Development Programs
Mixed Delta/Mu Agonists
Our preclinical and clinical evidence indicates that simultaneous mu-and delta-receptor stimulation will maintain or even enhance the analgesic efficacy of the classic mu-receptor opioids while reducing the incidence and severity of the mu-related side effects of respiratory depression and vomiting. We also have evidence in a preclinical model that dependence, a mu-related side effect of chronic therapy, is mitigated by concomitant delta receptor agonism.
Selective Delta Agonists
We have found that selective stimulation of delta receptors in preclinical models leads to specific pharmacologic actions that suggest unique treatment approaches to a variety of medical conditions. Unlike mu-receptor agonists or mixed delta/mu agonists, specific delta-receptor agonists are not known to be associated with abuse or dependence liability in preclinical studies. We are currently investigating selective delta receptor agonists in several indications:
- We have demonstrated that delta agonists improve urinary bladder function in several preclinical models of urinary incontinence.
- We believe we are the first company to recognize the importance of the delta receptor in ejaculatory physiology. Using a preclinical model we have demonstrated a dose-dependent inhibition of ejaculation in response to several of our selective delta agonists.
- Stimulation of delta receptors within the brain produces activating effects and, therefore, we believe that delta receptor agonists may be of significant value in depression. Our selective delta agonists have produced a faster onset of antidepressant activity, with overall efficacy equal to or greater than existing SSRIs (e.g., Prozac®, Paxil®, Zoloft®) and tricyclic antidepressants in preclinical models of depression.
- Preclinical models of cardiac ischemia demonstrate that delta agonists protect heart muscle when administered prior to the onset of the ischemic event.