Basic CHEMOTHERAPEUTICS of Malignant Diseases plus MCQs

MCQs are below…and steadily growing, so check back later!
Chemotherapy is most effective against replicating tumor cells. This is why some drugs target the cells as they are replicating.
Some drugs are cell cycle–nonspecific agents, however, the can be useful against tumors with few replicating cells.


Mechanism(s) of action for anthracycline anticancer agents:
A) blockade of DNA & RNA synthesis by intercalation
B) alteration of membrane fluidity partially correct: may disrupt ion transport
C) generation of oxygen free radicals partially correct: generation of semiquinoine free radicals and oxygen free radicals may also account for cadiotoxicity
D) all of the above

Major clinical use of this antracycline anticancer, antibiotic is in treatment of acute leukemia.
A) dactinomycin (Cosmegen) not an anthracycline: used in combination with surgery and vincristine (Oncovin) (+/- radiation) for Wilms’ tumor; along with methotrexate for treatment of gestational choriocarcinoma.
B) bleomycin (Blenoxane) not an anthracycline: may be curative in combinaton with vinblastine and cisplatin for testicular cancers. Many other uses.
C) daunorubicin (DaunoXome) much narrower spectum of action compared to doxorubicin

D) doxorubicin (Adriamycin) Major applications in treating carcinomas: breast, endometrial, ovarian, testicular, thyroid, lung. Effective in treating many sarcomas as well.

Among anticancer antibiotics: most toxic–
A) plicamycin (Mithramycin)
B) dactinomycin (Cosmegen)
C) doxorubicin (Adriamycin) bone-marrow suppression and cummulative, perhaps irreversible cardiotoxicity.
D) bleomycin (Blenoxane)

Antibiotic anticancer drug that is bioactivated to an alkylating agent. Hypoxic solid tumor stem cells may be most susceptible.
A) doxorubicin (Adriamycin)
B) mitomycin (Mutamycin) Used in combination protocols for treatment of squamous cell cervical carcinoma and for adenocarcinoms of stomach, pancreas and lung. Also, intravesical treatment of small bladder papillomas
C) vincristine (Oncovin) not an antibiotic anticancer drug: acts by depolymerizing microtubules
D) plicamycin (Mithramycin) Effective in reversing hypercalcemia associated with cancer; may be useful in treating testicular cancer, refractory to other therapy

Anthracycline analog useful in treating acute myeloid leukemia; In combination with cytarabine (ARA-C), it can produce complete remissions in patients with acute myelogenous leukemia.
A) plicamycin (Mithramycin) not an anthracycline:not used in treating leukemia.
B) idarubicin (Idamycin)
C) bleomycin (Blenoxane) used in treating testicular cancer;many squamous cell carcinomas. Used in combination therapy for lymphomas
D) paclitaxel (Taxol) not an anthracycline antibiotic

Anticancer drug: acts on osteoclasts to decrease serum calcium levels (independent of its antitumor action)
A) dactinomycin (Cosmegen)
B) doxorubicin (Adriamycin)
C) bleomycin (Blenoxane)
D) plicamycin (Mithramycin) mainly used to manage hypercalcemia.

Cancer type relatively resistant to treatment:
A) diffuse large cell lymphoma
B) Wilm’s tumor
C) choriocarcinoma
D) colon cancer
E) testicular cancer

Combination chemotherapy:
A) should involve drugs with comparable mechanisms differing mechanisms preferred
B) may be used in combination with surgical and radiation intervention
C) should involve drugs with differing toxicity profiles
D) B & C
E) A, B & C

Examples of malignant disorders that are likely curable by a combination chemotherapy:
A) colon cancer
B) testicular cancer lymphoma also
C) both
D) neither

Chemotherapeutic (anticancer) dosing principles:
A) drug should be administered at law or the maximum doses but with increased frequency drug should be administered near their maximum individual doses
B) drug should be administered infrequently to minimize side effects drug should be administered infrequently as possible-to maximize dose intensity-limiting tumor regrowth
C)  drugs more beneficial if major toxicities are nonoverlapping
D) drugs rarely effective in combination often more effective in combination due to possible synergism

