Capivasertib

China [CN]

1. Core Uses

Approved Indication: In combination with fulvestrant, for the treatment of locally advanced/metastatic HR+/HER2- breast cancer with PIK3CA/AKT1/PTEN mutations (Approved by FDA in 2023, EMA in 2024) NCIEMA

Indications under development: Prostate cancer, ovarian cancer, endometrial cancer, colorectal cancer, and other solid tumors with PI3K/AKT pathway abnormalities

Mechanism: Inhibits AKT kinase activity, blocking downstream signaling pathways such as mTOR and S6K, thereby inhibiting tumor cell proliferation, survival, and metastasis; combination with endocrine therapy can overcome drug resistance and significantly prolong PFS. EMAFDA Access Data

2. Key Clinical Information

Dosage Form: Oral film-coated tablets (160mg, 200mg) EMA

Dosage and Administration: 400mg twice daily (approximately 12 hours apart), for 4 consecutive days followed by 3 days off, repeating the cycle.

Core Advantages:

Pan-AKT inhibition: Simultaneously blocks AKT1/2/3, covering more tumors with pathway abnormalities

Synergistic effect: When combined with fulvestrant, it significantly improves PFS in HR+/HER2- breast cancer

Precise targeting: Effective only against PIK3CA/AKT1/PTEN mutated tumors, with controllable side effects