The use of cow urine (CU) in treating a variety of illness can be traced back to ancient ages. It has been referred as an important and integral component of Cowpathy – an age-old practice in Indian sub-continent since the Vedic period (1500 BC – 600 BC). The CU contains several important compounds that are essential in maintaining a balance between the well-being of human and the nature. It is composed of about 95 % water and other useful ingredients such as urea, hormones, lyase enzyme, and salts containing Fe, Ca, P, Mn, S, N, and K. In addition, it also contains lactose, cytokine, and amino acid which are the fundamental building blocks of protein. Researchers have developed various processes for the green synthesis of CU concentrate and evaluated its usefulness in treating various diseases owing to its antibacterial and antifungal properties. Further, CU has also shown promising immunity boosting and anti-oxidant characteristics. Even though human civilization has benefited from the use of CU in treating various types illness but the modern scientific understanding of the cause-effect relationships was partly developed in the last few decades. There exists a huge knowledge gap and a comprehensive study on exploring the science and application of CU hasn’t been reported. This paper reviews the historical perspective, compositional analysis, processing, applications, knowledge gap, and future research required in the field of therapeutic usage of CU.