Talabostat

Talabostat
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DOI:
10.1517/13543784.16.9.1459
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发表时间:
2007-09-01
影响因子:
6.1
通讯作者:
Cunningham, Charles Casey
Cunningham, Charles Casey
中科院分区:
医学2区
文献类型:
--
作者:
Cunningham, Charles Casey

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dTalabostat甲磺酸盐是一种口服活性的二肽基肽酶特异性抑制剂,包括肿瘤相关成纤维细胞活化蛋白。然而,通过独立的机制,塔拉司他还刺激细胞因子和趋化因子的上调,以产生肿瘤特异性宿主免疫应答,从而赋予其独特的双重作用机制。在临床试验中,talabostat已显示出显著的活性,包括在非小细胞肺癌和恶性黑色素瘤患者中实现完全缓解。
dTalabostat mesilate is an orally active, specific inhibitor of dipeptidyl peptidases, including tumor-associated fibroblast activation protein. However, by an independent mechanism, talabostat also stimulates the upregulation of cytokines and chemokines to engender a tumor-specific host immune response, thus giving it a unique dual mechanism of action. In clinical trials, talabostat has demonstrated significant activity, including achieving complete responses in patients with non-small-cell lung cancer and malignant melanoma.