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Drugs. 2015 Apr;75(5):543-51. doi: 10.1007/s40265-015-0379-9.
Palbociclib (Ibrance®) is an oral, reversible, selective, small-molecule inhibitor of cyclin-dependent kinases (CDK) 4 and CDK6 developed by Pfizer for the treatment of cancer. CDKs are important modulators of cell cycle entry and progression in response to growth signals, and inhibition of these kinases with palbociclib could enhance the activity of other anticancer drugs in tolerable regimens. Palbociclib, in combination with letrozole, was recently approved in the US for the first-line treatment of advanced breast cancer. Phase III development is underway worldwide investigating its use as first-line treatment in advanced breast cancer, as well as treatment of recurrent or advanced breast cancer and high-risk, early-stage breast cancer. A phase II trial is underway in the USA for non-small cell lung cancer under a US National Cancer Institute-funded research collaboration, and several phase I and II investigations are being conducted for various other solid tumour types and haematological malignancies. This article summarizes the milestones in the development of palbociclib leading to this first approval for use in postmenopausal women with estrogen-positive, human epidermal growth factor receptor (HER) 2-negative advanced breast cancer as initial endocrine-based therapy for their metastatic disease.
帕博西尼（Ibrance®）是辉瑞公司开发的一种口服、可逆、选择性、小分子细胞周期蛋白依赖性激酶（CDK）4 和 CDK6 抑制剂，用于治疗癌症。CDKs 是细胞周期进入和进展的重要调节剂，对这些激酶的抑制作用可能会增强其他抗癌药物在可耐受方案中的活性。帕博西尼联合来曲唑最近在美国被批准用于晚期乳腺癌的一线治疗。全球范围内正在进行 III 期开发，以研究其在晚期乳腺癌的一线治疗、复发性或晚期乳腺癌以及高危早期乳腺癌中的应用。在美国，一项非小细胞肺癌的 II 期试验正在进行中，这是在美国国立癌症研究所资助的研究合作下进行的，此外还正在进行多项针对各种实体瘤类型和血液恶性肿瘤的 I 期和 II 期研究。本文总结了帕博西尼开发过程中的里程碑事件，这些事件导致了该药首次批准用于绝经后妇女的雌激素阳性、人表皮生长因子受体（HER）2 阴性晚期乳腺癌，作为转移性疾病的初始内分泌治疗。
