Hormonal Treatments

Question 1

What is the MOA for Tyrosine kinase inhibitors?

Answer 1

Inhibits the proliferation of bcr-abl fusion protein, which is responsible for the unregulated activity of tyrosine kinase.

Question 2

Name the Tyrosine Kinase inhibitors.

Answer 2

Imatinib, dasatinib and nilotinib.

Question 3

What is the role of Monoclonal antibodies? (Trastuzumab)

Answer 3

Blocks human epidermal growth factor receptor; Helps in breast cancer

Question 4

What does Rituximab do?

Answer 4

A monoclonal antibody that depletes the host B-cells. Vaccines can only be given after rituximab is ineffective.

Question 5

What is the MOA of hypomethylating agents?

Answer 5

They inhibit DNA methyltransferase which inhibits the methylation of DNA; Results in Apoptosis. Azacitidine and Decitabine

Question 6

Discuss Tamoxifen

Answer 6

A partial estrogen agonist (bone) and antagonist (breast). Categorized as a selective estrogen receptor modulator; Pro-drug

Question 7

Discuss Aromatase inhibitors

Answer 7

Aromatase converts adrogens to estrogen in peripheral tissues, the primary source of estrogen synthesis in postmenopausal women. Can’t overcome ovarian aromatase activity.

Question 8

Describe the patient that benefits from Aromatase Inhibitors.

Answer 8

Patients with nonfunctioning ovaries that have breast cancer.

Question 9

Discuss Androgen deprivation

Answer 9

Block the actions of GnRH and CRH. Since prostate cancer is dependent on androgen malignancy, a blockade will cause prostate involution.

Question 10

What is the problem with Androgen deprivation?

Answer 10

It will cause a surge of LH/FSH which leads to testosterone release, causing the tumor to grow; Tumor flare. Mitigated by GnRH antagonist.