Pralsetinib

Pralsetinib is an oral, highly selective and potent inhibitor of rearrangement of transfection (RET).

1. Indications

Platinib is a selective RET kinase inhibitor, suitable for the following conditions:

1. RET fusion-positive non-small cell lung cancer (NSCLC) u2 00c:Treatment of adult patients with metastatic RET fusion-positive NSCLC confirmed by FDA-approved testing

2. RET fusion-positive thyroid cancer :Required for treatment of 12 years of age and older Patients with advanced or metastatic RET fusion-positive thyroid cancer who are refractory to systemic therapy and radioactive iodine (if radioactive iodine is applicable)

2. Usage and dosage

Standard dose :< /b>Adults and adolescents ≥12 years old take 400 mg orally once a day on an empty stomach (fasting from 2 hours before a meal to 1 hour after a meal)

Dose adjustment :Gradually reduce the dose to 300mg, 200mg or 100mg once a day

Handling of missed doses : If you miss a dose on the same day, you can take it as soon as possible, and resume the normal medication time the next day; there is no need to take a missed dose after vomiting

Surgical management : Stop medication for at least 5 days before elective surgery, and resume medication at least 2 weeks after major surgery and after the wound has healed

3. Side effects and precautions

Common adverse reactions (≥25%) :

1. Musculoskeletal pain, constipation, hypertension, diarrhea, fatigue, edema, fever and cough

2. Grade 3-4 laboratory abnormalities include lymphopenia, neutropenia Low hemoglobin, decreased phosphate, etc.

Severe risk warning :

1. Interstitial lung disease/pneumonia :The incidence rate is 12%, and grade 3-4 accounts for 3.3%. If respiratory symptoms occur, the drug should be stopped immediately and evaluated

2. Hypertension :The incidence rate is 35%, and grade 3 accounts for 18%. Blood pressure needs to be controlled before medication and monitored regularly during treatment

3. Hepatotoxicity : AST increased by 49% (Grade 3-4, 7%), ALT increased by 37% (Grade 3-4, 4.8%). Liver function needs to be monitored regularly

4. Bleeding events : The incidence rate of Grade 3 or above is 4.1%. Severe bleeding requires permanent discontinuation of the drug.

5. Wound healing disorder : U200c medication needs to be suspended before and after surgery. 6. Embryotoxicity : Contraindicated for pregnant women. Patients of childbearing age need to take effective non-hormonal contraceptive measures