Type-I photosensitizers (PSs) are among the most potential candidates for photodynamic therapy (PDT), as their low dependence on oxygen endow them with many advantages for treating hypoxic tumor. However, most of the reported type-I PSs have a contingency of molecular design, because electron transfer (ET) reaction is more difficult to achieve than energy transfer (EET) process. Therefore, it is urgent to understand molecular design mechanisms for type-I PSs. In this review, the two ways to achieve the type-I PSs, i.e., inhibiting EET process (type-II) or enhancing ET process (type-I), are detailly explained. In response, the current design strategies of type-I PSs are summarized from two perspectives: indirect strategy (inhibiting EET process: reducing the energy of the lowest triplet excited state (T