Lasofoxifene
- Atc Codes:G03XC03
- CAS Codes:190791-29-8
- PHARMGKB ID:190791-29-8
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Genes that may be involved
- Substrate of
- Drug Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe (d)
Austria: Fablyn; Bulgaria: Fablyn; Czech Republic: Fablyn; Estonia: Fablyn; Germany: Fablyn; Ireland: Fablyn; Latvia: Fablyn; Lithuania: Fablyn; Malta: Fablyn; Netherlands: Fablyn; Poland: Fablyn; Portugal: Fablyn; Romania: Fablyn; Slovakia: Fablyn; Slovenia: Fablyn; Sweden: Fablyn.
Drug combinations
Chemistry
Lasofoxifene Tartrate: C~32~H~37~NO~8~. Mw: 563.64. (1)(2S,3S)-2,3-dihydroxybutanedioic acid; (5R,6S)-6-phenyl-5-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-5,6,7,8-tetrahydronaphthalen-2-ol; (2)(5R,6S)-5,6,7,8-tetrahydro-6-phenyl-5-[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]-2-naphthalenol (2S,3S)-2,3-dihydroxybutanedioate (1:1). CAS-190791-29-8.
Pharmacologic Category
Hormones and Synthetic Substitutes; Estrogen Agonists-Antagonists. Selective Estrogen Receptor Modulator (SERM). (ATC-Code: G03XC03).
Mechanism of action
Lasofoxifene is a SERM whose biological actions are largely mediated through binding to estrogen receptors. This binding results in the activation of some estrogenic pathways and a blockade of others. Lasofoxifene produces tissue and cell-specific effects in estrogen-responsive tissues. Clinical data indicate that it has an estrogen-like agonist effect on bone as well as antagonistic effects on the breast. Its effects on bone are manifested as reductions in the serum and urine levels of bone turnover markers, increases in bone mineral density (BMD), and decreases in incidence of fractures.
Therapeutic use
Treatment of osteoporosis in postmenopausal women at increased risk of fracture.
Pregnancy and lactiation implications
Only for use in postmenopausal women. Must not be taken by women of child-bearing potential, pregnant or during lactation.
Unlabeled use
Contraindications
Hypersensitivity to the active substance or to any of the excipients. Active or past history of venous thromboembolic events, including deep vein thrombosis, pulmonary embolism and retinal vein thrombosis. Unexplained uterine bleeding. Only for use in postmenopausal women. Must not be taken by women of child-bearing potential, pregnant women or lactating women.
Warnings and precautions
Increased risk of venous thromboembolic events. Lasofoxifene has been associated with benign endometrial effects. Concomitant use with systemic estrogens not recommended. In women with prior history of breast cancer, should be used for the treatment of osteoporosis only after the treatment of breast cancer, including adjuvant therapy, has been completed. Does not eliminate risk of breast cancer. May increase incidence of hot flushes and is not effective in reducing hot flushes associated with estrogen deficiency. In patients with history of oral estrogen-induced hypertriglyceridemia (>5.6 mmol/L), lasofoxifene may be associated with a marked increase in serum triglycerides (monitoring of serum triglycerides is recommended). Lasofoxifene is highly protein-bound, predominantly cleared by metabolism and is likely to undergo enterohepatic circulation (should be used with caution in patients with liver function test >1.5 ULN). Should be used with caution in patients with severe renal insufficiency. Contains lactose (patients with rare hereditary problems of galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicinal product).