Novel Integrin Antagonists

Opportunity

This opportunity is led by Dr. Helen Sheldrake and is underpinned by a patent which is focused on covalently binding Alpha-v beta-3 (αvβ3) integrin antagonist to reduce both existing tumour growth and development of new metastases in solid tumours including advanced melanoma and glioblastoma.

The problem

αvβ3 integrin is a cell surface adhesion and signalling receptor involved in angiogenesis (new blood vessel formation), cancer progression and metastasis. However, no drug targeting αvβ3 has been successful in clinical trials. This invention provides αvβ3 antagonists to prevent/treat cancer progression with superior properties to previously developed agents.

Application

This invention can be used potentially for the treatment of cancer, osteoporosis, diseases involving angiogenesis such as age-related macular degeneration, atherosclerosis, thrombosis, fibrosis; functionalisation of surfaces to promote cell adhesion; preventing virus internalisation; medical imaging; immunocytochemistry.

Benefits

• Provides increased anticancer efficacy compared to existing small molecules by overcoming issues of short half-life, poor pharmacokinetics and poor bioavailability which can lead to poor target coverage and contributed to the failure of previous small molecule clinical candidates.
• Affords long duration target coverage at low doses reducing side effects.
• Provides high αvβ3 selectivity reducing risk of side-effects from binding related integrins such as αIIbβ3 or αvβ5.
• Possibility of oral administration not possible with peptides and antibodies previously developed.