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罗华比妥珠单抗特西利单抗:一种新型的 DLL3 靶向抗体药物偶联物。

Rovalpituzumab Tesirine: A Novel DLL3-Targeting Antibody-Drug Conjugate.

机构信息

Department of Internal Medicine, Abington, Jefferson Health, Abington, PA, USA.

Department of Hematology and Medical Oncology, Gundersen Health System, La Crosse, WI, USA.

出版信息

Drugs R D. 2018 Dec;18(4):255-258. doi: 10.1007/s40268-018-0247-7.

Abstract

Small cell lung cancer (SCLC) comprises about 15% of all cases of lung cancer. In recent years, owing to a change in the epidemiology of smoking habits, the incidence of the tumor has decreased; however, it remains a significant challenge to global health. While the tumor has a favorable initial response to chemoradiation, relapse is invariable, and second-line regimens may be intolerable given the severity of side effects. For patients with tumors resistant to second-line regimens, no current standard regimens exist. Rovalpituzumab tesirine is a novel antibody-drug conjugate, targeting delta-like protein 3, fundamental in the downstream cellular signaling for proliferation and apoptosis. This drug is reported to have shown promise in pre-clinical and phase I trials. It appears effective in decreasing tumor burden and is reported to be well tolerated, albeit with a significant adverse effect profile. Currently, it is being studied as part of initial and subsequent line chemotherapeutic regimens; it remains to be seen if this is a viable option in the treatment of SCLC. This may add to the agents that can be used against SCLC, and help improve outcomes.

摘要

小细胞肺癌(SCLC)约占所有肺癌病例的 15%。近年来,由于吸烟习惯的流行病学变化,肿瘤的发病率有所下降;然而,它仍然是全球健康的一个重大挑战。虽然肿瘤对放化疗有良好的初始反应,但复发是不可避免的,而且二线治疗方案可能因副作用的严重程度而无法耐受。对于对二线治疗方案耐药的患者,目前尚无标准的治疗方案。Rovalpituzumab tesirine 是一种新型抗体药物偶联物,靶向 delta 样蛋白 3,在增殖和凋亡的下游细胞信号传导中起重要作用。该药在临床前和 I 期试验中表现出良好的疗效。它似乎能有效减轻肿瘤负担,且耐受性良好,尽管不良反应谱显著。目前,它正作为初始和后续化疗方案的一部分进行研究;它是否是 SCLC 治疗的可行选择还有待观察。这可能会增加针对 SCLC 的治疗药物,并有助于改善预后。

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