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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