Vismodegib (GDC-0449, GDC0449),又称维莫德吉或维莫地尼,是用于治疗晚期皮肤基底细胞癌的新药之一,是特异性的hedgehog信号通路抑制剂,IC50值为3 nM。Vismodegib通过抑制SMO受体使转录因子GLT-1/2维持非活化状态,从而阻断hedgehog信号通路。
参考文献
[1]Scales SJ, et al. Mechanisms of Hedgehog pathway activation in cancer and implications for therapy. Trends Pharmacol Sci. 2009;30(6), 303-312.
[2]Zhang Y, et al. Hedgehog pathway inhibitor HhAntag691 is a potent inhibitor of ABCG2/BCRP and ABCB1/Pgp. Neoplasia. 2009;11(1), 96-101.
[3]Tian F, et al. The hedgehog pathway inhibitor GDC-0449 alters intracellular Ca2+ homeostasis and inhibits cell growth in cisplatin-resistant lung cancer cells. Anticancer Res. 2012;32(1), 89-94.
[4]Wong H, et al. Pharmacokinetic-pharmacodynamic analysis of vismodegib in preclinical models of mutational and ligand-dependent Hedgehog pathway activation. Clin Cancer Res. 2011;17(14), 4682-4692.
冰袋运输。粉末直接保存于-25~-15℃,有效期2年。建议干燥避光保存,避免反复冻融。