Background: Khār-i-Khasak/Gokhrū is a valuable medicinal plant in the Unani System of Medicine (USM). Gokhrū is classified into two types: Khār-i-Khasak Khurd (small caltrop) and Khār-i-Khasak Kalān(large caltrop).The small Caltrop (Tribulus terrestris) and the large Caltrop (Pedalium murex) belong to the Zygophyllaceae and Pedaliaceae families. These plants are well-known for their therapeutic benefits. It has medicinal applications in many ancient medical systems, including Unani, Ayurveda, Siddha, and others. Purpose of review: This review was to explain in detail the benefits of giving a scientific basis and classical references for the clinical usage of Gokhrū. Materials and Methods: This review was conducted by thoroughly searching the classical literature, Unani, ethnobotanical, and published research databases of ScienceDirect, PubMed, Web of Science, Google, Google Scholar, ResearchGate, and Elsevier. Results: Pharmaceutical businesses utilise this medication to prepare formulations and dietary supplements. It is growing in India, South Africa, the Middle East, Pakistan, Sri Lanka, and Mexico. In India, it is primarily found in Bihar, Andhra Pradesh, Tamil Nadu, the northwestern states, West Bengal, Madras, Gujarat, Awadh, and Rajputana. This plant has abundant therapeutic properties, including anti-ulcerative, anticancer, aphrodisiac, analgesic, stomachic, diuretic, cardiotonic, antibacterial, anti-inflammatory, nephroprotective, antispasmodic, and anti-carcinogenic. This plant is mostly used to treat urogenital problems, kidney disorders such as renal and vesical calculi, gallbladder stones, and sexual disorders such as infertility and erectile dysfunction in both men and women. Conclusion: It is concluded that abundant bioactive compounds identified and separated from Khār-i-Khasak Khurdand Khār-i-Khasak Kalānhave potential medicinal values on the male and female reproductive systems, as well as the urinary system (renal and vesical calculi), due to the presence of steroidal saponin compounds, flavonoids, alkaloids, and ursolic acid as the plant’s predominant active component.
