rupitasertib

Rupitasertib is an orally available small molecule inhibitor targeting the serine/threonine protein kinases ribosomal protein S6 kinase (p70S6K) and AKT1/AKT3. It is designed to efficiently block the PI3K/AKT/mTOR (PAM) signaling pathway while also controlling compensatory AKT feedback loops that often limit the efficacy of other PAM inhibitors. Rupitasertib has shown potential antineoplastic activity by inhibiting tumor cell proliferation in cancers with overactivated PI3K/AKT/p70S6K pathways. The drug has completed Phase 1 trials in patients with advanced or refractory solid tumors, including breast cancer, and is being developed for further evaluation in ER+ HER2- advanced breast cancer with ESR1 mutations. Originally developed by EMD Serono (a business of Merck KGaA), it is now being advanced by Evexta Bio[1][2][3][5].

Other names

rupitasertib