Characteristics of anticancer alkylating agents (Polly functional):
A) cell-cycle specific
B) example: chlorambucil (Leukeran) other examples include,among primary agents: cyclophosphamide (Cytoxan), mechlorethamine (Mustargen), and melphalan (Alkeran)
C) both
D) neither

Major mechanism of action: polyfunctional alkylating agents
A) alkyl group transfer to mitotic proteins
B) interaction with carboxyl, sulfhydryl, amino, hydroxyl, and phosphate groups of non-nuclear cellular constituents
C) alkylation of DNA
 D) B & C
 E) A, B & C

Toxicity/toxicities associated with polyfunctional alkylating anticancer drugs:
A) nausea and vomiting
B) bone marrow suppression
C) gonadal toxicity
D) A & B
E) A, B & C

Prodrug-requires activation by microsomal enzyme system:
A) chlorambucil (Leukeran)
B) semustine (methyl CCNU)
C) thiopeta (Thioplex)
D) cyclophosphamide (Cytoxan)

E)  mechlorethamine (Mustargen)

Bone marrow suppression is worse when alkylating agents are combined with other myelosuppressive drugs and/or radiation
A) true
B) false

Common long-term consequence of alkylating agent treatment:
A) ovarian failure
B) acute leukemia
C)  testicular failure
D)  A & C
E)  A, B & C

Most useful alkylating agent at present
A) busulfan (Myleran) specificity for granulocytes; useful in chronic myelogenous leukemia
B)   melphalan (Alkeran)
C)    mechlorethamine (Mustargen)
D)  cyclophosphamide (Cytoxan)
E)   thiopeta (Thioplex)

Oral Route of Administration available:
A) melphalan (Alkeran)
B) busulfan (Myleran)
C) chlorambucil (Leukeran)
D) cyclophosphamide (Cytoxan)
E) all the above

Nitrosoureas:not cross-reactive (with respect to tumor resistance) with other alkylating drugs
A) true
B) false

Major route of elimination for nitrosoureas:
A) hepatic
B)  pulmonary
C)  renal

Characteristic(s) of nitrosoureas:
A) sparingly lipid-soluble highly lipid-soluble, crossing the blood-brain barrier easily-useful in treating brain tumors
B) more effective against cells in exponential growth phase more effective against cells in the total phase rather than exponential growth phase
C) acts by cross-linking DNA
 D) B & C

 E) A, B & C

Most likely to be effective in insulin-secreting islet cell pancreatic carcinoma and sometimes in non-Hodgkin’s lymphoma:
A) busulfan (Myleran)
B)  mechlorethamine (Mustargen)
C) cyclophosphamide (Cytoxan)
D) streptozocin (Zanosar)
E) thiopeta (Thioplex)

In combination with bleomycin (Blenoxane) and vinblastine (Velban)-curative for nonseminomatous testicular cancer:
A) dacarbazine (DTIC) clinical use: melanoma, Hodgkin’s disease, soft tissue sarcoma– alkylating agent
B) procarbazine (Matulane) active in Hodgkin’s disease (with combination therapy)
C) cisplatin (Platinol) also effective in ovarian and bladder cancer; cisplatin (Platinol) inhibits DNA synthesis by cross-linking and guanine N7 site
E) altretamine (Hexalen) ovarian carcinoma; relatively mild myelosuppressive effects

