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The Study of Drug Metabolism Using Radiotracers
Published in Graham Lappin, Simon Temple, Radiotracers in Drug Development, 2006
[14C]-levormeloxifene (a partial estrogen agonist, used as an alternative to estrogen replacement therapy) was administered to the rat, Cynomolgus monkey, and postmenopausal women.43,44 The position of the 14C label was not stated. The six human volunteers were orally dosed 25 μCi (approximately 1 MBq) of radioactivity. Although not specifically stated, dosimetry studies would have been necessary to justify this dose in humans (Chapter 5, Appendix 1). The dose was administered as a 20-mL drinking solution. Oral administrations were also given to normal and bile duct-cannulated male and female rats, by gavage. One female rat was dosed into the stomach, with bile collected from another animal administered [14C]-levormeloxifene. Male and female Cynomolgus monkeys were administered [14C]-levormeloxifene by stomach tube. In all species, blood, urine and feces were collected (plus bile from bile duct-cannulated rats). All excreta were analyzed for total radioactivity by liquid scintillation counting.
Pharmacotherapeutic considerations and options for the management of osteoarthritis in women
Published in Expert Opinion on Pharmacotherapy, 2020
Sunny Trivedi, William Fang, Ishan Ayyalasomayajula, C. Thomas Vangsness
Another emerging field of pharmacological therapy for OA is hormonal treatment. Estrogen has been shown to play a role in bone growth and development [142]. Although multiple studies link estrogen deficiency to the development of Osteoarthritis [38], currently, there is insufficient research into the mechanism of involvement of estrogen in the disease development [143]. Research has shown that post-menopausal women who underwent hormone therapy were at reduced risk for osteoarthritis [143]. Further investigations of the pathophysiology of estrogen in osteoarthritis are necessary to improve treatment options specific to women. In recent years, there have been clinical studies testing the efficacy of estrogen and selective estrogen receptor modulators (SERMs) on treating OA. Studies testing the effects of estrogen on OA treatment have produced inconclusive results [143]. In these studies, estrogen has been shown to prevent joint degradation in OA patients as well as having negative effects on OA. Previous work has indicated that SERMs have dual agonist and antagonist effects in various tissues. Low doses of SERMs have been shown to affect chondrocytes, resulting in increased extracellular matrix deposition and increased resistance to damage [143]. Specifically, bazedoxifene has been shown to reduce bone loss and maintain bone mass density by reducing bone breakdown in post-menopausal women. Similarly, recent research indicates that levormeloxifene reduced cartilage degeneration [143].