A Visual Journey into AKT Inhibition

This content was funded by AstraZeneca and is intended for US healthcare professionals only.

Indication and Usage 

Capivasertib (TRUQAP®) 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 with one or more PIK3CA/AKT1/PTEN alteration as detected by an FDA-approved test following progression on at least one endocrine-based regimen in the metastatic setting or recurrence on or within 12 months of completing adjuvant therapy.

Description:

This animation shines a light on AKT inhibition, guiding you through the distinctive mechanism of action of capivasertib, which restricts the flow of oncogenic signaling within the PI3K/AKT/PTEN pathway.¹ You will discover how capivasertib’s inhibition of AKT, the ‘master switch’ of the PI3K/AKT/PTEN pathway, inhibits pathway hyperactivation driven by alterations in PIK3CA, AKT1 or PTEN.^2–6

Topics covered:

• Amplified oncogenic signaling can occur as a result of PIK3CA and AKT1 activating mutations, or PTEN inactivating alterations^3,5,6
• Capivasertib inhibits all three isoforms of AKT (AKT1, AKT2, and AKT3), which inhibits the phosphorylation of downstream AKT substrates¹
• By inhibiting AKT, the ‘master switch’ of the PI3K/AKT/PTEN pathway,² capivasertib restricts pathway hyperactivation driven by alterations in PIK3CA, AKT1 or PTEN^3–6

Select Safety Information About capivasertib (TRUQAP®) tablets 

TRUQAP is contraindicated in patients with severe hypersensitivity to TRUQAP or any of its components.

Serious adverse reactions include hyperglycemia, including diabetic ketoacidosis and fatal outcomes, diarrhea, and cutaneous adverse reactions. Monitor fasting glucose and hemoglobin A1C levels regularly. May cause fetal harm when administered to a pregnant woman. Among the 355 patients who received TRUQAP in CAPItello-291, the most common (≥20%) adverse reactions, including laboratory abnormalities, were diarrhea (72%), cutaneous adverse reactions (58%), increased random glucose (57%), decreased lymphocytes (47%), decreased hemoglobin (45%), increased fasting glucose (37%), nausea and fatigue (35% each), decreased leukocytes (32%), increased triglycerides (27%), decreased neutrophils (23%), increased creatinine (22%), vomiting (21%), and stomatitis (20%).

Please see full Prescribing Information, including Patient Information for TRUQAP. 

References:

1. TRUQAP® (capivasertib) [prescribing information]. Available at: https://www.accessdata.fda.gov/drugsatfda_docs/label/2025/218197s002lbl.pdf. Last accessed: 29 October 2025.
2. Uhlenbrock N et al. Structural and chemical insights into the covalentallosteric inhibition of the protein kinase Akt. Chem Sci. 2019;10(12):3573-85.
3. Skolariki A et al. Role of PI3K/Akt/mTOR pathway in mediating endocrine resistance: concept to clinic. Explor Target Antitumor Ther. 2022;3(2):172-99.
4. Andrikopoulou A et al. “The emerging role of capivasertib in breast cancer”. Breast. 2022;63:157–67.
5. Martorana F et al. AKT inhibitors: new weapons in the fight against breast cancer?. Front Pharmacol. 2021;12:662232.
6. Turner NC et al. Capivasertib in hormone receptor-positive advanced breast cancer. N Engl J Med. 2023;388(22):2058-70.

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US-105463 Last Updated 10/25