What information does the package insert of Serputinib/Serpatinib capsules contain?

1. Basic drug information

Generic name: Selpercatinib,

Product name:Retsevmo

Alias:LOXO-292

R&D company: Eli Lilly and Company (Eli Lilly and Company)

2. Scope of indications

1. RET fusion-positive non-small cell lung cancer (NSCLC)

Applicable to adult patients with locally advanced or metastatic disease RET gene fusion positive, usually used after confirmed diagnosis by molecular testing.

2. RET mutant medullary thyroid carcinoma (MTC)

Applicable to adult and pediatric patients aged 12 years and above, RET mutation-positive, advanced or metastatic, and requiring systemic treatment.

3. RET fusion-positive thyroid cancer

For patients 12 years old and above, RET gene fusion positive, advanced or metastatic, and refractory to radioactive iodine.

4. Others RET fusion-positive solid tumors

It is suitable for patients with locally advanced or metastatic disease who have previously received systemic therapy and whose disease has progressed, or who have no other satisfactory alternatives.

3. Usage and dosage

1. Recommended dosage

Weight<50kg: 120mg, taken orally twice a day; Weight≥50kg: 160mg, taken orally twice a day; Take at an interval of about 12 hours until disease progression or intolerance

2. Principles of dose adjustment

Gradually reduce the dose according to the grade of adverse reactions; Patients with severe liver function impairment need to reduce to twice a day 80mg

3. Pay attention to drug interactions

Avoid concurrent use of proton pump inhibitors, H2 receptor antagonists or antacids, and adjust the medication time if necessary

Strong or moderateCYP3A inhibitors may affect plasma concentrations, and the dose of serpatinib needs to be adjusted accordingly

4. Adverse reactions and safety

Common adverse reactions (≥25%): edema, diarrhea, fatigue, dry mouth, hypertension, abdominal pain, constipation, rash, nausea, headache

Severe adverse reactions (≥2%): pneumonia, pleural effusion, bleeding, dyspnea, hyponatremia, etc.

Fatal adverse reactions include sepsis, respiratory failure, cardiac arrest, etc., with an incidence rate of approximately3%

Laboratory abnormalities: lymphopenia,increased ALT/AST, and decreased sodium and calcium are more common

5. Storage conditions

Capsule preparation: Recommended to store20°C25°C, short-term fluctuations of 15°C30°C are acceptable

6. Mechanism of action and pharmacological characteristics

Seputinib blocks downstream oncogenic signaling pathways by highly selectively inhibiting RET kinases (including multiple RET mutations and fusions); is active against RET fusions (such as CCDC6-RET, KIF5B-RET) and mutants (such as V804M, M918T); in preclinical studies, it has demonstrated the ability to penetrate central nervous system metastatic lesions.

7. Clinical significance

The development of Seputinib has filled the gap in RET target precision therapy. As one of the first highly selective RET inhibitors, it not only significantly improves the treatment prognosis of patients with RET-related tumors, but also provides an example for future drug optimization of targeted therapies. With the popularization of genetic testing technology, the identification rate of RET fusions and mutations continues to increase, and the clinical use population of seputinib is gradually expanding.

Reference:https://en.wikipedia.org/wiki/Selpercatinib