Vennepureddy Adarsh, Atallah Jean-Paul, Terjanian Terenig
Department of Medicine, Staten Island University Hospital, Staten Island, NY 10305, USA.
Division of Hematology and Oncology, Staten Island University Hospital, Staten Island, NY 10305, USA.
World J Oncol. 2015 Oct;6(5):429-436. doi: 10.14740/wjon950e. Epub 2015 Oct 26.
Topotecan (TPT), a chemotherapeutic agent, is a topoisomerase-I inhibitor. Topoisomerase-I is a nuclear enzyme that relieves torsion strain in DNA by opening single strand breaks which helps in DNA replication. TPT inhibits this enzyme, thus preventing DNA replication and causes cell death. TPT has demonstrated to have broad spectrum of antitumor activity in tumors like cervical, ovarian, endometrial and small cell lung cancers (SCLCs). The intravenous (IV) formulation of the drug is currently approved by the US Food and Drug Administration for the treatment of patients with SCLC and ovarian cancer at a dose of 1.5 mg/m administered daily for five consecutive days, with treatment cycles repeated every 3 weeks. TPT has shown some promising activity in the treatment of non-small cell lung cancer (NSCLC) with favorable side effect profile. Several clinical trials have been conducted with TPT in either IV or oral formulation for the treatment of NSCLC as a first or second-line treatment. Here we reviewed all the clinical trials done with TPT to date in the treatment of NSCLC both as a single-agent and combination therapy.
拓扑替康（TPT）是一种化疗药物，属于拓扑异构酶-I抑制剂。拓扑异构酶-I是一种核酶，它通过打开单链断裂来缓解DNA中的扭转张力，这有助于DNA复制。TPT抑制这种酶，从而阻止DNA复制并导致细胞死亡。TPT已被证明在宫颈癌、卵巢癌、子宫内膜癌和小细胞肺癌（SCLC）等肿瘤中具有广泛的抗肿瘤活性。该药物的静脉注射（IV）制剂目前已被美国食品药品监督管理局批准，用于治疗SCLC和卵巢癌患者，剂量为1.5mg/m²，连续每日给药5天，每3周重复治疗周期。TPT在治疗非小细胞肺癌（NSCLC）方面显示出一些有前景的活性，且副作用较小。已经进行了多项关于TPT静脉注射或口服制剂治疗NSCLC作为一线或二线治疗的临床试验。在此，我们回顾了迄今为止使用TPT治疗NSCLC作为单药治疗和联合治疗的所有临床试验。
