Use of Rapamycin and Rapamycin Derivatives for the Treatment of Bone Loss
OwnerMichaela Kneissel, Mira Susa Springinventors
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Abstract
The present invention relates to a new use of rapamycin and rapamycin derivatives.
Claims10
A method for treating abnormally increased bone turnover or resorption in a subject in need thereof, comprising administering to said subject a therapeutically effective amount of a rapamycin derivative of formula I
- wherein
- R1 is CH3 or C3-6alkynyl,
- R2 is H or —CH2—CH2—OH, 3-hydroxy-2-(hydroxymethyl)-2-methyl-propanoyl or tetrazolyl, and
- X is ═O, (H,H) or (H,OH),
- provided that R2 is other than H when X is ═O and R1 is CH3,
- or a prodrug thereof when R2 is —CH2—CH2—OH, e.g. a physiologically hydrolysable ether thereof.
A method for treating abnormally increased bone turnover or resorption in a subject in need thereof, comprising administering to said subject a therapeutically effective amount of rapamycin or a rapamycin derivative, concomitantly or sequentially with a second drug selected from bone resorption inhibitor, a calcitonin or an analogue or derivative thereof;
- a steroid hormone, a partial estrogen agonist or estrogen-gestagen combination;
- a selective estrogen receptor modulator;
- vitamin D or an analogue thereof;
- Parathyroid Hormone (PTH), a PTH fragment or a PTH derivative;
- a bisphosphonate;
- a cathepsin K inhibitor;
- a PTH releaser;
- a selective androgen receptor molecule;
- and strontium ranelate.
A method for the treatment of osteoporosis;
- bone loss secondary to or due to medication;
- bone loss associated with immobilisation and space flight;
- bone loss associated with rheumatoid arthritis, osteopenia, osteogenesis imperfecta, hyperthyroidism, anorexia nervosa, organ transplantation, joint prosthesis loosening;
- periarticular bone erosions in rheumatoid arthritis;
- osteoarthritis;
- hypercalcemia;
- bone cancer and bone metastases;
- and/or multiple myeloma, in a subject in need thereof, comprising administering to said subject a therapeutically effective amount of rapamycin or a rapamycin derivative of formula I
- wherein
- R1 is CH3 or C3-6alkynyl,
- R2 is H or —CH2—CH2—OH, 3-hydroxy-2-(hydroxymethyl)-2-methyl-propanoyl or tetrazolyl, and
- X is ═O, (H,H) or (H,OH),
- provided that R2 is other than H when X is ═O and R1 is CH3,
- or a prodrug thereof when R2 is —CH2—CH2—OH, e.g. a physiologically hydrolysable ether thereof,
- concomitantly or sequentially with a second drug selected from bone resorption inhibitor, a calcitonin or an analogue or derivative thereof;
- a steroid hormone, a partial estrogen agonist or estrogen-gestagen combination;
- a selective estrogen receptor modulator;
- vitamin D or an analogue thereof;
- Parathyroid Hormone (PTH), a PTH fragment or a PTH derivative;
- a bisphosphonate;
- a cathepsin K inhibitor;
- a PTH releaser;
- a selective androgen receptor molecule;
- and strontium ranelate.
Dependencies are inferred from the claim text.