厄洛替尼(ELB)是一种酪氨酸激酶抑制剂,靶向健康细胞和癌细胞中发现的表皮生长因子受体(EGFR)蛋白的活性。它可逆地结合EGFR酪氨酸激酶的ATP结合位点。ELB于2004年被美国食品和药物管理局(FDA)批准用于至少一种其他疗法后复发的患者的晚期非小细胞肺癌(NSCLC)治疗。它于2005年被授权与吉西他滨一起用于治疗晚期胰腺癌。除了肺癌,ELB在其他癌症的治疗中显示出有希望的结果,包括乳房,前列腺,结肠,胰腺,子宫颈,卵巢,头颈癌.然而,其有限的水溶性,作为BCSII类药物,提出了生物制药问题。已经开发了纳米配方来克服这些问题,包括增加溶解度,控释,增强稳定性,肿瘤积聚,降低毒性,克服耐药性。在老年患者中,ELB管理应涉及根据年龄相关的药物代谢变化和密切监测不良反应的个体化给药。定期评估肾功能和肝功能至关重要。本文综述了ELB在治疗各种癌症中的作用。其相关的生物制药问题,以及与ELB相关的纳米技术干预措施的最新进展。它还涵盖了前几年授予的ELB专利和正在进行的临床试验。
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.