Anticancer 3

Question 1

MICROTUBULE INHIBITORS groups and two drugs in each?

Answer 1

VINCA ALKALOIDS
VINCRISTINE
VINBLASTINE

TAXANES
PACLITAXEL
DOCETAXEL

Question 2

Vinca alkaloids MOA?

Answer 2

Vinca alkaloids bind to β-tubulin and inhibit its
ability to polymerize into microtubules.
• This results in mitotic arrest in metaphase.
• Cell division stops. Cells die by apoptosis.

Question 3

AE of Vincristine?

Answer 3

Vincristine: Peripheral neuropathy. Bone

marrow depression is mild. Alopecia.

Question 4

Ae of vinblastine?

Answer 4

Vinblastine: Myelosuppression is the doselimiting
adverse effect. Other adverse effects
include alopecia and peripheral neuropathy

Question 5

Taxanes MOA?

Answer 5

Taxanes bind to the β-tubulin subunit of
microtubules and promote microtubule
polymerization.
• Stabilization of the microtubules in a polymerized
state arrests cells in mitosis and leads to apoptosis.

Question 6

AE of Paclitaxel?

Answer 6

Hypersensitivity, myelosuppression, peripheral
neuropathy, alopecia.
• Hypersensitivity is reduced by premedication with
dexamethasone, diphenhydramine and an H2
blocker

Question 7

Ae of Docetaxel?

Answer 7

Myelosuppression, peripheral neuropathy, fluid
retention, alopecia, mucositis.
• Pretreatment with dexamethasone is required to
prevent fluid retention.
• Docetaxel does not cause neuropathy as
frequently as paclitaxel.
• Myelosuppression is dose-limiting.

Question 8

EPIPODOPHYLLOTOXINS? MOA?

Answer 8

ETOPOSIDE
Inhibits topoisomerase II,
resulting in DNA damage
through strand breakage.
• Blocks cell in late S-G2 phase.

Question 9

What are the two Captothecans? MOA?

Answer 9

TOPOTECAN
IRINOTECAN
Inhibit topoisomerase I.
Inhibition results in DNA
damage.

Question 10

Prednisone use?

Answer 10

Glucocorticoids are lympholytic and suppress
mitosis in lymphocytes.
• They are used for acute leukemia and malignant
lymphomas.

Question 11

Three types of estrogen inhibitors?

Answer 11

SELECTIVE ESTROGEN-RECEPTOR
MODULATORS (SERMs)
SELECTIVE ESTROGEN-RECEPTOR
DOWNREGULATORS (SERDs)
AROMATASE INHIBITORS (AIs)

Question 12

Which two are SELECTIVE ESTROGEN-RECEPTOR

MODULATORS(SERMs)?

Answer 12

RALOXIFENE

Tamoxifen

Question 13

Describe Raloxifene and its uses?

Answer 13

Raloxifene is an antiestrogen in the uterus and
the breast, while promoting estrogenic effects in
the bone to inhibit resorption.
• Used for prevention of postmenopausal
osteoporosis and prophylaxis of breast cancer in
high risk postmenopausal women.

Question 14

Describe Tamoxifen?

Answer 14

TAMOXIFEN
• SERMs bind to estrogen receptors and act as
agonists or antagonist depending on the tissue.
• Tamoxifen is an antagonist on breast cancer.
• Tamoxifen is an agonist in nonbreast tissues.
• Used for receptor-positive breast cancer.
• Chemopreventive agent in women at risk for
breast cancer.

Question 15

Describe Fulvestrant?

Answer 15

SERDs are devoid of estrogen agonist activity.
• Fulvestrant binds to the estrogen receptor (ER)
inhibits its dimerization and increases its
degradation.
• ER-mediated transcription is abolished.

Question 16

Describe aromatase inhibitors?

Answer 16

Aromatase converts androstenedione to estrone.
• In postmenopausal women, this conversion is
the primary source of circulating estrogens.
• Aromatase inhibitors are the standard of care for
adjuvant treatment of postmenopausal women
with hormone receptor–positive breast cancer.

Question 17

Nonsteroidal and Reversible competitive inhibitors of aromatase?

Answer 17

ANASTROZOLE & LETROZOLE

Question 18

Steroidal and Irreversible inhibitor of aromatase?

Answer 18

EXEMESTANE

Question 19

ANDROGEN INHIBITORS subgroups?

Answer 19

GONADOTROPIN-RELEASING
HORMONE AGONISTS
ANDROGEN RECEPTOR BLOCKERS

Question 20

Preferred approach to prostate cancer?

Answer 20

use of GnRH agonists,
alone or in combination with an androgen
receptor blocker.

Question 21

Which two are gonadotropin releasing hormone agonists?

Answer 21

GOSERELIN

LEUPROLIDE

Question 22

Describe gonadotropin releasing hormone agonists?

Answer 22

When given continuously or as a depot, GnRH
agonists cause an initial surge in LH and FSH
levels, followed by inhibition of gonadotropin
release.
• Testosterone levels fall to 10% of their initial
values after a month.
• The initial surge can be counteracted by
concurrent administration of flutamide for 2-4
weeks.

Question 23

Describe Flutamide?

Answer 23

Synthetic, nonsteroidal antiandrogen.
• Metabolized to an active metabolite that acts as a
competitive antagonist at the androgen receptor,
preventing its translocation to the nucleus.

Question 24

Inhibitor of EDFR tyrosine kinase solely?

Answer 24

Gefitnib and Erlotinib

Question 25

Inhibitor of trysosine kinase BCr-abl

Answer 25

Imatinib

Question 26

Lapatinib inhibits?

Answer 26

Inhibitor of EGFR and ErbB2 tyrosine kinases.

Question 27

Trastuzumab acts against?

Answer 27

Monoclonal antibody against ErbB2.

Question 28

Asparginase MOA?

Answer 28

Most normal tissues synthesize
L-asparagine in amounts
sufficient for protein synthesis.
• Certain neoplastic tissues,
however, require exogenous
source.
• Asparaginase hydrolyzes serum
asparagine, depriving these cells
of the asparagine necessary for
protein synthesis, leading to cell
death.

Question 29

Ae of Asparaginase?

Answer 29

• Hypersensitivity.
• Decrease in clotting factors.
• Liver abnormalities.
• Pancreatitis, seizures, coma due to ammonia
toxicity.

Question 30

Describe Hydroxyurea?

Answer 30

Inhibits ribonucleotide reductase.
• This leads to depletion of deoxynucleoside
trisphosphate pools.
• DNA synthesis is thereby inhibited.
• Kills cells in S phase.
• Given orally.

Question 31

What is interferon gamma used for?

Answer 31

Approved for hairy cell leukemia, chronic
myelogenous leukemia (CML), malignant
melanoma and Kaposi’s sarcoma.

Question 32

AE of Interferon Gamma?

Answer 32

Depression.
• Fever with chills.
• Leukopenia, thrombocytopenia. Fatigue, malaise, anorexia, weight loss, alopecia,
transient elevation of liver enzymes.

Question 33

Uses for Hydroxyurea?

Answer 33

Used for melanoma, chronic myelocytic leukemia, and carcinoma of the ovary.
• Hydroxyurea used concomitantly with irradiation therapy is used for carcinomas of the
head and neck.
• Hydroxyurea is also approved for use in the treatment of adult sickle cell disease.