As a novel AKT kinase inhibitor, Capivasertib provides a new treatment option for patients with specific types of advanced breast cancer.

How Effective is Capivasertib in Treatment?

Pharmacological Action

Capivasertib inhibits the activity of AKT1/2/3 kinases, blocks the PI3K/AKT/mTOR signaling pathway, and exerts a significant inhibitory effect on tumor cells harboring PIK3CA/AKT1/PTEN gene mutations.

Comprehensive Efficacy Characteristics

Strong targeting: Specifically targets the population with specific gene mutations in HR+/HER2- breast cancer.

Synergistic effect in combination: Works synergistically with fulvestrant to enhance the anti-tumor effect.

Intermittent administration: Adopts a weekly cycle regimen of "4 days on, 3 days off" to balance efficacy and tolerability.

Suitable Population for Capivasertib

Main Eligible Population

Pathological confirmation: Locally advanced or metastatic breast cancer that is hormone receptor (HR)-positive and human epidermal growth factor receptor 2 (HER2)-negative.

Genetic testing: Presence of at least one gene mutation among PIK3CA/AKT1/PTEN (confirmation via FDA-approved detection methods is required).

Treatment history: Disease progression after receiving at least one line of endocrine therapy previously, or recurrence within 12 months after adjuvant therapy.

Precautions for Special Populations

Pregnant women: Pose a risk of embryo-fetal toxicity; strict contraception is required.

Lactating women: Breastfeeding is prohibited during treatment and within 1 month after the last dose.

Patients with hepatic or renal impairment: Caution is needed for patients with moderate to severe hepatic impairment; there is insufficient data to support use in patients with severe renal impairment.

Medication Monitoring for Capivasertib

Pre-Treatment Evaluation

Metabolic indicators: Baseline testing of fasting blood glucose and glycated hemoglobin (HbA1c).

Genetic testing: Confirmation of the mutation status of PIK3CA/AKT1/PTEN.

Concomitant medications: Screening for strong/moderate CYP3A inhibitors or inducers.

Monitoring During Treatment

Hyperglycemia: Regular blood glucose testing; vigilance against ketoacidosis.

Diarrhea: Early use of antidiarrheal drugs to prevent dehydration.

Skin reactions: Monitor the progression of rashes; consult a dermatologist if necessary.

Principles of Dose Adjustment

Temporary drug suspension → dose reduction → permanent drug discontinuation.

Dose reduction should be considered when grade ≥3 toxicity occurs for the first time.

Management of Drug Interactions

CYP3A inhibitors: Concurrent use with strong inhibitors should be avoided; dose reduction is required when used with moderate inhibitors.

CYP3A inducers: Concurrent use is prohibited to prevent adverse effects on efficacy.

Recommendations for Long-Term Management

Metabolic follow-up: Continuous monitoring of changes in blood glucose and blood lipids.

Skin care: Establish a record file for adverse reactions.

Fertility counseling: Sustained contraception is required during treatment and after drug discontinuation.