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BL-8030 is a potent and selective second-generation NS3/4A protease inhibitor developed as an oral treatment for Hepatitis C virus infection. It demonstrates excellent antiviral activity in the low nanomolar range against multiple HCV genotypes including 1a, 1b, 2a, and 4. The drug was invented by Professor Philippe Halfon and his team at Genoscience Pharma and co-developed with RFS Pharma. BioLineRx licensed worldwide exclusive rights to develop and commercialize BL-8030 in February 2012. The compound exhibits several advantageous characteristics including an improved resistance profile against common protease inhibitor mutants, high specificity to viral protease without activity against human proteases, and a favorable safety profile with minimal drug-drug interactions due to its clean profile versus human liver enzymes. Preclinical pharmacokinetic studies in rats demonstrated good oral bioavailability and favorable liver distribution with a liver-to-plasma ratio of 28.4 to 45.4, suggesting potential for once-daily dosing. In June 2013, BioLineRx entered into a collaboration with Jiangsu Chia-Tai Tianqing Pharmaceutical (CTTQ) for development and commercialization specifically in China.
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