NexGenix Pharmaceuticals has presented positive data on NXD30001, one of several novel, radicicol-based Hsp90 inhibitors in its compound series.
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NXD30001 demonstrated efficacy in breast cancer tumor xenograft models without evidence for liver and kidney toxicity. The potency, tolerability, pharmacokinetic and pharmacodynamic properties of NXD30001 and its derivatives indicate that it, or an analog, may be useful in the treatment of breast and other forms of cancer with an improved dosing and therapeutic window compared to 17AAG, the first-in-class Hsp90 inhibitor currently in Phase II clinical trials for cancer.
NXD30001 and its analogs efficiently inhibit cell proliferation and deplete multiple Hsp90 client proteins such as Her2, Akt, c-Raf, Cdk4, and Cyclin D1 in Her2-overexpressing breast and other cancer cell lines at low nanomolar concentrations.
Pharmacokinetic studies also demonstrate that NXD30001 can achieve potential therapeutic levels via intraperitoneal dosing and that the compound accumulates in tumors at above micromolar concentrations.
Allan Rubenstein, CEO of NexGenix, said: “Our intent is to progress an i.v. formulation of NXD30001 into IND-enabling studies for breast cancer, and to develop an oral formulation from the series for neural tumors, such as those found in neurofibromatosis Type 2, and for neurodegenerative disorders.”
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