Drug intelligence / Profile preview

Iclaprim

Development stage
Phase 3
Lead developer
Motif Bio
Modality
Small Molecules
Administration
Intravenous
01

Overview

Iclaprim is a novel, investigational diaminopyrimidine antibiotic that acts as a selective and potent **inhibitor** of bacterial dihydrofolate reductase (DHFR), an enzyme essential for the synthesis of thymidine and thus DNA replication in bacteria[1][2][5]. It was specifically designed to overcome resistance to trimethoprim by binding effectively to both wild-type and trimethoprim-resistant forms of DHFR, including those with common resistance mutations[1]. Iclaprim demonstrates broad-spectrum activity against Gram-positive pathogens, including methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-intermediate and vancomycin-resistant S. aureus, as well as resistant strains of Streptococcus pneumoniae[2][4][7]. Unlike trimethoprim, it does not require co-administration with sulfonamides. The drug is administered intravenously and has been primarily developed for the treatment of acute bacterial skin and skin structure infections (ABSSSI)[3][5]. Motif Bio developed iclaprim; it has not received FDA approval but was granted Qualified Infectious Disease Product (QIDP) status by the FDA for ABSSSI[3][5].

Other names
5-[[(2R)-2-cyclopropyl-7,8-dimethoxy-2H-chromen-5-yl]methyl]pyrimidine-2,4-diamineIclaprime2,4-Pyrimidinediamine, 5-[(2-cyclopropyl-7,8-dimethoxy-2H-1-benzopyran-5-yl)methyl]-AR 100AR100AR-100Ro-482622Ro482622Ro 482622
02

Targets

DHFR (Dihydrofolate reductase)

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