Anticancer Med Chem 2

Question 1

What are the hormonal agents in cancer therapy?

Answer 1

• Antiestrogens
• Aromatase Inhibitors
• Antiandrogens
• LHRH (GnRH) Analogues and Antagonist

Question 2

What are the antiestrogens cancer drugs?

Answer 2

• Tamoxifen Citrate
• Raloxifene
• Megestrol Acetate
• Fluvestrant

Question 3

What are the aromatase Inhibitors?

Answer 3

• Anastrazole
• Letrozole
• Exemestane

Question 4

What are the antiandrogen cancer therapy

Answer 4

• Flutamide
• Nilutamide
• Bicalutamide
• Enzalutamide

Question 5

What are the LHRH (GnRH) Analogues and Antagonst?

Answer 5

• Goserelin

- Leuprolide

Question 6

In which cancers would you use endocrine cancer therapy?

Answer 6

• Breast cancer
• Prostate cancer
• Endometrium cancer

Question 7

Why would estrogen therapy possibly work for breast cancer?

Answer 7

Breast cancer cells can be Estrogen receptor +. estrogen can drive growth of the cancer.

Question 8

What is Aromatase?

Answer 8

-a P450 enzyme. It catalyzes the last step of estrogen biosynthesis. It converts androstenedione to estrone (E1) and testosteerone to estraiol (E2)

Question 9

what do aromatase inhibitors do?

Answer 9

-They block the aromatase, and decrease estrogen levels

Question 10

What are AIs given to?

Answer 10

Postmeonpausal women who have a ER+ tumor.

Question 11

MOA of Exemestane?

Answer 11

• Androgen analogue
• IRREVERSIBLY binds to aromatase
• Called Suicide inhibitor.

Question 12

MOA of Anastrozole or Letrozole?

Answer 12

• Contains functional group that binds to heme ironn to the cytochrome P450, interfering with the hydroxylation rxns.
• Competes REVERRSIBLY for the andgrogen bindign site.

Question 13

Is SERMs tissue selective?

Answer 13

Yes

Question 14

How is CYP2D6 related to Tamoxifen?

Answer 14

TAM is dependent on its conversion by the hepatic drug-metabolizing enzyme cytochrome P450 2D6 to its metabolite, endoxifen.

Question 15

What medications would patients on Tamoxifen need to avoid?

Answer 15

-Avoid CYP2D6 inhibitors, like Fluoxetine, and paroxetine

Question 16

What is Raloxifene approved for?

Answer 16

• Prevention and treatment of osteoporosis in postmenopausal women
• Chemoprevention of invasive breast cancer in post menopausal women at high risk

Question 17

What is a Fluvestrant?

Answer 17

-A selective ER down-regulator (SERDs)…(promotes ER degradation, reduces ER rpotein level)

Question 18

Does Fulvestrant show cross-resistance with Tamoxifen?

Answer 18

No. Bc it is a pure ER antagonist

Question 19

What is the MOA of Enzalutamide?

Answer 19

• 5-8 fold higher affinity to AR compared to bicalutamide.
• It competes with androgens and binds to AR ligand binding domains to reduce AR nuclear translocation and inhibits the assocation of AR to androgen response elements (ARE)

Question 20

What does Abiraterone do?

Answer 20

-Blocks androgen biosynthesis.

Question 21

What is the first line treatment for advanced/metastatin prostate cancer?

Answer 21

-Androgen Deprivation Therapy (ADT)

Question 22

what is the leading ADT?

Answer 22

LHRH (GnRH) agonists

Question 23

Function of Protein Kinase?

Answer 23

-catalyze transfer of the terminal phosphate of ATP to proteinn substrates that usually contain a serine (S), Threonine (T), or tyrosine residue (Y)

Question 24

What are the three major types of kinases?

Answer 24

• Tyrosine Kinases
• Serine /Threonine Kinases
• Tyrosine/Serine/Threonine Kinases