Muscle wasting from cancer has a negative impact on the well-being and recovery of millions of patients, especially the elderly.
Drugs called selective androgen receptor modulators (SARMs) offer new hope for these patients. AUSRM-057, a new SARM under development for transdermal administration, promises excellent efficacy without affecting liver function and HDL levels.
This study was presented at the joint meeting of the International Society of Endocrinology and the Endocrine Society (ICE/ENDO 2014) in Chicago, Illinois.
Anabolic steroids are synthetic forms of the male hormones testosterone and dihydrotestosterone. Although they stimulate the growth of muscle and bone, anabolic steroids can cause hypertrophy of the prostate gland. SARMs also stimulate the growth of muscle and bone, but without undesirable side effects on the prostate gland.
Several SARMs have undergone animal testing and are currently in human clinical trials. However, all of these drugs are administered orally. Oral administration of SARMs causes enzyme levels in the liver to increase, and decreases HDL levels (“good” cholesterol). Transdermal drug delivery can overcome these adverse side effects.
“AUSRM-057 is the first SARM with excellent skin permeation properties. This may allow exploitation of the full therapeutic potential of SARMs,” said Hans-Joerg Keller, PhD, senior investigator at the Novartis Institutes for BioMedical Research in Basel, Switzerland.
In this preclinical drug discovery project, researchers identified a compound with high potential as a muscle-building drug in cell culture. Skin permeation tests, also conducted in cell culture, predicted that the drug would show good penetration of the skin during transdermal delivery. The drug worked as predicted when tested in rats, and did not show any of the masculinizing effects of SARMs that can harm the prostate gland.
AUSRM-057 may become the first drug in its class to offer stimulation of muscle growth without the negative impacts on prostate health. And transdermal delivery of this SARM avoids adverse effects on liver function and HDL levels.