Capivasertib is a novel kinase inhibitor developed by AstraZeneca. It first received approval from the U.S. Food and Drug Administration (FDA) for marketing in 2023, providing a new treatment option for breast cancer patients with specific gene mutation types.

Indications for Capivasertib

Eligible Patient Population

Capivasertib in combination with fulvestrant is indicated for the treatment of adult patients with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative locally advanced or metastatic breast cancer.

These patients must harbor one or more PIK3CA/AKT1/PTEN gene alterations confirmed by an FDA-approved detection method.

Treatment Timing Requirements

Disease progression occurs after receiving at least one endocrine-based treatment regimen in the metastatic disease setting.

Or recurrence occurs within 12 months after completion of adjuvant therapy. This clear treatment line specification ensures the drug is used in patient populations most likely to benefit from it.

Dosage Form and Properties of Capivasertib

Dosage Form and Strengths

Capivasertib is available as film-coated oral tablets.

The 160 mg tablets are beige, round, biconvex tablets, imprinted with "CAV" and "160" on one side, and blank on the other side.

The 200 mg tablets are beige, capsule-shaped, biconvex tablets, imprinted with "CAV200" on one side, and blank on the other side.

Chemical Composition

The chemical name of capivasertib is 4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-4-piperidinecarboxamide. Its molecular formula is C₂₁H₂₅ClN₆O₂, and its molecular weight is 428.92 g/mol.

The active pharmaceutical ingredient (API) is a white to off-white powder, and its solubility is pH-dependent—it is readily soluble in water at pH below 1.2, but almost insoluble at pH above 6.8.

Excipient Composition

In addition to the active ingredient, capivasertib tablets contain excipients such as croscarmellose sodium, calcium hydrogen phosphate, magnesium stearate, and microcrystalline cellulose.

The film coating contains ingredients including copovidone, hypromellose, iron oxide black, iron oxide red, iron oxide yellow, medium-chain triglycerides, polydextrose, polyethylene glycol 3350, and titanium dioxide.

Storage Methods for Capivasertib

Storage Conditions

Capivasertib tablets should be kept in the original packaging and stored at room temperature between 20°C and 25°C, with short-term exposure to temperatures ranging from 15°C to 30°C allowed.

Exposure to high temperatures, moisture, and direct sunlight should be avoided to prevent degradation of the drug components.

Capivasertib is relatively sensitive to moisture and should not be stored in humid places such as bathrooms.

Disposal Requirements

Unused or expired capivasertib should be disposed of in accordance with local regulations for pharmaceutical waste disposal. Random disposal to avoid environmental pollution or accidental ingestion by others is prohibited.