Truqap is a first-in-class, potent, adenosine triphosphate (ATP)-competitive inhibitor of all three AKT isoforms (AKT1/2/3). Truqap 400mg is administered twice daily according to an intermittent dosing schedule of four days on and three days off. This was chosen in early phase trials based on tolerability and the degree of target inhibition.
Truqap is approved in Japan, the US and several other countries for the treatment of adult patients with HR-positive, HER2-negative locally advanced or metastatic breast cancer with one or more biomarker alterations (PIK3CA, AKT1 or PTEN) following recurrence or progression on or after an endocrine-based regimen based on the results from the CAPItello-291 trial.
Truqap is currently being evaluated in Phase III trials for the treatment of multiple subtypes of breast cancer and in other tumour types in combination with established treatments. The ongoing clinical research programme is focused on tumours reliant on signalling via the PI3K/AKT pathway, and in tumours harbouring biomarker alterations in this pathway.
Truqap was discovered by AstraZeneca subsequent to a collaboration with Astex Therapeutics (and its collaboration with the Institute of Cancer Research and Cancer Research Technology Limited).
Faslodex is an endocrine therapy indicated for the treatment of estrogen receptor-positive, locally advanced or metastatic breast cancer in postmenopausal women not previously treated with endocrine therapy, or with disease relapse on or after adjuvant anti-estrogen therapy, or disease progression on anti-estrogen therapy.
In the US, EU and Japan, Faslodex is also approved in combination with CDK4/6 inhibitors for the treatment of women with HR-positive, HER2-negative advanced or metastatic breast cancer, whose cancer has progressed after endocrine medicine. Faslodex represents a hormonal treatment approach that helps to slow tumour growth by blocking and degrading the estrogen receptor – a key driver of disease progression.
Faslodex is approved as monotherapy or in combination with medicines from various drug classes including CDK4/6, PI3K and AKT inhibitors for the treatment of patients with HR-positive advanced breast cancer and is being evaluated in combination with medicines from other drug classes.
Breast cancer is a malignant tumor that originates in the cells of the breast, commonly affecting the ducts and lobules. It is the most common cancer among women worldwide, though it can also occur in men. The development of breast cancer involves the abnormal growth of breast cells that can invade surrounding tissues and spread to other parts of the body (metastasize). Risk factors include genetic mutations (such as BRCA1 and BRCA2), family history of breast cancer, hormonal influences, and certain lifestyle factors such as alcohol consumption and obesity.
Early detection through screening methods like mammography, breast self-examinations, and clinical breast exams is crucial for effective treatment and improved survival rates. Treatment options vary based on the stage and subtype of breast cancer and may include surgery, radiation therapy, chemotherapy, hormone therapy, and targeted therapy. Advancements in personalized medicine and ongoing research continue to enhance the understanding and management of breast cancer, leading to more tailored and effective treatment approaches.
Companion diagnostic testing is crucial for effectively treating breast cancer with the combination therapy of TRUQAP + FASLODEX, specifically in determining the presence of PIK3CA and AKT1/PTEN alterations in the tumor. The presence of PIK3CA mutations, for instance, can make a significant difference in the responsiveness to certain therapies that target PI3K pathways, like TRUQAP. Similarly, alterations in AKT1 or PTEN can influence treatment strategies due to their roles in cell growth and survival pathways. These tests help in tailoring treatment to exploit these specific genetic vulnerabilities, enhancing treatment efficacy and personalizing patient care.
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TRUQAP + FASLODEX combines two potent therapies: TRUQAP, which targets specific cancer growth pathways, and FASLODEX, which acts as a hormone antagonist blocking estrogen receptors. This dual approach is used to treat breast cancer that exhibits hormone receptor positivity and specific genetic mutations, aiming to inhibit cancer progression more effectively.
This therapy is specifically designed for patients with breast cancer that is hormone receptor-positive and exhibits genetic alterations like PIK3CA mutations or AKT1/PTEN abnormalities. It is suitable for those who have not responded adequately to other treatments.
TRUQAP inhibits specific signaling pathways that are crucial for cancer cell growth and survival, while FASLODEX binds to and degrades estrogen receptors, reducing the cancer’s ability to utilize estrogen. Together, they work synergistically to suppress tumor growth and reduce the likelihood of disease progression.
Using TRUQAP in combination with FASLODEX can enhance the therapeutic efficacy against breast cancer by targeting multiple pathways simultaneously. This approach may lead to improved response rates, delayed disease progression, and potentially better overall survival outcomes compared to single-agent therapies.
Patients may experience side effects such as nausea, fatigue, and joint pain, which are common to many cancer treatments. More serious risks include potential liver function abnormalities and changes in blood sugar levels, which require careful monitoring and management.
Companion diagnostic testing is crucial to identify the presence of PIK3CA mutations or AKT1/PTEN alterations in the tumor. This ensures that the combination therapy is specifically tailored to those who are most likely to benefit, thereby optimizing treatment outcomes and avoiding unnecessary side effects for those unlikely to respond.
AstraZeneca (LSE/STO/Nasdaq: AZN) is a global, science-led biopharmaceutical company that focuses on the discovery, development, and commercialisation of prescription medicines in Oncology, Rare Diseases, and BioPharmaceuticals, including Cardiovascular, Renal & Metabolism and Respiratory & Immunology. Based in Cambridge, UK, AstraZeneca operates in over 100 countries and its innovative medicines are used by millions of patients worldwide. Please visit astrazeneca.com and follow the Company on social media @AstraZeneca.
