2015 Antineoplastics

Estrogen receptor antagonists: FULVESTRANT, RALOXIFENE, TAMOXIFEN, TOREMIFENE

Example test questionMechanism

Types

  1. Critical fact iconSelective ER modulators (SERMs): may function as estrogen-receptor agonists, antagonists, or mixed agonist-antagonists, depending on the target tissue
    • RALOXIFENE, TAMOXIFEN, TOREMIFENE

  2. Selective ER downregulators (SERDs): competitive antagonists in every tissue
    • FULVESTRANT
Breast
Uterus
Bone
Estrogen
Proliferative
Proliferative
Anti-resorptive
TAMOXIFEN
SERM
Antagonist
(partial agonist)
Agonist
Agonist
(postmenopausal women only)
TOREMIFENE
SERM
Antagonist
Probably agonist
No effect
RALOXIFENE
SERM
Antagonist
Antagonist
Agonist
FULVESTRANT
SERD
Antagonist
Antagonist
Antagonist

 

Email: Dr. Janet Fitzakerley | ©2015 University of Minnesota Medical School Duluth | Last modified: 11-apr-15 9:39 AM