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UK-based SME offer novel small molecule for treatment of fibrosis caused by inflammatory bowel disease

Country of Origin: United Kingdom
Reference Number: TOUK20180413002
Publication Date: 13 April 2018

Summary

A UK-based SME has developed a novel small molecule shown to be able to prevent and reverse fibrosis caused by inflammatory bowel disease.This potent activity is combined with a good safety profile with no adverse effects shown in animal models tested. The SME is offering this small molecule to other pharmaceutical companies for further development and commercialisation. It is expected that the partnership will take the form of a licensing agreement or a technical cooperation

Description

Patients with inflammatory bowel disease (IBD) are at high risk of developing fibrosis that can cause narrowing and obstruction of the bowel. This occurs in 30-40% of patients within 10 years of their diagnosis and of these 80% require surgery but recurrence occurs in 70% of cases. Methods of preventing and treating this fibrosis are therefore needed.

A UK-based SME has developed a novel small molecule that has activity against ROCK 1 and 2 (Rho-associated coiled-coil-containing protein kinase), which are proteins involved in multiple aspects of the process of fibrosis. This novel small molecule has been shown to be potent and selective against its targets, with enantiomers having similar biological properties. This activity has been shown to prevent and even reverse fibrotic phenotypes in cell culture systems and mouse models. This is combined with a good safety profile with no adverse effects seen in animal models.

The SME is offering this novel small molecule to other companies operating in the pharmaceutical space. In particular those with an interest in fibrosis and fibrotic diseases. The molecule will be provided for further development and commercialisation with the partnership envisaged as a licensing agreement or a technical cooperation depending on circumstances.

Advantages and Innovations

The SMEs novel small molecule has the following advantages:

Potent and selective activity against ROCK 1/2 - efficacy is in the low nano-molar range.

Prevents and even reverses fibrotic changes, demonstrated both in vitro and in vivo.

Good safety profile in animal models.

Limited systemic exposure even at doses significantly above therapeutic levels with significant drug concentrations remaining in colon tissue 24 hours after oral dosing.

Stage Of Development

Under development/lab tested

Requested partner

The SME is looking to partner with other companies in the pharmaceutical sector and in particular those with interests in fibrosis and fibrotic diseases.

The SME will provide the novel small molecule to a partner for further development and ultimately commercialisation. It is expected that the partnership will take the form of a licensing agreement, although technical cooperations will be considered if the situation warrants it.

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