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Flashcards in anticancer2 Deck (16):
1

Vinca alkaloids, epipodophylotoxins and taxanes MOA

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

2

*Vincristine and Vionblastine SE*

*neurological* (Delayed)

3

Vinblastine Sulfate [VelbanR]

Vinca alkaloid
CCS: M phase

4

Vincristine Sulfate [Vincasar PFSR]

Vinca alkaloid
CCS: M phase

5

Etoposide [ToposarR]

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

6

Paclitaxel [TaxolR]

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

7

Prednisone [IntensolR]
Dexamethasone [BaycadronR]

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

8

corticosteroid SEs

-Iatrogenic Cushing's Syndrome, osteoporosis, infections.
-Psychiatric disturbances, peptic ulceration, hypertension, edema, ETC.

9

Tamoxifen [NolvadexR]
use?

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

10

Tamoxifen [NolvadexR] SEs
*most serious SE*

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*

11

Imatinib Mesylate (Gleevec®)

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

12

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

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

13

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

cell proliferation
apoptosis

14

Imatinib Mesylate (Gleevec®) *indications for use*

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

15

Trastuzumab (Herceptin®)

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

16

Trastuzumab (Herceptin®) *uses*

-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