This event has passed. View key highlights below.
At the 2024 American Epilepsy Society (AES) Annual Meeting, Xyzagen presented new research showcasing its next-generation Kv7 channel opener chemistry for the treatment of seizures and related neurological disorders.
The presentation, titled “New Kv7 Channel Opener Chemistry for the Treatment of Seizures,” highlighted novel compounds designed to address neuronal hyperexcitability with improved potency, efficacy, and translational potential compared to existing therapies in clinical development.
Presentation Details
- Poster Title: “New Kv7 Channel Opener Chemistry for the Treatment of Seizures”
- Session: Poster Session 1.396, December 8, 2024
- Authors: Christopher Crean, Stevie Pope, Polina Danshina, Matthew Rich, David Fischler, Sarah Thrasher, and Angela Dixon
Key Presentation Insights
- Superior Potency: Some molecules demonstrated an EC50 of 50 nM on Kv7.2/7.3 in a patch clamp, surpassing current Kv7 modulators, such as XEN1101 and BHV7000.
- Enhanced Efficacy: Molecules exhibit a >200-fold improvement in Kv7.2 channel opening, with a 25% increase in Emax over ezogabine.
- In Vivo Validation: In rodent models, molecules showed full protection against maximal electroshock-induced seizures (MES) at doses as low as 3 mg/kg in rats and 7 mg/kg in mice, with ED50 values > 0.3 mg/kg in rat, achieving superior efficacy compared to drugs in clinical development.
- PK/PD Relationship: Plasma levels > 200 nM and brain levels > 40 nM led to > 75% of the mice and rats tested protected from the MES induced convulsion.
- Translational Potential: Pharmacokinetic allometric 2-species scaling suggests a 5 mg human dose to be above the 200 nM threshold for 24 h after a single dose, exhibit a half-life of 31 h and allow for self-titration.
Executive Quote
“The AES Annual Meeting provided an invaluable opportunity to share our novel Kv7 chemistry with the epilepsy research community,” said Chris Crean, Founder and CEO of Xyzagen. “These compounds represent a step forward in addressing the unmet medical needs of patients with epilepsy and other neurological disorders and provide another potential treatment within the expanding clinical Kv7 therapeutic space.”
Final Takeaways
Xyzagen’s work in this area highlights its integrated expertise in pharmacology, pharmacokinetics, and translational drug development—supporting the progression of novel CNS therapies from discovery through clinical evaluation.
Xyzagen has partnered with 100+ life science innovators, including early NIH-funded biotechs, small and mid-size pharma companies, and venture capital firms and brings a practical, decision-focused approach to complex drug development challenges.
If you’re interested in how Xyzagen can support your epilepsy or broader CNS development program through integrated pharmacology and PK expertise, we’d welcome the opportunity to connect. Contact us today to learn more.
About Xyzagen, Inc.
Xyzagen augments a client’s pharmacology and pharmacokinetics drug development team. As a leading pharmacokinetics consultancy and contract research organization with wet lab and rodent vivarium facilities, Xyzagen is able to push model informed drug development into its First-in-Rat® and First-in-Mouse® discovery platforms as well as support late-stage clinical noncompartmental PK, PopPK, and Quantitative Medicine. Our knowledge in pharmacology/pharmacogenomics and in vitro/in vivo pharmacokinetics allows the client to expand their core scientific team during the critical period of candidate selection up to the PreIND meeting and through clinical development and the preNDA meeting. We’re a boutique organization which allows for small clients and CROs to work directly with experts.
Media Contact:
Christopher Crean
Founder & CEO
Xyzagen, Inc.
Phone: (919)-762-2072
Email: [email protected]
