Iclaprim

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Iclaprim
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Systematic (IUPAC) name
(RS)-5-[(2- cyclopropyl- 7,8-dimethoxy- 2H- chromen- 5-yl) methyl] pyrimidine- 2,4- diamine
Clinical data
Routes of
administration
Intravenous (oral under investigation)
Legal status
Legal status
  • Investigational
Pharmacokinetic data
Bioavailability Good (oral)[1]
Identifiers
CAS Number 192314-93-5
ATC code J01EA03 (WHO)
PubChem CID 213043
Chemical data
Formula C19H22N4O3
Molar mass 354.403 g/mol[[Script error: No such module "String".]]
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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

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Further reading

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de:Iclaprim
  1. 1.0 1.1 Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  2. 2.0 2.1 "Arpida Submits New Drug Application for Intravenous Iclaprim for Treatment of Skin Infections" (Press release). Reuters. March 19, 2008. http://www.reuters.com/article/pressRelease/idUS92327+19-Mar-2008+PRN20080319. Retrieved 2008-08-24. 
  3. 3.0 3.1 "Arpida's iclaprim MAA Accepted for Review by EMEA" (Press release). PR Newswire. August 21, 2008. http://www.breitbart.com/article.php?id=prnw.20080821.UKTH008&show_article=1. Retrieved 2008-08-24. 
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