KSHN001075

KSHN001075 is an orally bioavailable prodrug of fulvestrant, a selective estrogen receptor degrader (SERD), developed by Kashiv BioSciences for the treatment of advanced or metastatic breast cancer. Fulvestrant is typically administered via intramuscular injection due to its poor solubility, low permeability, and high presystemic metabolism. KSHN001075 was designed by appending structurally diverse pro-moieties to fulvestrant to improve its physicochemical and ADME profiles, enabling oral delivery with significantly enhanced bioavailability. In preclinical MCF-7 xenograft models, oral administration of KSHN001075 demonstrated robust antitumor efficacy and tumor volume regression.