The use of raloxifene<b>in osteoporosis treatment</b>

D’Amelio, Patrizia; Isaia, Giovanni Carlo

doi:10.1517/14656566.2013.782002

Cited by 57 publications

(31 citation statements)

References 64 publications

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“…Tamoxifen, a first generation SERM, provided the desired protective effect in the breast [31,32] and raloxifene, a second generation SERM, had protective properties in breast and bone tissues [26,27,103]. However, as these SERMS have been linked to the increased occurrence of hot flashes and stimulated endometrial growth (tamoxifen), the search continues [28,34,35]. Third generation SERMs, such as lasoxifene and bazedoxifene, are currently in development, but the focus has shifted to osteoporosis treatment with protection against breast cancer as a beneficial side effect [104-106].…”

Section: Discussionmentioning

confidence: 99%

“…This attribute is beneficial in bone [18,20,21] and for hot flashes [18,21], but detrimental in the breast [6,21,22] and uterus [21,23] as it increases the risk of tumorigenesis. In contrast, the selective estrogen receptor modulators (SERMs), although not ER subtype specific [24,25], act as agonists in certain tissues, such as bone [26-28], and as antagonists in others, such as breast [9,10,29]. Although, the well-known SERMs, raloxifene and tamoxifen [30], have been shown to decrease the risk of breast cancer [18,31,32] and increase bone mineral density [26-28,33], they have also been linked to an increased risk of venous thromboembolism and occurrence of hot flashes, and can stimulate endometrial growth [28,34-36].…”

Section: Introductionmentioning

confidence: 99%

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Cyclopia Extracts Act as ERα Antagonists and ERβ Agonists, In Vitro and In Vivo

2013

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Hormone replacement therapy associated risks, and the concomitant reluctance of usage, has instigated the search for new generations of estrogen analogues that would maintain estrogen benefits without associated risks. Furthermore, if these analogues display chemo-preventative properties in breast and endometrial tissues it would be of great value. Both the selective estrogen receptor modulators as well as the selective estrogen receptor subtype modulators have been proposed as estrogen analogues with improved risk profiles. Phytoestrogen containing extracts of Cyclopia, an indigenous South African fynbos plant used to prepare Honeybush tea may serve as a source of new estrogen analogues. In this study three extracts, P104, SM6Met, and cup-of-tea, from two species of Cyclopia, C. genistoides and C. subternata, were evaluated for ER subtype specific agonism and antagonism both in transactivation and transrepression. For transactivation, the Cyclopia extracts displayed ERα antagonism and ERβ agonism when ER subtypes were expressed separately, however, when co-expressed only agonism was uniformly observed. In contrast, for transrepression, this uniform behavior was lost, with some extracts (P104) displaying uniform agonism, while others (SM6Met) displayed antagonism when subtypes were expressed separately and agonism when co-expressed. In addition, breast cancer cell proliferation assays indicate that extracts antagonize cell proliferation in the presence of estrogen at lower concentrations than that required for proliferation. Furthermore, lack of uterine growth and delayed vaginal opening in an immature rat uterotrophic model validates the ERα antagonism of extracts observed in vitro and supports the potential of the Cyclopia extracts as a source of estrogen analogues with a reduced risk profile.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Cyclopia Extracts Act as ERα Antagonists and ERβ Agonists, In Vitro and In Vivo

2013

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“…Taken together, the overall metabolic, cardiovascular, and neuronal actions of RAL we can enunciate its clinical importance (Figure 3.). Numerous studies have already confirmed its pivotal role in the prevention of osteoporosis [58][59][60]; however, in this review, we approached its cardiometabolic and neuroprotective impacts. It has been shown that RAL has a potential therapeutic perspective in the moderation of obesity, dyslipidemia, and endothelial dysfunction thus on reducing the occurrence of atherosclerotic processes.…”

Section: Discussionmentioning

confidence: 99%

Distinct Approaches of Raloxifene: Its Far-Reaching Beneficial Effects Implicating the HO-System

et al. 2020

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Selective estrogen receptor modulators (SERMs) were discovered in the mid-1900s in connection with estrogen-related pathological conditions. They were developed to antagonize the adverse effects of estrogen and have been shown to be effective against postmenopausal disorders manifested by estrogen deficiency. Raloxifene (RAL), one of the most widely used SERMs, expresses estrogen-like effects on bones, while it is found to be an antagonist on breast and uterus. RAL has multiple beneficial effects throughout the body, including antioxidant and anti-inflammatory properties, because of which it gains particular attention. Additionally, previous studies have revealed that RAL is an efficient modulator of heme-oxygenase (HO) expression. HO, through its general activity, participates in comprehensive cell defense processes, thus the induction of HO by RAL administration indicates a major role in its therapeutic efficacy. In this review, we compile the current knowledge about the overall metabolic, neurocognitive, and cardiovascular effects of RAL involving the cytoprotective HO-system.

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“…Anti-resorptive drugs decrease the excess of bone resorption by targeting osteoclast activity. Examples of these compounds include bisphosphonates [198], raloxifene [199] or denosumab [200]. The excess of bone resorption can be counteracted using anabolic agents, which are compounds able to stimulate bone formation.…”

Section: General Concepts On Osteoporosismentioning

confidence: 99%

Mesoporous Silica Nanoparticles for the Treatment of Complex Bone Diseases: Bone Cancer, Bone Infection and Osteoporosis

2020

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Bone diseases, such as bone cancer, bone infection and osteoporosis, constitute a major issue for modern societies as a consequence of their progressive ageing. Even though these pathologies can be currently treated in the clinic, some of those treatments present drawbacks that may lead to severe complications. For instance, chemotherapy lacks great tumor tissue selectivity, affecting healthy and diseased tissues. In addition, the inappropriate use of antimicrobials is leading to the appearance of drug-resistant bacteria and persistent biofilms, rendering current antibiotics useless. Furthermore, current antiosteoporotic treatments present many side effects as a consequence of their poor bioavailability and the need to use higher doses. In view of the existing evidence, the encapsulation and selective delivery to the diseased tissues of the different therapeutic compounds seem highly convenient. In this sense, silica-based mesoporous nanoparticles offer great loading capacity within their pores, the possibility of modifying the surface to target the particles to the malignant areas and great biocompatibility. This manuscript is intended to be a comprehensive review of the available literature on complex bone diseases treated with silica-based mesoporous nanoparticles—the further development of which and eventual translation into the clinic could bring significant benefits for our future society.

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The use of raloxifenein osteoporosis treatment

Cited by 57 publications

References 64 publications

Cyclopia Extracts Act as ERα Antagonists and ERβ Agonists, In Vitro and In Vivo

Cyclopia Extracts Act as ERα Antagonists and ERβ Agonists, In Vitro and In Vivo

Distinct Approaches of Raloxifene: Its Far-Reaching Beneficial Effects Implicating the HO-System

Mesoporous Silica Nanoparticles for the Treatment of Complex Bone Diseases: Bone Cancer, Bone Infection and Osteoporosis

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