A patient with fluorouracil-nonresponsive colon cancer is given this prodrug which following activation is a topoisomerase I inhibitor. Following administration, the patient experiences very severe diarrhea which causes hypovolemia. This drug probably was:
A) vincristine (Oncovin)
B) irinotecan (Camptosar)
C) paclitaxel (Taxol)
D) docetaxel (Taxotere)
Active in late S-G2 phase of the cell cycle, the mechanism of this semisynthetic derivative of podophyllotoxin anticancer drug is through inhibition of topoisomerase II.
A) vincristine (Oncovin) acts on microtubules (depolymerization)
B) paclitaxel (Taxol) enhances tubulin polymerization
C) topotecan (Hycamtin) inhibits the action of topoisomerase I
D) etoposide (VP-16,VePe-sid)
Derivative from the Western Yew and European Yew tree, this anticancer drug acts by enhacing tubulin polymerization.
A) vincristine (Oncovin) not derived from the Yew; depolymerizes microtubules
B) paclitaxel (Taxol) useful in treating ovarian and advanced breast cancer
C) irinotecan (Camptosar) its active metabolite is a topoisomerase I inhibitor; used in treating color and recal cancer.
D) etoposide (VP-16,VePe-sid) active as a topoisomerase II inhibitor

May be useful in control of metastatic ovarian cancer, this topoisomerase I inhibitor’s dose-limiting adverse effects include: neutropenia, thromobcytopenia and anemia.
A) vincristine (Oncovin)
B) topotecan (Hycamtin)
C) doxorubicin (Adriamycin) mechanism of action includes topoisomerase II inhibition.
D) mitomycin (Mutamycin) following metabolism: an alkylating agent
Administration of this plant alkaloid anticancer agent is associated with significant incidence of neurotoxicity.
A) topotecan (Hycamtin)
B) vincristine (Oncovin)
C) vinblastine (Velban)
D) prednisone (Deltasone)
Anticancer agent that works by depolymerization of microtubules:
A) azatadine (Optimine)
B) vinblastine (Velban)
C) cladribine (Leustatin)
D) methotrexate
microtubular depolymerization results in mitotic arrest
Leucovorin “rescue”
A) busulfan (Myleran)
B) mercaptopurine (Purinethol)
C) methotrexate
D) daunorubicin (DaunoXome)
Leucovorine (ctrovorum factor) is used following methotrexate overdosage (accidental) or after very high-dose methotrexate protocols. Leucovorin is used along with certain chemotherapy drugs in the treatment of cancer. Most of the complications and side effects of methotrexate can be either prevented or treated by using leucovorin, which is usually given 24 hours after
This pyrimidine analog is used systemically to treat adenocarcinomas, topically for skin cancer and works through inhibition of DNA synthesis.
A) cytarabine (ARA-C)
B) vinblastine (Velban)
C) fluorouracil (5-FU)
D) cladribine (Leustatin)
Folic acid antagonist: binds to catalytic site of dihydrofolate reductase-
A) altretamine (Hexalen)
B) cisplatin (Platinol)
C) methotrexate
 D) fludarabine (Fludara)
in addition to anticancer action, methotrexate is used to treat rheumatoid arthritis
Q. Which cancers are most most vulnerable to chemotherapeutic agents?
1. Cancers that are rapidly dividing
2. Cancers that are not rapidly dividing (examples: colon and lung carcinoma )

Q: What is the most severe emetogenic cancer drug?
1. cisplatin (Platinol)
2. Big Mac
Not all chemotherapeutic drugs are equally emetogenic:
Most severe: cisplatin (Platinol)
 Dacarbazine (DTIC)
 Doxorubicin (Adriamycin, Rubex, Doxil)
Relatively mild– antimetabolites:
Flurouracil (5-FU)
Agents that cause the most significant hair loss:
Cyclophosphamide (Cytoxan)
Dactinomycin (Cosmegen)
Doxorubicin (Adriamycin, Rubex, Doxil)
Paclitaxel (Taxol)
Vincristine (Oncovin)
3. a benign epithelial cell neoplasm derived from non-glandular surfaces is referred to as:
A. papilloma
B. sarcoma
C. adenoma
D. hamartoma
E. squamous cell carcinoma
1. a malignant epithelial cell neoplasm derived from any of the three(e) germ layers is referred to as:
A. sarcoma
B. carcinoma
C. teratoma
D. mixed cell tumor
E. adenoma
The following are characteristics  of a tumor cells except
A)Dedifferentiation and loss of function
B) controlled  proliferation
C) Invasiveness
D) Metastatic potential
Which of the following agents shows Cell –Cycle-Specific cytotoxicity ?
A) Methotrxate (S -phase)
B) Dactinomysin
C) Cisplatin
D) Mechlorethamine
Combination of Allupurinol with this anticancer drug can cause increase in toxicity.
A)  6 thioguanine
B)  Flurouracil
C)  6 mercaptopurine
D)  Azathdine

