Avapritinib is a selective tyrosine kinase inhibitor targeting KIT D816V, PDGFRA D842V, and other KIT mutations with potent IC50s (<25 nM). It blocks autophosphorylation and cell proliferation in mutant cell lines and shows anti-tumor activity in imatinib-resistant GIST and mastocytoma models.
Avapritinib
Generic Name/API:Avapritinib
Packaging:25-mg, 50-mg, 100-mg, 200-mg and 300-mg tablets
Storage:Store at 20°C to 25°C (68°F to 77°F)
Dosage:For dosage information, please check the General Information section.
Strength:Tablets containing 25 mg, 50 mg, 100 mg, 200 mg and 300 mg avapritinib.
Indication:Avapritinib is a kinase inhibitor designed to target potent mutations in KIT and PDGFRA, including the challenging PDGFRA D842V mutation. It offers a targeted treatment option for advanced systemic mastocytosis and gastrointestinal stromal tumors (GIST). With strong central nervous system penetration and selectivity, avapritinib demonstrates high efficacy and durable responses. Its unique mechanism supports use in mutation-driven cancers with limited treatment options.
Ayvakit (Avapritinib) is indicated for the treatment of adults with unresectable or metastatic GIST harboring a platelet-derived growth factor receptor alpha (PDGFRA) exon 18 mutation, including PDGFRA D842V mutations, advanced systemic mastocytosis (AdvSM) including patients with aggressive systemic mastocytosis (ASM), systemic mastocytosis with an associated hematological neoplasm (SM-AHN), and mast cell leukemia (MCL) and indolent systemic mastocytosis (ISM).
Avapritinib is not recommended for the treatment of patients with AdvSM or ISM with platelet counts of less than 50 X 109/L. Avapritinib is a selective tyrosine kinase inhibitor targeting KIT D816V, PDGFRA D842V, and multiple KIT mutations with potent IC50s (<25 nM). It inhibits autophosphorylation and cell proliferation in KIT/PDGFRA mutant cell lines and shows anti-tumor activity in xenograft models, including imatinib-resistant GIST and mastocytoma.
STRENGTH
Tablets containing 25 mg, 50 mg, 100 mg, 200 mg and 300 mg avapritinib.
DOSAGE:
Recommended dosage for
GIST Harboring PDGFRA Exon 18 Mutations
- 300 mg orally once daily
Dosage Modifications for Adverse Reactions
- First dose reduction : 200 mg orally once daily
- Second dose reduction: 100 mg orally once daily
Advanced Systemic Mastocytosis
- 200 mg orally once daily
Dosage Modifications for Adverse Reactions
- First dose reduction: 100 mg orally once daily
- Second dose reduction: 50 mg orally once daily
- Third dose reduction: 25 mg orally once daily
Indolent Systemic Mastocytosis
- 25 mg orally once daily
Dosage Modifications for Severe Hepatic Impairment:
A modified starting dosage of AYVAKIT is recommended for patients with severe hepatic impairment (Child-Pugh Class C)
- GIST: 200 mg orally once daily
- AdvSM: 100 mg orally once daily
- ISM: 25 mg orally every other day
SIDE EFFECTS
Adverse reactions associated with avapritinib are as follows:
- Intracranial hemorrhage
- Cognitive effects
- Photosensitivity
STORAGE :
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).
- Intracranial hemorrhage: (occured in 2.9% patients) Monitor patients with risk factors such as prior hemorrhage, stroke, vascular aneurysm, use of anticoagulants, or low platelets. Symptoms may include headache, nausea, vision changes, or confusion—advise urgent medical care if these occur. Permanently discontinue AYVAKIT if any intracranial hemorrhage occurs. In GIST, manage platelet counts <50 × 10⁹/L with dose interruption or reduction; platelet support may be needed. Thrombocytopenia was reversible by changing or stopping dose.
- Cognitive effects: (occurred in 33% patients) this kind of adverse reactions may be managed with dose interruption and/ or reduction when required. Depending on severity and indication, withhold avapritinib and then continue the same dose or reduced dose once improvement is seen in patient condition, or permanent discontinuation may be needed.
- Photosensitivity : (occured in 2.5% patients) Avapritinib may cause photosensitivity reactions in patients. Patients are advised to limit direct UV exposure during and one week post discontinuation of avapritinib treatment.
- Embryo-fetal toxicity: As avapritinib can cause fetal harm, pregnant women are advised to use effective contraception during and for 6 weeks post final dose of treatment.
FAQ
What is avapritinib used for?
Avapritinib is used in the treatment of GIST harboring PDGFRA exon 18 mutations, advanced systemic mastocytosis and indolent systemic mastocytosis.
What are the common side effects of avapritinib use?
The common side effects of avapritinib use include intracranial hemorrhage, cognitive effects and photosensitivity.
Can avapritinib be used in specific populations i.e. for pregnant, breastfeeding, pediatric and geriatric use?
There is no data on the presence of avapritinib or its metabolites in human milk or effects on breastfed children or milk production. Hence, advise women not to breastfeed during treatment or two weeks following the final dose. Advise effective contraception during treatment and for 6 weeks post final dose due to potential fetal harm. Avapritinib may impair male and female fertility. Safety and effectiveness in pediatric patients not established. No overall differences in safety or effectiveness in patients above 65 years of age, compared to younger patients. No dose adjustment required for patients with mild or moderate renal or hepatic impairment. Recommended dose not established for patients with severe renal impairment. A lower starting dose for patients with severe hepatic impairment is advised.
What is the cost of Avapritinib?
Avapritinib price in India may vary, as the medicine is not approved in India and must be imported. Factors such as international currency exchange rates (USD/EUR) and import duties can affect the final cost. For more details, please contact 247 QualityMeds.
How to buy Avapritinib (Ayvakit) tablets online in India?
To buy Avapritinib (Ayvakit) tablets online in India at a genuine price, contact 24/7 QualityMeds. We assist you with the legal import process and ensure safe delivery at the best possible cost.
What are the key criteria for selecting a supplier of Avapritinib or Ayvakit?
While selecting a supplier, patient or their family essentially ensure that the supplier holds a valid Good Distribution Practice (GDP) certificate and possesses a valid operating license. These credentials confirm that the supplier’s adherence to international standards for the proper distribution of medicinal products.
To know the cost of Ayvakit please contact 247 QualityMeds.
