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APO866APO866 is a potent and specific inhibitor of NMPRT, a key enzyme involved in the synthesis of NAD. Apoxis, now TopoTarget Switzerland S.A., acquired the worldwide development and marketing rights to APO866 from Astellas in October 2005. APO866 has a novel mechanism of action and therefore a new therapeutic approach to cancer. TopoTarget believes that this product has potential both as a monotherapy and in combination with other chemotherapeutic agents or radiotherapy.APO866 inhibits the growth of human tumours in a wide variety of in vivo xenograft models using nude mice. The production of vascular endothelial growth factor ("VEGF") by tumour cells in vitro was significantly reduced by APO866. The in vitro anti-cancer effects of APO866 were not modified by the main mechanisms of multidrug resistance, suggesting that APO866 may retain efficacy as a monotherapy in tumours that have become resistant to commonly used chemotherapeutic agents. APO866 has been shown in both in vitro and in vivo studies to enhance the anti-tumour activity of DNA-damaging anticancer drugs. APO866 has also been shown to enhance the effectiveness of radiation therapy. APO866 for the treatment of advanced melanoma
TopoTarget has initiated an open-label Phase II study to assess the efficacy and safety of 3 cycles of APO866 in 43 patients with advanced melanoma.APO866 for the treatment of Cutaneous T-cell lymphoma (CTCL)
TopoTarget has initiated an open-label Phase II study to assess the efficacy, tolerability and safety of 3 cycles of APO866 in 23 patients with refractory or relapsed CTCL. APO866 for the treatment of refractory or relapsed B-Chronic Lymphocytic Leukemia (B-CLL)
TopoTarget has initiated an open-label Phase I/II proof-of-concept study to assess the safety and tolerability of one cycle of APO866 in 10 patients with refractory B-CLL who are not fit for allogeneic hematopoietic stem cell transplantation ("aHSCT"). Useful links :
Therapeutic Areas
- Solid tumours and haematology
Science
- NAD+
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