Amcenestrant is an investigational selective estrogen receptor degrader (SERD) being developed primarily for the treatment of estrogen receptor-positive (ER+) breast cancer. It works by binding to estrogen receptors in breast cancer cells and promoting their degradation, thereby inhibiting estrogen-driven tumor growth. This mechanism makes it particularly useful in postmenopausal women and others with advanced or metastatic ER+ breast cancer who may have become resistant to other endocrine therapies such as aromatase inhibitors or selective estrogen receptor modulators (SERMs). One of the key advantages of amcenestrant is its oral bioavailability, allowing for convenient daily dosing compared to injectable SERDs. It has shown promise in clinical trials, both as a monotherapy and in combination with other targeted agents like CDK4/6 inhibitors, potentially enhancing antitumor activity. Due to its targeted action, it may offer a favorable safety profile with fewer systemic hormonal side effects compared to traditional hormone therapies. Ongoing research continues to evaluate its efficacy, optimal dosing, and long-term benefits in various stages of ER+ breast cancer.