EP4643858A1 — Methods and pharmaceutical composition for the treatment of uterine disease

USPTO Abstract

Control tissues and different lesions of either adenomyosis or endometriosis were exposed in vitro during 24 hours either to vehicle (DMSO) or different doses of BYL719 or ST420, a PIK3CA inhibitor. Inventors observed that lesions treated with DMSO had a higher recruitment of the PIK3CA pathway compared to healthy endometrium. Importantly, both inhibitors were able to shut down the phosphorylation of AKT. They concluded that PIK3CA inhibition is a good therapeutic target for patients with endometriosis and adenomyosis. They also investigated the role of the PIK3CA pathway in myoma, another benign uterine condition. They observed that either alpelisib or ST420 were able to inhibit the pathway in myoma. They concluded that myoma demonstrate PIK3CA/AKT pathway activation with somatic mutation and are accessible to targeted treatment. Accordingly, the invention relates to method for treating uterine disease in a subject in need thereof comprising a step of administrating the subject with a therapeutically effective amount of PIK3CA inhibitor such as compound of formula (I), or a deuterated or tritiated form of the compound of formula (I), BYL719.