RAD140 (RAD-140, Vosilasarm) is a potent, orally bioavailable, nonsteroidal selective androgen receptor modulator (SARM), shows excellent affinity for the androgen receptor (Ki=7 nM).
RAD140 displays good selectivity over other steroid hormone nuclear receptors, with the closest off target receptor being the progesterone receptor.
RAD140 exhibits in vitro functional androgen agonist activity with EC50 of 0.1 nM in the C2C12 osteoblast differentiation assays.
RAD140 stimulates muscle weight increases at a lower dose than that required to stimulate prostate weight increases in vivo.
Oral administration of RAD140 substantially inhibited the growth of AR/ER+ breast cancer patient-derived xenografts (PDX).
Coadministration of RAD140 and palbociclib showed improved efficacy in the AR/ER+ PDX models.
