anticancer2

Question 1

Vinca alkaloids, epipodophylotoxins and taxanes MOA

Answer 1

bind tubulin–>disruption of mitotic spindle apparatus (M Phase) (CCS)–>Prevents segregation of chromosomes lined up in metaphase- ->metaphase arrest

Question 2

Vincristine and Vionblastine SE

Answer 2

neurological (Delayed)

Question 3

Vinblastine Sulfate [VelbanR]

Answer 3

Vinca alkaloid

CCS: M phase

Question 4

Vincristine Sulfate [Vincasar PFSR]

Answer 4

Vinca alkaloid

CCS: M phase

Question 5

Etoposide [ToposarR]

Answer 5

derivative of podophyllotoxin
-Forms a complex with topoisomerase II and DNA, resulting in DNA breaks,
no resealing of the break, and cell death
CCS: G2 Phase

Question 6

Paclitaxel [TaxolR]

Answer 6

antimicrotubule agent
-promotes microtubule assembly, by enhancing tubulin polymerization, stops dynamic process by stabilizing microtubules
CCS: G2 and M phase

Question 7

Prednisone [IntensolR]

Dexamethasone [BaycadronR]

Answer 7

adrenocorticosteroids
MOA: lipid soluble agents–>diffuse into cells–>bind to a cytosoluble receptor–>translocates into nucleus–>inhibition/stimulation of gene transcription
CCS: G1

Question 8

corticosteroid SEs

Answer 8

• Iatrogenic Cushing’s Syndrome, osteoporosis, infections.

- Psychiatric disturbances, peptic ulceration, hypertension, edema, ETC.

Question 9

Tamoxifen [NolvadexR]

use?

Answer 9

Nonsteroidal antiestrogen
-used for ER+ invasive breast cancer, approved for adjuvant (additional) therapy of breast cancer
CCS: G1 phase

Question 10

Tamoxifen [NolvadexR] SEs

most serious SE

Answer 10

menopausal symptoms

• Short term: Hot flashes, ha, fatigue, N/V, vaginal dryness or itching, skin rashes
• Long term: visual disturbances; vaginal bleeding, ocular toxicity, thromboembolic events, moderate thrombocytopenia and leukopenia
• Most serious: its potential tumor-promoting activity which may result in increased incidence of endometria cancer which may be related to tamoxifen’s estrogenic activity*

Question 11

Imatinib Mesylate (Gleevec®)

Answer 11

Tyrosine Kinase inhibitor
-inhibits the Bcr-Abl tyrosine kinase, preventing the phosphorylation of the kinase substrate by ATP
SEs: not much BM suppression
CCS: G1 phase

Question 12

Bcr-Abl fusion protein is a constitutive abnormal tyrosine kinase created by the ??

Answer 12

t(9:22) Philadelphia chromosomal translocation in CML (95% of patients).

Question 13

Imatinib inhibits ?? and induces ?? in Bcr-Abl- positive leukemia cell lines derived from patients with CML (chronic myeloid leukemia) in blast crisis.

Answer 13

cell proliferation

apoptosis

Question 14

Imatinib Mesylate (Gleevec®) indications for use

Answer 14

• Acute lymphocytic leukemia (ALL).
• Ph+ Chronic myeloid leukemia (CML) in blast crisis
• c-Kit (CD117) receptor positive-GI stromal tumor

Question 15

Trastuzumab (Herceptin®)

Answer 15

humanized IgG1 monoclonal
-antibody binds human epidermal growth factor (EGF) receptor HER-2
-blocks EGF binding and down-regulates the EGF receptor’s tyrosine kinase signaling activity
CCS: G1 phase

Question 16

Trastuzumab (Herceptin®) uses

Answer 16

• Adjuvant breast cancer: EGR2 over expressing breast cancers (30%) in combination with doxorubicin, cyclophosphamide and paclitaxel.
• Metastatic breast cancer: in combination with paclitaxel for first-line treatment of HER2-overexpressing metastatic breast cancer