New potassium channel blockers - extended ShK analogues
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- Summary
- Novel, highly potent peptide inhibitors of the Kv1.3 potassium channel, an emerging target for autoimmune diseases. The Monash peptides offer numerous advantages, including high Kv1.3 selectivity, minimising the potential for off-target side effects, efficacy across a range of experimental models and high yield production (recombinant or synthetic).
- Technology Benefits
- - Novel lead peptide inhibitors of Kv1.3 having high potency (low pM affinity), selectivity (over Kv1.1) and stability
- Clinical ‘Proof of Mechanism’ of related peptides demonstrated in Phase 1b clinical studies
- Suitable for recombinant manufacture GMP-scale production, as well as peptide synthesis
- Multiple therapeutic product opportunities
- Technology Application
- Our approach is to develop a best in class Kv1.3 blocker that is potent, cheap to manufacture, and sufficiently stable to better exploit the full range of opportunities in autoimmune diseases.
- Detailed Technology Description
- Researchers from the Monash Institute of Pharmaceutical Sciences and their collaborators have designed two different lead series based on ShK and HsTX1 (from scorpion venom). These lead series are potent and highly selective inhibitors of Kv1.3, with potency in the low pM range.
Compared with Dalazatide, the Monash peptides have enhanced selectivity for Kv1.3 over Kv1.1 and other ion channels, offering potential safety benefits. They also offer potential manufacturing advantages as they are chemically more stable and can be produced cheaply by recombinant expression.
The peptides have demonstrated efficacy in a range of AI disease models, including RA, where the results support once-weekly injectable administration. We are currently in lead optimisation stage and demonstrating the suitability of these classes for diverse administration routes.
- Type of Cooperation
- Licensing
- Application Date
- 14/08/2015 00:00:00
- Application No.
- AU2015303825
JA2017-508102
Others
- Others
- Monash seeks a partner to clinically develop and translate this opportunity.
- ID No.
- 2014-024
- Country/Region
- Australia
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