- Clinical Pipeline
- Guadecitabine (SGI-110) DNMT inhibitor (Hematological Malignancies and Solid Tumors)
- ASTX029 Extracellular Signal-Related Protein Kinases (ERK 1/2) Inhibitor (Solid Tumors)
- Oral Decitabine and Cedazuridine (ASTX727) (Hematological Malignancies)
- ASTX660 Dual IAP Antagonist (Solid Tumors & Lymphomas)
- ASTX295 Oral Murine Double Minute 2 (MDM2) antagonist (Solid Tumors)
- Partnered Products and Programs
- Kisqali®(ribociclib) CDK4/6 inhibitor (Oncology)
- Balversa® (erdafitinib) FGFr inhibitor (Oncology)
- Truqap™ PKB/Akt Inhibitor (Oncology)
- Multiple Targets and Therapeutic Areas
- Pyramid™ Discovery Platform
- Oncology and CNS Discovery
- Sustaining Innovation
|Discovery||Phase 1||Phase 2||Phase 3||Marketed|
PKB/Akt Inhibitor (Oncology)
Mechanism of Action: Protein kinase B (PKB) / serine/threonine protein kinase (AKT) inhibition
Discovery: TruqapTM (capivasertib, formerly known as AZD5363) was discovered by AstraZeneca in 2010 subsequent to its drug discovery collaboration with Astex Therapeutics that commenced in July 2005, and Astex’s earlier drug discovery collaboration that began in 2003 with the Institute of Cancer Research (ICR) and Cancer Research Technology Limited (CRT).
How this therapy can help
TruqapTM (capivasertib) is a first-in-class, potent, adenosine triphosphate (ATP)-competitive inhibitor of all three AKT isoforms (AKT1/2/3). Inhibition of AKT prevents the phosphorylation of AKT substrates that mediate cellular processes, such as cell division, apoptosis, and glucose and fatty acid metabolism. A wide range of solid and hematological malignancies show dysregulated PI3K/AKT/mTOR signalling due to mutations in multiple signalling components. By targeting AKT, the key node in the PIK3/AKT signalling network, this agent has the potential to be used as monotherapy or combination therapy for a variety of human cancers.
TruqapTM (capivasertib) in combination with Faslodex® received approval from the US FDA in November 2023 for the treatment of adult patients with hormone receptor (HR)-positive, HER2-negative locally advanced or metastatic breast cancer with one or more biomarker alterations (PIK3CA, AKT1 or PTEN). Eligible patients will have progressed on at least one endocrine-based regimen in the metastatic setting or experienced recurrence on or within 12 months of completing adjuvant therapy.
Concurrently with this approval, the FDA also approved a companion diagnostic test to detect relevant alterations (PIK3CA, AKT1 and PTEN).
TruqapTM (capivasertib) is currently being evaluated in Phase III trials for the treatment of multiple subtypes of breast cancer and in other tumor types either as monotherapy or in combination with established treatments. The ongoing clinical research program is focused on tumors reliant on signalling via the PI3K/AKT pathway, and in tumors harbouring biomarker alterations in this pathway.