Preclinical synergy of sra737 and PARP inhibitor

SAREUM HOLDINGS PLC

("Sareum" or "the Company")

Sareum notes that Sierra Oncology will report preclinical data demonstrating SRA737 Synergy with PARP inhibitors at the AACR 2018 Annual Meeting

Sareum Holdings plc (AIM: SAR), the specialist cancer drug discovery and development business, notes that Sierra Oncology, the licence holder advancing clinical cancer candidate SRA737, announced yesterday that it will present preclinical data demonstrating that its Chk1 inhibitor, SRA737, synergizes with niraparib, a poly ADP-ribose (PARP) inhibitor, in a poster at the American Association of Cancer Research (AACR) Annual Meeting 2018 being held in Chicago, USA from 14-18 April.

PARP inhibitors prevent the repair of DNA damage and are developed as treatments for cancer and other indications. Niraparib is an orally active small molecule PARP inhibitor approved in the US to treat ovarian cancer.

Sierra Oncology holds exclusive and worldwide rights for the Chk1 inhibitor, SRA737, having licensed the programme from Sareum's co-investment partner, the CRT Pioneer Fund in September 2016.

Dr Tim Mitchell, Chief Executive Officer of Sareum, commented: "We are pleased to note this positive development from preclinical studies exploring the combination of SRA737 with the PARP inhibitor niraparib. Combining these two modalities to induce synthetic lethality in cancer cells is a compelling proposition and we look forward to further data and details of a potential clinical development programme during the year."

The Press release from Sierra Oncology can be found by clicking here

Poster Title: The Chk1 inhibitor, SRA737, synergizes with niraparib to kill cancer cells via multiple cell death pathways

Date and Time: Monday 16 April 2018 8:00 AM - 12:00 PM

Location: McCormick Place South, Exhibit Hall A, Poster Section 37

Poster Board Number: 11

Permanent Abstract Number: 1853

The Poster will be available on 16 April 2018 on www.sierraoncology.com 

Sierra Oncology will host a Program Update on Tuesday, 27 February from 10:00 AM - 12:00PM Eastern Time (ET) in New York, NY, during which the senior management team will present a strategic update on the development programme for SRA737. A live audio webcast and archive of the presentation will be accessible through www.sierraoncology.com.

For further information, please contact: 

Notes for editors: 

Sareum is a drug discovery and development company delivering targeted small molecule therapeutics, focusing on cancer and autoimmune disease, and licensing them to pharmaceutical and biotechnology companies at the preclinical or early clinical trials stage.

Sareum operates an outsourced research model, working with international collaborators and a world-wide network of research providers. Its most advanced programme (Chk1) commenced clinical trials in May 2016 and was licensed to NASDAQ-listed Sierra Oncology in September 2016.

SKIL® (Sareum Kinase Inhibitor Library) is Sareum's drug discovery technology platform that has so far produced the Company's Aurora+FLT3 and TYK2 kinase cancer and autoimmune disease research programmes, which are in the IND-enabling preclinical and lead optimisation stages respectively. SKIL® can also generate drug research programmes against other kinase targets.

Sareum Holdings plc is listed on the AIM market of the London Stock Exchange, trading under the symbol SAR. For further information, please visit www.sareum.co.uk

Checkpoint Kinase 1 (Chk1) and SRA737 (formerly CCT245737):

SRA737 is a highly selective, orally available, small molecule inhibitor of Checkpoint kinase 1 (Chk1).

DNA is continuously subject to damage through a variety of endogenous and exogenous mechanisms and, in turn, cells have developed complex processes to resolve this DNA damage. Chk1 is a central regulator in the DNA Damage Repair ("DDR") network of cellular pathways that detect and repair DNA damage. Chk1 impacts multiple cell-cycle checkpoints, temporarily inhibiting the progression of cell replication and division in order for DNA repair processes to be undertaken.

Malignant cells tolerate substantially greater levels of DNA damage than would be acceptable in healthy cells. Cancer cells survive and replicate, despite accumulating DNA damage due to replicative stress, via an over-reliance on select components of the DDR network including Chk1. As such, inhibition of Chk1 by SRA737 may be synthetically lethal to cancer cells and of potential benefit in the treatment of certain cancers.

Certain standard chemotherapeutic agents and radiotherapy also induce DNA damage in order to kill cancer cells. There exists potential for synergy between these standard therapies and Chk1 inhibitors such as SRA737.

SRA737737 was discovered and initially developed by scientists in the Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research (ICR) in collaboration with Sareum, with funding provided by Cancer Research UK, the ICR and Sareum. The program was licensed by CRT and the ICR to the CRT Pioneer Fund, a specialist cancer investment fund established by Sixth Element Capital LLP (6EC), Cancer Research Technology (CRT) and the European Investment Fund (EIF) and managed by 6EC, in September 2013 and a co-investment partnership with Sareum was formed to progress the candidate drug through clinical trials.

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