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引用次数: 0
摘要
厄洛替尼(ELB)是一种酪氨酸激酶抑制剂,能抑制健康细胞和癌细胞中表皮生长因子受体(EGFR)蛋白的活性。它可逆地与表皮生长因子受体酪氨酸激酶的 ATP 结合位点结合。ELB 于 2004 年获得美国食品和药物管理局(FDA)批准,用于治疗至少接受过一种其他疗法后复发的晚期非小细胞肺癌(NSCLC)患者。2005 年,它被授权与吉西他滨一起用于晚期胰腺癌的治疗。除肺癌外,ELB 在治疗其他癌症(包括乳腺癌、前列腺癌、结肠癌、胰腺癌、宫颈癌、卵巢癌和头颈部癌症)方面也取得了可喜的成果。然而,作为 BCS II 类药物,ELB 的水溶性有限,给生物制药带来了问题。为了克服这些问题,人们开发了纳米制剂,包括提高溶解度、控制释放、增强稳定性、肿瘤蓄积、降低毒性和克服耐药性。对于老年患者,ELB 管理应根据与年龄相关的药物代谢变化进行个体化给药,并密切监测不良反应。定期评估肝肾功能至关重要。本综述概述了 ELB 在治疗各种癌症中的作用、相关的生物制药问题以及 ELB 相关纳米技术干预的最新进展。它还涵盖了前几年授予的 ELB 专利和正在进行的临床试验。
Multifaceted role of erlotinib in various cancer: nanotechnology intervention, patent landscape, and advancements in clinical trials.
Erlotinib (ELB) is a tyrosine kinase inhibitor that targets the activity of Epidermal Growth Factor Receptor (EGFR) protein found in both healthy and cancerous cells. It binds reversibly to the ATP-binding site of the EGFR tyrosine kinase. ELB was approved by the US Food and Drug Administration (FDA) in 2004 for advanced non-small cell lung cancer (NSCLC) treatment in patients who relapsed after at least one other therapy. It was authorized for use with gemcitabine in 2005 for the treatment of advanced pancreatic cancer. In addition to lung cancer, ELB has shown promising results in the treatment of other cancers, including breast, prostate, colon, pancreatic, cervical, ovarian, and head and neck cancers. However, its limited water solubility, as a BCS class II drug, presents biopharmaceutical problems. Nanoformulations have been developed to overcome these issues, including increased solubility, controlled release, enhanced stability, tumor accumulation, reduced toxicity, and overcoming drug resistance. In older patients, ELB management should involve individualized dosing based on age-related changes in drug metabolism and close monitoring for adverse effects. Regular assessments of renal and hepatic functions are essential. This review provides an overview of ELB's role of ELB in treating various cancers, its associated biopharmaceutical issues, and the latest developments in ELB-related nanotechnology interventions. It also covers ELB patents granted in previous years and the ongoing clinical trials.
期刊介绍:
Medical Oncology (MO) communicates the results of clinical and experimental research in oncology and hematology, particularly experimental therapeutics within the fields of immunotherapy and chemotherapy. It also provides state-of-the-art reviews on clinical and experimental therapies. Topics covered include immunobiology, pathogenesis, and treatment of malignant tumors.