Among many different neurodegenerative diseases, Alzheimer’s Disease (AD) marks the most affected neurodegenerative disease in the world’s population, contributing to the utmost suffering of the people and society. Even with the advancements in modern scientific research, the most relatable cause of AD is the amyloid beta (Aβ) plaque formation, and the increasing reactive oxygen species are the ones concentrated, and the therapies are mostly to be implied for their interactive breakdowns. The acetylcholine esterase (AChE), which in involved in the neurotransmitter activity, helps in the cognitive development that is used in many different therapeutic approaches; where some of their combinations aid the best therapeutic approaches for AD, one such is the implication of phototherapeutic compounds. The compounds, like azotacrine, are molecules able to switch shape with exposure to blue and UV light, thereby changing the AChE activity, contributing to the reduction of side effects like hepatotoxicity and ensuring the precise controlling of the enzyme activity. The use of photosensitizers, which comprise the light-activated compounds (such as thioflavin-T derivatives, quinolinium derivatives, curcumin derivatives, boron-dipyrromethene, N- or O-heterocyclic compounds, porphyrins, fullerenes and their derivatives, fused azobenzene–boron complexes, and other transition metal compounds), which have the ability to generate singlet oxygen on exposure to light, are now implied in the targeting of Aβ plaques, a promising strategy for AD treatment. Many nanotechnological approaches also contribute to the better phototherapeutic compound discovery, like the polyoxometalates and mesoporous silica nanoparticles coated with a copolymer like poly(N-isopropylacrylamide-co-acrylamide), which are thermally stable, chemically highly porous with biocompatibility and bioavailability, and act as a photothermal agent, making the compound stand out for AD treatment with a phototherapic approach. Some other nanoparticle phototherapy compounds include carbon dots, polymeric nanoparticles, lanthanide-doped upconversion nanoparticles; 2D nanomaterials like graphene oxide, black phosphorus, and carbon nitride aid in AD treatment. Another great improved technique of the phototherapic approach is the photobiomodulation, which uses the low-intensity red light or near-infrared light; it is found to support neuronal health by increasing the ATP production and reducing the toxin production and inflammation rates and is thus used in the treatment of AD, PD, and also some kinds of traumatic injuries. It also suppresses the PERK/eIF2α pathway by triggering the release of exosomes from microglia carrying miR-7670-3p. Overall, this chapter focuses on these innovative phototherapeutic strategies that offer a promising and multifaceted approach for the effective, targeted, and noninvasive treatment of AD, paving the way for next-generation neuroprotective therapies.