LuciSel Selpercatinib Capsules

Product Name

Generic Name: Selpercatinib

Approved Name (China): Selpercatinib Capsules

Brand Names: Ruituo, Retevmo, LuciSel

English Name: Selpercatinib

Specification: 40 mg/capsule; 120 capsules per box

Dosage Form: Oral hard capsules

Manufacturer: Lucius Pharmaceutical (Laos) Co., Ltd.

National Drug Approval Number: 02 L 1063/24

Pharmacology

Mechanism of Action: Selpercatinib is a potent, highly selective small-molecule inhibitor of RET (Rearranged during Transfection) kinase. It specifically targets and inhibits the activity of RET kinase—including wild-type RET and RET variants activated by gene fusions or mutations—thereby inhibiting tumor cell proliferation and inducing apoptosis.

Pharmacodynamics: It demonstrates potent anti-tumor activity in tumors harboring RET gene fusions or mutations, and exhibits significant penetration into the central nervous system (CNS), effectively controlling brain metastases.

Indications

Indicated for the treatment of adult and adolescent patients aged 12 years and older with the following RET gene abnormalities:

1.  Non-Small Cell Lung Cancer (NSCLC): Locally advanced or metastatic RET fusion-positive NSCLC.

2.  Thyroid Cancer:

Advanced or metastatic RET-mutant medullary thyroid cancer requiring systemic therapy. 

Advanced or metastatic RET fusion-positive thyroid cancer requiring systemic therapy and radioactive iodine-refractory (if applicable).

Dosage and Administration

Dosage Basis: Determined by body weight.

Body Weight < 50 kg: 120 mg, twice daily.

Body Weight ≥ 50 kg: 160 mg, twice daily.

Administration Method: Oral administration; may be taken with or without food.

Dosage Adjustment: In the event of severe adverse reactions (e.g., hepatotoxicity, QT interval prolongation, hemorrhage, etc.), treatment should be interrupted, the dose reduced, or the drug permanently discontinued, depending on the severity of the reaction. Adverse Reactions

Common adverse reactions include:

Laboratory Abnormalities: Elevated aspartate aminotransferase (AST), elevated alanine aminotransferase (ALT), elevated blood glucose, elevated total cholesterol, elevated creatinine, thrombocytopenia, and hyponatremia.

Other Clinical Events: Dry mouth, diarrhea, hypertension, rash, edema, fatigue, constipation, etc.

Important Risks: Hepatotoxicity, QT interval prolongation, hemorrhage, hypersensitivity reactions, and risk of impaired wound healing.

Contraindications

Contraindicated in patients with a history of severe hypersensitivity to any component of this drug.

Precautions

1.  Hepatotoxicity: May cause severe drug-induced liver injury. Liver function should be monitored every 2 weeks during the first 3 months of treatment, and periodically thereafter. If hepatotoxicity occurs, the drug should be temporarily withheld, the dosage reduced, or the drug permanently discontinued.

2.  QT Interval Prolongation: May cause dose-dependent QT interval prolongation. ECG and electrolytes should be monitored periodically prior to and during treatment. Particular caution is advised in patients with, or at risk of developing, QT interval prolongation.

3.  Hemorrhagic Events: Serious hemorrhage may occur. In patients experiencing severe or life-threatening hemorrhage, the drug should be permanently discontinued.

4.  Hypersensitivity Reactions: If hypersensitivity symptoms—such as fever, rash, or arthralgia—occur during treatment, the drug should be temporarily withheld and symptomatic treatment administered.

5.  Hypertension: Blood pressure should be monitored periodically during treatment, and any emergent hypertension should be managed with standard therapy.

6.  Impaired Wound Healing: For patients undergoing elective surgery, it is recommended to withhold the drug for at least 7 days prior to surgery; resumption of treatment post-surgery should be determined based on the status of wound healing.

7.  Embryo-Fetal Toxicity: May be harmful to the fetus; patients of reproductive potential should use effective contraception during treatment and for a period of time following the last dose.

Drug Interactions

Strong CYP3A Inhibitors: Concomitant use should be avoided. If concomitant use is unavoidable, the dosage of selpercatinib should be reduced.

Strong CYP3A Inducers: Concomitant use should be avoided, as they may significantly reduce selpercatinib plasma concentrations, thereby compromising efficacy. P-gp and BCRP Substrates: Selpercatinib may increase the exposure of drugs such as digoxin and rosuvastatin; when co-administered, adverse reactions associated with these drugs should be monitored.

Storage

Store in the original sealed container at room temperature (20°C–25°C).