Introduction: Plants have long been used to cure diverse ailments and disorders as a source of conventional medicines. Many of these medicinal plants are also fantastic phytochemical sources, many of which have strong therapeutic practices. Broussonetia papyrifera, also known as paper mulberry, is a well-known traditional natural resource that has been in application for decades and the renowned advances must be presented to researchers for further betterment, product innovation, exploring novel applications, and uncover miscellaneous ideas. Aim: Reviewing some pharmacologically active phytoconstituents present in B. papyrifera Linn. Methodology: The systematic literature compilation about the basic aspects, distribution, plant profile, pharmacological advances, key plant parts, ethnopharmacology, and other crucial information about B. papyrifera was performed through freely available scientific databases / natural products databases such as ScienceDirect, Google Scholar, PubMed, etc. Results: This current fascinating article expansively emphasized the general aspects, plant profile (Kingdom, Sub-Kingdom, Infra-Kingdom, Division, Sub-Division, Super-Division Class, Order, Super-Order, Family, Genus, and Species), traditional uses, distribution, major phytoconstituents, significant pharmacotherapeutic attributes (anti-viral, anti-cancer, anti-oxidant, cytotoxic potentials, anti-inflammatory, anti-diabetic, anti-microbial, anti-nociceptive, anti-gout, and anti-proliferative) mediated by diverse parts (seed, root, leaf, stem, and fruit). Conclusion: This information will be reasonably functional for the passionate contemporary investigators of several areas (natural products, pharmacognosy, medicine, chemistry, botany, pharmacy, etc.) in developing miscellaneous essential formulations for treating numerous disorders such as inflammation, cancer, high blood sugar, pain, infection, along with exhibiting cellular protective effects. This study will pave a new way for modern nature-pharmacotherapeutics for human applications