Avapritinib
Gastrointestinal Stromal Tumors
.svg)
Drug Status
Government Approvals
US(FDA), UK(BNF)
WHO Essential Medicine
NO
Known Teratogen
No
Pharmaceutical Class
Kinase Inhibitor
Controlled Drug Substance
No
Avapritinib
Summary
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).
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.
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.
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.
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
How does Avapritinib work?
Avapritinib is a tyrosine kinase inhibitor, which means it blocks specific proteins that help cancer cells grow. Think of it like turning off a switch that powers cancer cell growth. By blocking these proteins, Avapritinib helps slow down or stop the growth of cancer cells. This targeted approach makes it effective for treating certain cancers, like gastrointestinal stromal tumors (GIST) with specific genetic mutations. The medication helps manage the disease and improve health outcomes for patients with these specific cancer types.
Is Avapritinib effective?
Avapritinib is effective for treating certain types of cancer, such as gastrointestinal stromal tumors (GIST) with specific genetic mutations. Clinical studies show that Avapritinib can shrink tumors and improve survival rates in patients with these mutations. The medication works by targeting and inhibiting specific proteins that promote cancer cell growth. This targeted approach helps manage the disease and improve health outcomes for patients with these specific cancer types.
What is Avapritinib?
Avapritinib is a medication used to treat certain types of cancer, such as gastrointestinal stromal tumors (GIST) with specific genetic mutations. It belongs to a class of drugs called tyrosine kinase inhibitors, which work by blocking specific proteins that promote cancer cell growth. By targeting these proteins, Avapritinib helps slow down or stop the growth of cancer cells. This medication is typically used when other treatments have not been effective or when the cancer has specific mutations.
Directions for Use
For how long do I take Avapritinib?
Avapritinib is usually a long-term medication for managing certain types of cancer, like gastrointestinal stromal tumors (GIST) with specific mutations. You'll typically take Avapritinib every day as a lifelong treatment unless your doctor suggests otherwise. Stopping this medication without medical advice could cause your condition to worsen. How long you'll need this medication depends on your body's response, any side effects you experience, and changes in your overall health. Always talk with your doctor before changing or stopping your Avapritinib treatment.
How do I dispose of Avapritinib?
If you can, bring unused Avapritinib to a drug take-back program or collection site at a pharmacy or hospital. They will dispose of this medicine properly so it doesn't harm people or the environment. If you can't find a take-back program, you can throw most medicines in the trash at home. But first, take them out of their original containers, mix them with something undesirable like used coffee grounds, seal the mixture in a plastic bag, and throw it away.
How do I take Avapritinib?
Take Avapritinib exactly as your doctor prescribes. It's usually taken once daily, in the morning, with or without food. Swallow the tablet whole; do not crush or chew it. If you miss a dose, take it as soon as you remember unless it's almost time for your next dose. In that case, skip the missed dose and continue your regular schedule. Never take two doses at once. Follow any dietary or beverage restrictions your doctor advises.
How long does it take for Avapritinib to start working?
Avapritinib begins working in your body shortly after you take it, but the time to see noticeable effects can vary. Some patients may notice improvements in symptoms within a few weeks, while others may take longer. The full therapeutic effect might take several months to become apparent. How quickly the medication works can depend on factors like the type of cancer, your overall health, and how your body responds to the treatment. Take it exactly as prescribed for the best results.
How should I store Avapritinib?
Store Avapritinib at room temperature, between 68°F to 77°F, in a tightly closed container to protect it from moisture and light. Don't keep your medicine in humid places like bathrooms, where moisture in the air could affect how well the medication works. Always store Avapritinib out of children's reach to prevent accidental swallowing. Remember to check the expiration date regularly and properly dispose of any unused or expired medication.
What is the usual dose of Avapritinib?
The usual starting dose of Avapritinib for adults is 300 mg once daily. Your doctor may adjust your dose based on your response and any side effects. The maximum recommended dose is 300 mg daily. Always follow your doctor's specific dosing instructions for your health needs. Special populations, such as the elderly, may require dose adjustments, so consult your doctor for personalized advice.
Warnings and Precautions
Can Avapritinib be taken safely while breastfeeding?
Avapritinib is not recommended while breastfeeding. We don't have much information about whether this medication passes into human breast milk. However, due to potential risks to the developing infant, it's advised to avoid breastfeeding while on Avapritinib. If you're taking Avapritinib and want to breastfeed, talk with your doctor about safer medication options that would allow you to nurse your baby safely.
