Being of high potency and importance, rapamycin attracts continuous attention for further investigations and studies. Rapamycin exhibits various biological activities especially as a potent immunosuppressant. Also it exerts antitumor, antiviral, anti-inflammatory, antiproliferative, antiangiogenic, antifibrotic, anticancer, lifespan extension and antiaging, neuroprotective and neuroregenerative activities, in addition to its role in organs transplantation. Rapamycin is characterized also by causing no nephrotoxic effect. This review aim to understand the importance of rapamycin, its chemistry, production, biosynthesis, and biosynthetic gene cluster. In addition to highlighting its current status in drug market.