What important information is included in the package insert for Capivasertib?

Capivasertib (Capivasertib), as a new type of targeted anti-cancer drug, has attracted international attention for its clinical application in the treatment of breast cancer. According to the currently disclosed instructions, the drug information of capositinib details indications, usage and dosage, safety, metabolic pathways, potential drug interactions and other aspects, which is an important basis for clinical medication.

1. Basic information and pharmacological mechanisms of drugs

Caposetinib is a selectiveAkt inhibitor that can target multiple key points in the PI3K/Akt/PTEN pathway, especially AKT1, AKT2, and AKT3. This pathway is the core pathway for the proliferation and survival of various tumor cells. Capacetinib inhibits the phosphorylation of Akt kinase and blocks tumor cell signaling to achieve therapeutic goals such as inhibiting cancer cell growth and reversing drug resistance. The drug is an oral preparation with strong targeting and relatively controllable systemic toxicity.

2. Scope of approved indications

According to the latest labeling, capositinib is approved for use in combination with fulvestrant to treat patients with the following specific types of breast cancer:

Hormone receptor positive (HR+), HER2 negative;

There are molecular changes in tumor cellsPIK3CA, AKT1 mutations, or PTEN loss;

Progression after having received at least one endocrine-based therapy for metastatic disease, or relapse within 12 months of completion of adjuvant therapy

This population is often resistant to traditional endocrine therapy. In this context, capositinib provides a new treatment option, especially suitable for precise treatment strategies with positive molecular markers.

3. Recommended usage and dosage

The recommended dose of capositinib is once400 mg, taken orally twice daily, on an empty stomach or with food. Adopt a cyclic medication mode: take it continuously for 4 days, then stop taking it for 3 days, forming a complete 7-day treatment cycle (4 days ON/3 days OFF). This intermittent dosing helps reduce long-term toxicity, improve patient tolerance, and improve treatment compliance. Physicians can evaluate whether dosage adjustments are needed based on the patient's actual tolerance and response.

4. Adverse reactions and safety monitoring

The instructions mention that common adverse reactions of capositinib include:

Gastrointestinal reactions, such as diarrhea, nausea, and decreased appetite;

Skin reactions, including rash, dryness and itching;

Metabolic abnormalities, such as hyperglycemia and hypophosphatemia;

Systemic symptoms such as fatigue and dizziness.

Special attention needs to be paid to monitoring blood sugar, electrolytes (such as phosphorus, potassium), liver and kidney function and other indicators, especially during long-term treatment. In addition, if the patient experiences grade 3 or 4 toxic reactions, suspension of medication or dose adjustment should be considered.

5. Contraindications and medication recommendations for special groups

Capositinib is not suitable for use in patients who are allergic to its active ingredients or excipients. At the same time, it is not recommended for pregnant women, lactating women and people with severe hepatic insufficiency because the drug may affect fetal development and newborns. For women of childbearing age, the instructions recommend taking reliable contraceptive measures during treatment and for a certain period of time after stopping the drug.

6. The importance of implementing molecular testing

The efficacy of capositinib significantly depends on biomarker status, so it is recommended to perform tissue or liquid biopsy before treatment to determine whetherPIK3CA, AKT1 mutations or PTEN deletions are present. Precise screening of the target population will greatly improve treatment benefits and reduce unnecessary side effect exposure.

Reference materials:https://www.drugs.com/mtm/capivasertib.html