Tibolone inhibits bone resorption without secondary positive effects on cartilage degradation.
BACKGROUND
Osteoarthritis is associated with increased bone resorption and increased cartilage degradation in the subchondral bone and joint. The objective of the present study was to determine whether Tibolone, a synthetic steroid with estrogenic, androgenic, and progestogenic properties, would have similar dual actions on both bone and cartilage turnover, as reported previously with some SERMS and HRT.


METHODS
This study was a secondary analysis of ninety-one healthy postmenopausal women aged 52-75 yrs entered a 2-yr double blind, randomized, placebo-controlled study of treatment with either 1.25 mg/day (n = 36), or 2.5 mg/day Tibolone (n = 35), or placebo (n = 20), (J Clin Endocrinol Metab. 1996 Jul;81(7):2419-22) Second void morning urine samples were collected at baseline, and at 3, 6, 12, and 24 months. Urine CrossLaps ELISA (CTX-I) and Urine CartiLaps ELISA (CTX-II) was investigated as markers of bone resorption and cartilage degradation, respectively.


RESULTS
Tibolone significantly (P < 0.001) suppressed bone resorption by approximately 60%. In contrast, no effect was observed on cartilage degradation.


CONCLUSIONS
These data suggest uncoupling of the bone and cartilage effects of the synthetic steroid, Tibolone. Bone resorption was significantly decreased, whereas cartilage degradation was unchanged. These effects are in contrast to those observed some SERMs with effects on both bone and cartilage degradation. These effects may in part be described by the complicated pharmacology of Tibolone on testosterone, estrogen and progesterone receptors.
Karsdal
M A
MA
Nordic Bioscience A/S, Herlev, Denmark. mk@nordicbioscience.com
Byrjalsen
I
I
Leeming
D J
DJ
Christiansen
C
C
D000368:Aged; D001862:Bone Resorption / Q000188:drug therapy* / Q000378:metabolism; D001842:Bone and Bones / Q000187:drug effects / Q000378:metabolism*; D002358:Cartilage, Articular / Q000187:drug effects / Q000378:metabolism*; D024161:Collagen Type XI / Q000652:urine; D024082:Collagen Type XII / Q000652:urine; D004305:Dose-Response Relationship, Drug; D004311:Double-Blind Method; D020847:Estrogen Receptor Modulators / Q000494:pharmacology / Q000627:therapeutic use*; D005260:Female; D006801:Humans; D008137:Longitudinal Studies; D008875:Middle Aged; D009652:Norpregnenes / Q000494:pharmacology / Q000627:therapeutic use*; D011944:Receptors, Androgen / Q000187:drug effects; D011960:Receptors, Estrogen / Q000187:drug effects; D011980:Receptors, Progesterone / Q000187:drug effects
D024161:Collagen Type XI; D024082:Collagen Type XII; D020847:Estrogen Receptor Modulators; D009652:Norpregnenes; D011944:Receptors, Androgen; D011960:Receptors, Estrogen; D011980:Receptors, Progesterone; C027385:tibolone