Recent progress in the development of antagonists to the chemokine receptors CCR3 and CCR4.

Introduction: The chemokine receptors CCR3 and CCR4 have been shown to be important therapeutic targets for the treatment of a variety of diseases. Although only two chemokine receptor inhibitors have been approved so far, there are numerous compounds that are in various stages of development.

Areas Covered: In this review article, the authors provide an update on the progress made in the identification of antagonists against the chemokine receptors CCR3 and CCR4 from 2009 to the present. The rationale of writing this review article is to cover the most important approaches to identifying antagonists to these two receptors, which could prove to be useful therapeutics in treating proinflammatory diseases.

Expert Opinion: Pharmaceutical companies have expended a considerable amount of money and effort to identify potent inhibitors of CCR3 and CCR4 for the treatment of asthma and atopic diseases. Although a variety of compounds have been described and several have progressed into the clinic, none have so far made it as approved drugs. There are, however, novel approaches such as mogamulizumab, a monoclonal antibody to CCR4 currently is in clinical trials for cancer and ASM8, an antisense nucleotide to CCR3, which is in Phase II clinical trials for asthma that might still prove to be successful new therapeutics.