Hormone antagonists are currently used to treat what 3 types of cancers?
Lymphomas/leukemias, breast cancer, and prostate cancer
What group of hormone antagonist drugs is used to treat lymphomas and leukemias?
Glucocorticoids
List 3 different types of hormone antagonists that are used to treat breast cancer.
SERMs (Selective Estrogen-Receptor Modulators), SERDs (SER Downregulators), and aromatase inhibitors
Complete androgen ablation therapy requires 2 different kinds of hormone antagonists. What are these 2 categories?
GnRH analogs and nonsteroidal androgen-receptor blockers
Name the 2 glucocorticoid hormone antagonists.
Prednisone and dexamethasone
Which hormone antagonist is a SERM (selective estrogen-receptor modulator)?
Tamoxifen
Which hormone antagonist is a SERD (selective estrogen-receptor downregulator)?
Fulvestrant
What are the 4 aromatase inhibitors?
Aminoglutethamide, anastrozole, letrozole, and exemestane
What are the 2 GnRH analogs?
Leuprolide and goserelin
Name the 2 nonsteroidal androgen-receptor blockers.
Flutamide and bicalutamide
By what mechanism do the glucocorticoids inhibit cancer?
They inhibit lymphocyte mitosis
Which hormone antagonist is used to treat ALL, as well as Hodgkins, non-Hodgkins, multiple myeloma, and CLL.
Prednisone
How is dexamathasone typically used?
In conjunction with radiation therapy, to reduce edema in brain and spinal cord tumors
As a group, the hormone antagonists are notable for not inducing what common chemotherapy side-effect?
They do not cause myelosuppression
Which hormone antagonist, which can be administered orally, is the most widely used anti-estrogen therapy?
Tamoxifen
Tamoxifen therapy is unfortunately accompanied by hot flushes, alopecia, and increased risk of what 2 events?
Increased risks of endometrial cancer and of thromboembolism
How do tamoxifen and fulvestrant compare in terms of their mechanistic effect on ERs (estrogen/estradiol receptor)?
Fulvestrant binds ER with ~100x greater affinity than tamoxifen does, and reduces overall ER levels while tamoxifen stabilizes or even increases ER expression.
List 3 circumstances in which tamoxifen might be used.
For metastatic ER-positive breast cancer, as adjuvant therapy following breast tumor excision, or for prevention in high-risk (strong family history) patients
Even though we refer to the “hormone antagonists” as a class of cancer drugs, only 1 breast cancer drug is a true “anti-estrogen” antagonist that blocks estrogen from its receptor without displaying any agonist activity. Which drug is this?
Fulvestrant
Which aromatase inhibitor is a first-line therapy for treating ER(+) breast cancer in postmenopausal women?
Anastrozole
What is an obvious, must-not-miss feature that should be found for a cancer before it is treated with estrogen or androgen inhibiting drugs?
The cancer must be ER(+) or AR(+)
Which first generation estrogen inhibitor has fallen out of favor because it is relatively weak and has significant toxicity?
Aminoglutethamide
Which aromatase inhibitor is a steroidal inhibitor, meaning that it binds covalently and irreversibly?
Exemestane
Which estrogen inhibitors are used only on postmenopausal women?
Fulvestrant, anastrozole, letrozole, and exemestane
What receptor do leuprolide and goserelin bind to, and what hormones are not released as a result?
Binds GnRH receptor, inhibiting FSH and LH release
What 2 hormone antagonists work by competing with androgen for AR binding?
Flutamide and bicalutamide
