BI 1181181

BI 1181181 is an orally active small molecule inhibitor of beta-site amyloid precursor protein cleaving enzyme 1 (BACE1), also known as a beta-secretase inhibitor. It was initially discovered by Vitae Pharmaceuticals using their proprietary Contour platform and later clinically developed in partnership with Boehringer Ingelheim. The drug was designed to lower brain amyloid beta (Aβ) levels by inhibiting BACE1, a key enzyme involved in the production of amyloid-beta peptides implicated in Alzheimer's disease pathology. Preclinical studies demonstrated significant reductions in Aβ levels in animal models. Phase I clinical trials showed that single doses were well tolerated and produced substantial and sustained reductions of cerebrospinal fluid Aβ, with dose-proportional pharmacokinetics suitable for once-daily dosing. However, development was discontinued after early clinical trials due to safety concerns related to skin reactions observed during multiple rising dose studies[5][7].

Other names

BI-1181181BI1181181BI 1181181VTP-37948VTP37948VTP 37948