AYVAKIT (avapritinib) tablets,To treat adults with unresectable or metastatic gastrointestinal stromal tumor (GIST)

What is AYVAKIT?

AYVAKIT is a prescription medicine used to treat adults with 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

It is not known if AYVAKIT is safe and effective in children,

INDICATIONS AND USAGE

AYVAKIT is a kinase inhibitor indicated for the treatment of adults with unresectable or metastatic gastrointestinal stromal tumor (GIST) harboring a platelet-derived growth factor receptor alpha (PDGFRA) exon 18 mutation, including PDGFRA D842V mutations.

DOSAGE AND ADMINISTRATION

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

The recommended dosage is 300 mg orally once daily on an empty stomach, at least one hour before and two hours after a meal.

DOSAGE FORMS AND STRENGTHS-Tablets: 100 mg, 200 mg and 300 mg

-WARNINGS AND PRECAUTIONS

• Intracranial Hemorrhage: Withhold AYVAKIT for Grade 1 or 2 reactions until resolution and then resume at a reduced dose. Permanently discontinue for recurrent Grade 1 or 2 reactions or first occurrence of Grade 3 or 4 reactions.
• Central Nervous System (CNS) Effects: CNS adverse reactions include cognitive impairment, dizziness, sleep disorders, mood disorders, speech disorders, and hallucinations. Depending on the severity, continue AYVAKIT at same dose, withhold and then resume at same or reduced dose upon improvement, or permanently discontinue.
• Embryo-Fetal Toxicity: Can cause fetal harm. Advise females of reproductive potential of the potential risk to a fetus and to use effective contraception.

ADVERSE REACTIONS

The most common adverse reactions (incidence ≥ 20%) are edema, nausea, fatigue/asthenia, cognitive impairment, vomiting, decreased appetite, diarrhea, hair color changes, increased lacrimation, abdominal pain, constipation, rash and dizziness.

DRUG INTERACTIONS

• Strong and Moderate CYP3A Inhibitors: Avoid coadministration of AYVAKIT with strong and moderate CYP3A inhibitors. If coadministration of AYVAKIT with a moderate inhibitor cannot be avoided, reduce dose of AYVAKIT.
  
• Strong and Moderate CYP3A Inducers: Avoid coadministration of AYVAKIT with strong and moderate CYP3A inducers.

Referance;

1. .https://www.ayvakit.com
2. https://www.blueprintmedicines.com/uspi/AYVAKIT.pdf