Gavreto

Non-small cell lung cancer — RET gene fusion-positive, metastatic, as detected by an FDA-approved test

400 mg orally once daily on an empty stomach (no food for at least 2 hours before and 1 hour after dose)
Dose reductions: 300 mg → 200 mg → 100 mg
Strong CYP3A inhibitors: Reduce to 200 mg once daily

Capsules: 100 mg

None listed.

• Hepatotoxicity: AST increase in 42%, ALT increase in 39% (Grade 3-4: 5-6%). Monitor LFTs every 2 weeks for 3 months, monthly for 3 months, then periodically.
• Interstitial Lung Disease (ILD)/Pneumonitis: 10% (Grade 3-4: 2.7%). Withhold for suspected ILD.
• Hypertension: 29% (Grade 3: 14%). Monitor BP regularly.
• Hemorrhage: Serious hemorrhagic events in 3.1%, including fatal events.
• Impaired Wound Healing: Withhold 5 days before and for at least 2 weeks after major surgery.
• Embryo-Fetal Toxicity

Fatigue (35%), constipation (35%), musculoskeletal pain (32%), hypertension (29%), diarrhea (24%), edema (21%), cough (19%), abdominal pain (17%), dyspnea (16%), AST increase (42%), ALT increase (39%), decreased lymphocytes (52%), decreased neutrophils (44%)

Consult the complete prescribing information for a comprehensive list of adverse reactions and their frequencies.

Consult the complete prescribing information for drug interactions, including effects on CYP enzymes, transporters, and concomitant medications that may require dose adjustments or monitoring.

Consult the full prescribing information for pregnancy-related considerations.

Refer to prescribing information for lactation guidance.

Pediatric safety and efficacy information is detailed in the full label.

Dose modifications for organ impairment are specified in the complete prescribing information.

Pralsetinib is a kinase inhibitor targeting wild-type RET and oncogenic RET fusions and mutations, including V804L/M gatekeeper mutations. It inhibits RET phosphorylation and downstream signaling pathways including MAPK and PI3K/AKT, blocking tumor cell proliferation.

Tmax: 2-4 hours. Half-life: approximately 14.7 hours. Protein binding: 97.1%. Metabolized primarily by CYP3A4. Fecal excretion (73%), urinary excretion (6%).

Clinical efficacy and safety data supporting the approval are available in the full prescribing information and from the clinical trials listed below.

• ARROW — Pralsetinib in RET fusion-positive NSCLC and RET-altered thyroid cancer. Phase I/II, n=438.
  🔬 NCT03037385 ↗ 📄 Primary Publication ↗

Gavreto has FDA-approved indications across the following cancer types covered on PipelineEvidence: