RAD140

개요RAD140 (also known as Testolone) is an oral nonsteroidal selective androgen receptor modulator (SARM) that cannot be converted to estrogen by aromatase. It has been demonstrated that RAD140 has high AR affinity and target selectivity, showing marked tissue-selective AR agonist activity comparable to natural androgens in breast cancer cells, while lacking agonist activity in prostate cancer cells.We have recently reported anti-tumor activity of RAD140 in multiple in vivo and in vitro models of AR/ER+ breast cancer as a single agent and in combination with inhibitors of CDK4/6 and mTOR.Pharmacodynamic investigation indicates RAD140 acted as an AR agonist in breast cancer cells while suppressing ER signaling and reduced ESR1 mRNA expression.RAD140 exhibited anti-tumor activity in patient-derived xenograft (PDX) models of AR/ER+ breast cancer, as single agent and in combination with inhibitors of CDK4/6 or mTORRAD140 inhibited ER signaling and ESR1 mRNA level in the HBCx-22 PDX model.

용도RAD140 is a potent, orally bio-available, and non-steroidal selective androgen receptor modulator (SARM) for the treatment of conditions such as muscle wasting and breast cancer.