Chinese instructions for the targeted drug Pralsetinib

[drug name]

Generic Name: Platinib

English name:Pralsetinib

Trade name:Gavreto (common overseas trade name)

【Indications】

Platinib is an oral small moleculeRETtyrosine kinase inhibitor, used to treat patients with advanced or metastatic solid tumors with RET gene fusion mutations, mainly including the following types of patients:

Patients with RET fusion gene-positive non-small cell lung cancer (NSCLC);

Thyroid cancer patients withRET fusion positive;

Responsive to radioactive iodine therapyRETFusion-positive papillary thyroid carcinoma;

Other patients evaluated by clinicians as suitable forRET targeted therapy.

【Usage and Dosage】

The recommended dose is 400 mg once daily, orally, on an empty stomach. The medication should be taken at a fixed time, at least 1 hours before meals or 2 hours after meals.

Patients should swallow the tablet whole and not chew, crush or break it. If the patient misses a dose, he should take it as soon as possible. However, if it is close to the time of the next dose, skip the missed dose and do not take a double dose at one time.

【Pharmacological effects】

Platinib selectively inhibits RETtyrosine kinases, including RET fusion proteins and RET point mutant proteins. RET Abnormal activation of the gene is closely related to the occurrence of various cancers, such as non-small cell lung cancer, thyroid cancer, etc. By inhibiting the RET signaling pathway, platinib can effectively block the proliferation and metastasis of tumor cells.

【Clinical research data】

In the ARROW study, the objective response rate (ORR) of platinib in patients with RET fusion-positive non-small cell lung cancer exceeded 60%, and some patients achieved complete response. RETPatients with fusion-positive thyroid cancer and medullary thyroid cancer also showed good response rates and durable responses, demonstrating broad anti-tumor activity.

【Adverse reactions】

Common adverse reactions include:

Blood system: anemia, neutropenia, thrombocytopenia;

Gastrointestinal symptoms: nausea, constipation, diarrhea, decreased appetite;

Abnormal liver function:ALT, AST are elevated;

Abnormal renal function: elevated serum creatinine;

Others: high blood pressure, fatigue, cough, rash, etc.

Most adverse reactions can be alleviated by dose adjustment or symptomatic treatment. Individual patients may develop adverse events such as severe interstitial lung disease and prolonged QT interval, and require close monitoring.

【Contraindications】

It is contraindicated in those allergic to platinib or any of its excipients.

【Notes】

Patients with impaired liver and kidney function: The dose needs to be adjusted according to the patient's specific conditions;

Pregnant and lactating women: Since animal experiments have shown that it may have adverse effects on the fetus, it is recommended to avoid use during pregnancy; the risks of medication should be weighed during lactation, and it is recommended to suspend breastfeeding;

Children and the elderly: There is still a lack of sufficient safety and effectiveness data, and the benefits and risks need to be assessed before use;

Drug interactions: Combination with CYP3A inhibitors or inducers may affect the plasma concentration of platinib, so attention should be paid to adjusting the medication regimen.

【Drug use for special groups】

Use with caution in patients with moderately or severely impaired liver function;

Patients with severe renal insufficiency require individualized evaluation before use.

【Drug Storage】

Should be stored in a cool, dry place away from direct sunlight, kept at room temperature (20-25°C), and kept out of the reach of children.

[Specification packaging]

The common specifications are100mg tablets, and the common overseas packaging is 100mg×30tablets/ bottles.

[Approval and Accessibility]

Platinib is developed byBlueprint Medicines and jointly promoted with Roche. The drug has been approved by the FDA in the United States for the treatment of RET fusion-positive advanced non-small cell lung cancer and thyroid cancer. It has not yet been launched on a large scale in my country. If patients need medication, they need to obtain original drugs or generic drugs through overseas drug purchase channels. Generic versions are already on the market in India, Laos and other places, and the prices are relatively low.

【Remarks】

Before using platinib, a RET gene fusion test is required to confirm that the patient has the target before using the drug to avoid ineffective treatment. It is recommended that oncologists with experience in targeted therapy guide its use during treatment.

Reference materials:https://gavreto.com/