LONDON, April 5, 2017 /PRNewswire/ --
- AZD4635 (HTL-1071), a novel adenosine A2A receptor antagonist, reverses adenosine-mediated
- New preclinical results presented at AACR Annual Meeting
Heptares Therapeutics ("Heptares"), a wholly owned
AZD4635 is a potent and selective, orally available, small molecule adenosine A2A receptor antagonist discovered by Heptares and licensed to AstraZeneca in 2015.
The milestone was triggered by the successful completion of a preclinical programme that demonstrated a clear effect of AZD4635 in reversing adenosine-mediated T-cell suppression and enhancing anti-tumour immunity. Blockade of A2A signalling with AZD4635 was found to reduce tumour growth when used alone and in combination with anti-PD-L1 checkpoint inhibitors. Results from this programme will be presented by scientists from Heptares and AstraZeneca in a poster (abstract 5580) today at the American Association of Cancer Research Annual Meeting (1-5 April, 2017; Washington, DC, USA).
AZD4635 is currently in a Phase 1 clinical trial as a single agent and in combination with AstraZeneca's durvalumab (anti-PD-1L antibody) in patients with solid malignancies.
Tumour cells have evolved mechanisms to evade the immune system, including through the production of a natural anti-inflammatory molecule called adenosine. By stimulating A2A receptors, adenosine prevents T-cells within the immune system from being activated and reduces their ability to destroy cancer cells. Blocking A2A receptors can therefore promote the anti-cancer response of T-cells within the tumour microenvironment.
"The preclinical study results are very exciting and confirm that inhibition of A2A signalling offers an attractive mechanism to treat cancers by preventing tumours from evading the immune system and making them susceptible to checkpoint inhibitors," said Fiona Marshall, CSO of Heptares and Sosei. "We now look forward to the results from the first clinical study with AZD4635 around the end of the year."
Notes to Editors
About Heptares Therapeutics
Heptares is a clinical-stage company creating transformative medicines targeting G protein-coupled receptors (GPCRs), a superfamily of 375 receptors linked to a wide range of human diseases. Heptares' proprietary StaRŪ technology and structure-based drug design (SBDD) capabilities enable us to engineer and develop drugs for highly validated, yet historically undruggable or challenging GPCRs. Using this approach, we are building an exciting pipeline of new medicines (small molecules and biologics) with the potential to transform the treatment of Alzheimer's disease, schizophrenia, cancer immune-oncology, migraine, addiction, metabolic disease and other indications. We have partnerships for our novel candidates and technologies with leading pharmaceutical and biotechnology companies, including Allergan, AstraZeneca, Daiichi Sankyo, Kymab, MedImmune, MorphoSys, Pfizer and Teva.
Heptares is a wholly owned subsidiary of Sosei Group Corporation. For more information, please visit http://www.heptares.com and http://www.sosei.com.
HEPTARES is a registered trademark in the EU, Switzerland, US and Japan;
StaRŪ is a registered trademark in the EU and Japan.
Sosei is a biopharmaceutical company originating from Japan but with global presence. Sosei's primary business model is based on identifying novel and/or differentiated product assets or technology platforms and, through supporting these in preclinical and clinical development and establishing commercial partnerships, advancing new medicines to patients worldwide. For more information about Sosei, please visit http://www.sosei.com.
SOURCE Heptares Therapeutics
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