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Quarfloxin QPLX/Nucleolin Inhibitor (CX-3543): Quarfloxin 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 amplified in cancer cells. As a result, 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 demonstrated signs of biological benefit for patients with C/NET in Phase I clinical trials. Moreover, biodistribution studies revealed that quarfloxin accumulates in the tissues in which C/NET arise. 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 Phase II development in patients with carcinoid/neuroendocrine tumors(C/NET). In this open-label Phase II trial, quarfloxin will be administered to patients with low or intermediate grade C/NET, including those receiving concomitant treatment with a stable dose of octreotide. This multicentered study will include an assessment of improvements in patients’ symptoms and biochemical markers, in addition to RECIST tumor response measurements. The first patient was enrolled and treated at Front Range Cancer Specialists in Fort Collins, CO under the care of Robert Marschke Jr. M.D. This study is expected to enroll up to 25 patients at several leading cancer centers. |
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