VNP40541 is an anticancer agent in late-stage preclinical development. It exhibited anticancer activity in preclinical studies and is activated under hypoxic (low oxygen) conditions.
A: VNP40541 is a hypoxia-selective anticancer agent that is being evaluated in preclinical studies. Hypoxic, or low-oxygen, tumor cells, representing a fraction of the whole tumor, are resistant to cancer treatment modalities including radiation and chemotherapy. VNP40541 converts to a cytotoxic compound only under hypoxic conditions. VNP40541 remains relatively inactive under oxic conditions. Upon activation in hypoxic conditions, VNP40541 liberates the DNA chloroethylating species 90CE, which is the same active metabolite released by Cloretazine® (VNP40101M). 90CE produces interstrand DNA cross-links that are difficult to repair and are toxic to cells.
A: Human clinical trials are expected to commence in 2008.