Rintodestrant

Rintodestrant is an orally bioavailable selective [estrogen receptor degrader] discovered in Greg Thatcher's lab at UIC and developed by G1 Therapeutics for the treatment of estrogen receptor-positive breast cancer. Structurally inspired by the 6-OH-benzothiophene scaffold used in arzoxifene and raloxifene, rintodestrant selectively binds to the estrogen receptor and inhibits ER signaling, demonstrating efficacy in endocrine-resistant tumors.
A phase I clinical trial evaluated rintodestrant as monotherapy and in combination with the CDK4/6 inhibitor palbociclib in patients with ER+/HER2- advanced breast cancer.