APD334 is Arena Pharmaceuticals’ novel therapeutic remedy to potentially treat autoimmune diseases like multiple sclerosis (MS) and ulcerative colitis. The drug is an oral formulation agonist (a substance which exerts its effect after binding to a particular receptor), and targets the S1P1 receptor. This receptor is involved in the regulation of immune responses in the body, and a potent target of treatments for autoimmune disorders.
How APD334 Works
S1P1 receptors are heavily involved in immune modulation, immune cell regulation and development, as well as the suppression of innate immune responses from T-cells. S1P1 receptor agonists are immunosuppressive and anti-inflammatory in nature owing to their ability to modulate leukocyte trafficking, sequestering lymphocytes in secondary lymphoid tissues, and/or enhancing vascular integrity. By keeping lymphocytes in lymph nodes, fewer immune cells are in circulating blood to cause tissue damage. This is the mode of action of APD334 – a small oral formulation shown to successfully reduce rates of inflammation in preclinical mouse models.
APD334 in Clinical Testing
With positive results from preclinical studies, a Phase Ib randomized, double-blind and placebo-controlled trial was undertaken to evaluate the safety, tolerability, pharmacodynamics and pharmacokinetics of multiple-ascending doses of APD334. Results from this study, in 50 healthy volunteers given APD334 and 10 others on placebo, demonstrated that the drug could reduce the lymphocyte count in blood, with mean decreases of up to 69% over a 21-day period from baseline. No serious adverse effects were recorded, and those reported were mild to moderate cases of dizziness, headache, constipation or diarrhea.
The company has begun a Phase 2 proof-of-concept trial of APD334 in ulcerative colitis patients that is expected to conclude in late 2016.
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