RESEARCH CHEMICAL CLINICAL TRIALS

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GW-501516

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

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LGD-4033

Pharmacokinetics Study

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.

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LGD-4033

Cachexia Treatment

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.

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MK-677

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.

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MK-677

7-day Treatment Effects

To assess the
of GH-releasing
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
days. A

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MK-2866

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.

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RAD-140

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.

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RAD-140

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.

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SARMs

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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