inhibitor.

Avapritinib

What are the uses of this medicine?

This medicine is used to treat:

• a certain type of stomach, bowel, or esophagus cancer called gastrointestinal stromal tumor (GIST) that cannot be treated with surgery or that has spread to other parts of the body (metastatic), and that is caused by certain abnormal platelet-derived growth factor receptor alpha (PDGFRA) genes. Your healthcare provider will perform a test to make sure that you have this abnormal PDGFRA gene and that Ayvakit is right for you.
• advanced systemic mastocytosis (AdvSM), including aggressive systemic mastocytosis (ASM), systemic mastocytosis with an associated hematological neoplasm (SM-AHN), and mast cell leukemia (MCL).
• Ayvakit is not recommended for the treatment of AdvSM in people with low platelet counts (less than 50 × 109/L).

How does this medicine work?

• An orally bioavailable inhibitor of specific mutated forms of platelet-derived growth factor receptor alpha (PDGFR alpha; PDGFRa) and mast/stem cell factor receptor c-Kit (SCFR), with potential antineoplastic activity.
• Upon oral administration, avapritinib specifically binds to and inhibits specific mutant forms of PDGFRa and c-Kit, including the PDGFRa D842V mutant and various KIT exon 17 mutants.
• This results in the inhibition of PDGFRa- and c-Kit-mediated signal transduction pathways and the inhibition of proliferation in tumor cells that express these PDGFRa and c-Kit mutants.
• PDGFRa and c-Kit, protein tyrosine kinases and tumor-associated antigens (TAAs), are mutated in various tumor cell types; they play key roles in the regulation of cellular proliferation.

Who Should Not Use this medicine ?

• This medicine have no usage limitations.

What drug interactions can this medicine cause?

• Avoid coadministration of Ayvakit with strong or moderate CYP3A inhibitors. If coadministration of Ayvakit with a moderate CYP3A inhibitor cannot be avoided, reduce the dose of Ayvakit.
• Avoid coadministration of Ayvakit with strong or moderate CYP3A inducers.

Is this medicine FDA approved?

• It was approved for use in the United States in 2020.

How should this medicine be used?

• Select patients for treatment with Ayvakit based on the presence of a PDGFRA exon 18 mutation.

Recommended Dosage for GIST Harboring PDGFRA Exon 18 Mutations

• The recommended dosage of Ayvakit is 300 mg orally once daily in patients with GIST. Continue treatment until disease progression or unacceptable toxicity.

Recommended Dosage for Advanced Systemic Mastocytosis

• The recommended dosage of Ayvakit is 200 mg orally once daily in patients with AdvSM. Continue treatment until disease progression or unacceptable toxicity.

Administration

• Take Ayvakit exactly as your healthcare provider tells you to take it.
• Do not change your dose or stop taking Ayvakit unless your healthcare provider tells you to.
• Take Ayvakit 1 time each day.
• Take Ayvakit tablet(s) on an empty stomach at least 1 hour before or at least 2 hours after a meal.
• If you miss a dose of Ayvakit, take it as soon as you remember unless your next scheduled dose is due within 8 hours. Take the next dose at your regular time.
• If you vomit after taking a dose of Ayvakit, do not take an extra dose. Take your next dose at your next scheduled time.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form: As Tablets: 25 mg, 50 mg, 100 mg, 200 mg and 300 mg.

This medicine is available in fallowing brand namesː

• Ayvakit

What side effects can this medication cause?

The most common side effects of Ayvakit in people with GIST include:

• fluid retention or swelling
• nausea
• tiredness
• muscle weakness
• vomiting
• decreased appetite
• diarrhea
• increased eye tearing
• stomach area (abdominal) pain
• constipation
• rash
• dizziness
• hair color changes
• changes in certain blood tests

The most common side effects of Ayvakit in people with AdvSM include:

• fluid retention or swelling
• diarrhea
• nausea
• tiredness
• changes in certain blood tests

Ayvakit may cause serious side effects, including:

• Bleeding in your brain

Cognitive effects may include:

• forgetfulness
• confusion
• getting lost
• trouble thinking
• drowsiness
• trouble staying awake (somnolence)
• word finding problems
• seeing objects or hearing things that are not there (hallucinations)
• change in mood or behavior

What special precautions should I follow?

• Do not drive or operate heavy machinery if you have confusion or trouble thinking during treatment with Ayvakit.
• This medicine may cause intracranial hemorrhage. Permanently discontinue for any occurrence of any grade
• A broad spectrum of cognitive adverse reactions can occur in patients receiving Ayvakit. Depending on the severity, continue Ayvakit at same dose, withhold and then resume at same or reduced dose upon improvement, or permanently discontinue.
• This medicine Can cause fetal harm. Advise females and males of reproductive potential of the potential risk to a fetus and to use effective contraception.

What to do in case of emergency/overdose?

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.

Can this medicine be used in pregnancy?

• Ayvakit can cause fetal harm when administered to a pregnant woman.
• There are no available data on Ayvakit use in pregnant women.

Can this medicine be used in children?

• The safety and effectiveness of Ayvakit in pediatric patients have not been established.

What should I know about storage and disposal of this medication?

• Store at 20°C to 25°C (68°F to 77°F); excursions are permitted from 15°C to 30°C (59°F to 86°F).

• Dailymed label info on Avapritinib
• FDA Avapritinib

Avapritinib Resources
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