Synonyms: AR-100 | AR100 | Mersarex® | RO-48-2622 | RO-482622
Compound class:
Synthetic organic
Comment: Iclaprim is a dihydrofolate reductase (DHFR) inhibitor that reduces folic acid synthesis. It is a diaminopyrimidine antibacterial that has broad-spectrum activity against Gram +ve pathogens [1]. Iclaprim is a racemic mixture of stereoisomers. We show the 'flat' structure to represent the mixture.
![]() Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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References |
1. Bryant AE, Gomi S, Katahira E, Huang DB, Stevens DL. (2019)
The effects of iclaprim on exotoxin production in methicillin-resistant and vancomycin-intermediate Staphylococcus aureus. J Med Microbiol, 68 (3): 456-466. [PMID:30676310] |
2. Drugs.com.
iclaprim. Accessed on 06/05/2020. Modified on 06/05/2020. www.drugs.com, https://www.drugs.com/nda/iclaprim_190214.html |
3. EMA.
Mersarex: Withdrawal of the marketing authorisation application. Accessed on 06/05/2020. Modified on 06/05/2020. Euorpean Medicines Agency, https://www.ema.europa.eu/en/medicines/human/withdrawn-applications/mersarex |
4. Huang DB, Strader CD, MacDonald JS, VanArendonk M, Peck R, Holland T. (2018)
An Updated Review of Iclaprim: A Potent and Rapidly Bactericidal Antibiotic for the Treatment of Skin and Skin Structure Infections and Nosocomial Pneumonia Caused by Gram-Positive Including Multidrug-Resistant Bacteria. Open Forum Infect Dis, 5 (2): ofy003. [PMID:29423421] |
5. Sader HS, Fritsche TR, Jones RN. (2009)
Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates. Antimicrob Agents Chemother, 53 (5): 2171-5. [PMID:19289528] |