考布他汀A4磷酸酯(CA4P)抗肿瘤作用研究进展

Advances in the study of the anti-tumor activity of combretastatin A4 phosphate

考布他汀A4磷酸酯(combretastatin A4 phosphate,CA4P)是小分子血管破坏剂的代表药物之一,可结合微管蛋白,选择性破坏现存肿瘤血管。其快速特异性阻断肿瘤血管的作用已被众多临床前及临床研究应用多种观测技术所证实。CA4P可致肿瘤组织快速坏死,遗留外周活瘤带,可增强放化疗、免疫疗法、血管生成抑制剂等的抗癌作用。该药目前已进入Ⅲ期临床研究。

Combretastatin A4 phosphate（CA4P）is one of the most potent low-molecular-weight vascular-disrupting agents（VDAs）,which binds to tubulin and targets existing tumor blood vessels.Pronounced tumor blood flow shutdown has been demonstrated in preclinical models and patients by various techniques.CA4P typically induces rapid tumor necrosis in the center of the tumor and leaves a rim of viable cells in the periphery.In oncology,CA4P appears to be more efficacious when combined with chemotherapy,antiangiogenic therapy and radiation therapy.The drug is currently undergoing phase Ⅲ clinical trials.