034. Action mechanism of anticancer drugs belonging to plant alkaloids:
a) Inhibition of DNA-dependent RNA synthesis
b) Cross-linking of DNA
c) Mitotic arrest at a metaphase
d) Nonselective inhibition of aromatases
035. General contraindications for anticancer drugs are:
a) Depression of bone marrow
b) Acute infections
c) Severe hepatic and/or renal insufficiency
d) All of the above
036. Action mechanism of methotrexate is:
a) Inhibition of dihydrofolate reductase
b) Activation of cell differentiation
c) Catabolic depletion of serum asparagine
d) All of the ab
037. Tick the anticancer drug belonging to inorganic metal complexes:
a) Dacarbazine
b) Cisplatin
c) Methotrexate
d) Vincristine

030. Tick the anticancer drug, a pyrimidine antagonist:
a) Fluorouracil
b) Mercaptopurine
c) Thioguanine
d) Methotrexate
031. Methotrexate is:
a) A purine antagonist
b) A folic acid antagonist
c) An antibiotic
d) An alkylating agent
032. Tick the antibiotic for cancer chemotherapy:
a) Cytarabine
b) Doxorubicin
c) Gentamycin
d) Etoposide
033. Fluorouracil belongs to:
a) Antibiotics
b) Antimetabolites
c) Plant alkaloids
d) Bone marrow growth factor

027. Tick the anticancer alkylating drug, a derivative of alkylsulfonate:
a) Fluorouracil
b) Carboplatin
c) Vinblastine
d) Busulfan
028. Tick the anticancer drug of plant origin:
a) Dactinomycin
b) Vincristine
c) Methotrexate
d) Procarbazine
029. Action mechanism of alkylating agents is:
a) Producing carbonium ions altering protein structure
b) Producing carbonium ions altering DNA structure
c) Structural antagonism against purine and pyrimidine
d) Inhibition of DNA-dependent RNA synthesis

023. Rational combination of anticancer drugs is used to:
a) Provide synergism resulting from the use of anticancer drugs with different mechanisms combination
b) Provide synergism resulting from the use of anticancer drugs with the same mechanisms combination
c) Provide stimulation of immune system
d) Provide stimulation of cell proliferation
024. Tick the anticancer alkylating drug, a derivative of chloroethylamine:
a) Methotrexate
b) Cisplatin
c) Cyclophosphamide
d) Carmustine
025. Tick the anticancer alkylating drug, a derivative of ethylenimine:
a) Mercaptopurine
b) Thiotepa
c) Chlorambucil
d) Procarbazine
026. Tick the group of hormonal drugs used for cancer treatment:
a) Mineralocorticoids and glucocorticoids
b) Glucocorticoids and gonadal hormones
c) Gonadal hormones and somatotropin
d) Insulin

019. Tick the unwanted effects of didanozine:
a) Hallucinations, dizziness, insomnia
b) Anemia, neutropenia, nausea
c) Hypertension, vomiting, diarrhea
d) Peripheral neuropathy, pancreatitis, diarrhea, hyperuricemia
022. All of the following effects are disadvantages of anticancer drugs, EXCEPT:
a) Low selectivity to cancer cells
b) Depression of bone marrow
c) Depression of angiogenesis
d) Depression of immune system

9. mechanism of anticancer drugs belonging to plant alkaloids:
a) Inhibition of DNA-dependent RNA synthesis
b) Cross-linking of DNA
c) Mitotic arrest at a metaphase
d) Nonselective inhibition of aromatases

All of the following Anticancer agents cause bone marrow depression except?
A. Chlorambucil
B. Daunorubicin
C. Doxorubicin
D. Flutamide

Correct answer : D. Flutamide
Side effects of flutamide are gynaecomastia, breast tenderness, liver damage, nausea and hot flushes. It has anti androgenic action.

