Rezera Announces Phase 1 Results for Trabzanoflast, which was Generally Well Tolerated and Demonstrated High Central Nervous System Exposure (CNS)

Continuous cerebrospinal fluid sampling confirmed high CNS exposure, with a Kp,uu of 1.9

BOSTON, Sept. 30, 2026 (GLOBE NEWSWIRE) — Rezera Inc. (the “Company”), a clinical-stage biotechnology company developing a portfolio of internally-invented and wholly owned oral inhibitors of NLRP3 to address inflammatory drivers of cardiovascular and neurologic diseases, today announced topline results from its Phase 1 first-in-human clinical trial of trabzanoflast, an investigational oral, brain-penetrant NLRP3 inhibitor for the treatment of neuroinflammatory diseases. The results support continued clinical development of trabzanoflast.

The study showed that trabzanoflast was generally well tolerated across a range of single and multiple ascending dose cohorts in healthy volunteers. There were no serious adverse events, no adverse events leading to discontinuation, and no clinically significant changes in laboratory values relevant to safety monitoring. Pharmacokinetic analysis showed dose-proportional exposure across all doses tested, and pharmacodynamic assessments confirmed strong target engagement in both cerebrospinal fluid (CSF) and blood. Continuous CSF sampling confirmed high CNS exposure, with a Kp,uu of 1.9. Brain exposure to trabzanoflast is expected to remain above the IC₉₀ at trough, based on preclinical data.

“Chronic inflammation in the CNS compartments, including the brain, eye, ear and spinal cord, is implicated in the initiation of and contributes to the onset and progression of many neurologic diseases, yet these compartments have historically been difficult to reach with meaningful drug exposure,” said Jyothis George, MBBS, Ph.D., Chief Medical Officer at Rezera. “Trabzanoflast was designed to achieve high penetration in these compartments. These Phase 1 data provide encouraging clinical evidence of CNS exposure in humans, NLRP3 pathway engagement in the CNS, and an anti-neuroinflammatory biomarker profile that supports further development of trabzanoflast as a potentially differentiated oral therapy for diseases where NLRP3-driven neuroinflammation plays a causal role.”

About the study

The Phase 1 first-in-human clinical trial evaluated the safety, tolerability, pharmacokinetics and pharmacodynamics of trabzanoflast in healthy adult volunteers. The primary endpoint was safety and tolerability following single and repeated daily administration. The study enrolled 55 participants, including healthy elderly participants, across single and multiple ascending dose cohorts and included CSF sampling to assess CNS exposure.

About trabzanoflast

Trabzanoflast (f/k/a NT-0150) is an investigational, structurally-differentiated, potent, orally available, brain-penetrant small-molecule NLRP3 inhibitor discovered by Rezera. Its unique chemotype is being optimized to achieve high levels of brain penetration and robust CNS exposure. In preclinical animal CNS models, trabzanoflast demonstrated effective brain target coverage and anti-neuroinflammatory activity. Trabzanoflast has successfully completed long-term toxicology studies supporting clinical progression.

About Rezera

Rezera is a clinical-stage biotechnology company developing a portfolio of internally-invented and wholly owned oral inhibitors of NLRP3 to address inflammatory drivers of cardiovascular and neurologic diseases driven by the NLRP3 inflammation pathway. The Company’s lead program, ruvonoflast (f/k/a NT-0796), is being developed for cardiovascular diseases and recently announced topline data from its Phase 2 RESOLVE-1 study.

Rezera is headquartered in Boston, Massachusetts, with an R&D base in Cambridge, UK.

Learn more at http://www.rezera.com/ or follow the Company on LinkedIn.

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Argot Partners
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