The Safety, Pharmacokinetics, and Effects of LGD-4033, a Novel Nonsteroidal Oral, Selective Androgen Receptor Modulator, in Healthy Young Men

Basaria, Shehzad; Collins, Lauren F; Dillon, E. Lichar; Orwoll, Katie; Storer, Thomas W.; Miciek, Renee; Ulloor, Jagadish; Zhang, Anqi; Eder, Richard; Zientek, Heather; Gordon, Gilad; Kazmi, Syed Jamil Hasan; Sheffield‐Moore, Melinda; Bhasin, Shalender

doi:10.1093/gerona/gls078

Cited by 127 publications

(138 citation statements)

References 39 publications

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“…Virilisation was not noted in any of the patients (96) . A novel class of drugs, selective androgen receptor modulators, has recently received tremendous research endeavour for their ability to increase muscle mass in clinical studies; however, their effects on musle strength or exercise capacity are not yet convincing (97)(98)(99)(100)(101) . Studies in HF are not available.…”

Section: Treatment Approaches To Wasting In Heart Failurementioning

confidence: 99%

The wasting continuum in heart failure: from sarcopenia to cachexia

Haehling

2015

Proc. Nutr. Soc.

104

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Conference on 'Nutrition and age-related muscle loss, sarcopenia and cachexia' Symposium 2: Mechanisms for loss of muscle mass, strength and clinical measurement of malnutrition and cachexiaThe wasting continuum in heart failure: from sarcopenia to cachexiaStephan von Haehling Sarcopenia (muscle wasting) and cachexia share some pathophysiological aspects.Sarcopenia affects approximately 20 %, cachexia <10 % of ambulatory patients with heart failure (HF). Whilst sarcopenia means loss of skeletal muscle mass and strength that predominantly affects postural rather than non-postural muscles, cachexia means loss of muscle and fat tissue that leads to weight loss. The wasting continuum in HF implies that skeletal muscle is lost earlier than fat tissue and may lead from sarcopenia to cachexia. Both tissues require conservation, and therapies that stop the wasting process have tremendous therapeutic appeal. The present paper reviews the pathophysiology of muscle and fat wasting in HF and discusses potential treatments, including exercise training, appetite stimulants, essential amino acids, growth hormone, testosterone, electrical muscle stimulation, ghrelin and its analogues, ghrelin receptor agonists and myostatin antibodies.

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Section: Treatment Approaches To Wasting In Heart Failurementioning

confidence: 99%

The wasting continuum in heart failure: from sarcopenia to cachexia

Haehling

2015

Proc. Nutr. Soc.

104

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“…Clinical studies of these SARMs are focused on the correction of sarcopenia in elderly, patients with chronic diseases and cancer cachexia [140,141] and not for androgen replacement therapy. Use of these agents for treatment of hypogonadism is not a priority for development for many of these new agents.…”

Section: Options For Testosterone Replacement Therapymentioning

confidence: 99%

An update on male hypogonadism therapy

Surampudi

Swerdloff

Wang

2014

Expert Opinion on Pharmacotherapy

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Introduction Men who have symptoms associated with persistently low serum total testosterone level should be assessed for testosterone replacement therapy. Areas covered Acute and chronic illnesses are associated with low serum testosterone and these should be recognized and treated. Once the diagnosis of male hypogonadism is made, the benefits of testosterone treatment usually outweigh the risks. Without contraindications, the patient should be offered testosterone replacement therapy. The options of testosterone delivery systems (injections, transdermal patches/gels, buccal tablets, capsules and implants) have increased in the last decade. Testosterone improves symptoms and signs of hypogonadism such as sexual function and energy, increases bone density and lean mass and decreases visceral adiposity. In men who desire fertility and who have secondary hypogonadism, testosterone can be withdrawn and the patients can be placed on gonadotropins. New modified designer androgens and selective androgen receptor modulators have been in preclinical and clinical trials for some time. None of these have been assessed for the treatment of male hypogonadism. Expert opinion Despite the lack of prospective long-term data from randomized, controlled clinical trials of testosterone treatment on prostate health and cardiovascular disease risk, the available evidence suggests that testosterone therapy should be offered to symptomatic hypogonadal men.

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“…The phase I trial showed an increase in muscle mass in a short period, with no effect on fat mass. 65) Enobosarm (GTx-024) is an orally bioavailable non-steroidal SARM. The use of enobosarm led to significant improvements in lean body mass and physical function in a phase II, double-blind, placebo-controlled studies both in healthy elderly adults and in cancer patients.…”

Section: )mentioning

confidence: 99%

Current Status of Sarcopenia in Korea: A Focus on Korean Geripausal Women

Park¹

2018

Ann Geriatr Med Res

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Sarcopenia is defined as an age-associated decline in muscle mass and function caused by several etiologies and mechanisms. Muscle mass and function do not decrease concurrently, and a loss of muscle function may be more highly associated with adverse health outcomes. Despite the clinical significance of sarcopenia, no universally operational definition of sarcopenia or standardized intervention programs are currently available. Sarcopenia, osteoporosis, and obesity share several pathophysiological mechanisms, and a combination of these entities may lead to an increased risk of musculoskeletal, cardio-metabolic, and psychological morbidities especially in geripause populations. Treatment for sarcopenia is mainly nonpharmacological, however, various drugs are currently being developed. It is conceivable that sarcopenia is the next immediate clinical target in musculoskeletal science.

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The Safety, Pharmacokinetics, and Effects of LGD-4033, a Novel Nonsteroidal Oral, Selective Androgen Receptor Modulator, in Healthy Young Men

Abstract: LGD-4033 was safe, had favorable pharmacokinetic profile, and increased lean body mass even during this short period without change in prostate-specific antigen. Longer randomized trials should evaluate its efficacy in improving physical function and health outcomes in select populations.

Cited by 127 publications

References 39 publications

The wasting continuum in heart failure: from sarcopenia to cachexia

The wasting continuum in heart failure: from sarcopenia to cachexia

An update on male hypogonadism therapy

Current Status of Sarcopenia in Korea: A Focus on Korean Geripausal Women

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