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Abstract Details

Development of a Novel, Clinical-stage Drug for the Prevention of Migraine Based on Receptor Activity Mapping and Achievement of a Target Receptor Profile
Headache
Headache Posters (7:00 AM-5:00 PM)
099

Many classes of drugs that have been successfully used to treat neurological diseases have polypharmaceutical attributes: they affect multiple receptors resulting in both beneficial and unintended effects. One such drug class, the ergot alkaloids, included the drug methysergide, the first migraine preventive. While the capability to affect multiple receptors likely augmented the therapeutic effect of such compounds, their use was hindered by side effects such as those associated with agonism at off-target dopaminergic and serotonergic receptors.

Xoc correlated novel receptor activity assessments with observed clinical effects to elucidate which molecular moieties and receptor interactions were responsible for the desired efficacy and unintended side effect profiles.

XC101-D13H, and its receptor profile, represent an important innovation in designing a novel compound with an optimal receptor profile for migraine prevention.

To design a novel molecule for the prevention of migraine by exploiting known efficacious activity profiles, while avoiding undesirable tolerability effects.

Xoc conducted a thorough review of the clinical literature to determine the therapeutic and side effect profiles of drugs used as migraine preventives and developed a receptor activity profile for favorable efficacy and tolerability. Receptor binding and activity profiles were developed for compounds of interest where literature data were absent.

A receptor profile intended to provide therapeutic benefit for migraine prevention while avoiding side effects was developed.  Xoc subsequently developed a series of novel chemical entities with receptor profiles that compare favorably with the target profile. The receptor profile for XC101-D13H has important similarities – and key differences – with that for methysergide, a drug known to be effective as a migraine preventive, but with known serious side effects.

Xoc developed a novel clinical stage compound, XC101-D13H, with the desired target receptor profile for safe and effective migraine preventive therapy.  XC101-D13H entered human clinical trials in 2019.

Authors/Disclosures
Miguel Guzman (Xoc Pharmaceuticals)
PRESENTER
Miguel Guzman has received personal compensation for serving as an employee of Xoc Pharmaceuticals. Miguel Guzman has received stock or an ownership interest from Xoc Pharmaceuticals. Miguel Guzman has received personal compensation in the range of $100,000-$499,999 for serving as a VP, Product Development with Xoc Pharmaceuticals.
Scott Borland (Xoc Pharmaceuticals, Inc.) Scott Borland has received personal compensation for serving as an employee of Xoc Pharmaceuticals, Inc.. Scott Borland has received personal compensation in the range of $0-$499 for serving as an officer or member of the Board of Directors for Xoc Pharmaceuticals, Inc.. Scott Borland has received stock or an ownership interest from Xoc Pharmaceuticals, Inc..
Robert Fishman, MD (Butler Hospital ) Dr. Fishman has nothing to disclose.
Thomas Armer (Xoc Pharmaceuticals) Thomas Armer has received personal compensation for serving as an employee of Xoc Pharmaceuticals. Thomas Armer has received stock or an ownership interest from Xoc Pharmaceuticals.