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Table 3 Effects of selective estrogen receptor modulators on joint tissues

From: Are estrogen-related drugs new alternatives for the management of osteoarthritis?

Drug name Type of study Effects on joint tissues Reference
Tamoxifen In-vivo rabbit with OVX + MMX-OA Reduction of cartilage damage [48]
In-vivo rabbit with MMX-OA Reduction of cartilage damage [46]
In-vivo intact male rabbit with OA Reduction of cartilage damage [47]
In-vivo rabbit with OVX + MMX-OA Antagonism of chondrodestructive effects of high-dose estradiol intraarticular administration [45]
CHPPPC In-vivo Sprague–Dawley rats with OVX Inhibition of the OVX-induced acceleration of bone and cartilage turnover, and suppression of cartilage damage [49]
Levormeloxifene In-vivo Sprague–Dawley rats with OVX Prevention of the OVX-induced cartilage and bone changes [50]
RCT postmenopausal women Decrease of CTX-I I by approximately 50 % [50]
Lasofoxifene In-vivo DBA/1 mice with OVX + arthritis Reduction of the grade of histologic synovitis and erosions on cartilage and bone [51]
Bazedoxifene In-vivo DBA/1 mice with OVX + arthritis Reduction of the grade of histologic synovitis and erosions on cartilage and bone [51]
In-vivo cynomolgus monkeys with OVX Inhibition of OVX-induced vertebral deterioration of structural properties [52]
Prospective study in postmenopausal women with type 2 diabetes Improvement of bone resorption markers [57]
RCT in postmenopausal women with OP Lowered significantly the cumulative incidences of new vertebral fractures and maintained total hip bone mineral density [58]
Exploratory analysis women with increased fracture risk Geometry-related improvements in bone strength [59]
RCT in women with menopausal symptoms Improvement of lumbar spine and total hip BMD [60]
RCT in postmenopausal women with OP Reduction of the incidences of vertebral and nonvertebral fractures [61]
Raloxifene In-vitro rat OA-like chondrocytes Ceases or reduces the matrix degeneration in OA [53]
In-vitro human OA-like chondrocytes Augmented in proteoglycans and a significant decrease of MMP-3 and NO levels [54]
Cross-sectional study in older women with knee OA Less subchondral bone attrition and bone marrow edema-like abnormalities [33]
RCT in postmenopausal women with back or knee pain Amelioration of bone and joint pain [62]
Genistein In-vitro human OA-like chondrocytes Decrease of NO and IL-1β level in supernatant [55]
  1. OA osteoarthritis, OVX ovariectomy, OP osteoporosis, MMX-OA medial meniscectomy-induced OA, CHPPPC cis-3,4-7-hydroxy-3-phenyl-4-(4-(2-pyrrolidinoethox) phenyl)chromane, RCT randomized controlled trial, CTX-II C-terminal cross-linked telopeptide type II collagen, BMD bone mineral density, MMP matrix metalloproteinase, NO nitric oxide