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Quarfloxin QPLX/Nucleolin Inhibitor (CX-3543): Quarfloxin (CX-3543) is a ground-breaking small-molecule targeted cancer therapeutic derived from the validated fluoroquinolone class of drugs. Rationally designed to selectively inhibit ribosomal RNA (rRNA) Biogenesis in cancer cells, Quarfloxin disrupts the interaction between the Nucleolin protein and a G-quadruplex DNA structure in the ribosomal DNA (rDNA) template, a critical interaction for rRNA Biogenesis and one that is overexpressed in cancer cells. More specifically, Quarfloxin is built upon the template of the highly successful fluroquinolone class of drugs; by disrupting the G-quadruplex DNA:protein interaction critical in aberrant rRNA Biogenesis in cancer cells, Quarfloxin selectively induces apoptotic cell death in cancers. Many commercialized cancer therapeutics act indirectly on rRNA Biogenesis through upstream modulators, but Quarfloxin is the first agent to directly target this cancer-specific aberrant cell function.
Quarfloxin demonstrates potent in vivo efficacy against a broad range of tumors with a considerable therapeutic window in animal xenograft models, and no drug resistance has been observed to date. Moreover, Quarfloxin has been well tolerated in humans and has shown early signs of biological effects in the Phase I clinical trial. Due to its unique mechanism of action, we believe that Quarfloxcin may have application to a diverse array of human cancers, including colorectal, breast, pancreas, lung, prostate, ovarian, lymphoma and others. Clinical Development of Quarfloxin Quarfloxin is in early Phase II development in patients with chronic lymphocytic leukemia (CLL) and is in late Phase I trials in patients with advanced solid tumors or lymphomas. The Phase I trials have been conducted at two leading cancer centers in the United States: the Institute of Drug Development at the Cancer Therapy and Research Center in San Antonio, Texas, and at the Mayo Clinic Arizona in Scottsdale, Arizona. In the initial Phase I study, Quarfloxin was administered once daily for five consecutive days, followed by two weeks and two days off therapy. |
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