Drug Discovery – Cancer & Auto-Immune Disease Drug Programmes

Sareum's pipeline is built on the expertise of its founders in pre-clinical drug discovery, particularly in the field of cancer. Sareum operates as a "virtual" research organisation i.e. all our research is carried out in the laboratories of third-party providers. This enables us to access drug discovery expertise throughout the world with a very flexible cost base.

Sareum concentrates its research on targeted small molecule therapeutics. Targeted cancer therapies disrupt specific biochemical processes necessary for tumour growth and survival. Because these processes are specific to cancer cells, targeted therapies may be more effective than other types of treatments, such as chemotherapy and radiotherapy, and less harmful to normal cells. Small molecule therapeutics (as opposed to "biological" drugs such as antibodies) are able to penetrate into the interior of a cancer cell and thus can be targeted at the full range of processes in a biochemical pathway. Small molecule therapeutics also have the potential of being able to be administered orally (e.g. as a pill) rather than by injection.

Our strategy is to focus on developing best in class therapies where pre-clinical and early clinical data is available to indicate that disrupting the targeted biochemical process will indeed prevent tumour growth and survival without significant side-effects, and to indicate whether or not the therapy needs to be administered in combination with additional cancer therapies.

Cancer cells differ from normal cells in many different ways. In particular, cancer cells divide and grow much more rapidly than normal cells. Biochemical processes targeted by Sareum that control cell growth and division include Checkpoint Kinase 1 (Chk1), Aurora Kinase (Aurora), FMS-like Tyrosine Kinase 3 (FLT3), Anaplastic Lymphoma Kinase (ALK), Polo-Like Kinase (PLK) and B-raf. Once a solid tumour reaches a certain size, it needs to be connected to the body's blood and lymph systems to receive nutrients and remove waste. Vascular Endothelial Growth Factor Receptor 3 Kinase, (VEGFR-3, sometimes referred to as Fms-like Tyrosine Kinase 4, FLT4) is importantly involved in the generation of new blood and lymph vessels to a tumour. VEGFR-3 is also involved in the control of metastasis, which is the main cause of death in cancer patients. Many cancer cells are highly dependent on fatty acid levels of which Fatty Acid Synthase (FASN) is a key regulator.

Kinase enzymes are also involved in the control of the immune response. FMS-like Tyrosine Kinase 3 (FLT3) is implicated in the maturation of dendritic cells, implicated in multiple sclerosis, rheumatoid arthritis and other auto-immune diseases. Tyrosine Kinase 2 (TYK2) controls the JAK-STAT pathway which is over-activated in many auto-immune disorders, including rheumatoid arthritis, psoriasis and Crohn's disease.

All of these programmes are available for partnering and/or research collaboration.

Further information is available on these programmes:

Chk-1 (download pdf) Aurora+FLT3&ALK (download pdf) VEGFR-3 (download pdf)

FLT3 (download pdf) TYK2 (download pdf)

*Chk1 is a joint discovery programme between Sareum, The Institute for Cancer Research (ICR) and Cancer Research Technologies (CRT).

For more information on Targeted Cancer Therapies, please see http://www.cancer.gov/cancertopics/factsheet/Therapy/targeted