PDA 1 exam 2 (SERMS and Androgens0

tamoxifen

• SERM

• agonist at bone and antagonist at breast

• agonist at endometrium

• treatment for metastatic breast cancer

toremifene

• SERM

• agonist at bone and antagonist at breast

• agonist at endometrium

• treatment for metastatic breast cancer

raloxifene

• SERM

• agonist at bone and antagonist at breast

• antagonist at endometrium

• prevent osteoporosis in postmenopausal women

bazedoxifene

• SERM

• agonist at bone and antagonist at breast

• antagonist at endometrium

• prevent osteoporosis in postmenopausal women

ospemifene

• SERM

• dyspareunia and vaginal dryness

clomiphene

• antagonist or partial agonist

• Increase LH and FSH for ovulation induction

• treating infertility in anovulatory or oligoovulatory women

SERM as ER agonist

• Binding of SERMs or estradiol induces a different conformation of ER

  • Cofactor Y can’t bind to the ER-SERM complex

  • Cofactor Y can bind to the ER-estrogen complex

• Specific cofactors in different tissues confer selectivity of SERMs

Imlunestrant

• SERD

• ER positive advance or metastatic breast cancer

• degradation of ER

Camizestrant

• SERD

• ER positive advance or metastatic breast cancer

• degradation of ER

Vepdegestrant

• SERD

• ER positive advance or metastatic breast cancer

• degradation of ER via proteosome pathway

androgen and androgenic affects

• anabolic effects

• increases synthesis and decreased breakdown of proteins

testosterone main adverse effects

• suppresses testicular activity

• decreases testes size

danazol

• androgen receptor agonist

• treat endometriosis

flutamide

• synthetic androgen receptor antagonist

• locally confined and metastatic prostate cancer

  • hirsutism, PCOS, female hair loss

• combined with GnRH agonist or antagonist

bicalutamide

• synthetic androgen receptor antagonist

• metastatic prostate cancer

• less adverse effects, including liver toxicity

• combined with GnRH agonist or antagonist

darolutamide

• synthetic androgen receptor antagonist

• locally confined and metastatic prostate cancer

• less adverse effects, including liver toxicity

• combined with GnRH agonist or antagonist

enzalutamide

• synthetic androgen receptor antagonist

• locally confined and metastatic prostate cancer

• less adverse effects, including liver toxicity

• combined with GnRH agonist or antagonist

clascoterone

• synthetic androgen receptor antagonist

• acne

• topical crease

dihydrotestosterone

• a 5a reductase inhibitors

• for BPH

• male pattern hair loss