HE3286: A Novel Synthetic Steroid as an Oral Treatment for Autoimmune Disease

HE3286 (17α‐ethynyl‐5‐androstene‐3β, 7β, 17β‐triol) is a synthetic derivative of a natural anti‐inflammatory steroid, β‐AET (5‐androstene‐3β, 7β, 17β‐triol). HE3286 is orally bioavailable and treats established disease in models of ulcerative colitis, collagen‐induced arthritis, and collagen antibody‐induced arthritis, reducing clinical signs of disease and proinflammatory signals, including IL‐6 and matrix metallopeptidase 3. HE3286 modulates nuclear factor κB through an unknown mechanism but does not interact with any of the steroid‐binding nuclear hormone receptors and is not immune suppressive. HE3286 was safe and well tolerated in phase I studies and is under evaluation in multicenter phase I/II clinical trials for ulcerative colitis and arthritis. HE3286 may provide a new treatment option for patients with inflammatory and autoimmune diseases.