CSF-1R inhibitor Discovery Programme

Categories for this invention

Drug Discovery

Oncology

Intellectual Property

TRICYCLIC HETEROCYCLIC DERIVATIVES AND USES THEREOF

National Phase Application

WO2018083635

Seeking:

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Summary

An intuitive approach of using a unique scaffold and structure based approach to synthesis highly potent CSF-1R inhibitors for cancer therapy.

Problems Addressed

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

Technology

By combining our knowledge in medicinal chemistry 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 compounds 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.

Applications

Targeting CSF-1R (c-FMS Kinase) activity has the potential to treat various pathologies and conditions such as:

1. Cancer

2. Inflammation

3. Autoimmune diseases

4. Bone disease

5. Allograft rejection

6. Arteriosclerosis and atherosclerosis

Advantages

• Unique scaffold which differentiates our program from competitors.

• Used a structure based design approach using this scaffold docked with CSF1R structure.

• Our compounds have low nM potency and high degrees of selectivity with respect to other class III kinases.

• Specificity and control – reduced risk of off-target effects and increased potency.

• A world-class medicinal chemistry team at Auckland Cancer Society Research Centre with experience in design and evaluation of orally-active drug candidates.

• Promising results as a single agent and in combination with checkpoint inhibitors.

Questions about this Technology?

Contact Dr Sandhya Badrinarayanan