Avapritinib

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Approved Treatment Indication:

Gastrointestinal Stromal Tumors

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Summary

What conditions is Avapritinib used for?
Avapritinib is used for treating adults with unresectable or metastatic gastrointestinal stromal tumors (GIST) that harbor a PDGFRA exon 18 mutation. It's also used for treating advanced systemic mastocytosis (AdvSM), which includes aggressive systemic mastocytosis (ASM), systemic mastocytosis with an associated hematological neoplasm (SMAHN), and mast cell leukemia (MCL). Additionally, it is indicated for indolent systemic mastocytosis (ISM).
How does Avapritinib work in the body?
Avapritinib is a tyrosine kinase inhibitor. It targets specific mutations in proteins like KIT and PDGFRA, which are involved in cell growth and proliferation. By inhibiting these proteins, Avapritinib disrupts the signaling pathways that promote cancer cell growth, thereby slowing or stopping the progression of the disease.
What are the usual dosages and routes of administration for Avapritinib?
Avapritinib is taken orally once a day. For GIST with PDGFRA exon 18 mutations, the recommended dose is 300 mg daily. For AdvSM, the recommended dose is 200 mg daily. For ISM, the dose is 25 mg daily. It should be taken on an empty stomach, at least 1 hour before or 2 hours after a meal.
What are the most commonly observed adverse effects of Avapritinib?
Common side effects of Avapritinib include edema (72%), nausea (64%), fatigue (61%), cognitive impairment (48%), vomiting (38%), decreased appetite (38%), diarrhea (37%), and abdominal pain (31%). Serious adverse effects can include intracranial hemorrhage, cognitive effects, and photosensitivity.
What are important safety warnings and contraindications for Avapritinib?
Avapritinib can cause intracranial hemorrhage, cognitive effects, and photosensitivity. Patients should be monitored for signs of bleeding, cognitive changes, and skin reactions. It's contraindicated in patients with known hypersensitivity to the drug or its components. It's not recommended for use in patients with low platelet counts or those who are pregnant or breastfeeding due to potential harm to the fetus or infant.

Government Approvals

US(FDA), UK(BNF)

WHO Essential Medicine

NO

Known Teratogen

NO

Pharmaceutical Class

Kinase Inhibitor

Controlled Drug Substance

NO

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Drug Ingredient

Avapritinib

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Summary

What conditions is Avapritinib used for?
Avapritinib is used for treating adults with unresectable or metastatic gastrointestinal stromal tumors (GIST) that harbor a PDGFRA exon 18 mutation. It's also used for treating advanced systemic mastocytosis (AdvSM), which includes aggressive systemic mastocytosis (ASM), systemic mastocytosis with an associated hematological neoplasm (SMAHN), and mast cell leukemia (MCL). Additionally, it is indicated for indolent systemic mastocytosis (ISM).
How does Avapritinib work in the body?
Avapritinib is a tyrosine kinase inhibitor. It targets specific mutations in proteins like KIT and PDGFRA, which are involved in cell growth and proliferation. By inhibiting these proteins, Avapritinib disrupts the signaling pathways that promote cancer cell growth, thereby slowing or stopping the progression of the disease.
What are the usual dosages and routes of administration for Avapritinib?
Avapritinib is taken orally once a day. For GIST with PDGFRA exon 18 mutations, the recommended dose is 300 mg daily. For AdvSM, the recommended dose is 200 mg daily. For ISM, the dose is 25 mg daily. It should be taken on an empty stomach, at least 1 hour before or 2 hours after a meal.
What are the most commonly observed adverse effects of Avapritinib?
Common side effects of Avapritinib include edema (72%), nausea (64%), fatigue (61%), cognitive impairment (48%), vomiting (38%), decreased appetite (38%), diarrhea (37%), and abdominal pain (31%). Serious adverse effects can include intracranial hemorrhage, cognitive effects, and photosensitivity.
What are important safety warnings and contraindications for Avapritinib?
Avapritinib can cause intracranial hemorrhage, cognitive effects, and photosensitivity. Patients should be monitored for signs of bleeding, cognitive changes, and skin reactions. It's contraindicated in patients with known hypersensitivity to the drug or its components. It's not recommended for use in patients with low platelet counts or those who are pregnant or breastfeeding due to potential harm to the fetus or infant.

Indications and Purpose

What is Avapritinib used for?

Avapritinib is indicated for the treatment of adults with unresectable or metastatic gastrointestinal stromal tumors (GIST) harboring a PDGFRA exon 18 mutation, including PDGFRA D842V mutations. It is also used to treat advanced systemic mastocytosis (AdvSM), which includes aggressive systemic mastocytosis (ASM), systemic mastocytosis with an associated hematological neoplasm (SM-AHN), and mast cell leukemia (MCL).

How does Avapritinib work?

Avapritinib is a kinase inhibitor that targets specific proteins involved in the growth and spread of cancer cells. It blocks the action of abnormal proteins, such as KIT and PDGFRA, which signal cancer cells to multiply. By inhibiting these proteins, Avapritinib helps to slow or stop the progression of cancer.

