Capivasertib 160mg Tablets

Capivasertib 160mg Tablets represent a targeted therapeutic approach for specific forms of advanced breast cancer. Pharmacologically, this medication is a potent, adenosine triphosphate (ATP)-competitive inhibitor of all three isoforms of the serine/threonine kinase AKT (AKT1, AKT2, and AKT3). The PI3K/AKT/PTEN pathway is a critical signaling route that regulates cell survival, proliferation, and metabolism.

In many cancers, genetic alterations (such as mutations in PIK3CA or AKT1, or alterations in PTEN) cause this pathway to become hyperactivated, driving tumor growth and resistance to endocrine therapies. By binding to and inhibiting the AKT enzyme, Capivasertib 160mg Tablets block the phosphorylation of downstream substrates. This inhibition effectively cuts off the survival signals the cancer cells rely on, restoring sensitivity to hormone therapies and inducing tumor cell death.

Indications / Uses of Capivasertib 160mg Tablets

Capivasertib 160mg Tablets are indicated for the treatment of adult patients with hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) locally advanced or metastatic breast cancer. Specific clinical scenarios include:

• Biomarker-Positive Disease: Indicated for patients whose tumors have one or more specific genetic alterations: PIK3CA/AKT1 mutations or PTEN alterations, as detected by an FDA-approved test.
• Combination Therapy: Prescribed specifically in combination with fulvestrant, an endocrine therapy. This combination is used for patients who have progressed on at least one endocrine-based regimen in the metastatic setting or who have recurred within 12 months of completing adjuvant therapy.
• Overcoming Resistance: By targeting the AKT pathway, the medication addresses a key mechanism of resistance to standard hormone therapies, providing a new option for disease control.

Key Features

• Pan-AKT Inhibition: Unlike some inhibitors that target only one isoform, Capivasertib inhibits all three isoforms (AKT1, 2, and 3), providing broad suppression of the pathway.
• Biomarker-Driven Precision: Efficacy is closely linked to the genetic profile of the tumor; patients with specific pathway alterations show the most significant benefit.
• Intermittent Dosing Schedule: The standard dosing regimen is often 400mg twice daily for 4 days on, followed by 3 days off, repeated weekly. This schedule helps manage toxicity while maintaining efficacy.
• Oral Administration: The tablet formulation allows for convenient oral dosing, taken with or without food.
• Improved Progression-Free Survival: Clinical trials (such as CAPItello-291) demonstrated that adding Capivasertib to fulvestrant significantly doubled the time to disease progression in the biomarker-altered population compared to fulvestrant alone.

Storage for Capivasertib 160mg Tablets

To ensure the stability and safety of Capivasertib 160mg Tablets, proper storage is essential. Store the medication at controlled room temperature, typically between 20°C and 25°C (68°F to 77°F). Brief excursions are permitted between 15°C and 30°C (59°F to 86°F). Keep the tablets in their original blister pack or bottle until just before use to protect them from moisture. Do not store the medication in humid environments like bathrooms. Ensure the container is kept out of the reach and sight of children and pets.

Important Note on Capivasertib 160mg Tablets

Treatment with Capivasertib 160mg Tablets requires careful monitoring for specific adverse effects. Hyperglycemia (high blood sugar) is a common and significant risk because the AKT pathway is involved in insulin signaling and glucose metabolism. Fasting blood glucose and HbA1c levels should be evaluated prior to starting treatment and monitored regularly thereafter.

Diarrhea is another frequent side effect. Patients should be advised to start antidiarrheal treatment, increase fluids, and notify their healthcare provider at the first sign of loose stools.

Cutaneous adverse reactions (skin rashes), including severe cases like erythema multiforme, can occur. Early intervention with topical corticosteroids or antihistamines may be necessary.

Capivasertib can cause fetal harm and is not recommended for pregnant women. Females of reproductive potential should use effective contraception during treatment and for one month after the last dose. As a substrate of CYP3A4, strong CYP3A4 inhibitors should be avoided if possible, as they can increase drug exposure and toxicity. Always review your full medication list with your oncologist.