第一個治療乳癌的週期素依賴性激酶抑制劑：Palbociclib

Palbociclib: Cyclin-Dependent Kinase Inhibitor (CDK 4/6)

10.3966/168395442018061801004

許派洲(Pai-Chou Hsu)

乳癌 ； 週期素依賴性激酶抑制劑 ； breast cancer ； Cyclin-dependent kinase inhibitor

腫瘤護理雜誌

18卷1期（2018 / 06 / 01）

39 - 43

繁體中文

乳癌是全世界最普遍的惡性腫瘤類型之一，而荷爾蒙受體陽性是乳癌中最常見的表型。治療結果雖逐年繼續改善，但許多患有晚期疾病或疾病復發的病人逐漸對荷爾蒙治療產生抗藥性。週期素依賴性激酶4/6抑制劑（cyclin-dependent kinase 4 and 6 （CDK4/6） inhibitor）的發現，已經為乳癌治療開立另一新契機。Palbociclib於2015年被美國FDA通過，成為世界上第一個上市的週期素依賴性激酶4/6抑制劑。Palbociclib於2017年在台灣上市，已經被證實對具有荷爾蒙受體呈陽性且第二型人類上皮細胞生長因子（HER2）呈陰性的乳癌有治療角色。它可與芳香環轉化酶抑制劑（aromatase inhibitor）合併使用作為第一線治療，亦可與fulvestrant合併使用於先前曾接受過內分泌治療的病人。Palbociclib是一種具選擇性的週期素依賴性激酶4/6抑制劑。它可阻止乳癌細胞從細胞週期的G1期進展至S期，降低細胞增生的作用進而導致細胞死亡。Palbociclib經由口服方式給藥。最常見的副作用包括嗜中性白血球低下症、貧血、白血球低下症與疲倦。

Breast cancer is the most prevalent type of malignant neoplasm worldwide and hormone-receptor-positive breast cancer is the most common phenotype. The treatment outcomes continue to improve, but many patients with advanced disease or recurrence have progressively developed drug resistance to endocrine therapy. The discovery of cyclin-dependent kinase 4 and 6 (CDK4 and CDK6) inhibitor has provided a new opportunity in breast cancer treatment. In 2015, palbociclib became the first cyclin-dependent kinase 4 and 6 inhibitor approved by FDA, and in 2017 approved by Taiwan Food and Drug Administration as it started to play its effective role in the treatment of hormone-receptor-positive and HER2-negative breast cancer. It can be used in combination with aromatase inhibitors as a first-line treatment, or with fulvestrant in patients who have previously received endocrine therapy. Palbociclib is a selective inhibitor of the cyclin-dependent kinase 4 and 6. It reduced cellular proliferation of breast cancer cells by blocking progression of the cell from G1 into S phase of the cell cycle and caused cell death. Palbociclib is taken orally. The most common adverse effects are neutropenia, anemia, leucopenia, and fatigue.

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