KSHN001126

KSHN001126 is an orally bioavailable prodrug of fulvestrant, developed as a steroidal selective estrogen receptor degrader (SERD). It was designed by exploring multiple estrogen receptor (ER) protein conformations and identifying a subpocket around the core hydrophobic site to enhance oral delivery. The drug acts as an antagonist of estrogen receptors, aiming to block ER signaling in hormone-dependent cancers. Preclinical studies demonstrated that KSHN001126 achieves higher bioavailability compared to subcutaneous fulvestrant, providing a novel strategy for oral administration in patients with advanced metastatic disease. Its primary indication is breast cancer, particularly hormone receptor-positive types[1][2][4].