Active Ingredients

Iclaprim – Effect, Application & Risks


Iclaprim is a medical drug that is currently (as of 2017) still in the approval process. It is manufactured by the Swiss pharmaceutical and biopharmaceutical company ARPIDA based in Reinach and is intended to treat complicated skin and skin structure infections. From a pharmacological-medical point of view, it is an antibiotic whose mechanism of action stems from an inhibition of bacterial dihydrofolate reductase.

What is Iclaprim?

Iclaprim is to be used in the near future to treat various infections of the skin and skin structure. The active ingredient is manufactured by the Swiss pharmaceutical company APRIDA, which also holds the patents on the substance. The antibiotic is still in the approval phase in the European Union (EU) and the United States of America (USA).

In 2009, the US regulatory authority Food and Drug Administration (FDA) refused fast-track approval in an urgent procedure and referred to the regular approval that APRIDA is currently striving for. Iclaprim is therefore not yet available on the drug markets. If an approval is granted, the drug may only be given to patients with a doctor’s prescription. The ordering of a pharmacy obligation is also common for comparable medicines.

In chemistry and pharmacology , iclaprim is described by the empirical formula C 19 – H 22 – N 4 – O 3 . The molecular formula C 20 – H 26 – N 4 – O 6 – S is used for the also common iclaprim mesilate. This corresponds to a moral mass of 354.4 g/mol or 450.51 g/mol. The mechanism of action of iclaprim is based on inhibition of bacterial dihydrofolate reductase. The antibiotic is regarded as a beacon of hope for the treatment of diseases caused by resistant strains of pathogens.

Pharmacological effect on body & organs

Due to its pharmacological properties and the mechanism of action used, iclaprim is an antibiotic. It is assigned to the active substance group of diaminopyrimidines, which also includes the drugs pyrimethamine , kopexil and aminopterin. Typical of this group is the presence of an organic compound consisting of a base and two amino groups on a pyrimidine ring. The empirical formula of the diaminopyrimidines therefore always shows carbon (C), hydrogen (H) and nitrogen (N).

Iclaprim is considered to be a potent inhibitor of a bacterium ‘s dihydrofolate reductase . There are therefore similarities with trimethoprim , which also belongs to the group of diaminopyrimidines. The special feature of iclaprim is that it is also active on numerous pathogen strains on which trimethoprim is no longer effective.

Medical studies performed outside of the living organism (in vitro) have shown that iclaprim can be used against a wide range of gram-positive bacteria. Those pathogens that turn blue when a differential staining procedure (Gram stain) is carried out are Gram-positive. Iclaprim is therefore regarded as a beacon of hope for the treatment of skin diseases that are caused by resistant bacteria.

Medicinal Application & Use for Treatment & Prevention

Iclaprim is said to be used to combat skin and skin structure infections. In the clinical studies carried out to date, administration has been either oral or intravenous, so that these forms of administration will probably also be indicated in practice.

When taken orally in the form of film-coated tablets, the bioavailability of the antibiotic is around 40%. A dose of 160 mg is recommended for average patients. Here, a plasma level of up to 0.5 µg/ml can be reached.

If iclaprim is administered intravenously, the recommended dosage is between 0.4 and 0.8 mg per body weight. Here, plasma concentrations of up to 0.87 µg/ml are possible. The plasma half-life is set at two hours.

Risks & side effects

As with all drugs, undesirable side effects can also occur after taking Iclaprim . According to the current state of knowledge, numerous comparisons can be made with the drug linezolid . The most common side effects are therefore complaints of the gastrointestinal tract , which can manifest themselves in the form of diarrhea, loose stools , vomiting , abdominal pain , constipation , nausea or nausea . Also, headaches and loss of taste are potential side effects.

In addition, changes in blood values ​​are possible. Decreased white blood cell count , neutrophil deficiency, or platelet deficiency may also occur. Fever and skin reactions are also to be expected. The latter are expressed in particular by itching , redness and rashes .

In addition, Iclaprim must not be used if there is a medical contraindication (indication). In medicine, this refers to a circumstance that makes the use of a certain preparation seem unreasonable because unforeseeable risks and side effects are likely. This is especially the case if an intolerance to the active ingredient is known. In the case of allergies to diaminopyrimidines, special caution must be exercised, so that a careful opportunity-benefit analysis must be carried out.

In addition, interactions with other drugs should be taken into account. The doctor treating you must therefore be informed at regular intervals about all the preparations you are taking. In this way, risks can be minimized and made more calculable.

Lisa Newlon
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Hello! I am Lisa Newlon, and I am a medical writer and researcher with over 10 years of experience in the healthcare industry. I have a Master’s degree in Medicine, and my deep understanding of medical terminology, practices, and procedures has made me a trusted source of information in the medical world.