Iclaprim
Encyclopedia
Iclaprim 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 trial
s, 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.
Diaminopyrimidine
Diaminopyrimidines are a class of organic chemical compounds that include two amine groups on a pyrimidine ring.They include many dihydrofolate reductase inhibitor drugs .Some have been patented as anti-cancer drugs....
dihydrofolate reductase
Dihydrofolate reductase
- Function :Dihydrofolate reductase converts dihydrofolate into tetrahydrofolate, a methyl group shuttle required for the de novo synthesis of purines, thymidylic acid, and certain amino acids...
inhibitor
Enzyme inhibitor
An enzyme inhibitor is a molecule that binds to enzymes and decreases their activity. Since blocking an enzyme's activity can kill a pathogen or correct a metabolic imbalance, many drugs are enzyme inhibitors. They are also used as herbicides and pesticides...
being developed for the treatment of complicated skin and soft tissue infections caused by antibiotic-resistant
Antibiotic resistance
Antibiotic resistance is a type of drug resistance where a microorganism is able to survive exposure to an antibiotic. While a spontaneous or induced genetic mutation in bacteria may confer resistance to antimicrobial drugs, genes that confer resistance can be transferred between bacteria in a...
bacteria. It is structurally related to trimethoprim
Trimethoprim
Trimethoprim is a bacteriostatic antibiotic mainly used in the prophylaxis and treatment of urinary tract infections.It belongs to the class of chemotherapeutic agents known as dihydrofolate reductase inhibitors...
. In Phase III clinical trial
Clinical trial
Clinical trials are a set of procedures in medical research and drug development that are conducted to allow safety and efficacy data to be collected for health interventions...
s, intravenously
Intravenous therapy
Intravenous therapy or IV therapy is the infusion of liquid substances directly into a vein. The word intravenous simply means "within a vein". Therapies administered intravenously are often called specialty pharmaceuticals...
-administered iclaprim was found to be as effective as and better tolerated than linezolid
Linezolid
Linezolid is a synthetic antibiotic used for the treatment of serious infections caused by Gram-positive bacteria that are resistant to several other antibiotics...
in people with skin and soft tissue infections, many caused by methicillin-resistant Staphylococcus aureus
Methicillin-resistant Staphylococcus aureus
Methicillin-resistant Staphylococcus aureus is a bacterium responsible for several difficult-to-treat infections in humans. It is also called multidrug-resistant Staphylococcus aureus and oxacillin-resistant Staphylococcus aureus...
(MRSA). In vitro
In vitro
In vitro refers to studies in experimental biology that are conducted using components of an organism that have been isolated from their usual biological context in order to permit a more detailed or more convenient analysis than can be done with whole organisms. Colloquially, these experiments...
, iclaprim is highly active against MRSA, vancomycin-resistant Staphylococcus aureus
Vancomycin-resistant Staphylococcus aureus
Vancomycin-resistant Staphylococcus aureus refers to strains of Staphylococcus aureus that have become resistant to the glycopeptide antibiotic vancomycin. With the increase of staphylococcal resistance to methicillin, vancomycin is often a treatment of choice in infections with...
(VRSA), strains of Streptococcus pneumoniae
Streptococcus pneumoniae
Streptococcus pneumoniae, or pneumococcus, is Gram-positive, alpha-hemolytic, aerotolerant anaerobic member of the genus Streptococcus. A significant human pathogenic bacterium, S...
resistant to several common antibiotics, and some Gram-negative bacteria.
A new drug application
New drug application
The New Drug Application is the vehicle in the United States through which drug sponsors formally propose that the Food and Drug Administration approve a new pharmaceutical for sale and marketing...
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
European Medicines Agency
The European Medicines Agency is a European agency for the evaluation of medicinal products. From 1995 to 2004, the European Medicines Agency was known as European Agency for the Evaluation of Medicinal Products.Roughly parallel to the U.S...
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
Hospital-acquired pneumonia
Hospital-acquired pneumonia or nosocomial pneumonia refers to any pneumonia contracted by a patient in a hospital at least 48–72 hours after being admitted. It is usually caused by a bacterial infection, rather than a virus....
.
Iclaprim has been granted fast track
FDA Fast Track Development Program
The FDA Fast Track Development Program is a designation of the United States Food and Drug Administration that accelerates the approval of investigational new drugs undergoing clinical trials with the goal review time of 60 days...
status by the FDA.