Optical imaging is an excellent non-invasive method for viewing visceral organs and, above all, safer as compared to ionizing radiation-based methods like x-rays. By making use of the properties of photons, this technique generates high-resolution images of cells, molecules, organs, and tissues using visible, ultraviolet, and infrared light. This makes the technique useful for repeated applications in monitoring the progression of the disease and responses to treatment without having exposure of a significant amount of radiation to the patient. Recent advancements have been made in optical contrast agents, particularly in fluorescent probes that have significantly enhanced the capabilities in optical imaging. These probes can selectively target specified biomarkers, thereby allowing for molecular imaging with the possibility of early detection of abnormalities. In this article, the latest developments in the area of optical contrast agents are overviewed for their applications in medical imaging and in revolutionizing diagnostics and therapeutics. This work therefore explores the frontiers of fluorescent probes and molecular imaging to accelerate the translation of optical imaging into clinical practice for improved patient outcomes and transformation of the landscape of medical imaging.