Is Avapritinib effective?

Avapritinib has been shown to be effective in treating certain types of gastrointestinal stromal tumors (GIST) and systemic mastocytosis. Clinical trials, such as NAVIGATOR and PATHFINDER, have demonstrated significant overall response rates in patients with PDGFRA exon 18 mutations and advanced systemic mastocytosis. These studies provide evidence of Avapritinib's ability to reduce tumor size and improve symptoms in these conditions.

How does one know if Avapritinib is working?

The benefit of Avapritinib is evaluated through regular medical appointments and laboratory tests. Your doctor may order imaging studies to monitor tumor size and blood tests to assess your body's response to the medication. It is important to keep all scheduled appointments and communicate any side effects or changes in symptoms to your healthcare provider.

Directions for Use

What is the usual dose of Avapritinib?

The usual daily dose of Avapritinib for adults varies based on the condition being treated. For gastrointestinal stromal tumors (GIST) with PDGFRA exon 18 mutations, the recommended dose is 300 mg once daily. For advanced systemic mastocytosis (AdvSM), the dose is 200 mg once daily. For indolent systemic mastocytosis (ISM), the dose is 25 mg once daily. Avapritinib is not recommended for use in children, as its safety and effectiveness have not been established in pediatric patients.

How do I take Avapritinib?

Avapritinib should be taken orally once daily on an empty stomach, at least 1 hour before or 2 hours after a meal. It is important to take it at the same time each day. Patients should avoid eating grapefruit or drinking grapefruit juice while taking Avapritinib, as it may interact with the medication.

For how long do I take Avapritinib?

Avapritinib is typically used until disease progression or unacceptable toxicity occurs. The duration of use can vary significantly depending on the individual's response to treatment and the specific condition being treated. It is important to follow your doctor's guidance on how long to continue taking Avapritinib.

How long does it take for Avapritinib to start working?

The time it takes for Avapritinib to start working can vary depending on the individual and the condition being treated. In clinical trials, some patients began to see a response within a few weeks, but it may take longer for others. It is important to follow your doctor's guidance and attend regular check-ups to monitor your progress.

How should I store Avapritinib?

Avapritinib should be stored at room temperature, between 68°F to 77°F (20°C to 25°C). It should be kept in its original container, tightly closed, and out of reach of children. Avoid storing it in the bathroom or any area with excess heat and moisture. Proper storage ensures the medication remains effective and safe to use.

Warnings and Precautions

Who should avoid taking Avapritinib?

Important warnings for Avapritinib include the risk of intracranial hemorrhage, cognitive effects, and photosensitivity. Patients should be monitored for signs of bleeding, cognitive changes, and skin reactions. Avapritinib is contraindicated in patients with a history of severe bleeding or recent stroke. It is also not recommended for use in patients with low platelet counts or severe liver impairment. Pregnant women should avoid Avapritinib due to potential harm to the fetus.

Can I take Avapritinib with other prescription drugs?

Avapritinib can interact with strong and moderate CYP3A inhibitors, which may increase its plasma concentration and the risk of side effects. It is advised to avoid coadministration with these inhibitors. Additionally, Avapritinib may interact with CYP3A inducers, potentially decreasing its effectiveness. Patients should inform their healthcare provider of all medications they are taking to avoid potential interactions.

Can I take Avapritinib with vitamins or supplements?

From all available and reliable information, there is no confirmed data on this. Please consult a doctor for personalized advice.

Can Avapritinib be taken safely while pregnant?

Avapritinib can cause fetal harm when administered to pregnant women, based on animal studies and its mechanism of action. Women of reproductive potential should use effective contraception during treatment and for 6 weeks after the final dose. If pregnancy occurs while taking Avapritinib, it is important to inform your doctor immediately. There is no strong evidence from human studies, but the potential risk to the fetus is significant.

Can Avapritinib be taken safely while breastfeeding?

Women are advised not to breastfeed while taking Avapritinib and for at least 2 weeks after the final dose. There is no data on the presence of Avapritinib in human milk or its effects on the breastfed child, but due to the potential for serious adverse reactions, breastfeeding should be avoided during treatment.

Is Avapritinib safe for the elderly?

For elderly patients, no overall differences in safety or efficacy of Avapritinib have been observed compared to younger adults. However, older patients may experience more severe side effects, such as cognitive effects and fatigue. It is important for elderly patients to be closely monitored by their healthcare provider, and any side effects should be reported promptly to adjust the treatment plan as needed.

Is it safe to exercise while taking Avapritinib?

Avapritinib may cause side effects such as fatigue, dizziness, and cognitive effects, which could potentially limit the ability to exercise. If you experience these symptoms, it is important to discuss them with your doctor. They can provide guidance on safe levels of physical activity and any necessary adjustments to your treatment plan.

Is it safe to drink alcohol while taking Avapritinib?

From all available and reliable information, there is no confirmed data on this. Please consult a doctor for personalized advice.