Palanisamy R Priyadharsini
Department of Pharmacology, JIPMER, Puducherry, India.
J Cancer Res Ther. 2016 Oct-Dec;12(4):1220-1223. doi: 10.4103/0973-1482.168988.
Breast cancer being one of the common cancers has high morbidity and mortality. Despite the conventional treatment, the burden of the disease increases year after year. There is a need for newer drugs that target the different mechanisms in the pathogenesis. The interaction of cyclins with cyclin dependent kinases (CDKs) plays a major role in the abnormal cell cycle in cancer and it is considered to be an important target. Palbociclib is a CDK inhibitor currently approved for the treatment of breast cancer. The preclinical studies with breast cancer lines were sensitive to palbociclib and the clinical trials phase I, phase II (PALOMA 1), and phase III (PALOMA 2, 3, PENTELOPE, PEARL) showed that the drug was efficacious when combined other conventional drugs for breast cancer. Palbociclib was also been tested in various other germ cell tumors, melanoma, multiple myeloma, glioblastoma multiforme etc., The major adverse effect of the drug includes hematological toxicity mainly neutropenia, gastrointestinal adverse effects.
乳腺癌作为常见癌症之一，发病率和死亡率都很高。尽管有传统治疗方法，但该疾病的负担仍逐年增加。需要有针对发病机制中不同机制的新型药物。细胞周期蛋白与细胞周期蛋白依赖性激酶（CDK）的相互作用在癌症异常细胞周期中起主要作用，被认为是一个重要靶点。帕博西尼是一种目前已获批用于治疗乳腺癌的CDK抑制剂。对乳腺癌细胞系的临床前研究表明其对帕博西尼敏感，而I期、II期（PALOMA 1）和III期（PALOMA 2、3、PENTELOPE、PEARL）临床试验表明，该药物与其他乳腺癌常规药物联合使用时有效。帕博西尼也已在各种其他生殖细胞肿瘤、黑色素瘤、多发性骨髓瘤、多形性胶质母细胞瘤等中进行了测试。该药物的主要不良反应包括血液学毒性，主要是中性粒细胞减少，以及胃肠道不良反应。
