小分子治疗诊断试剂在肿瘤靶向、成像和治疗方面展示了三元特性，越来越受到关注，作为经典小分子抗肿瘤药物的潜在补充或改进。光敏剂具有成像和光治疗的双重功能，在过去的十年中广泛用于构建基于光敏剂的小分子治疗诊断试剂。在本综述中，我们总结了过去十年中在光敏剂基础上研究的小分子治疗诊断试剂的代表性试剂，并突出它们在肿瘤靶向监测和光治疗方面的特点和应用。还讨论了光敏剂在构建小分子治疗诊断试剂用于肿瘤诊断和治疗方面所面临的挑战和未来前景。版权所有 © 2023 The Author(s). 由Elsevier Inc.出版，保留所有权利。

Small molecule theranostic agents for tumor treatment exhibited triadic properties in tumor targeting, imaging, and therapy, which have attracted increasing attention as a potential complement for, or improved to, classical small molecule antitumor drugs. Photosensitizer have dual functions of imaging and phototherapy, and have been widely used in the construction of small molecule theranostic agents over the last decade. In this review, we summarized representative agents that have been studied in the field of small molecule theranostic agents based on photosensitizer in the last decade, and highlighted their characteristics and application in tumor-targeted monitoring and phototherapy. The challenges and future perspectives of photosensitizers in building small molecule theranostic agents for diagnosis and therapy of tumors were also discussed.Copyright © 2023 The Author(s). Published by Elsevier Inc. All rights reserved.