Week 7 - Chapter 103 Anticancer Drugs II Flashcards Preview

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Flashcards in Week 7 - Chapter 103 Anticancer Drugs II Deck (28):


Antiestrogens are drugs that block ERs, and hence only work against cells that are ER positive. Benefits derive from depriving tumor cells of the growth-promoting influence of estrogen. Three antiestrogens—tamoxifen, toremifene, and fulvestrant—are approved for adjuvant treatment. Of these, tamoxifen is by far the most widely used.


Tamoxifen - use

Used for established breast cancer disease and for reducing occurrence in high-risk patients
Adjuvant therapy after surgery
Treatment of metastatic disease


Aromatase Inhibitors

The aromatase inhibitors are used to treat ER-positive breast cancer in postmenopausal women. These drugs block the production of estrogen from androgenic precursors, and thereby deprive breast cancer cells of the estrogen they need for growth. Aromatase inhibitors do not block production of estrogen by the ovaries, and hence are of little benefit in premenopausal women. In fact, aromatase inhibitors may cause a compensatory rise in estradiol in premenopausal patients. Aromatase inhibitors are more effective than tamoxifen and have a different toxicity profile. Unlike tamoxifen, aromatase inhibitors pose no risk of endometrial cancer and only rarely cause thromboembolism. However, they can increase the risk of fractures and have been associated with moderate to severe myalgias.


Anastrozole - use

Used to treat ER-positive breast cancer in postmenopausal women


Localized Prostate Cancer

Surgery + Radiation. (Optional Drug Treatment)


Metastatic Prostate Cancer

Drug Treatment, Castration


Androgen Deprivation Therapy

Lowers testosterone production
Drugs used to block testosterone receptors
Slows progression, increases comfort
Gonadotropin Releasing Hormone Agonists
Gonadotropin Releasing Hormone Antagonists


Gonadotropin-Releasing Hormone Agonists

The gonadotropin-releasing hormone (GnRH) agonists suppress production of androgens by the testes—but not by the adrenal glands and prostate cancer cells. Currently, four GnRH agonists are available: leuprolide, triptorelin, goserelin, and histrelin. All four are indicated for cancer of the prostate. In addition, leuprolide is used for endometriosis


Leuprolide - use

Advanced prostate cancer
Palliation, not cure, is primary benefit


Gonadotropin-Releasing Hormone Antagonists

Like the GnRH agonists, the GnRH antagonists suppress production of androgens by the testes. However, in contrast to the GnRH agonists, the GnRH antagonists do not produce an initial tumor flare. Currently, only one GnRH antagonist—degarelix—is available.


Degarelix - use

palliative therapy of advanced prostate cancer in men who are not candidates for a GnRH agonist, and who do not want surgical castration
Suppress production of androgens
Do not produce initial tumor “flare”


Leuprolide - mechanism of action

Stimulates pituitary to release ICSH (TestisAndrogens). After initial surge, pituitary becomes desensized to stimulationreduced ICSH
Cotreatment with an androgen receptor blocker
Prevents surge effects
Blocks androgens produced by other sources


Leuprolide - adverse effects

Generally well tolerated
Hot flashes
Testosterone loss may aggravate bone pain and urinary obstruction
Concurrent treatment with androgen receptor blocker can minimize these effects


Degarelix - mechanism of action

blockade of GnRH receptors in the anterior pituitary, which decreases release of luteinizing hormone and follicle-stimulating hormone, which in turn deprives the testes of the stimulus they need for testosterone production.


Degarelix - adverse reactions

hot flashes, reduced libido, erectile dysfunction, gynecomastia, decreased muscle mass, decreased bone mass with associated increased risk of fractures and injection site reactions.


Tamoxifen - category



Anastrozole - category

Aromatase Inhibitors


Leuprolide - category

Gonadotropin-Releasing Hormone Agonists


Degarelix - category

Gonadotropin-Releasing Hormone Antagonists


Androgen Receptor Blockers

Androgen receptor blockers, or simply antiandrogens, are indicated only for advanced androgen-sensitive prostate cancer—and only in combination with surgical castration or chemical castration using a GnRH agonist. Currently, three androgen receptor blockers are available: flutamide, bicalutamide, and nilutamide.


Flutamide - use

Indicated for advanced androgen-sensitive prostate cancer with castration.
(1) It can prevent tumor flare when GnRH therapy is started and (2) it can block the effects of adrenal and prostatic androgens.


Flutamide - mechanism of action

the combination of an androgen antagonist plus a GnRH agonist—so-called complete androgen blockade—is reserved for suppressing the initial flare and for suppressing the tumor after it has stopped responding to a GnRH agonist alone. The combination is not used continuously because it does not increase survival, but does increase toxicity.


Flutamide - category

Androgen Receptor Blockers


Flutamide - adverse reaction

hot flashes, reduced libido, erectile dysfunction, gynecomastia, decreased muscle mass, and decreased bone mass with associated increased risk of fractures. Nausea, vomiting, and diarrhea are also common.


Abiraterone - use

Combined use with prednisone to treat metastatic, castration-resistant prostate cancer (previously treated with docetaxel)


Abiraterone - mechanism of action

the underlying mechanism is inhibition of the cytochrome P450 enzyme 17 (CYP17), an enzyme needed by the adrenals, testes, and prostate tumors for androgen synthesis. When tested in men with metastatic castration-resistant prostate cancer, the combination of abiraterone plus prednisone increased overall survival by nearly 4 months, and progression-free survival by 2 months.


Abiraterone - category

CYP17 Inhibitor


Abiraterone - adverse reactions

Hypokalemia, joint swelling, muscle discomfort, hepatotoxicity

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