CSFR-1 Inhibitor Discovery Programme
Categories for this invention
TRICYCLIC HETEROCYCLIC DERIVATIVES AND USES THEREOF
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Contact: Sandhya Badrinarayanan
An intuitive approach of using a unique scaffold and structure based approach to synthesis highly potent CSF-1R inhibitors for cancer therapy
Colony-stimulating factor 1 receptor (CSF1R), is a cell-surface receptor and plays an important role as regulator of the development, morphology, survival, and functions of tissue macrophages as well as tumor-associated macrophages (TAMs). CSF1 is involved in the recruitment and survival of macrophages in tumors. Increased CSF1 expression is implicated in tumor progression and metastasis, and is associated with poor prognosis in some cancers.
Targeting CSF-1R (c-FMS Kinase) activity has the potential to treat various pathologies and condition such as: 1. Cancer 2. Inflammation 3. Autoimmune diseases
By combining our knowledge in medicinal chemsitry and biology, we have developed a novel series of highly potent and selective CSF-1R inhibitors that are currently at lead stage. We have identified a unique scaffold consisting of a tricyclic heterocyclic compound with improved selectively over competitors’ programmes. These componds show good efficacy as a single agent but have potential in combination therapies with PD-1, PDL-1, CTLA-4 antibodies, IDO inhibitors and cancer vaccines.