Sparian Biosciences Announces Results from the Phase 1 Clinical Trial of First in Class Novel Arylepoxamide Receptor (AEAr) Agonist Analgesic SBS-1000

• SBS-1000 was shown to be safe and well tolerated in healthy volunteers in this Phase 1 Single Ascending Dose (SAD) study
• No serious adverse events observed
• Sedation at higher doses proved the dose limiting toxicity
• Cold Pressor Test demonstrated a positive trend toward analgesic efficacy

Sparian Biosciences, Inc. (“Sparian”), a clinical-stage CNS-focused biopharmaceutical company, today announced results from the Phase 1 clinical trial of the first in class novel arylepoxamide receptor (AEAr) agonist analgesic SBS-1000. The Phase 1 single ascending dose (SAD) study evaluated safety and tolerability as well as the pharmacokinetic profile of SBS-1000 IV infusion over a range of doses in healthy adult volunteers. The study also included pharmacodynamic measures including the Cold Pressor Test and pupillometry.

The arylepoxamide receptors (AEAr) are a novel class of receptors widely distributed throughout the brain and spinal cord and are believed to modulate pain signaling and pain perception. SBS-1000 is the first in class AEAr agonist that, in pre-clinical models, demonstrates highly potent analgesia without dangerous side effects such as respiratory depression, abuse liability and physical dependence. “In rigorous and reproducible animal models of severe pain, SBS-1000 has repeatedly proved itself a potent analgesic with remarkable safety,” said Jeff Reich, M.D. CEO and CoFounder of Sparian. “If we can successfully translate the pre-clinical results to the clinic, SBS-1000 has the potential to replace opioids in the management of acute and chronic moderate to severe pain.” Dr. Reich added, “None of the new non opioid analgesics with novel targets have yet to demonstrate comparable efficacy”.

In this Phase 1 SAD, a range of doses were explored in adult healthy volunteers. There were no serious adverse events. In particular, respiratory parameters including respiratory rate, pulse oximetry and end tidal CO2 were maintained within normal range in all subjects at all doses studied. Sedation at the higher doses proved to be the rate limiting toxicity. In the pre-clinical studies sedation also proved to be a dose limiting toxicity but improved over time with repeat dosing. Since this was a single dose study, tolerance to sedation could not be demonstrated. A full pharmacokinetic profile of SBS-1000 IV infusion was also characterized.

Pharmacodynamic measurements in the Phase1 study included Cold Pressor Test and pupillometry. The Cold Pressor Test is a measure of analgesia acceptable to study in healthy volunteers but was not powered for statistical significance. Nonetheless, it showed a positive trend toward efficacy. Pupillometry is typically used as a measure of off-target binding, chiefly at the mu opioid receptor (MOR). In the Phase 1 at all doses including the doses causing sedation there was no significant impact on pupillary diameter, specifically no evidence of pupillary constriction, indicating no MOR activation.

“While we are pleased with our SAD for SBS-1000, our current plans are underway to advance the next generation AEAr agonist – SBS-147, which can be administered via all routes of administration, not just IV,” commented Dr. Reich. “We would like to submit an IND this time next year for a combined Phase 1 SAD/MAD trial. Our clinical experience with SBS-1000 should help inform the planning and execution of the clinical program for the follow-on compound.”

SBS-1000 has been supported by a National Institutes of Health/ National Institute of Drug Abuse UG3/UH3 grant.