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quarfloxin
- Development stage
- Phase 2
- Lead developer
- Cylene Pharmaceuticals
- Modality
- Small Molecules
- Administration
- Intravenous[3][4]
01
Overview
Quarfloxin is a small molecule antineoplastic agent and a fluoroquinolone derivative developed as an investigational cancer therapeutic. Its mechanism of action involves selectively disrupting the interaction between nucleolin protein and G-quadruplex DNA structures in ribosomal DNA (rDNA) within the nucleolus, thereby inhibiting RNA polymerase I-mediated transcription. This disruption impairs ribosomal RNA (rRNA) biogenesis, leading to apoptosis in cancer cells—a process that is particularly amplified in malignancies due to their increased rRNA synthesis demands. Quarfloxin was primarily investigated for use in neuroendocrine tumors, carcinoid tumors, lymphoma, and advanced solid tumors. Clinical development was discontinued after phase II trials due to lack of significant clinical benefit or strategic reasons[1][3][4][5][6].
- Brand names
- Quarfloxin
- Other names
- ItarnafloxinItarnafloxinaItarnafloxineItarnafloxinumQuarfloxacin
02
Targets
Pol I (RNA polymerase I)NCL (Nucleolin)PfG4 (Plasmodium falciparum G-quadruplex DNA)rDNA G4 (Ribosomal DNA G-quadruplex)
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