Burris H A, Fields S
Institute for Drug Development, Cancer Therapy and Research Center, San Antonio, TX 78229.
Semin Oncol. 1994 Oct;21(5 Suppl 10):14-9; discussion 19-20.
The semisynthetic vinca alkaloid vinorelbine (Navelbine; Burroughs Wellcome Co, Research Triangle Park, NC; Pierre Fabre Médicament, Paris, France) is unique in its chemical structure, microtubule selectivity, and neurotoxicity profile. In preclinical studies, vinorelbine showed encouraging activity against a variety of cell lines and human xenografts. In phase I studies, partial responses were noted in a variety of tumor types, including lung, breast, and head and neck cancers; melanoma; and lymphoma. Toxicity has centered around neutropenia, with minimal nonhematologic toxicity observed. Neurotoxicity has been primarily limited to reversible paresthesias. Because of its broad spectrum of antitumor activity and mild toxicity profile, vinorelbine is a promising anticancer agent.
半合成长春花生物碱长春瑞滨(诺维本;百时美施贵宝公司,北卡罗来纳州三角研究园;法国巴黎皮尔法伯制药公司)在化学结构、微管选择性和神经毒性方面具有独特性。在临床前研究中,长春瑞滨对多种细胞系和人异种移植物显示出令人鼓舞的活性。在Ⅰ期研究中,在多种肿瘤类型中观察到部分缓解,包括肺癌、乳腺癌和头颈癌;黑色素瘤;以及淋巴瘤。毒性主要集中在中性粒细胞减少,非血液学毒性极小。神经毒性主要局限于可逆性感觉异常。由于其广泛的抗肿瘤活性和轻微的毒性特征,长春瑞滨是一种很有前景的抗癌药物。