Jiacheng Zhu, Guoshun Luo, Hua Xiang
Steroids represent a major class of biomolecules with widespread distribution in nature and critical roles in numerous biological processes. Natural steroids and their synthetic derivatives have been extensively utilized as core scaffolds for drugs effective in contraception, oncology, anti-inflammation, antibacterial, and antiviral therapy. Between 2000 and 2025, 23 steroidal drugs gained initial approval for therapeutic, diagnostic, or reproductive health applications. This perspective summarizes, for the first time, these approved steroidal drugs, categorizing them by mechanistic features into four therapeutic areas: gender-related needs or diseases, inflammatory-related diseases, neurological disorders, and cardiovascular/metabolic diseases. Furthermore, the physiological roles of these steroidal drugs upon receptor binding, their structure-activity relationships, and clinical significance are emphasized. This perspective aims to provide strategic insights that facilitate the future development of clinically valuable steroidal therapeutics.