Can Avapritinib be taken safely while pregnant?
Avapritinib is not recommended during pregnancy due to potential harm to the unborn baby. Animal studies show that this medication can cause birth defects and other developmental issues. We don't have much information about Avapritinib use in pregnant women, but the risks are considered significant. If you're pregnant or planning to become pregnant, talk with your doctor about safer treatment options. Your doctor can help create a pregnancy-specific treatment plan that protects both you and your baby.
Can I take Avapritinib with other prescription drugs?
Avapritinib can interact with certain medications, increasing the risk of side effects or reducing its effectiveness. Strong CYP3A inhibitors, like ketoconazole, can increase Avapritinib levels, leading to more side effects. Strong CYP3A inducers, like rifampin, can decrease Avapritinib levels, reducing its effectiveness. Always inform your doctor about all medications you're taking to avoid potential interactions. Your doctor can adjust your treatment plan to ensure safety and effectiveness.
Does Avapritinib have adverse effects?
Adverse effects are unwanted reactions to a medication. Common adverse effects of Avapritinib include nausea, fatigue, and vomiting. These occur in more than 10% of patients. Serious side effects like intracranial hemorrhage and liver problems are less common but require immediate medical attention. If you notice any new or worsening symptoms while taking Avapritinib, contact your doctor. They can help determine if these symptoms are related to the medication and suggest appropriate actions.
Does Avapritinib have any safety warnings?
Yes, Avapritinib has important safety warnings. It can cause serious side effects like intracranial hemorrhage, which is bleeding in the brain. If you experience severe headaches, confusion, or vision changes, seek medical help immediately. Avapritinib can also cause liver problems, so regular liver function tests are recommended. Not adhering to these warnings can lead to severe health issues. Always follow your doctor's advice and report any unusual symptoms.
Is Avapritinib addictive?
Avapritinib is not addictive or habit-forming. This medication doesn't cause dependency or withdrawal symptoms when you stop taking it. Avapritinib works by targeting specific proteins in cancer cells and doesn't affect brain chemistry in ways that could lead to addiction. You won't experience cravings for this medication or feel compelled to take more than prescribed. If you have concerns about medication dependence, you can feel confident that Avapritinib doesn't carry this risk.
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 drink alcohol while taking Avapritinib?
It's best to avoid alcohol while taking Avapritinib. Alcohol can increase the risk of liver problems, which is a concern with this medication. Drinking alcohol may also worsen side effects like dizziness or nausea. If you do choose to drink occasionally, limit how much alcohol you consume and watch for warning signs like unusual fatigue or stomach pain. Talk with your doctor about alcohol use while taking Avapritinib to get personalized advice based on your specific health situation.
Is it safe to exercise while taking Avapritinib?
You can exercise while taking Avapritinib, but keep a few things in mind. This medication can cause fatigue and dizziness, which might affect your ability to exercise. To exercise safely, listen to your body and avoid strenuous activities if you feel unwell. Drink plenty of water before, during, and after physical activity. If you notice symptoms like dizziness or unusual fatigue, slow down or stop exercising and rest. Check with your doctor if you have concerns about your specific situation.
Is it safe to stop Avapritinib?
Stopping Avapritinib suddenly can cause your condition to worsen. It's usually used for long-term treatment of certain cancers. If you stop taking it without medical advice, the cancer may progress. Always talk with your doctor before stopping Avapritinib. They might suggest gradually reducing your dose or switching to a different medication to keep your condition under control. Your doctor will help you make any medication changes safely to protect your health.
What are the most common side effects of Avapritinib?
Side effects are unwanted reactions that can happen when taking a medication. Common side effects of Avapritinib include nausea, fatigue, and vomiting, affecting more than 10% of people. Diarrhea and decreased appetite are also common. If you notice new symptoms after starting Avapritinib, they might be temporary or unrelated to the medication. Talk with your doctor before stopping any medication to ensure your treatment remains effective.
Who should avoid taking Avapritinib?
Don't take Avapritinib if you're allergic to it or its ingredients. Serious allergic reactions, which cause rash, hives, or swelling that makes breathing difficult, require immediate medical help. Avapritinib is not recommended for patients with severe liver impairment, as it can worsen liver function. Pregnant women should avoid this medication due to potential harm to the unborn baby. Always consult your doctor about these concerns before starting Avapritinib.
