REVIEW Mubritinib (TAK-165) is a HER2/ErbB2 protein kinase inhibitor with IC50 of 6 nM; no activity to EGFR, FGFR, PDGFR, JAK1, Src and Blk. The compound was under development by Takeda for the treatment of cancer. Mubritinib reduced HER2/Neu-enhanced phosphorylated AR and MAP kinase, indicating that the MAP kinase pathway seems to be involved in the phosphorylation of the AR by HER2/Neu. Both HER2/Neu inhibitor Mubritinib successfully reduced the HER2/Neu-induced transactivation activity of the AR in PC-3 and DU-145 cells, suggesting that such an inhibitor was a possible therapeutic drug for patients with hormone-refractory prostate cancer. Mubritinib completed phase I clinical trials but appears to have been discontinued, as no new information on the drug has surfaced since December 2008.
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Sugita, Shozo; Kawashima, Hidenori; Tanaka, Tomoaki; Kurisu, Takeshi; Sugimura, Kazunobu; Nakatani, Tatsuya Effect of type I growth factor receptor tyrosine kinase inhibitors on phosphorylation and transactivation activity of the androgen receptor in prostate cancer cells: Ligand-independent activation of the N-terminal domain of the androgen receptor, Oncology Reports (2004), 11(6), 1273-1279.
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Nagasawa, Joji; Mizokami, Atsushi; Koshida, Kiyoshi; Yoshida, Sei; Naito, Kenichiro; Namiki, Mikio Novel HER2 selective tyrosine kinase inhibitor, TAK-165, inhibits bladder, kidney and androgen-independent prostate cancer in vitro and in vivo International Journal of Urology (2006), 13(5), 587-592.
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