Drug intelligence / Profile preview

STX213

Development stage
Preclinical
Lead developer
Ipsen
Modality
Small Molecules
Administration
Oral
01

Overview

STX213 is an orally active, second-generation **steroid sulfatase (STS) inhibitor** developed for the treatment of hormone-dependent cancers, including breast and endometrial cancers. It is a D-ring modified steroid-like compound with potent inhibitory activity (IC50 of 0.5 nM) against STS, an enzyme that regulates the conversion of steroid sulfates into active estrogens, thereby reducing estrogenic stimulation of tumors. Preclinical studies in both cell and animal models have shown that STX213 completely inhibits liver and tumor STS activity, reduces plasma estradiol levels, and significantly inhibits the growth of hormone-dependent tumors. Compared to the first-generation compound STX64, STX213 offers enhanced pharmacokinetics and a longer duration of action, maintaining efficacy even with less frequent dosing[1][3][5][7].

Other names
STX213STX-213STX 213
02

Targets

STS (Steroid sulfatase)CA2 (Carbonic Anhydrase 2)

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