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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Other protein kinase inhibitors
pralsetinib
L01EX23
Adult Dosing
- Non-Small Cell Lung Cancer (NSCLC): 400 mg orally once daily on an empty stomach
- Thyroid Cancers (MTC/DTC): 400 mg orally once daily on an empty stomach
- Modify dose for toxicity: First reduction to 300 mg daily, second reduction to 200 mg daily, third reduction to 100 mg daily
Pediatric Dosing
- Safety and efficacy not established in pediatric patients (< 18 years)
Indications
- Metastatic rearranged during transfection (RET) fusion-positive non-small cell lung cancer (NSCLC)
- Advanced or metastatic RET-mutant medullary thyroid carcinoma (MTC) requiring systemic therapy
- Advanced or metastatic RET fusion-positive thyroid cancer radioactive iodine-refractory requiring systemic therapy
Mechanism of Action
- Kinase inhibitor of wild-type RET and multiple RET gene alterations
- Inhibits RET alterations including V804L and V804M gatekeeper mutations associated with resistance to other kinase inhibitors
Adverse Reactions
- Musculoskeletal pain
- Constipation
- Hypertension
- Diarrhea
- Fatigue
- Edema
- Laboratory abnormalities: decreased lymphocytes, decreased neutrophils, decreased hemoglobin, decreased platelets, increased AST/ALT, increased creatinine
Drug Interactions
- Strong or moderate CYP3A inhibitors: Avoid coadministration; if unavoidable, reduce pralsetinib dose
- Strong or moderate CYP3A inducers: Avoid coadministration
- P-gp inhibitors: Avoid coadministration if possible
- Acid-reducing agents (PPIs, H2 blockers, antacids): Avoid coadministration; use local antacids if necessary separated by time
Curated Content: Needs Vetting Before Put to Clinical Use