How Effective is Capivasertib?

Capivasertib is an oral kinase inhibitor that targets all three isoforms of the AKT enzyme (AKT1, AKT2, and AKT3).

How Effective is Capivasertib?

The CAPItello-291 study is a phase Ⅲ, double-blind, randomized controlled clinical trial designed to evaluate the efficacy of Truqap (capivasertib) in combination with fulvestrant, compared with placebo plus fulvestrant, for the treatment of patients with locally advanced (unresectable) or metastatic hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-low or negative breast cancer (defined as immunohistochemistry (IHC) score 0 or 1+, or IHC 2+/in situ hybridization (ISH)-negative by testing).

This global clinical trial enrolled a total of 708 adult patients with histologically confirmed HR-positive, HER2-low or negative breast cancer. All enrolled patients experienced disease recurrence or progression during or after aromatase inhibitor therapy; among them, some had previously received cyclin-dependent kinase 4/6 (CDK4/6) inhibitor treatment while others had not. In addition, all patients had received no more than one chemotherapy regimen for advanced disease.

Administration of Capivasertib in Special Populations

Pregnancy

Based on animal study findings and its mechanism of action, capivasertib may cause fetal harm if administered to pregnant women. Pregnant women and females of reproductive potential should be informed of the potential fetal risks. Confirm the pregnancy status of females of reproductive potential before initiating treatment.

Females of Reproductive Potential

Use effective contraceptive measures during treatment and for 1 month after the last dose of capivasertib.

Males with Female Partners of Reproductive Potential

Use effective contraceptive measures during treatment and for 4 months after the last dose of capivasertib.

Lactation

There are no data available regarding the presence of capivasertib or its metabolites in human milk, as well as their effects on milk production or breastfed infants. It is recommended that women discontinue breastfeeding during capivasertib treatment.

How Does Capivasertib Work?

AKT is a serine/threonine kinase involved in numerous cellular processes, including cell division, apoptosis, as well as glucose and fatty acid metabolism. In cancer cells, AKT may be hyperactivated due to stimulation from upstream signaling pathway activation, AKT1 gene mutations, loss of PTEN function (PTEN is a protein that normally inhibits AKT activity), or PIK3CA gene mutations. The PIK3CA gene encodes a component of phosphatidylinositol 3-kinase (PI3K), an enzyme that activates AKT. By inhibiting AKT, capivasertib can interfere with these pro-cancer signals, thereby slowing or inhibiting tumor growth.