Aromatase Inhibitors

Question 1

What drugs are in the Aromatase Inhibitors class?

Answer 1

Drugs in this class are:
- Anastrozole
- Exemestane
- Letrozole

Question 2

What is the brand name of Anastrozole?

Answer 2

The brand name of this generic drug is:
- Arimidex

Question 3

What is the brand name of Exemestane?

Answer 3

The brand name of this generic drug is:
- Aromasin

Question 4

What is the brand name of Letrozole?

Answer 4

The brand name of this generic drug is:
- Femara

Question 5

What is the generic of name of Arimidex?

Answer 5

The generic name of this brand name drug is:
- Anastrozole

Question 6

What is the generic of name of Aromasin?

Answer 6

The generic name of this brand name drug is:
- Exemestane

Question 7

What is the generic of name of Femara?

Answer 7

The generic name of this brand name drug is:
- Letrozole

Question 8

What are the main/common indications of the Aromatase Inhibitors class?

Answer 8

The main/common indications of this drug class are:
- Breast Cancer

Question 9

What is the class and MOA of Anastrozole?

Answer 9

This drug in the following class:
- Aromatase Inhibitors

This drug’s MOA is as follows:
- Inhibits aromatase which is the enzyme responsible for the conversion of androgens to estrogens, this leads to a significant decrease in circulating estrogen.
- This thus reduces estrogen mediated stimulation of breast cancer tissue
- This one is a non-steroidal aromatase inhibitor - it decreases estrogen synthesis without compromising adrenal steroid synthesis

Question 10

What is the class and MOA of Exemestane?

Answer 10

This drug in the following class:
- Aromatase Inhibitors

This drug’s MOA is as follows:
- Inhibits aromatase which is the enzyme responsible for the conversion of androgens to estrogens, this leads to a significant decrease in circulating estrogen.
- This thus reduces estrogen mediated stimulation of breast cancer tissue
- This one is a steroidal aromatase inhibitor - it has a similar structure to androgen and irreversibly binds to aromatase

Question 11

What is the class and MOA of Letrozole?

Answer 11

This drug in the following class:
- Aromatase Inhibitors

This drug’s MOA is as follows:
- Inhibits aromatase which is the enzyme responsible for the conversion of androgens to estrogens, this leads to a significant decrease in circulating estrogen.
- This thus reduces estrogen mediated stimulation of breast cancer tissue
- This one is a non-steroidal aromatase inhibitor - it decreases estrogen synthesis without compromising adrenal steroid synthesis

Question 12

What are the notable/common monitoring parameters for the Aromatase Inhibitors class?

Answer 12

The notable/common monitoring parameters for this drug class are:
- Baseline and periodic bone mineral density screening (every 1 to 2 years).
- Cholesterol and hepatic function tests at baseline and periodically during therapy.

Question 13

Describe the emetic potential of the Aromatase Inhibitors class.

Answer 13

The emetic potential of this drug class is:
- None, N/A

Question 14

Describe the extravasation risk and management strategies for the Aromatase Inhibitors class.

Answer 14

The extravasation risk and management strategies for this drug class are as follows:
- None, N/A (all are oral)

Question 15

Describe the metabolism of the Aromatase Inhibitors class.

Answer 15

The metabolism of this drug class is as follows:
- Extensively hepatic

Question 16

What are the notable/common ADRs of the Aromatase Inhibitors class?

Answer 16

The notable/common ADRs of this drug class are:
- Musculoskeletal side effects including carpal tunnel. arthralgias. joint stiffness. and/or bone pain

Question 17

Describe the strategy and rationale for management of Musculoskeletal side effects caused by Aromatase Inhibitors.

Answer 17

The strategy and rationale for management of this condition caused by these drugs are:
- This includes carpal tunnel, arthralgias, joint stiffness, and/or bone pain.
- In up to 1/3 of patients these symptoms can be severe and may be the cause of treatment discontinuation in 10-20% of patients on Als.
- The best strategy for managing these adverse effects includes exercise and nonsteroidal anti-inflammatory drugs.

Question 18

What are the clinical pearls of the Aromatase Inhibitors class?

Answer 18

The clinical pearls of this drug class are as follows:
- 70% estradiol reduction after 24 hours; 80% after 2 weeks of therapy
- Aromatase inhibitors work in the peripheral fat to decrease estrogen synthesis.
- In pre-menopausal women, estrogen is also produced by the ovaries so aromatase inhibitors are NOT effective therapy as monotherapy for pre-menopausal women. Some sort of ovarian suppression must be used in pre-menopausal women receiving Als.
- An Al is the preferred adjuvant treatment of post-menopausal women, although tamoxifen is an acceptable alternative for women who are intolerant of Als.
- Data shows similar clinical outcomes and tolerability between the AIs. Individuals may tolerate one of these agents better than another. Consider switching to an alternative Al if the initial Al is poorly tolerated and strategies to manage the side effects have been ineffective.
- ASCO recommends a maximum duration of 5 years of AI therapy for postmenopausal women. Als may be combined with tamoxifen for a total duration of up to 10 years of endocrine therapy.
- Aromatase inhibitors are currently being studied as risk reduction agents in post-menopausal women at a high risk for breast cancer