TTC-352

TTC-352 is an orally bioavailable, small-molecule selective human estrogen receptor alpha (ERα) partial agonist (ShERPA). It is designed to treat metastatic or hormone-refractory ER-positive breast cancer, particularly in patients who have progressed after at least two lines of hormonal therapy including one with a CDK4/6 inhibitor. TTC-352 mimics the action of 17β-estradiol by binding to ERα in the nucleus and induces tumor regression in resistant cancers while aiming to avoid the gynecologic side effects associated with estradiol. Preclinical studies demonstrated efficacy against tamoxifen-resistant breast cancer models without uterine proliferation. Phase 1 clinical trials showed that TTC-352 is safe and has early evidence of antitumor activity in heavily pretreated patients, with no dose-limiting toxicities observed and a favorable safety profile[1][5][6][7][9][10].

Other names

selective human estrogen receptor alpha partial agonistShERPA