Formulation and Specifications: Tablets: 100mg, 200mg, 300mg
Indications: Treatment of adult patients with unresectable or metastatic gastrointestinal mesenchymal tumors carrying platelet-derived growth factor receptor a (PDGFRA) exon 18 mutations, including the PDGFRAD842V mutation.
Key points for rational drug use:
1. The recommended daily oral dose is 300 mg, administered at least 1 hour before and 2 hours after meals on an empty stomach; continue therapy until disease progression or intolerable toxicity occurs.
2. Avoid combination with potent or intermediate-acting CYP3A inhibitors; if combination with intermediate-acting CYP3A4 inhibitors cannot be avoided, the starting dose may be reduced to 100 mg once daily.
3. This indication was granted conditional approval based on the results of a clinical study of NAVIGATOR that included 81 cases of PDGFRA exon 18 mutations.
4. No dose adjustment is required in patients ≥65 years of age; use with caution in pediatric and adolescent patients under 18 years of age.
5. Dose adjustment is not recommended for patients with mild to moderate hepatic or renal impairment; use with caution in patients with severe hepatic or renal impairment.
6. Common adverse reactions must be noted during administration, including nausea, fatigue, anemia, periorbital edema, facial edema, hyperbilirubinemia, diarrhea, vomiting, peripheral edema, increased lacrimation, decreased appetite, and impaired memory; the most common serious adverse reactions are anemia and pleural effusion.