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New potassium channel blockers - extended ShK analogues

总结

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).

技术优势

- 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

技术应用

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.

详细技术说明

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.

合作类型

Licensing

申请日期

14/08/2015 00:00:00

申请号码

AU2015303825
JA2017-508102
Others

其他

Monash seeks a partner to clinically develop and translate this opportunity.

ID号码

2014-024

国家/地区

澳洲