Iclaprim

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)
Identifiers
CAS Number	192314-93-5
ATC code	J01EA03 (WHO)
PubChem	CID 213043
Chemical data
Formula	C19H22N4O3
Molar mass	354.403 g/mol[[]]

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). 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.

A new drug application for iclaprim was filed with the U.S. Food and Drug Administration in March 2008, 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.

Iclaprim has been granted fast track status by the FDA.

Further reading

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