Ado-trastuzumab Emtansine：第一個用於固態腫瘤之抗體結合藥品

Ado-Trastuzumab Emtansine: The First Monoclonal Antibody Conjugate in Treating Solid Tumor

姜紹青(Shao-Chin Chiang)

《腫瘤護理雜誌》 14卷2期 (2014/12) Pp. 19-26

https://doi.org/10.3966/168395442014121402003

摘要

Ado-trastuzumab emtansine是一個革命性藥品，將單株抗體與傳統性化學藥品結合，用於治療固態性腫瘤。此藥具有相當高的專一性，藉著抗體引導細胞毒性藥品到達癌細胞，在不破壞其他正常細胞的情況下，直接攻擊癌細胞。它主要是由三個部份包括單株抗體trastuzumab、細胞毒性藥品emtansine以及連結物硫醚鍵（thioether linkage）所構成。臨床試驗中被證明對於曾接受trastuzumab治療的後期或轉移性乳癌有相當好的良效。常見的副作用為血小板過低、肝指數上升、和左心室射出率下降。治療時，輸注反應發生率很低，不需預防性用藥。建議病人在接受治療前應該確認HER2狀態、懷孕狀態、肝指數、膽紅素、血小板以及左心室射出分率。雖然Ado-trastuzumab emtansine目前只被核准用於之前使用過Trastuzumab與紫杉醇的轉移性乳癌病人，許多的臨床試驗正在進行中，將來很可能會被廣泛的單獨或合併其他藥品用於治療乳癌。

關鍵字

抗體藥品結合體 ； 人型化單株抗體 ； 轉移性乳癌

並列摘要

For the treatment of solid tumors, Ado-trastuzumab emtansine has been known as a revolutionary drug that is a conjugation of a monoclonal antibody and a traditional cytotoxic antineoplastic agent. The specificity of this drug is so high that the toxicity of emtansine could be tolerated that no medicine is needed for its high toxicities. This conjugated product is made up by three components: the monoclonal antibody-trastuzumab, the cytotoxic agent-emtansine, and the linkage-the thioether bond. Clinical studies have demonstrated that adotrastuzumab emtansine is effective in treating advanced and metastatic breast cancer already treated with trastuzumab. The common adverse effects are thrombocytopenia, elevation in liver function test, and decrease in left ventricular ejection fraction (LVEF). The rate of infusionrelated reaction is low, and thus premedication is not required. Before the start of treatment, the patient should be evaluated on the status of HER2, pregnancy, hepatic transaminases, serum bilirubin, platelet number, and LVEF. Its use could be expanded for other stages of breast cancer as monotherapy or in combination with other therapy in the future with proofs from extensive clinical studies.

並列關鍵字

Antibody-drug conjugates ； ado-trastuzumab emtansine ； humanized monoclonal antibody ； metastatic breast cancer