Photocatalysis has been one of the recent technologies in drug discovery. This is one of the growing branch of organic synthesis with organic compounds is visible-light photocatalysis that counts on the ability of photocatalysts to absorb the visible light and are involved in single electron transfer (SET) or energy transfer (ET) reactions. The emergence of this catalytic field gave an open platform for radical based organic conversions that unleash exclusive reaction routes. The selection of most suitable light source for the intensity of light provides an exclusive pathway for the construction of a variety of drugs and their derivatization. Photocatalysis gives a regulation of radical generation which has attracted chemists all over the world. This mild and effective approach of photocatalysis helps to understand the photochemical and photophysical properties of pharmaceutical products. The potential of the different drugs examined under photocatalysis can be easily exploited through the wide functionality lenience, site explicit reactivity or selectivity, and simply operatable. This chapter will focus on the current developments of visible-light photocatalysis through late-stage functionalization, Csp3-Csp2 cross-coupling reactions comprising C–C, C-N, or C-O bonds, and bioconjugations.