Pralsetinib (Gavreto) is a new-generation highly selective RET inhibitor, offering a breakthrough treatment option for patients with RET fusion-positive non-small cell lung cancer and thyroid cancer.

What Are the Precautions for Pralsetinib (Gavreto) Administration?

Patient Selection Criteria

The presence of RET gene fusion must be confirmed by an FDA-approved testing method (for non-small cell lung cancer) or the RET fusion status verified by laboratory testing (for thyroid cancer). This is a fundamental prerequisite for ensuring treatment efficacy.

Next-Generation Sequencing (NGS) is recommended for genetic testing, and blood or plasma samples can be used as auxiliary diagnostic materials.

Baseline Examination Items

A comprehensive baseline profile should be established prior to the initiation of treatment, including key indicators such as liver function (AST, ALT), renal function, blood pressure monitoring, complete blood count (with special attention to lymphocytes, neutrophils, and hemoglobin), and electrolytes (serum phosphorus, serum sodium, serum calcium).

Special attention should be paid to patients with uncontrolled hypertension, who must receive antihypertensive treatment until their blood pressure stabilizes before starting pralsetinib therapy.

Pulmonary Toxicity Management

Interstitial lung disease/pneumonitis may occur in 12% of patients, with 3.3% of cases presenting as grade 3–4 reactions.

Close monitoring for respiratory symptoms such as dyspnea, cough, and fever is required.

In the event of grade 1–2 reactions, treatment should be suspended until symptoms resolve, then resumed at a reduced dose.

If interstitial lung disease recurs or grade 3–4 reactions develop, permanent discontinuation of the drug is required immediately.

Drug Interactions

Close attention should be paid to interactions with CYP3A/P-gp inhibitors (e.g., itraconazole, cyclosporine) and the impact of CYP3A inducers (e.g., rifampicin) on drug concentrations.

No dose adjustment is needed when co-administering with acid-suppressing medications such as proton pump inhibitors.

Medication Monitoring for Pralsetinib (Gavreto)

Cardiovascular System Monitoring

Hypertension occurs in 35% of patients, with 18% of cases classified as grade 3.

Blood pressure should be monitored during the first week of treatment, then at least once a month thereafter.

For grade 3 hypertension, treatment should be suspended until blood pressure is controlled; permanent discontinuation is required for grade 4 hypertension.

Liver Function Monitoring System

Elevated AST levels occur in 49% of patients, and elevated ALT levels in 37% of patients.

Liver function should be monitored every 2 weeks during the first 3 months of treatment, then monthly thereafter.