JOURNAL OF BACTERIOLOGY AND VIROLOGY ISSN:1598-2467(Print) 2093-0429(Online)

The ongoing problem of antibiotic resistance is widely recognized as a contributing factor to the decline in community health. Several novel dihydrofolate reductase (DHFR) inhibitors have recently advanced into clinical development because of their potent anticancer and antibacterial activities. To combat bacterial infections, DHFR inhibitors such as trimethoprim are often used in combination with sulfonamide. Iclaprim is an inhibitor of bacterial DHFR, interferes with thymidine synthesis and is primarily metabolized by the enzymes CYP3A4 and CYP2C19. This review aimed to investigate the pharmacological progression of its efficacy, tolerability, microbiology, and in vitro susceptibility in the treatment of serious skin infections and nosocomial pneumonia. Related articles were searched from 1995 to 2023 using specific keywords in PubMed and Google Scholar, with articles excluded based on some criteria such as including antibiotics, iclaprim etc and excluding duplicate articles, editorials, commentaries, letters to the editor etc. The discussion presents the pharmacological studies based on experimental findings and provides an overview of three phases of clinical trial. However, several crucial parameters still require further research and development. In addition, selected in vitro results are presented. Clinical trials investigating hospital-associated iclaprim for pneumonia are currently underway. Currently, iclaprim, an antimicrobial agent against Gram-positive organisms, has shown potential in the treatment of skin infections. However, further studies are needed to clarify its potential role in clinical practice.