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Drug Names(s): CX-3543
Description: Quarfloxin is a small-molecule targeted cancer therapeutic derived from the validated fluoroquinolone class of drugs. Fluoroquinolone are commonly used broadspectrumantibiotics, which are relatively nontoxicand inhibit type II DNA topoisomerase in mammalian cells and bacterial DNA gyrase. Thisenzyme is responsible for replication, transcription,supercoiling and chromosomal separationof prokaryotic DNA.
Quarfloxin is thought to disrupt the interaction between the Nucleolin protein and a G-quadruplex DNA structure in the ribosomal DNA (rDNA) template. More specifically, Quarfloxin is built upon the template of the 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.
In March 2013, Cylene announced that it has entered into an exclusive, worldwide Option and License Agreement that will allow TetraGene to advance the development of Quarfloxin and Cylenes associated anticancer quadruplex-targeting technologies. Cylene will receive an upfront fee, as well as potential milestone payments and royalties on product sales for the exclusive license. TetraGene has the option to acquire worldwide rights to the technologies licensed from Cylene, which include the Phase II compound Quarfloxin and several registered patents.
In 2013, Cylene Pharmaceuticals, Inc. ceased operations.
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