The Sound of Evolution
Axitinib
阿昔替尼
Mechanism of action:
Axitinib 是一種小分子酪胺酸激酶抑制劑（tyrosine kinase inhibitor），主要針對血管內皮生長因子受體（VEGFR）家族的酪胺酸激酶活性進行選擇性抑制，包含 VEGFR-1、VEGFR-2、VEGFR-3。Axitinib 阻斷 VEGF 訊息傳遞，抑制腫瘤相關血管新生與供血訊號，進而抑制腫瘤細胞生長。
Reference(s):
1. Cohen EE et al. (2008). Axitinib is an active treatment for all histologic subtypes of advanced thyroid cancer: results from a phase II study. J Clin Oncol.
2. Inai T et al. (2004). Inhibition of vascular endothelial growth factor (VEGF) signaling in cancer causes loss of endothelial fenestrations, regression of tumor vessels, and appearance of basement membrane ghosts. Am J Pathol.
3. Rugo HS et al. (2005). Phase I trial of the oral antiangiogenesis agent AG-013736 in patients with advanced solid tumors: pharmacokinetic and clinical results. J Clin Oncol.