RESEARCH CHEMICAL CLINICAL TRIALS
Lipid Metabolism Study
The Peroxisome Proliferator-Activated Receptor β/δ Agonist, GW501516, Regulates the Expression of Genes Involved in Lipid Catabolism and Energy Uncoupling in Skeletal Muscle Cells
Concerns about potential adverse effects of testosterone on prostate have motivated the development of
selective androgen receptor modulators that display tissue-selective activation of androgenic signaling. LGD-4033, a
novel non-steroidal, oral selective androgen receptor modulator, binds androgen receptor with high affinity and selectivity.
The term cachexia embraces a complex metabolic syndrome
characterized by loss of body weight that may develop as a
consequence of loss of muscle mass with or without loss of
fat mass. LGD-4033 is currently undergoing trials to treat this syndrome.
IGF-1 Stimulation Study
Aging is associated with declining activity of the GH axis, possibly contributing to adverse body composition changes and increased incidence of cardiovascular disease. The stimulatory effects on the GHinsulin-like growth factor I (IGF-11 axis of orally administered MK-677, a GH-releasing peptide mimetic, were investigated.
7-day Treatment Effects
To assess the
effects of prolonged administration of a novel analog
peptide (MK-6771, nine healthv voune men narticipated
in a randomized, double blind, three-periodcros~over cbmparison
of orally administered placebo and 5- and 25-mg doses of MK-677.
Each period involved bedtime administration of the drug for 7 consecutive
Androgen Receptor / SARMs efficacy
Androgen receptor (AR) plays a critical role in the function of several organs including primary and accessory
sexual organs, skeletal muscle, and bone, making it a desirable therapeutic target. Selective androgen receptor
modulators (SARMs) bind to the AR and demonstrate osteo- and myo-anabolic activity; however, unlike
testosterone and other anabolic steroids, these nonsteroidal agents produce less of a growth effect on prostate
and other secondary sexual organs.
Design, Synthesis, and Characterization of RAD140
This report describes the discovery of RAD140, a potent, orally
bioavailable, nonsteroidal selective androgen receptor modulator (SARM). The
characterization of RAD140 in several preclinical models of anabolic androgen
action is also described.
RAD140 Is Neuroprotective
The decline in testosterone levels in men during normal aging increases risks of dysfunction and
disease in androgen-responsive tissues, including brain. The use of testosterone therapy has the
potential to increase the risks for developing prostate cancer and or accelerating its progression.
SARMs and Physical Function
The last decade has witnessed unprecedented discovery effort to develop
selective androgen receptor modulators (SARMs) that improve physical function and bone health
without adversely affecting the prostate and cardiovascular outcomes. This review describes the
historical evolution, the rationale for SARM development, and the mechanisms of testosterone
action and SARM selectivity.
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