Iclaprim

Iclaprim is a novel antibiotic that belongs to the dihydrofolate reductase inhibitor class. It is designed to treat serious skin infections and pneumonia caused by methicillin-resistant Staphylococcus aureus (MRSA) and other Gram-positive bacteria.

History

Iclaprim was initially developed by Roche, but the development was discontinued in the late 1990s. The rights to the drug were later acquired by Arpida, a Swiss biotech company, which further developed the drug and submitted it for approval to the Food and Drug Administration (FDA) in the United States and the European Medicines Agency (EMA) in Europe. However, both agencies rejected the application due to concerns about the drug's safety and efficacy.

In 2015, the rights to Iclaprim were acquired by Motif Bio, a biopharmaceutical company based in the United States. Motif Bio conducted two Phase III clinical trials and resubmitted the drug for approval to the FDA. However, in 2019, the FDA again rejected the application, citing the need for additional clinical data.

Mechanism of Action

Iclaprim works by inhibiting the enzyme dihydrofolate reductase (DHFR), which is essential for the synthesis of tetrahydrofolate. Tetrahydrofolate is a crucial component in the synthesis of purines and pyrimidines, which are the building blocks of DNA. By inhibiting DHFR, Iclaprim prevents the bacteria from synthesizing DNA, thereby stopping their growth and reproduction.

Clinical Use

Iclaprim is intended for the treatment of serious skin infections and pneumonia caused by MRSA and other Gram-positive bacteria. It is administered intravenously and has a broad spectrum of activity against Gram-positive bacteria, including resistant strains.

Side Effects

The most common side effects of Iclaprim include nausea, vomiting, diarrhea, and headache. In rare cases, it can cause serious side effects such as anemia, neutropenia, and elevated liver enzymes.

Future Development

Despite the setbacks, Motif Bio continues to develop Iclaprim and is currently conducting additional clinical trials to address the FDA's concerns. The company is also exploring the potential use of Iclaprim in other indications, such as bacterial meningitis and endocarditis.

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  Iclaprim 2D ACS Structure

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  (R)-Iclaprim Structural Formula

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  (S)-Iclaprim Structural Formula