Division of Hematology & Oncology, Department of Medicine, Medical College of Wisconsin, 9200 W Wisconsin Avenue, Milwaukee, WI 53226, USA.
Future Med Chem. 2012 Jun;4(10):1257-72. doi: 10.4155/fmc.12.69.
There is an ever pressing need to develop new drugs for the treatment of cancer. Gallium nitrate, a group IIIa metal salt, inhibits the proliferation of tumor cells in vitro and in vivo and has shown activity against non-Hodgkin's lymphoma and bladder cancer in clinical trials. Gallium can function as an iron mimetic and perturb iron-dependent proliferation and other iron-related processes in tumor cells. Gallium nitrate lacks crossresistance with conventional chemotherapeutic drugs and is not myelosuppressive; it can be used when other drugs have failed or when the blood count is low. Given the therapeutic potential of gallium, newer generations of gallium compounds are now in various phases of preclinical and clinical development. These compounds hold the promise of greater anti-tumor activity against a broader spectrum of cancers. The development of gallium compounds for cancer treatment and their mechanisms of action will be discussed.
对于癌症的治疗，开发新的药物一直是当务之急。作为 IIIa 族金属盐的硝酸镓，在体外和体内都能抑制肿瘤细胞的增殖，并在临床试验中显示出对非霍奇金淋巴瘤和膀胱癌的活性。镓可以作为铁模拟物，扰乱肿瘤细胞中依赖铁的增殖和其他与铁相关的过程。硝酸镓与传统化疗药物无交叉耐药性，且无骨髓抑制作用；当其他药物无效或血象较低时，可以使用。鉴于镓的治疗潜力，新一代的镓化合物目前处于临床前和临床开发的各个阶段。这些化合物有望对更广泛的癌症具有更强的抗肿瘤活性。本文将讨论用于癌症治疗的镓化合物的开发及其作用机制。
