Gavreto Pralsetinib Capsules

1. Indications and Usage
Metastatic Non-Small Cell Lung Cancer (NSCLC):
Indicated for the treatment of adult patients with metastatic RET fusion-positive NSCLC.
Thyroid Cancer:
Indicated for the treatment of adult and pediatric patients (12 years and older) with advanced or metastatic RET fusion-positive thyroid cancer who require systemic therapy and are radioactive iodine-refractory (if radioactive iodine is appropriate).
2. Dosage and Administration
Recommended Dosage:
Dose: 400 mg orally once daily.
Administration: Take on an empty stomach (no food for at least 2 hours before and at least 1 hour after taking). Swallow capsules whole with water.
Dose Modifications:
Toxicity: Interrupt treatment for Grade ≥ 3 toxicities; resume at reduced dose (300 mg, 200 mg, or 100 mg) upon recovery.
3. Mechanism of Action
RET Inhibition:
Pralsetinib is a potent and selective inhibitor of RET wild-type and RET fusion proteins.
Physiological Effect:
It inhibits RET kinase activity and downstream signaling pathways (such as RAS-RAF-MEK-ERK), thereby inhibiting tumor cell proliferation and survival.
4. Safety and Warnings
Interstitial Lung Disease (ILD)/Pneumonitis:
Can cause severe, life-threatening, or fatal ILD/pneumonitis. Monitor for respiratory symptoms.
Hypertension:
Hypertension can occur. Do not initiate treatment until hypertension is controlled. Monitor blood pressure.
Hepatotoxicity:
Elevated transaminases (ALT/AST) have been reported. Monitor liver function tests (LFTs) before initiation and regularly during treatment.
Hemorrhage:
Severe or fatal bleeding events have occurred.
Impaired Wound Healing:
Withhold Pralsetinib prior to surgery and during wound recovery.
5. Adverse Reactions
Most Common:
Constipation, hypertension, fatigue, musculoskeletal pain, and diarrhea.
Serious Adverse Events:
ILD/pneumonitis, hypertension, hepatotoxicity, and hemorrhage.
6. Drug Interactions
Strong CYP3A Inhibitors:
Increase Pralsetinib exposure. Avoid concomitant use with strong CYP3A inhibitors (e.g., itraconazole) and P-gp inhibitors.
Strong CYP3A Inducers:
Decrease Pralsetinib exposure. Avoid concomitant use with strong CYP3A inducers (e.g., rifampin).
7. Pharmaceutical Information
Chemical Composition:
Active Ingredient: Pralsetinib.
Storage:
Store at 25°C (77°F); excursions permitted to 15-30°C (59-86°F). Keep in original package.