Photodynamic therapy (PDT) is undoubtedly a cutting-edge strategy for precise tumor therapy because of its unprecedented superiorities, such as negligible long-lasting adverse effects, high spatial and temporal selectivity, and inappreciable drug resistance. While the operation wavelengths of the commonly used photosensitizers (PSs) are located in visible or first near-infrared (NIR-I, 650–900 nm) region. The lights in these regions possess relatively low penetration depth, which makes PDT unsuitable for deep-tissue treatment. Near-infrared-II (NIR-II, 1000–1700 nm) light with high tissue penetration ability can be employed as excitation source for PDT, which provides a promising alternative for precision therapy of deep-seated tumors. However, designing NIR-II activated PSs is in its infancy, and still faces many challenges, such as severe nonradiative relaxation and difficulties in adjusting energy levels. This paper reviews the therapeutic mechanisms of PDT and recent strategies for designing NIR-II activated inorganic PSs. The inorganic NIR-II PSs are classified based on their functions (such as type II PSs, type I PSs, and PSs with specific properties), and their applications for effective and precision deep-tissue treatment are summarized comprehensively. Furthermore, the major issues of applying these PSs in clinical practices are also discussed.

光动力疗法 （PDT） 无疑是精准肿瘤治疗的前沿策略，因为它具有前所未有的优势，例如可忽略不计的长期不良反应、高空间和时间选择性以及难以察觉的耐药性。而常用光敏剂 （PS） 的工作波长位于可见光或第一近红外 （NIR-I， 650–900 nm） 区域。这些区域的光具有相对较低的穿透深度，这使得 PDT 不适合深层组织治疗。具有高组织穿透能力的近红外 II （NIR-II， 1000–1700 nm） 光可用作 PDT 的激发源，这为深部肿瘤的精准治疗提供了一种有前途的替代方案。然而，设计 NIR-II 活化的 PS 尚处于起步阶段，仍面临许多挑战，例如严重的非辐射弛豫和难以调整能量水平。本文综述了 PDT 的治疗机制和设计 NIR-II 活化无机 PSs 的最新策略。根据其功能（如 II 型 PSs、I 型 PSs 和具有特定性能的 PS）对无机 NIR-II PS 进行分类，并全面总结了它们在有效和精确的深层组织治疗中的应用。此外，还讨论了在临床实践中应用这些 PS 的主要问题。