Third cancer drug success for Astex drug discovery collaboration

Published: 30-Nov-2023

AstraZeneca’s Truqap™ (capivasertib) in combination with Faslodex® (fulvestrant) receives US FDA marketing approval 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)

Astex Pharmaceuticals (UK), a pharmaceutical company dedicated to the discovery and development of novel small molecule therapeutics for oncology and diseases of the central nervous system, announced today that it is in line to receive a milestone payment from AstraZeneca on first commercial sale of the drug in the US and royalties from AstraZeneca on future sales following the US Food and Drug Administration’s (FDA) approval of Truqap™ plus Faslodex®  as a treatment for adult patients with 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. 

This is the third cancer drug in the last five years to reach market approval that has been discovered and developed under, or subsequent to, an Astex drug discovery collaboration.  In addition to Truqap, Astex’s other partnered programs that have been highly successful in translating research into new cancer medicines include Novartis’ Kisqali®(ribociclib) and Janssen’s BALVERSA® (erdafitinib).

Truqap is a first-in-class oral targeted inhibitor of the cancer-driving protein AKT, also known as PKB. AKT is an enzyme that plays a key role in the PI3K/AKT tumor cell survival pathway, and dysregulation of this pathway leads to tumor resistance to a number of important anti-cancer medicines.  Truqap was discovered by AstraZeneca following an earlier drug discovery research collaboration between Astex, The Institute of Cancer Research, London, and Cancer Research Technology (CRT; now Cancer Research Horizons) that was signed in 2003.  As part of that earlier foundational research, Astex and The Institute of Cancer Research (ICR) used the 3D X-ray crystal structure of the AKT protein target to identify small molecule modulators of AKT activity using an approach known as fragment-based drug discovery.  In 2005 a series of prototype drug compounds discovered by Astex and the ICR was shown to have very promising activity against a range of human tumors grown in mice and was licensed to AstraZeneca.  In 2010, AstraZeneca announced its discovery of Truqap, and began to develop the drug as a potential treatment for various forms of cancer.

Following the marketing approval, Astex is eligible to receive a milestone payment from AstraZeneca on first commercial sale of the drug in the US as well as royalties on future sales.

Harren Jhoti PhD, President and Chief Executive Officer of Astex, UK, said: “We are incredibly proud that another of our drug discovery partnerships has resulted in such a successful outcome.  We applaud our valued colleagues at AstraZeneca for their tenacity and exceptional work in the discovery and development of this first-in-class medicine.”  

“The early research was a great collaborative effort, and I would like to acknowledge the impressive pioneering research carried out by our colleagues at the ICR, including solving the 3D crystal structure of AKT, which was vital in enabling our initial drug discovery approach. This is also a great example of UK Biotech-Academia-Pharma collaboration and underlines the strength of the UK life sciences ecosystem.”

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