AFP-464 + fulvestrant

AFP-464 + fulvestrant is an investigational combination therapy studied primarily for estrogen receptor-positive (ER+) breast cancer. AFP-464 is a lysyl prodrug of aminoflavone that acts as a novel antitumor agent by activating the aryl hydrocarbon receptor (AhR) signaling pathway. Upon activation, it is metabolized to compounds that covalently bind DNA, leading to p53 activation and apoptosis in tumor cells. Preclinical studies have shown its cytotoxicity against various tumor cell lines—especially those from breast, ovarian, lung, and renal cancers—and its ability to modulate the immune response by reducing immunosuppressive cells and promoting a pro-inflammatory macrophage phenotype[3][6][7][9]. Fulvestrant is an estrogen receptor antagonist used in hormone-receptor positive advanced or metastatic breast cancer; it binds competitively to estrogen receptors and accelerates their degradation[8]. The combination was evaluated in phase 2 clinical trials for ER+ breast cancer patients with the aim of overcoming endocrine resistance[1][2][3].

Brand names

Faslodex

Other names

aminoflavone + fulvestrantAFP464 + Faslodex