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Iclaprim
Systematic (IUPAC) name
(RS)-5-[(2- cyclopropyl- 7,8-dimethoxy- 2H- chromen- 5-yl) methyl] pyrimidine- 2,4- diamine
Identifiers
CAS number 192314-93-5
ATC code J01EA03
PubChem 213043
Chemical data
Formula C 19H22N4O3  
Mol. mass 354.403 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability Good (oral)[1]
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status Investigational
Routes Intravenous (oral under investigation)

Iclaprim (INN), codenamed AR-100 and RO-48-2622, is a diaminopyrimidine dihydrofolate reductase inhibitor being developed for the treatment of complicated skin and soft tissue infections caused by antibiotic-resistant bacteria. It is structurally related to trimethoprim. In Phase III clinical trials, intravenously-administered iclaprim was found to be as effective as and better tolerated than linezolid in people with skin and soft tissue infections, many caused by methicillin-resistant Staphylococcus aureus (MRSA).[2][3] In vitro, iclaprim is highly active against MRSA, vancomycin-resistant Staphylococcus aureus (VRSA), strains of Streptococcus pneumoniae resistant to several common antibiotics, and some Gram-negative bacteria.[1]

A new drug application for iclaprim was filed with the U.S. Food and Drug Administration in March 2008,[2] and a marketing authorisation application (MAA) was accepted by the European Medicines Agency on August 21, 2008. Phase II clinical trials are being conducted to assess whether iclaprim can be taken by mouth as well as intravenously and whether it is effective for the treatment of hospital-acquired pneumonia.[3][4]

Iclaprim has been granted fast track status by the FDA.[5]

References

  1. ^ a b Kohlhoff SA, Sharma R (September 2007). "Iclaprim". Expert Opin Investig Drugs 16 (9): 1441–8. doi:10.1517/13543784.16.9.1441. PMID 17714029.  
  2. ^ a b Reuters (March 19, 2008). "Arpida Submits New Drug Application for Intravenous Iclaprim for Treatment of Skin Infections". Press release. http://www.reuters.com/article/pressRelease/idUS92327+19-Mar-2008+PRN20080319. Retrieved 2008-08-24.  
  3. ^ a b PR Newswire (August 21, 2008). "Arpida's iclaprim MAA Accepted for Review by EMEA". Press release. http://www.breitbart.com/article.php?id=prnw.20080821.UKTH008&show_article=1. Retrieved 2008-08-24.  
  4. ^ Peppard WJ, Schuenke CD (February 2008). "Iclaprim, a diaminopyrimidine dihydrofolate reductase inhibitor for the potential treatment of antibiotic-resistant staphylococcal infections". Curr Opin Investig Drugs 9 (2): 210–25. PMID 18246524.  
  5. ^ Morgan A, Cofer C, Stevens DL (March 2009). "Iclaprim: a novel dihydrofolate reductase inhibitor for skin and soft tissue infections". Future Microbiol 4 (2): 131–44. doi:10.2217/17460913.4.2.131. PMID 19257839.  

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