Antineoplasics

Question 0

cyclophophamide

Answer 0

bischloroethylamines (nitrogen mustards); alkylating agent
PO
activated in liver and tumors (tumor selective)

Question 1

Mechlorethamine

Answer 1

bischloroethylamines (nitrogen mustards); alkylating agent
IV
Short Half life
Most toxic

Question 2

nitrosoureas

Answer 2

alkylating agents, similar action to bischloroethylamines

cross BBB->brain tumor tx

Question 3

Procarbazine

Answer 3

alkylating agent
Multiple cytotoxic intermediates (alkylating and free radicals)
little cross resistance
leukemogenic 10-15%
used in MOPP for Hodgkin's lymphoma

Question 4

MOPP

Answer 4

Mechlorethamine, (oncovin) vincristine, procarbazine, prednisone
tx Hodgkin’s lymphoma

Question 5

Methotrexate

Answer 5

anti-metabolite
folic acid analog
DHFR inhibitor: blocks synthesis, of DNA, RNA, proteins
accumulates polyglutamates-> increased localization/toxicity
S phase specific
resistance: amplification of DHFR, DHFR mutation escape, decrease uptake, increased efflux (MRP 2/4)
Leucovorin used for “rescue”

Question 6

6-mercaptopurine

Answer 6

anti metabolite
purine antagonist
fraudulent incorporation
s phase specific
activated by hypoxanthine guanine phosphoribosyl transferase (HGPRT) 
inactivated by xanthine oxidase

Question 7

6-thioguanine

Answer 7

anti metabolite
purine antagonist
fraudulent incorporation
s phase specific
activated by hypoxanthine guanine phosphoribosyl transferase (HGPRT)

Question 8

Fluorouracil (5-FU)

Answer 8

Anti metabolite
Pyrimidine antagonist
metabolized to FdUMP
inhibits thymidylate synthetase (->thymineless death)
also fraudulent incorperation
s phase specific
IV usually
Synergistic effect with leucovorin

Question 9

Capecitabine

Answer 9

anti metabolite
pyrimidine antagonist
PO
activated selective in tumors
coln and refractory breast ca

Question 10

cytarabine (araC)

Answer 10

anti metabolite
pyrimidine analog
converted to araCTP
fraudulent incorporation halts polymeration
resistance from mutational loss of deoxycytine kinase

Question 11

anthracyclines (daunorubicin, doxorubicin)

Answer 11

antibiotic
broad spectrum
intercalating agent
topoisomerase II inhibitor
cardiac tocixity

Question 12

bleomycin

Answer 12

antibiotic
DNA strand scission
broad spectrum
no myelosuppresion
pulmonary toxicity
anaphylactic potential 
in ABVD for Hodgkin's lymphoma

Question 13

ABVD

Answer 13

Doxorubricin- anthracycline antibiotic
Bleomycin- antibiotic
vinblastine- mitotic spindle poison
dacarbazine- alkylating agent

Question 14

Vinblastine

Answer 14

Vinca alkyloid
M phase specific
AE N/V, bone marrow depression (does limiting)
resistance via tubulin gene mutation
in ABVD for Hodgkin's lymphoma

Question 15

vincristine

Answer 15

Vinca alkyloid
mitotic spindle poison
no acute side effects
AE dose limiting neurotoxicity
resistance via tubulin mutation
in MOPP for Hodgkin's lymphoma
tx acute childhood leukemia

Question 16

Paclitaxel (taxol)

Answer 16

mitotic spindle poison (disassembly)

ovarian and breast CA

Question 17

Topetcan, irinotecan

Answer 17

topoisomerase I inhibitor
s phase specific
blocks religation

Question 18

etoposide

Answer 18

topoisomerase II inhibitor
s phase specific
blocks religation

Question 19

Cisplatin, carboplatin

Answer 19

Platinum coordination
DNA Cross linking
cell cycle non specific
various combination regimens for ovarian and testicular CA
nephrotoxicity (hydration important)
acoustic nerve damage
resistance from dna repair machinery

Question 20

Tamoxiphen

Answer 20

SERM
Low AE (hot flashes, thrombosis, endrometrial CA)
requires ER+ tumors, breast or endrometrial ca
prophylactic tx in high risk
lower bone fx risk in post menopausal women

Question 21

raloxifene

Answer 21

anti CA hormone

breast CA with osteoporosis

Question 22

letrozole, anastrozole, exemestrane

Answer 22

aromatase inhibitors
post menopausal women
more effective then tamoxifen
no increase risk for thrombosis or uterine CA
AE joint px and lower bone density

Question 23

leuprolide

Answer 23

anti androgen
synthetic GnRH
few side effects

Question 24

flutamide

Answer 24

anti androgen receptor antagonist used with leuprolide to managae initial androgen flare short individual efficacy due to receptor mutation escape

Question 25

Prednisone

Answer 25

adrenocorticosteroid cause apoptosis in leukemic cells used in multidrug regimens (e.g. MOPP): leukemia, lymphoma, myeloma palliative for inflammation and nausea

Question 26

Erlotinib

Answer 26

targeted agent EGF receptor tyrosine kinase small molecule strong initial response with quick resistance Non small cell lung ca (nsclc) and head/neck CAs

Question 27

cetuximab

Answer 27

targeted agent EGF receptor tyrosine kinase monoclonal AB Colon and Head/neck CAs

Question 28

Lapatinib

Answer 28

targeted agent HER2 protein tyrosine kinase small molecule HER2+ breast CA (an aggressive variety)

Question 29

trastuzumab

Answer 29

``` targeted agent monoclonal AB HER2 protein tyrosine kinase (herceptin) Immune response and cytotoxic ```

Question 30

pertuzumab

Answer 30

targeted agent monoclonal AB HER2 protein tyrosine kinase breast ca

Question 31

Imatinib

Answer 31

``` targeted agent BCR/ABL tyrosine kinase small molecule CML GI stromal ca (kit mutation) Chronic Myelomonocytic leukemia (ETV6-PDGFR) ```

Question 32

Brentuximab vedotin

Answer 32

targeted agent monoclonal AB + mitotic spindle poison CD30 surface antigen (B cell specific): hodgkins and non Hodgkin's lymphoma anaplastic large cell lymphoma

Question 33

vemuratenib

Answer 33

targeted agent B-RAF (V600) tyrosine kinase 50% of melanoma