Iclaprim

  • (RS ) -5 - [(2- cyclopropyl -7 ,8- dimethoxy -2H- chromen- 5-yl) methyl] pyrimidine-2 ,4 -diamine IUPAC
  • Iclaprimum Latin
  • AR-100
  • Ro 48-2622
  • C19H22N4O3 ( Iclaprim )
  • C20H26N4O6S ( Iclaprim · mesilate )

J01EA03

Antibiotics

Inhibiting bacterial dihydrofolate

  • 354.40 g · mol -1 ( Iclaprim )
  • 450.51 g · mol -1 ( Iclaprim · mesilate )

Template: Infobox chemical / molecular formula search available

Iclaprim ( proposed trade name Iclaprim Arpida ®; manufacturer Arpida ) is an antibiotic belonging to the group of Diaminopyrimidine. Iclaprim is located in the approval process and should be approved for the treatment of complicated skin and skin structure infections ( cSSSI ).

  • 2.1 Mechanism of action ( pharmacodynamics )
  • 2.2 Absorption and distribution in the body ( pharmacokinetics )

Clinical information

Areas of application and action spectrum

Iclaprim is an antibiotic belonging to the group of Diaminopyrimidine. It acts as a potent inhibitor of bacterial dihydrofolate reductase, such as trimethoprim, another representative of this class of substances. In many trimethoprim- resistant strains Iclaprim other hand, is still effective. In in vitro studies Iclaprim shows high activity against the most clinically relevant gram-positive bacteria. The spectrum of activity includes resistant strains that were isolated from patients with severe MRSA and VRSA infections. Compared with anaerobes Iclaprim shows little effect.

  • Enterococci including vancomycin - resistant strains ( VRE),
  • Streptococci including penicillin - resistant strains.

Pharmacological properties

Mechanism of action ( pharmacodynamics )

Iclaprim acts by inhibiting bacterial dihydrofolate reductase without inhibiting the human enzyme essential. As a result, there is an inhibition of the synthesis of DNA, and blocks cell death.

Uptake and distribution in the body ( pharmacokinetics )

In clinical trials Iclaprim is administered either intravenously or orally. When given orally, the bioavailability is about 40%. Recommended doses of 160 mg and oral administration, peak plasma levels of 0.5 ug / ml are reached 90 minutes after ingestion. Intravenous administration of 0.4 and 0.8 mg / kg body weight, plasma concentrations of 0.37 and 0.87 g / ml can be achieved. The plasma half-life of about two hours.

Other Information

Iclaprim was on the fast-track approval process of the U.S. Food and Drug Administration Food and Drug Administration (FDA) approval has not been granted by decision of January 2009 for the time being.

Stereochemistry CAS registry number Mesylate PubChem Anatomical Therapeutic Chemical Classification System Regulation of therapeutic goods Digital Object Identifier Robert Koch Institute
407033
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