Pharm
Selective Estrogen Receptor Modulator
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Selective Estrogen Receptor Modulator
, SERM, Droloxifene, Idoxifene, Toremifene
See Also
Raloxifene
Tamoxifen
Definitions
Selective Estrogen Receptor Modulator (SERM)
Diverse group of agents that bind
Estrogen
receptors with variable activity depending on their target tissue
Most SERMs in use are
Agonist
s are estrogen
Antagonist
s at
Breast
and endometrial tissue
Indications
Indications vary with specific SERM effects
Hormone Replacement
in postmenopausal women
Beyond hot flash stage
Estrogen Replacement
contraindicated (
Breast Cancer
)
Raloxifene
Breast
Cancer Prevention
in post-menopausal women
Breast Cancer
risk >1.66% in 5 years
Raloxifene
Tamoxifen
Breast
Cancer Prevention
in pre-
Menopause
Breast Cancer
risk >1.66% in 5 years and age over 35 years old
Tamoxifen
Refractory
Atrophic Vaginitis
with severe
Dyspareunia
Ospemifene (Osphena)
Osteoporosis Prevention
in postmenopausal women
HRT is now only recommended for menopausal symptom management
Raloxifene
Contraindications
Venous Thromboembolism
Perioperative period
Prolonged immobilization
History of
Cerebrovascular Accident
(CVA) or
Transient Ischemic Attack
(TIA)
Medications
Raloxifene
Indicated for breast
Cancer Prevention
in post-menopausal women and
Hormone
replacment therapy
Historically used for
Osteoporosis Prevention
HRT is now only recommended for menopausal symptom management
Tamoxifen
Indicated for Breast
Cancer Prevention
in pre-
Menopause
al and post-menopausal women
Ospemifene (Osphena)
Indicated for refractory
Atrophic Vaginitis
with severe
Dyspareunia
Bazedoxifene
Combined with
Estrogen
in
Duavee
, a
Tissue-selective Estrogen Complex
(
TSEC
)
Indicared for
Estrogen Replacement Therapy
in patients with an intact
Uterus
Alternative to combination
Estrogen
with
Progesterone
Other agents
Droloxifene
Idoxifene
Toremifene
Adverse Effects
Hot Flashes
Leg Cramp
s
Increased
Deep Vein Thrombosis
and
Thromboembolism
risk
DVT, PE and
Cardiovascular Risk
is an FDA black box warning
More likely to occur in first 4 months of treatment
Similar to risk with
Estrogen Replacement
Efficacy
Lower efficacy than
Tamoxifen
for breast
Cancer Prevention
(but lower
Venous Thromboembolism
,
Endometrial Cancer Risks
)
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