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Oligonucleotides have a high therapeutic potential for the treatment of various diseases including cancer and metabolic diseases. The major hurdle of oligonucleotide applications is their intracellular delivery after systemic in vivo application. By using particle based delivery, most of the oligo drugs were delivered into the liver, whereas only partial amounts arrive cancerous tissue. Overdosing in order to reach peripheral (tumor) tissue does induce side effects in the liver and often stimulates the immune system.
BianoScience Peptide-siRNA prodrug approach aimes to reduce these side effects. Based on covalently bound peptides on the 5`antisense strand, the siRNA is applied as an inactive prodrug. Since the peptide contains a cleavage side for specific proteases expressed in the target tissue, siRNA-prodrug is specifically cleaved and activated. On this bases, side effects (especially in the liver) can be massively reduced leading to specific effecs in the target tissue and offering the possibility to increase dosing/side effects ratio.
Based on the Peptide-siRNA prodrug approach, BianoScience devellops drug candidates to treat Triple-Negative Mammary Cancer with the focus on liver metastases. Intensive animal experiments showed great tolerability and activity of the drug compounds using lipid nanoparticle based delivery strategy. Recent activities aim to optimise delivery and formulation of the oligonucleotide drug compounds, GMP production and start of the clinical phase-1/2a.
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Source: https://bianoscience.com/Drug_development