Hormone therapy Flashcards
Prednisolone
Class: Glucocorticoid
Mechanism of action: Inhibit mitosis in lymphocytes.
Therapies: ALL (in addition to vincristine)
Hodgkin’s and Non-Hodgkin’s combo therapy (MOPP, CHOP)
Multiple myeloma, CLL
Dexamethasone
Class: Glucocorticoid
Mechanism of action: Inhibit mitosis in lymphocytes.
Therapies: Used in conjunction with radiotherapy to reduce edema related to brain and spinal cord tumors
Tamoxifen
Class: Selective Estrogen Receptor Modulator (SERM)
Mechanism of action: Competitively inhibits ER. When binds it inactivates the receptor. Stabilizes and even increases the amount of ER expression.
Therapeutic uses: metastatic breast cancer, adjuvant therapy following breast tumor resection, prevention of breast cancer in people with strong FH
Toxicity: Hot flushes, hair loss, nausea, vomiting
Increases risk of endometrial cancer (weak ER agonist in endometrium)
Increases the risk of thromboembolic events
Fulvestrant
Class: Selective Estrogen Receptor Downregulator (SERM)
Mechanism of action: Binds to ER with a much higher affinity than tamoxifen and inhibits dimerization of ER and increases its degradation reducing the number of ERs in the cell.
Therapeutic uses: postmenopausal women with ER positive metastatic breast cancer
Aminoglutethamide
Class: Aromatase Inhibitor (first generation)
Mechanism of action: Inhibits the function of aromatase.
Therapeutics: Weak response on breast cancer
Toxicity: Significant
Anastrozole
Class: Aromatase inhibitor (3rd generation)-nonsteroidal
Mechanism of action: Inhibits (reversible) the function of aromatase.
Therapeutics: first line therapy for treatment of ER positive breast cancer in postmenopausal women.
Letrozole
Class: Aromatase inhibitor (3rd generation)-nonsteroidal
Mechanism of action: Inhibits (reversible) the function of aromatase.
Therapeutics: first line therapy for treatment of ER positive breast cancer in postmenopausal women.
Exemestane
Class: Aromatase inhibitor (3rd generation)-steroidal
Mechanism of action: Inhibits (irreversibly) the function of aromatase particularly targeting the androstenedione to estrone pathway.
Therapeutics: first line therapy for treatment of ER positive breast cancer in postmenopausal women.
Leuprolide
Class: GnRH analog
Mechanism of action: binds the GnRH receptor and inhibits the release of FSH and LH resulting in testicular production of testosterone.
Therapeutics: Prostate cancer (Androgen ablation therapy, along with AR analogs)
Goserelin
Class: GnRH analog
Mechanism of action: binds the GnRH receptor and inhibits the release of FSH and LH resulting in testicular production of testosterone.
Therapeutics: Prostate cancer (Androgen ablation therapy, along with AR analogs)
Flutamide
Class: nonsteroidal AR blockers
Mechanism of action: compete with the natural hormone for binding to the AR and prevent its translocation to the nucleus.
Therapeutics: Prostate cancer (Androgen ablation therapy, along with GnRH analogs)
Bicalutamide
Class: nonsteroidal AR blockers
Mechanism of action: compete with the natural hormone for binding to the AR and prevent its translocation to the nucleus.
Therapeutics: Prostate cancer (Androgen ablation therapy, along with GnRH analogs)
