CAJ | 학술논문

依鲁替尼(ibrutinib,商品名Imbruvica)是由Pharmacyclics公司和强生旗下子公司杨森制药共同研制的第一个口服布鲁顿酪氨酸激酶抑制剂.至2015年1月,FDA已批准其用于4种B细胞恶性肿瘤的治疗,在其他B细胞淋巴瘤适应证的扩展研究仍值得期待.依鲁替尼通过对布鲁顿酪氨酸激酶的不可逆抑制机制发挥疗效,其被认为是迄今为止治疗套细胞淋巴瘤最重要的突破,并有望把慢性淋巴细胞白血病从死刑判决变成可控制的慢性疾病.笔者就依鲁替尼的研发历程、基本性质、作用机制、药动学、药效学、临床试验及应用等研发动态作一概述,以期能为医院临床用药起到指导作用.
의로체니(ibrutinib,상품명Imbruvica)시유Pharmacyclics공사화강생기하자공사양삼제약공동연제적제일개구복포로돈락안산격매억제제.지2015년1월,FDA이비준기용우4충B세포악성종류적치료,재기타B세포림파류괄응증적확전연구잉치득기대.의로체니통과대포로돈락안산격매적불가역억제궤제발휘료효,기피인위시흘금위지치료투세포림파류최중요적돌파,병유망파만성림파세포백혈병종사형판결변성가공제적만성질병.필자취의로체니적연발역정、기본성질、작용궤제、약동학、약효학、림상시험급응용등연발동태작일개술,이기능위의원림상용약기도지도작용.
Ibrutinib(trade name Imbruvica) is the first oral irreversible inhibitors of Bruton tyrosine kinase (BTK) developed by Pharmacyclics and Johnson. Until January 2015, It has been approved for the treatment of four kinds of B-cell lymphomas by FDA. Ibrutinib plays a signiifcant effect by inhibiting BTK activity irreversibly, and is thought to be a breakthrough for the treatment of MCL and even expected to turn the CLL from a potential death into a manageable chronic disease. The development process, properties, mechanism, pharmacokinetics, pharmacodynamics, clinical trials and applications of Ibrutinib was reviewed in this article.