Anti-Androgens

Question 1

What drugs are in the Anti-Androgens class?

Answer 1

Drugs in this class are:
- Flutamide
- Abiraterone acetate
- Apalutamide
- Bicalutamide
- Enzalutamide
- Nilutamide
- Darolutamide

Question 2

What is the brand name of Flutamide?

Answer 2

The brand name of this generic drug is:
- Eulexin

Question 3

What is the brand name of Abiraterone acetate?

Answer 3

The brand name of this generic drug is:
- Yonsa
- Zytiga

Question 4

What is the brand name of Apalutamide?

Answer 4

The brand name of this generic drug is:
- Erleada

Question 5

What is the brand name of Bicalutamide?

Answer 5

The brand name of this generic drug is:
- Casodex

Question 6

What is the brand name of Enzalutamide?

Answer 6

The brand name of this generic drug is:
- Xtandi

Question 7

What is the brand name of Nilutamide?

Answer 7

The brand name of this generic drug is:
- Nilandron

Question 8

What is the brand name of Darolutamide?

Answer 8

The brand name of this generic drug is:
- Nubeqa

Question 9

What is the generic of name of Eulexin?

Answer 9

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

Question 10

What is the generic of name of Yonsa?

Answer 10

The generic name of this brand name drug is:
- Abiraterone acetate

Question 11

What is the generic of name of Zytiga?

Answer 11

The generic name of this brand name drug is:
- Abiraterone acetate

Question 12

What is the generic of name of Erleada?

Answer 12

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

Question 13

What is the generic of name of Casodex?

Answer 13

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

Question 14

What is the generic of name of Xtandi?

Answer 14

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

Question 15

What is the generic of name of Nilandron?

Answer 15

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

Question 16

What is the generic of name of Nubeqa?

Answer 16

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

Question 17

What are the main/common indications of the Anti-Androgens class?

Answer 17

The main/common indications of this drug class are:
- Prostate cancer

Question 18

What is the class and MOA of Flutamide?

Answer 18

This drug in the following class:
- Anti-Androgens

This drug’s MOA is as follows:
- Non-steroidal anti-androgen that inhibits androgen uptake and inhibits binding of androgen in target tissues

Question 19

What is the class and MOA of Abiraterone acetate?

Answer 19

This drug in the following class:
- Anti-Androgens

This drug’s MOA is as follows:
- Selectively and irreversibly inhibits CYP17 an enzyme required for biosynthesis and inhibits the formation of testosterone

Question 20

What is the class and MOA of Apalutamide?

Answer 20

This drug in the following class:
- Anti-Androgens

This drug’s MOA is as follows:
- Nonsteroidal androgen receptor antagonist

Question 21

What is the class and MOA of Bicalutamide?

Answer 21

This drug in the following class:
- Anti-Androgens

This drug’s MOA is as follows:
- Selectively and irreversibly inhibits CYP17 an enzyme required for biosynthesis and inhibits the formation of testosterone

Question 22

What is the class and MOA of Enzalutamide?

Answer 22

This drug in the following class:
- Anti-Androgens

This drug’s MOA is as follows:
- Pure androgen receptor signaling inhibitor

Question 23

What is the class and MOA of Nilutamide?

Answer 23

This drug in the following class:
- Anti-Androgens

This drug’s MOA is as follows:
- Non-steroidal anti-androgen that inhibits androgen uptake and inhibits binding of androgen in target tissues

Question 24

What is the class and MOA of Darolutamide?

Answer 24

This drug in the following class:
- Anti-Androgens

This drug’s MOA is as follows:
- Competitive androgen receptor inhibitor, also inhibits androgen receptor translocation and androgen receptor-mediated transcription

Question 25

What are the notable/common monitoring parameters for the Anti-Androgens class?

Answer 25

The notable/common monitoring parameters for this drug class are:
- Serum transaminases at baseline, monthly for 4 months. and periodically thereafter: monitor liver function tests at the first sign or symptom of liver dysfunction
- Prostate specific antigen (PSA) to monitor response to therapy

Question 26

Describe the emetic potential of the Anti-Androgens class.

Answer 26

The emetic potential of this drug class is:
- N/A (minimal)

Question 27

Describe the metabolism of the Anti-Androgen class.

Answer 27

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

Question 28

What are the notable/common ADRs of the Anti-Androgens class?

Answer 28

The notable/common ADRs of this drug class are:
- Headache
- Peripheral edema
- Hot flashes
- Gynecomastia
- Secondary infections

Question 29

What are the clinical pearls of Flutamide?

Answer 29

The clinical pearls of this drug are as follows:
- See common pearls for class
- Used in combination with a GNRH agonist
- Response rate = 50-87%

Question 30

What are the clinical pearls of Abiraterone acetate?

Answer 30

The clinical pearls of this drug are as follows:
- See common pearls for class
- Approved for metastatic, castration-resistant prostate cancer in combination with a steroid BID.
- Co-administration with the recommended dose of steroid compensates for drug-induced reductions in serum cortisol and blocks the compensatory increase in adrenocorticotropic hormone seen with this drug

Question 31

What are the clinical pearls of Bicalutamide?

Answer 31

The clinical pearls of this drug are as follows:
- See common pearls for class
- Used in combination with a GNRH agonist
- Response rate = 54-70%

Question 32

What are the clinical pearls of Enzalutamide?

Answer 32

The clinical pearls of this drug are as follows:
- See common pearls for class
- Requires dose adjustments for strong CYP2C8 inhibitors and CYP3A4 inducers

Question 33

What are the clinical pearls of Nilutamide?

Answer 33

The clinical pearls of this drug are as follows:
- See common pearls for class
- Used in combination with orchiectomy
- Response rate = 40%

Question 34

What are the clinical pearls of the Anti-Androgens class?

Answer 34

The clinical pearls of this drug class are as follows:
- Monotherapy is less effective than GNRH agonist therapy and is not currently recommended to be used alone (unless patient had orchiectomy)
- Therefore, used in combination with androgen ablation therapy
- Overall efficacy is similar, but bicalutamide is generally preferred due to better toxicity profile

Question 35

Describe the dosing schedule and administration for the anti-androgen class.

Answer 35

Dosing schedule and administration for drug class:
- All are given PO
- All are given once daily except:
- Flutamide (TID)
- Abiraterone acetate (BID)
- Darolutamide (BID)

Question 36

Describe the dosing schedule and administration for flutamide.

Answer 36

Dosing schedule and administration for this drug:
- PO TID

Question 37

Describe the dosing schedule and administration for abiraterone acetate.

Answer 37

Dosing schedule and administration for this drug:
- PO BID

Question 38

Describe the dosing schedule and administration for apalutamide.

Answer 38

Dosing schedule and administration for this drug:
- PO once daily

Question 39

Describe the dosing schedule and administration for bicalutamide.

Answer 39

Dosing schedule and administration for this drug:
- PO once daily

Question 40

Describe the dosing schedule and administration for enzalutamide.

Answer 40

Dosing schedule and administration for this drug:
- PO once daily

Question 41

Describe the dosing schedule and administration for nilutamide.

Answer 41

Dosing schedule and administration for this drug:
- PO once daily

Question 42

Describe the dosing schedule and administration for darolutamide.

Answer 42

Dosing schedule and administration for this drug:
- PO BID