Khan Saif, Jandrajupalli Suresh Babu, Bushara Nashwa Zaki Ali, Raja Rama Devi Patel, Mirza Shadab, Sharma Kuldeep, Verma Rajan, Kumar Ashish, Lohani Mohtashim
Department of Basic Dental and Medical Sciences, College of Dentistry, University of Ha'il, Ha'il 55473, Saudi Arabia.
Department of Preventive Dental Sciences, College of Dentistry, University of Ha'il, Ha'il 55473, Saudi Arabia.
Cells. 2024 Dec 22;13(24):2126. doi: 10.3390/cells13242126.
Advanced triple-negative breast cancer (TNBC) has poorer outcomes due to its aggressive behavior and restricted therapeutic options. While therapies like checkpoint inhibitors and PARP inhibitors offer some benefits, chemotherapy remains ineffective beyond the first line of treatment. Antibody-drug conjugates (ADCs) like sacituzumab govitecan-hziy (SG) represent a significant advancement. SG combines SN-38, an irinotecan derivative, with a Trop-2-targeting antibody via a pH-sensitive linking moiety, achieving a good drug:antibody ratio. In a phase I-II study involving metastatic TNBC (mTNBC) individuals, SG achieved an overall response rate of 33.3% and a median response period of 7.7 months. The phase III ASCENT trial demonstrated SG's efficacy in relapsed or refractory TNBC, improving median progression-free survival and median overall survival compared to chemotherapy. Common side effects include neutropenia, nausea, and fatigue. This article highlights the clinical potential, pharmacokinetics, safety profile, and resistance mechanisms of SG along with key ongoing clinical trials, emphasizing its role in managing refractory mTNBC, especially in third-line therapy. The review also discusses current strategies for managing adverse reactions and sequencing ADC treatments in clinical practice, along with the predicted basis of resistance. The optimal sequencing of SG relative to other ADCs, such as trastuzumab deruxtecan or T-DXd, remains an evolving question, especially as newer agents with distinct mechanisms of action and safety profiles enter the field. Further research is essential to establish evidence-based strategies for sequencing SG and addressing disease progression post-ADC therapy.
晚期三阴性乳腺癌(TNBC)因其侵袭性生物学行为和有限的治疗选择而预后较差。虽然检查点抑制剂和聚腺苷二磷酸核糖聚合酶(PARP)抑制剂等疗法有一定益处,但化疗在一线治疗后仍然无效。抗体药物偶联物(ADC),如戈沙妥珠单抗(SG),代表了一项重大进展。SG通过一个对pH敏感的连接部分将伊立替康衍生物SN-38与靶向人滋养层细胞表面抗原2(Trop-2)的抗体结合,实现了良好的药物与抗体比例。在一项针对转移性TNBC(mTNBC)患者的I-II期研究中,SG的总缓解率为33.3%,中位缓解期为7.7个月。III期ASCENT试验证明了SG在复发或难治性TNBC中的疗效,与化疗相比,改善了中位无进展生存期和中位总生存期。常见的副作用包括中性粒细胞减少、恶心和疲劳。本文重点介绍了SG的临床潜力、药代动力学、安全性概况和耐药机制,以及正在进行的关键临床试验,强调了其在治疗难治性mTNBC中的作用,尤其是在三线治疗中。该综述还讨论了临床实践中处理不良反应和安排ADC治疗顺序的当前策略,以及耐药的预测基础。SG相对于其他ADC,如德曲妥珠单抗(T-DXd)的最佳用药顺序仍是一个不断发展的问题,特别是随着具有不同作用机制和安全性概况的新型药物进入该领域。进一步的研究对于建立基于证据的SG用药顺序策略和解决ADC治疗后疾病进展问题至关重要。