通过靶向分子制剂（特别是肽）的开发，新兴的癌症治疗诊断领域取得了进步。这些药物利用特定受体的过度表达或突变，例如表皮生长因子受体 (EGFR) 和 αVβ3 整合素，它们在肿瘤生长、血管生成和转移中至关重要。尽管对基于抗体的疗法进行了广泛的研究并取得了有希望的结果，但肽因其较小的尺寸、易于修饰和快速的生物利用度而提供了一种引人注目的替代方案，这些因素可能增强肿瘤渗透并降低全身毒性。然而，肽在临床中的应用面临着挑战。与抗体相比，它们的结合亲和力较低且从血流中快速清除通常限制了其治疗功效和诊断准确性。本概述为全面回顾当前与 EGFR 和整合素 αVβ3 靶向肽相关的研究格局奠定了基础。我们的目标是深入研究它们的合成、放射性标记技术以及临床前和临床评估，强调它们在癌症治疗诊断学中的潜力和局限性。这篇综述不仅综合了现有文献，概述了针对 EGFR 和整合素 αVβ3 的肽类药物的进展，而且还确定了可以为未来研究方向提供信息的关键差距。通过解决这些差距，我们为提高癌症治疗的诊断精度和治疗效果做出了更广泛的讨论。

The burgeoning field of cancer theranostics has witnessed advancements through the development of targeted molecular agents, particularly peptides. These agents exploit the overexpression or mutations of specific receptors, such as the Epidermal Growth Factor receptor (EGFR) and αVβ3 integrin, which are pivotal in tumor growth, angiogenesis, and metastasis. Despite the extensive research into and promising outcomes associated with antibody-based therapies, peptides offer a compelling alternative due to their smaller size, ease of modification, and rapid bioavailability, factors which potentially enhance tumor penetration and reduce systemic toxicity. However, the application of peptides in clinical settings has challenges. Their lower binding affinity and rapid clearance from the bloodstream compared to antibodies often limit their therapeutic efficacy and diagnostic accuracy. This overview sets the stage for a comprehensive review of the current research landscape as it relates to EGFR- and integrin αVβ3-targeting peptides. We aim to delve into their synthesis, radiolabeling techniques, and preclinical and clinical evaluations, highlighting their potential and limitations in cancer theranostics. This review not only synthesizes the extant literature to outline the advancements in peptide-based agents targeting EGFR and integrin αVβ3 but also identifies critical gaps that could inform future research directions. By addressing these gaps, we contribute to the broader discourse on enhancing the diagnostic precision and therapeutic outcomes of cancer treatments.