Promics Pty Limited

Michael Wellesley Whitehouse

Stephen Maxwell Taylor

Ian Alexander Shiels

David P Fairlie

Darren Ray March

Lindsay Charles Brown

This invention relates to the use of an antagonist of a G protein-coupled receptor in the prevention and/or treatment of fibrosis, such as the treatment of fibrosis associated with myocardial infarction or diabetes or certain pulmonary conditions. In a preferred embodiment, the antagonist is a C5a receptor antagonist, more preferably a cyclic peptide antagonist of the C5a receptor. In particular, the invention provides a method of prevention, treatment or alleviation of a fibrotic condition, comprising the step of administering an effective amount of an antagonist of a G protein-coupled receptor to a subject in need of such treatment.

Use of C5a receptor antagonist in the treatment of fibrosis

The invention relates to novel cyclic compounds which have the ability to modulate the activity of G protein-coupled receptors. The compounds preferably act as antagonists. In preferred embodiments, the invention provides cyclic peptidic and peptidomimetic antagonists of C5a receptors, which are active against C5a receptors on polymorphonuclear leukocytes and macrophages. The compounds of the invention are both potent and selective, and are useful in the treatment of a variety of inflammatory conditions.

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Holland Park, Australia

Michael Wellesley Whitehouse