Photoacoustic imaging is a hybrid modality that combines high-contrast and spectroscopy-based optical imaging specificity with the high spatial resolution of ultrasonography. This review highlights the development and progress of photoacoustic imaging technology over the past decade. This imaging technology has evolved to be more user-friendly, cost-effective, and portable, demonstrating its potential for diverse clinical applications. A potential clinical application lies in the use of photoacoustic imaging as a guiding tool for photothermal therapy. This review was conducted by initially filtering through three databases, namely, Google Scholar, PubMed, and Scopus, resulting in 460 articles published between 2019 and May 2023. Of these, 54 articles were deemed suitable for review after identification. The selected articles were research papers focusing on the development of therapeutic agents that enhance contrast in photoacoustic imaging. All reviewed articles tested these agents both and . This review focuses on wavelength absorption and radiation sources for photothermal therapy. The developed agents predominantly used NIR-I wavelengths, whereas the NIR-II region has been less explored, indicating significant potential for future research. This review provides comprehensive insights into the advancement of compounds serving as therapeutic agents and contrast agents in photoacoustic imaging-guided photothermal therapy.