Near-infrared (NIR)-light-triggered therapy platforms are now considered as a new and exciting possibility for clinical nanomedicine applications. As a promising photothermal agent, polypyrrole (PPy) nanoparticles have been extensively studied for the hyperthermia in cancer therapy due to their strong NIR light photothermal effect and excellent biocompatibility. However, the photothermal application of PPy based nanomaterials is still in its preliminary stage. Developing PPy based multifunctional nanomaterials for cancer treatment in vivo should be the future trend and object for cancer therapy. In this review, the synthesis of PPy nanoparticles and their NIR photothermal conversion performance were first discussed, followed by a summary of the recent progress in the design and implementation on the mulitifunctionalization of PPy or PPy based therapeutic platforms, as well as the introduction of their exciting biomedical applications based on the synergy between the photothermal conversion effect and other stimulative responsibilities.