OUR PIPELINE
We are developing a pipeline of innovative macrocyclic therapeutics across a wide range of debilitating neuropsychiatric, neuroendocrine, and neurometabolic diseases, each targeting a novel mechanism of action.
Development Programs
Indication
Discovery
Preclinical
IND
Phase I
Phase II/III
Neuropsychiatry
Major Depressive Disorder
Neurometabolic
Obesity
Neuropsychiatry
Addiction
Novel Targets and New Indications
We plan to expand our R&D pipeline of investigational candidates through internal discovery and development as well as strategic collaborations or partnerships with pharmaceutical or biotechnology companies or academic organizations.
Therapeutic Indications
Major Depressive Disorder (MDD)
MDD is a serious illness with lifetime prevalence of ~20.6%1. MDD was ranked third in terms of disease burden in 2018 by WHO, and it is predicted to rank first by 20302.
Current antidepressants pharmacological treatment remains inadequate, and when effective, they are delayed in their onset of action and complicated by side effects, underlining the huge unmet need in targeting depression. Progress towards small molecule drugs has been slow. An alternative is to use endogenous peptides. The unmet needs with peptide drugs for major depression are delivery to the blood-brain-barrier, thus projecting the hurdle for the therapeutic development of novel compounds.
Introducing an AI-powered hydrocarbon-stapling technology in our body’s natural neuropeptide-receptor system, and combined with the translational routes of delivery in preclinical models, our lead candidate has demonstrated the potential of this neuropeptide-receptor system in reversing the major depression disorder.
Obesity
An escalating global epidemic of overweight and obesity – “globesity” is taking over many parts of the world. Nationally, over four in 10 U.S. adults are obese3. Worldwide, adult obesity has more than doubled since 1990, and adolescent obesity has quadrupled4. Obesity is a chronic condition that increases the risk of hypertension, type 2 diabetes, coronary heart disease, stroke, and certain cancers5. There is a growing unmet need for more effective treatment of obesity and its complications.
Current FDA approved anti-obesity drugs have major setbacks such as high risk of weight-regain, rapidly metabolized by proteolytic enzymes, and most common side effects include nausea, vomiting, diarrhea, and damage to liver and pancreas6. The physiological systems that regulate body weight are thus of great interest for anti-obesity agents. Peptidergic systems are critical to regulating energy homeostasis by key regions in the hypothalamus and brainstem.
To date, our group has made significant progress in this regard. Non-invasive delivery of our lead stapled peptidomimetic led to reduce body weight gain in male SD rats. This provides evidence and possibility of using stapled endogenous peptide-receptor system as a method of translational delivery that can modulate feeding behavior and weight gain in human and non-human animals.
References
1. Hasin DS, Sarvet AL, Meyers JL, Saha TD, Ruan WJ, Stohl M, et al. Epidemiology of Adult DSM-5 Major Depressive Disorder and Its Specifiers in the United States. JAMA Psychiatry. 2018;75(4):336-46.
2. Cui L, Li S, Wang S, Wu X, Liu Y, Yu W, et al. Major depressive disorder: hypothesis, mechanism, prevention and treatment. Signal Transduct Target Ther. 2024;9(1):30.
3. Mitchell NS, Catenacci VA, Wyatt HR, Hill JO. Obesity: overview of an epidemic. Psychiatr Clin North Am. 2011;34(4):717-32.
4. Hales CM, Carroll MD, Fryar CD, Ogden CL. Prevalence of Obesity and Severe Obesity Among Adults: United States, 2017-2018. NCHS Data Brief. 2020(360):1-8.
5. Emmerich SD, Fryar CD, Stierman B, Ogden CL. Obesity and Severe Obesity Prevalence in Adults: United States, August 2021-August 2023. NCHS Data Brief. 2024(508).
6. Finer N. Future directions in obesity pharmacotherapy. Eur J Intern Med. 2021;93:13-20.