Capivasertib: First Approved AKT inhibitor for the Treatment of Patients with Breast Cancer

Area of Science:

• Oncology
• Pharmacology
• Genetics

Background:

• Breast cancer affects many women, with PI3K/mTOR/AKT pathway gene mutations implicated in nearly 50% of cases.
• Targeting specific molecular pathways is crucial for advancing breast cancer treatment.
• The PI3K/AKT pathway plays a significant role in cell growth and survival, making it a key target in cancer therapy.

Purpose of the Study:

• To provide a comprehensive overview of Capivasertib, the first approved AKT inhibitor.
• To discuss the drug's properties, mechanism, and clinical application in breast cancer treatment.
• To summarize key aspects including synthesis, pharmacokinetics, and adverse events.

Main Methods:

• Review of Capivasertib's physicochemical properties and synthesis.
• Analysis of its mechanism of action and binding mode.
• Examination of pharmacokinetic data, drug interaction studies, and adverse event profiles.

Main Results:

• Capivasertib is the first US FDA-authorized AKT inhibitor, approved on November 16, 2023.
• It is indicated for adult patients with specific genetic alterations (PIK3CA/AKT1/PTEN) in HR-positive, HER2-negative metastatic breast cancer.
• The discussion covers essential pharmacological and clinical data relevant to its use.

Conclusions:

• Capivasertib represents a significant advancement in targeted therapy for a subset of breast cancer patients.
• Understanding its properties and clinical data is vital for effective patient management.
• This perspective highlights the clinical relevance of targeting the PI3K/AKT pathway in breast cancer.