Endocrine therapies

Question 1

example of endocrine therapies

Answer 1

Antiestrogens
•Selective Estrogen Receptor Modulators
- Tamoxifen
•Pure antiestrogens

Antiaromataseagents
•Nonsteroidal inhibitors
•Steroidal inactivators

LHRH agonists

Antiandrogens

Question 2

Tamoxifen MOA and indication and other acitivity

Answer 2

SERM (antiestrogen)
- MOA: Inhibit nuclear binding of the estrogen receptor, block estrogen stimulating of breast cancer cells

• Indicated for treatment of estrogen-receptor positive breast cancer, also effective in advanced endometrial cancer
• • Tissue-specific activity
    o Antagonist activity (antiestrogenic)
     Breast epithelial cells (normal & cancer cells)

o Agonist activity (estrogenic)
 Bone – therefore stronger bone.
 Lipids – Better lipid profile
 Endometrium – increase risk of endometrium cancer

Question 3

Tamoxifen good and bad

Answer 3

Tamoxifen good:

• Reduce breast cancer
• Reduce cholesterol
• Reduces fractures

Tamoxifen bad:

• Increases cataracts
• Hypothalamus – increases vasomotor symptoms
• Liver – increases thromboembolism
• Uterus – increases endometrial cancer, fibroids, polyps and vaginal discharge.

Question 4

Antiaromatase agent MOA

Answer 4

Aromatase is an enzyme that converts testosterone to estradiol and androstenedione to estrone.
Estradiol and estrone are female sex hormones (oestrogen).
Antiaromatase agents block this conversation

Question 5

Antiaromatase agent

Answer 5

• Anastrozole(Arimidex®)
• Letrozole(Femara®)
• Exemestane(Aromasin®)

Question 6

•Anastrozole(Arimidex®)

Answer 6

Antiaromatase agent

Question 7

•Letrozole(Femara®)

Answer 7

Antiaromatase agent

Question 8

•Exemestane(Aromasin®)

Answer 8

Antiaromatase agent

Question 9

SE of Antiaromatase agent

Answer 9

• Fatigue
• Hot flashes
• Myalgia/Arthralgia
• Bone loss (must supplement with Calcium and Vitamin D)