Bazedoxifene
Bazedoxifene Uses, Dosage, Side Effects, Food Interaction and all others data.
Bazedoxifene is a third generation selective estrogen receptor modulator (SERM), developed by Pfizer following the completion of their takeover of Wyeth Pharmaceuticals. In late 2013, Pfizer received approval for bazedoxifene as part of the combination drug DUAVEE in the prevention (not treatment) of postmenopausal osteoporosis. It is approved in the European Union (marketed in Italy and Spain) and Japan as monotherapy. In 2013, the combination product containing conjugated estrogens and bazedoxifene was approved by the FDA for the treatment of moderate to severe vasomotor symptoms associated with menopause, as well as the prevention of postmenopausal osteoporosis in women.
| Trade Name | Bazedoxifene |
| Generic | Bazedoxifene |
| Bazedoxifene Other Names | Bazedoxifene, Bazedoxifeno |
| Type | |
| Formula | C30H34N2O3 |
| Weight | Average: 470.613 Monoisotopic: 470.256942963 |
| Protein binding | 98-99%. |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Bazedoxifene is a selective estrogen receptor modulator (SERM) used to treat moderate to severe vasomotor symptoms in menopause and osteoporosis alone or in combination with conjugated estrogens.
Indicated for following conditions alone or in combination with conjugated estrogens in women with a uterus:
Treatment of moderate to severe vasomotor symptoms associated with menopause
Prevention of postmenopausal osteoporosis
Bazedoxifene is also used to associated treatment for these conditions: Postmenopausal Osteoporosis, Moderate Menopausal Vasomotor Symptoms, Severe Vasomotor Symptoms Associated With Menopause
How Bazedoxifene works
Bazedoxifene belongs to a class of compounds known as selective estrogen receptor modulators (SERMs). Bazedoxifene acts as both an oestrogen-receptor agonist and/or antagonist, depending upon the cell and tissue type and target genes. Bazedoxifene decreases bone resorption and reduces biochemical markers of bone turnover to the premenopausal range. These effects on bone remodelling lead to an increase in bone mineral density (BMD), which in turn contributes to a reduction in the risk of fractures. Bazedoxifene functions primarily as an oestrogen-receptor antagonist in uterine and breast tissues.
Food Interaction
- Administer calcium supplement. If calcium intake from food is inadequate administer calcium supplements to prevent hypocalcemia.
- Administer vitamin supplements. If dietary intake of vitamin D is inadequate, then administer vitamin D supplements to avoid deficiency of vitamin D and calcium.
- Take at the same time every day.
- Take with or without food. Taking bazedoxifene with food may increase its AUC by 25% but does not impact the Cmax.
Volume of Distribution
Following intravenous administration of a 3 mg dose of bazedoxifene, the volume of distribution is 14.7 ± 3.9 l/kg.
Elimination Route
Bazedoxifene is rapidly absorbed with a tmax of approximately 2 hours and exhibits a linear increase in plasma concentrations for single doses from 0.5 mg up to 120 mg and multiple daily doses from 1 mg to 80 mg. The absolute bioavailability of bazedoxifene is approximately 6%.
Half Life
~30 hours.
Clearance
The apparent oral clearance of bazedoxifene is approximately 4 to 5 l/h/kg.
Elimination Route
The major route of elimination of radio-labelled bazedoxifene is the faeces, and less than 1% of the dose is eliminated in urine.
Innovators Monograph
You find simplified version here Bazedoxifene
