RAD140 is an investigational selective androgen receptor modulator (SARM) that is developed by Radius Health, Inc. for use in androgen replacement therapy. It was licensed to Ellipses Pharmaceuticals in 2020.Some of the potential benefits under investigation are for the treatment of conditions such as muscle wasting and bone loss.

Effect

RAD140 is an orally bioavailable, nonsteroidal selective androgen receptor modulator (SARM) that binds to the androgen receptor with a Ki value of 7 nM.1 At 0.03-0.3 mg/kg, it has been shown to stimulate muscle weight increase without affecting prostate or seminal vesicle in castrated male rats.1 At 0.3-1 mg/kg, RAD140 demonstrates partial antagonist activity in seminal vesicle and prostate.

Clinical trials

The first-in-human study was initiated in October of 2017 and completed in September 2020 in postmenopausal women with breast cancer.

In early 2020 a single case report of drug-induced liver injury following use of RAD 140 was published.

Animal studies

RAD 140 appears to be safer than testosterone replacement therapy (TRT) in rats.

RAD 140 slightly increased lean muscle mass when used in primates, by targeting androgen receptors in skeletal tissue.

Side Effects

When taken by mouth: Testolone is possibly unsafe for most people when taken by mouth. Side effects include liver damage, heart attack, stroke, and others.