Halia Therapeutics has dosed the first subject in a Phase I clinical trial of HT-6184 in healthy human participants to analyse its potential for treating diseases driven by chronic inflammation.

A new small-molecule inhibitor of NEK7 and NLRP3 pathway, HT-6184 is the lead molecule from the company’s structure-based drug design strategy.

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This approach had created a pipeline of new drug candidates that act on crucial mediators of inflammation to potentially treat various ailments.

They include heart disease, Alzheimer’s and Parkinson’s disease, fatty liver diseases, cancers, inflammatory bowel disorders and others that are associated with chronic inflammation.

The placebo-controlled, single-centre, randomised, single ascending dose trial will analyse the safety, tolerability, pharmacokinetics and pharmacodynamics of HT-6184 in up to 32 healthy subjects. 

The company’s therapeutic hindering of NLRP3 signalling through NEK7 averts the NLRP3 inflammasome development and can boost the disassembly once formed, thereby suppressing the production and release of pro-inflammatory cytokines, IL-1β and IL-18. 

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Halia Therapeutics president and CEO Dr David Bearss said: “Leveraging our deep insight into the NLRP3 inflammasome biology, we specifically designed HT-6184 with a novel mechanism of action to allosterically target NEK7, a key component of the NLRP3 complex. 

“HT-6184 is part of a new class of compounds that target both NLRP3 priming and assembly, and we are excited to have advanced HT-6184 into the clinic and look forward to exploring its potential to treat diseases driven by chronic inflammation. 

“We believe that, by inhibiting NLRP3 signalling through allosteric NEK7 targeting, we can shut down an important driver of chronic inflammation implicated in a number of major diseases.”

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