26 February 2014

(“Sareum” or the “Company”)

Research Update & Co-Development Collaborations

Sareum (AIM: SAR), the specialist cancer drug discovery and development business, is pleased to announce positive progress with its cancer and auto-immune disease research programmes and reports the following updates on each of these programmes.

Checkpoint Kinase 1 (CHK1)

Studies on the CHK1 inhibitor candidate continue, following the agreement with the CRT Pioneer Fund and BACIT Limited, announced in September 2013.  These studies are focused on completing the pre-clinical development phase of the programme, which include demonstrating control of the production of the candidate molecule and an assessment of its safety profile.  If successful, it will lead to the submission of a clinical trial application to the UK regulator, MHRA.  If this is approved, the first-in-human trials in cancer patients would then be initiated.

In the meantime, the intellectual property estate that underpins the CHK1 programme continues to develop.  This included the granting of a patent for one of the inventions associated with the CHK1 cancer programme by the U.S. Patent and Trademark Office in December 2013.  This, combined with the patent applications currently under consideration in several territories, including two applications published in 2013, will provide broad geographical protection for the CHK1 programme currently being pursued if it is granted.

The Directors note with interest recent reports in scientific literature that CHK1 inhibition may be an effective strategy against cancers caused by mutations in a gene known as Myc. These mutations lead to spontaneous unregulated cell proliferation and have been identified in certain lymphomas and prostate, breast, lung and stomach cancers. This suggests that CHK1 inhibitors may be effective as single agents in a wider range of Myc-driven cancers, in addition to the previously reported neuroblastoma.


In July 2013 we announced the nomination of a pre-clinical development candidate in our Aurora+FLT3 programme.  The candidate molecule was selected after head-to-head studies with the two most promising programme compounds. Both molecules demonstrated excellent efficacy in disease models, but the selected candidate was superior in models of safety and predicated human exposure. The primary disease focus of the programme is Acute Myeloid Leukaemia (AML), but the candidate molecule has also demonstrated potent cell-killing activity against other cancers, particularly Acute Lymphoblastic Leukaemia (ALL), neuroblastoma and Anaplastic Large-Cell Lymphoma.

Following the nomination of the candidate, we signed a co-development agreement with Hebei Medical University Biomedical Engineering Center ("HMUBEC") in December.  As with CHK1, the first task is to demonstrate control of production and to assess its safety profile. This phase of the development work is still in its early stages and we look forward to providing further data in due course.

Auto-immune diseases and inflammatory disorders – TYK2+JAK1

Our auto-immune diseases programme is conducted in collaboration with SRI International (SRI), following the agreement announced in April 2013.  The disease biology expertise at SRI has focused on disease models that demonstrate how programme compounds are able to block TYK2 dependent signalling. 

Steady progress has been made since our last update. In a psoriasis disease model established at SRI, oral administration of the lead molecules leads to a significant reduction in the scaling and redness associated with the disease. Furthermore, the levels of many of the cytokines (signalling molecules) and other proteins thought to be responsible for the symptoms of psoriasis, were shown to be reduced by the addition of programme compounds. In a “rapid efficacy” model also established at SRI, levels of interferon-gamma, a cytokine involved in a number of autoimmune and inflammatory diseases, were shown to be reduced following oral administration of our lead compounds. This model allows us to rapidly screen compounds for biological activity before progressing them into more resource-intensive disease models.

These studies have also indicated that certain of our lead compounds are producing this effect via a combination of TYK2 and JAK1 inhibition. JAK1, like TYK2, is another member of the JAK family of kinases, and is essential for signalling by a number of cytokines also involved in psoriasis, as well as inflammatory bowel disease and rheumatoid arthritis.  Our compounds will be tested on models of these diseases in due course. Research into JAK1 has been the subject of considerable scientific interest of late and has resulted in several valuable clinical stage licensing deals.

We are planning to publish the results of our studies in scientific literature and present them at conferences during 2014. An additional patent application protecting programme compounds was published in September 2013.


The feasibility study phase of this programme is reaching its final stages, supported by the grant that was awarded by the Technology Strategy Board Biomedical Catalyst. This was awarded in April 2013 and we expect to issue further updates later in the year.

Sareum’s CEO, Dr. Tim Mitchell, commented:

“With three of our programmes now being advanced via collaborations, we have been able to secure significant additional resource and expertise to take them to later stages of development. By taking this route, we have also been able to maintain exposure to the greater upside associated with advanced programmes whilst mitigating much of the risk and cost had we attempted to take them forward alone.  We are now in a position to undertake further internal research to identify and develop new programmes.”


Sareum Holdings plc


Tim Mitchell

01223 497 700

Sanlam  Securities UK Limited (Nomad)

Simon Clements / Scott Mathieson

020 7628 2200

Hybridan LLP (Broker)


Claire Noyce / William Lynne

020 7947 4350 / 4361

The Communications Portfolio (Media enquiries)


Ariane Comstive

020 7536 2028

Notes for editors:

About Sareum Holdings plc

Sareum is a drug discovery and development company, headquartered in Cambridge UK, that produces targeted small molecule therapeutics, focusing on cancer and autoimmune disease. Sareum aims to successfully deliver drug candidates for licensing to pharmaceutical and biotechnology companies at the pre-clinical or early clinical trials stage.

Sareum operates an outsourced research model, working with collaborators (SRI International, the CRT Pioneer Fund and Hebei Medical University Biomedical Engineering Center) and a world-wide network of research providers.  Its research pipeline includes two programmes undergoing pre-clinical IND-enabling studies.

SKIL® (Sareum Kinase Inhibitor Library) is Sareum's drug discovery technology platform that has so far produced the Company's Aurora+FLT3, Aurora+ALK, VEGFR-3, FLT3 & TYK2 kinase cancer and auto-immune disease research programmes. 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