GEn1E Lifesciences Publishes Breakthrough Research Unveiling Novel Mechanism of Action of Dual Signal Modulators for Anti-inflammatory and Endothelial-Stabilizing Therapies

PALO ALTO, Calif., Oct. 14, 2024 (GLOBE NEWSWIRE) — GEn1E Lifesciences, a clinical-stage Phase 2 company, and a leading innovator in precision therapies for inflammatory and rare diseases, with a strong partnership with the University of Maryland, Baltimore (UMB), today announced the publication of a landmark study in the prestigious Journal of Pharmacology and Experimental Therapeutics (JPET).

The study, titled First-in-Class Mitogen-Activated Protein Kinase p38α: MAPK-Activated Protein Kinase-2 (MK2) Dual Signal Modulator with Anti-inflammatory and Endothelial-Stabilizing Properties, marks a significant advancement of next-generation immunomodulatory therapeutics for treating inflammatory and autoimmune diseases.

“Our findings represent a new era in kinase pathways,” said Paul Shapiro, PhD, co-author and professor in the Department of Pharmaceutical Sciences at the University of Maryland School of Pharmacy and its associate dean for research. “We have reasoned that the past clinical failure of previous generation p38 catalytic inhibitors reflects an intrinsic flaw in the strategy of inhibiting kinase activity. So, we utilized an alternative and unique strategy based on the p38 MAPK structure and functions enabling us to modulate critical inflammatory pathways while minimizing off-target effects – a breakthrough that could transform the treatment of inflammatory diseases.”

Jeff Hasday, MD, the Dr. Herbert Berger Professor of Medicine and former Head of the Pulmonary and Critical Care Medicine Division at the University of Maryland School of Medicine and the study’s co-contributing author, emphasized the clinical relevance of the findings. “GEn-1124 offers a targeted way to destabilize the p38:MK2 complex without blocking p38 catalytic activity or ablating downstream signaling. The result is a rebalancing of downstream pro- and anti- inflammatory signaling, yielding anti-inflammatory, endothelial-stabilizing, and lung-protective effects with therapeutic potential in pulmonary diseases where inflammation and endothelial barrier dysfunction play key roles.”

Key Points from the Study:

• Targeted Modulation: GEn-1124 precisely disrupts the p38α:MK2 complex, maintaining downstream signaling essential for cellular function while selectively inhibiting pro-inflammatory responses.
• Efficacy in Preclinical Models: GEn-1124 demonstrated remarkable efficacy in preclinical studies, improving survival rates by 4-fold in acute lung injury and 5-fold in influenza-induced pneumonia along with the compound’s potential to halt disease progression.
• Endothelial-Stabilizing Properties: The compound showed robust barrier-stabilizing effects in human pulmonary artery endothelial cells (hPAEC), a key factor in treating diseases characterized by vascular leakage and inflammation.

The breakthrough findings are well-timed, as GEn1E Lifesciences, which has an exclusive, worldwide and all fields license from UMB is enrolling patients for a Phase 2 study for ARDS, a devastating disease costing $25B to the US society. 

“We’re thrilled to see the immense potential of next generation dual signal modulators unfold in this study,” said Ritu Lal, CEO, Co-founder of GEn1E Lifesciences and adjunct Associate Professor at the University of Maryland School of Pharmacy. “This breakthrough underscores our mission to develop precision therapies for inflammatory diseases and improve outcomes for patients suffering from devastating conditions.”

For more information, visit GEn1E’s website or follow GEn1E on LinkedIn.

About GEn1E Lifesciences:

GEn1E Lifesciences is a clinical-stage, Phase 2 company accelerating novel, dual signal modulator precision therapies for rare and inflammatory diseases. GEn1E Lifesciences is based in Palo Alto, California, with a laboratory in Mountain View, California and a strong collaboration with the University of Maryland, Baltimore.

GEn1E has developed a well-differentiated “Platform-in-a-Mechanism” model that uses AI to span the entire end-to-end drug development cycle. The company has accelerated several milestones with novel Signal Modulators being actively developed as first-in-class therapies for rare and inflammatory diseases with its lead compound in Phase 2 currently enrolling patients in the US.

For more information on GEn1E, visit www.gen1e.com and follow GEn1E on LinkedIn.

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