1 / 14

New Jersey, U.S.A.

YKP3089 Novel Neurotherapeutic ASENT March 2009 Martin Brecher, MD Life Science Fair Lawn, New Jersey. New Jersey, U.S.A. Seoul, Korea. Daejeon, Korea. Shanghai, China. YKP3089. YKP3089 Preclinical Summary. Anticonvulsant Profile. YKP3089. Data Source: NIH.

ora
Télécharger la présentation

New Jersey, U.S.A.

An Image/Link below is provided (as is) to download presentation Download Policy: Content on the Website is provided to you AS IS for your information and personal use and may not be sold / licensed / shared on other websites without getting consent from its author. Content is provided to you AS IS for your information and personal use only. Download presentation by click this link. While downloading, if for some reason you are not able to download a presentation, the publisher may have deleted the file from their server. During download, if you can't get a presentation, the file might be deleted by the publisher.

E N D

Presentation Transcript

  1. YKP3089 Novel Neurotherapeutic ASENT March 2009 Martin Brecher, MD Life Science Fair Lawn, New Jersey New Jersey, U.S.A. Seoul, Korea Daejeon, Korea Shanghai, China

  2. YKP3089 YKP3089 Preclinical Summary

  3. Anticonvulsant Profile YKP3089 Data Source: NIH

  4. Anticonvulsant Profile YKP3089

  5. YKP3089 Anticonvulsant Profile Data Source: NIH

  6. YKP3089 Anxiolytic Profile • Effective in a wide variety of anxiety models • Light-Dark Box • Social Interaction • Fear-Potentiated Startle • Marble-Burying • Elevated Plus Maze • Defensive withdrawal, etc. • Active in Rats and Mice +++ - ED50 <20mg/kg ++ - ED50 <30mg/kg

  7. YKP3089 Analgesic (Neuropathic Pain) Profile • Excellent activity in models of neuropathic pain • Improved efficacy compared to gabapentin +++ - ED50<50mg/kg ++ - ED50 <100mg/kg

  8. YKP3089 Additional Indication Profile

  9. YKP3089 Preclinical ADME/Safety/Toxicity • ADME • Excellent PK parameters • Rat PO • Monkey PO • Good metabolic stability • Moderate plasma protein binding • Good Tissue Distribution • Safety/Toxicity • Good Safety • hERG Channel • Monkey CV Telemetry • Respiratory • Gastric • Negative Gene Toxicity • Typical CNS clinical signs • Low teratogenicity potential

  10. YKP3089 YKP3089 Clinical Summary

  11. YKP3089 Single Dose PK

  12. YKP3089 Multiple Dose PK Both Cmax and AUC linearly correlated with dose Steady State occurred by Day 12

  13. YKP3089 Food Effect Study PK

  14. YKP3089 YKP3089 Highlights Efficacy • Potential versatile CNS drug: Epilepsy, Anxiety, Neuropathic Pain, Bipolar Disorder, Dementia, Schizophrenia, etc. • Broad spectrum: Epilepsy • Possible novel mechanism Safety & Toxicity • High safety margin • Low QTc prolongation potential • Low teratogenic potential Phase I Clinical Trials in USA • Favorable PK profile • Once a day dosing potential • Low adverse effects

More Related