Major toxicity of alkylating drugs:
A) alopecia
B) myelosuppression
C) renal damage
D) hepatic failure

Most common route of administration for cyclophosphamide (Cytoxan):
A) iv
B) oral
Little effect on the bone marrow: can cause significant renal dysfunction and sometimes acoustic nerve dysfunction.
A) methotrexate
B) cisplatin (Platinol)
C) lomustine (CCNU,CeeNU)
D) A & C

carboplatin, an analog, has less GI and renal toxicity but is myelosupressive.

Anticancer drug that is also used to treat psoriasis and rheumatoid arthritis:
A) mercaptomurine (6-MP)
B) methotrexate
C) procarbazine (Matulane)
D) allopurinol (Zyloprim, Purinol)

Q. What is the most likely adverse respone as a result of VINCRISTINE? 
a. nephrotoxicity,renal damage/failure 
c.Peripheral sensory and motor neuropathy 
d.pulmonary damage 

Vincristine is one of relatively few cytotoxic anticancer drugs that donot cause bone marrow suppression. 
rather vincristine causes 
neuropathies(motor & sensory) 
hearing loss can also occur 
muscle weakness and obtunded reflexes latter 
VINCRISTINE differs from other two vinca alkaloids,VINBLASTINE AND VINORELBINE, which do cause bone marrow suppression(and not neuropathies) 
VINCRISTINE WITH GLUCOCORTICOIDS is treatment of choice in childhood leukemia,pediatric solid tumors(wilms tumor,rhabdomyosarcoma,neuroblastoma) and lymphoma. 
All vinca alkaloids bind to tubulin and impair microtubular assembly,preventing mitosis(M-phase specific)

Q. Which antineoplastic drug is frequently used in combination therapy for testicular cancer?
A. Bleomycin
B. Cisplatinum
C. Etoposide
D. Leuprolide
E. Vinblastine

Answer B
1. Cisplatin is often combined with other chemotherapeutic agents for treatment of solid malignancies. The agent is used to treat cancers, including sarcomas, lung cancer, lymphomas and testicular tumors
2. Cisplatin is very effective against testicular cancer with a cure rate ranging from 10-90%
3. Major toxicity of cisplatin is nephrotoxicity. The dose should be reduced in patients with renal failure. All patients should be well hydrated and undergo diuresis to prevent kidney damage after drug infusion.
4. Nerve toxicity can also occur and to prevent lawsuits, patients must be examined prior to drug

File:Cross-linked DNA by nitrogen mustard.png

File:Cell cycle simple.png

File:Deoxcytidine, Gemcitidine and Decitabine.png

File:Microtubules and alkaloids.png
File:Topoisomerase Inhibitor.JPG

Cancer type Drugs Acronym
Breast cancer Cyclophosphamidemethotrexate5-fluorouracil CMF
Doxorubicin, cyclophosphamide AC
Hodgkin’s disease Mustine, vincristineprocarbazineprednisolone MOPP
Doxorubicin, bleomycinvinblastinedacarbazine ABVD
Non-Hodgkin’s lymphoma Cyclophosphamide, doxorubicin, vincristine, prednisolone CHOP
Germ cell tumor Bleomycin, etoposidecisplatin BEP
Stomach cancer Epirubicin, cisplatin, 5-fluorouracil ECF
Epirubicin, cisplatin, capecitabine ECX
Bladder cancer Methotrexate, vincristine, doxorubicin, cisplatin MVAC
Lung cancer Cyclophosphamide, doxorubicin, vincristine, CAV
Colorectal cancer 5-fluorouracil, folinic acidoxaliplatin FOLFOX
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