CHR-2797: a first-in-class oral aminopeptidase inhibitor
CHR-2797 is an aminopeptidase inhibitor that has demonstrated anti-tumour activity in a number of models of cancer, both as a single agent and in synergy with cytotoxic agents such as carboplatin and paclitaxel. In October 2004, CHR-2797 entered a Phase I clinical trial in the UK designed to evaluate its safety and tolerability in patients with treatment refractory metastatic cancer. In April 2006, CHR-2797 entered the phase I portion of a multi-centre Phase I/II clinical trial in patients with haematological malignancies, designed to assess safety, tolerability and efficacy in this patient group and in March 2007 entered the phase II portion of this study. In September 2006, patient dosing began in a Phase I solid tumour study combining CHR-2797 with paclitaxel. Further Phase II studies of CHR-2797 as monotherapy and combination therapy are planned to commence in the US and Europe during 2007. As far as Chroma is aware, CHR-2797 is the only small molecule aminopeptidase inhibitor under clinical development.