MPC-3100
MPC-3100 is a potent, small molecule drug candidate designed by Myriad Pharmaceuticals for the treatment of cancer.
About MPC-3100
MPC-3100 is a potent, orally bioavailable, synthetic small molecule inhibitor of heat shock protein 90 (HSP90). In animal models, MPC-3100 was effective at inhibiting growth of a variety of tumor xenografts. Remarkably, there was very little apparent toxicity in these animal studies when assessed by body weight and other parameters. We believe this excellent therapeutic index along with the good oral bioavailability will provide an opportunity for daily oral dosing with MPC-3100. Currently, we are completing ongoing preclinical studies with the aim to file an IND to the FDA in the first half of 2009.
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About Heat Shock Protein 90
The HSP90 molecular chaperone has emerged as an exciting target for cancer drug discovery. An attractive feature of HSP90 as a cancer drug target is its requirement for the conformational stability and function of a wide range of oncogenic client proteins, including HER2, EGFR, c-Raf-1, Flt-3, AKT, p53, c-Met, Polo-1 and telomerase hTERT. The client proteins of HSP90 span multiple signaling pathways that are critical for cancer cell survival. Inhibiting HSP90 should therefore lead to inhibition of many or all of the hallmarks of cancer including cell proliferation, survival, invasion, and angiogenesis. These traits give HSP90 inhibition the potential to be effective in a broad range of cancer types.
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Reference
- MPC-3100: A non-natural product Hsp90 inhibitor with anti-tumor activity in preclinical models. [Poster PDF]
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