Overview of the development of selective androgen receptor modulators (SARMs) as pharmacological treatment for osteoporosis (1998–2021)

Xie, Youquan; Tian, Yucheng; Zhang, Yuming; Zhang, Zhisheng; Chen, Rui; Li, Mian; Tang, Jia-Wei; Bian, Jinlei; Li, Zhiyu; Xu, Xi

doi:10.1016/j.ejmech.2022.114119

Cited by 13 publications

(8 citation statements)

References 134 publications

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“…To date, osteoporosis prevention and treatment remains a challenge. Primary osteoporosis has been treated with hormone replacement therapy and selective androgen receptor modulators (SARMs), but long-term use has been associated with increased rates of heart disease, stroke, and breast cancer and prostate cancer ( 219 ). Currently, bisphosphonates are recommended as the clinical first-line treatment for osteoporosis (primary and secondary) ( 220 ).…”

Section: Discussionmentioning

confidence: 99%

Osteoporosis: interferon-gamma-mediated bone remodeling in osteoimmunology

Li,

Liu,

2024

Front. Immunol.

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As the world population ages, osteoporosis, the most common disease of bone metabolism, affects more than 200 million people worldwide. The etiology is an imbalance in bone remodeling process resulting in more significant bone resorption than bone remodeling. With the advent of the osteoimmunology field, the immune system’s role in skeletal pathologies is gradually being discovered. The cytokine interferon-gamma (IFN-γ), a member of the interferon family, is an important factor in the etiology and treatment of osteoporosis because it mediates bone remodeling. This review starts with bone remodeling process and includes the cellular and key signaling pathways of bone remodeling. The effects of IFN-γ on osteoblasts, osteoclasts, and bone mass are discussed separately, while the overall effects of IFN-γ on primary and secondary osteoporosis are summarized. The net effect of IFN-γ on bone appears to be highly dependent on the environment, dose, concentration, and stage of cellular differentiation. This review focuses on the mechanisms of bone remodeling and bone immunology, with a comprehensive discussion of the relationship between IFN-γ and osteoporosis. Finding the paradoxical balance of IFN-γ in bone immunology and exploring the potential of its clinical application provide new ideas for the clinical treatment of osteoporosis and drug development.

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Section: Discussionmentioning

confidence: 99%

Osteoporosis: interferon-gamma-mediated bone remodeling in osteoimmunology

Li,

Liu,

2024

Front. Immunol.

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“…In bone-related disorder treatment especially osteoporosis, many researchers have focused on the ability to selectively modulate the receptors, which led to the preferable drug targets including SERMs (Clarke, 2020) and selective AR modulators (SARMs) that target steroid receptors (Solomon et al, 2019;Xie et al, 2022), selective PPAR modulators that aim at the non-steroid receptor (Liu et al, 2015;Marciano et al, 2015), and selective NR modulators (Sturm's) that target orphan receptors (Gallet and Vanacker, 2010;Kim et al, 2019;Zuo and Wan, 2017). Selective drug targets can be discovered by activating specific NRs with a specific set of target genes initiated by a specific ligand, which causes allosteric conformational changes in the NR.…”

Section: Roles Of Nrs In Bone Remodelingmentioning

confidence: 99%

The potential effects of isoflavones on nuclear receptor modulation in bone remodeling: A review

Hairi¹,

Mustafa²,

Jayusman³

et al. 2023

J App Pharm Sc

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Isoflavones are plant-based compounds that act as phytoestrogens by mimicking the action of estrogen. Osteoblasts and osteoclasts are the key cells for bone remodeling, a process that includes bone proliferation, differentiation, deposition, and resorption. Studies have demonstrated that isoflavones, a class of flavonoids found almost exclusively in soybeans, could prevent bone loss. Recent findings revealed that isoflavones could activate nuclear receptors (NRs) and regulate bone formation and resorption processes. This current research discussed the principal actions of isoflavones mediated by NRs on bone remodeling such as steroid receptors (estrogen receptor, estrogen-related receptor, and androgen receptor) and metabolic receptors including peroxisome proliferator-activated receptor-γ. Isoflavones modulate osteogenesis by fine-tuning physiological responses on NR sensors and their transcriptional networks. Hence, this present review will dive deep into the use of several isoflavones as potential osteoporosis treatment through NR-controlling gene regulation.

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“…Despite these positive findings, there is still insufficient evidence to support routine use of this treatment in older adults with T2DM without pathological hypogonadism [205,207]. To overcome adverse androgenic/virilising Diabetes Metab J 2023;47:719-742 https://e-dmj.org side effects associated with testosterone [208,209], selective androgen receptor modulators (SARMs) have been developed to stimulate anabolic effects in skeletal muscle and other tissues (e.g., bone) while minimising adverse effects on other tissues (e.g., prostate) [210,211]. Only one study has explored the effects of a SARM in a population with sarcopenia [212].…”

Section: Medicationsmentioning

confidence: 99%

Type 2 Diabetes Mellitus and Sarcopenia as Comorbid Chronic Diseases in Older Adults: Established and Emerging Treatments and Therapies

Mesinovic,

Fyfe,

Talevski

et al. 2023

Diabetes Metab J

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Type 2 diabetes mellitus (T2DM) and sarcopenia (low skeletal muscle mass and function) share a bidirectional relationship. The prevalence of these diseases increases with age and they share common risk factors. Skeletal muscle fat infiltration, commonly referred to as myosteatosis, may be a major contributor to both T2DM and sarcopenia in older adults via independent effects on insulin resistance and muscle health. Many strategies to manage T2DM result in energy restriction and subsequent weight loss, and this can lead to significant declines in muscle mass in the absence of resistance exercise, which is also a first-line treatment for sarcopenia. In this review, we highlight recent evidence on established treatments and emerging therapies targeting weight loss and muscle mass and function improvements in older adults with, or at risk of, T2DM and/or sarcopenia. This includes dietary, physical activity and exercise interventions, new generation incretin-based agonists and myostatin-based antagonists, and endoscopic bariatric therapies. We also highlight how digital health technologies and health literacy interventions can increase uptake of, and adherence to, established and emerging treatments and therapies in older adults with T2DM and/or sarcopenia.

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Overview of the development of selective androgen receptor modulators (SARMs) as pharmacological treatment for osteoporosis (1998–2021)

Cited by 13 publications

References 134 publications

Osteoporosis: interferon-gamma-mediated bone remodeling in osteoimmunology

Osteoporosis: interferon-gamma-mediated bone remodeling in osteoimmunology

The potential effects of isoflavones on nuclear receptor modulation in bone remodeling: A review

Type 2 Diabetes Mellitus and Sarcopenia as Comorbid Chronic Diseases in Older Adults: Established and Emerging Treatments and Therapies

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