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TH-302
Evofosfamide (INN, USAN; formerly known as TH-302) is a compound being evaluated in clinical trials for the treatment of multiple tumor types as a monotherapy and in combination with chemotherapeutic agents and other targeted cancer drugs. This compound has been evaluated in the treatment of solid tumors, as a hypoxia-activated prodrug (HAPs), such chemical agents in low oxygen conditions undergo bio-reduction to yield cancer fighting cytotoxic breakdown products. Many such agents have been developed, though this compound has been extensively studied, in preclinical and clinical studies. Dec 2015 : two Phase 3 trials fail, Merck will not apply for a license Collaboration Evofosfamide was developed by Threshold Pharmaceuticals Inc. In 2012, Threshold signed a global license and co-development agreement for evofosfamide with Merck KGaA, Darmstadt, Germany (EMD Serono Inc. in the US and Canada), which includes an option for Threshold to co-commercialize evofosfamide in the Uni ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hypoxia-activated Prodrug
Hypoxia-Activated Prodrugs (HAPs) are prodrugs that target regions of tumor hypoxia within tumor cells. HAPs may offer the potential, alone and in combination with conventional chemotherapy, of improving cancer therapy. It is believed that tumor hypoxia contributes significantly to treatment failure and relapse among cancer patients because cells in the hypoxic zones of solid tumors resist traditional chemotherapy for at least two reasons: first, most antitumor agents cannot penetrate beyond 50-100 micrometers from capillaries, thereby never reaching those cells in the hypoxic regions. Secondly, the lower nutrient and oxygen supply to cells in the hypoxic zones of tumors cause them to divide more slowly than their well oxygenated counterparts, so hypoxic tumor cells exhibit greater resistance to chemotherapies and radiation which target rapidly dividing cells or require oxygen for efficacy. Hypoxia also contributes to the invasive and metastatic phenotypes of aggressive cancers by p ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |