1.
Name the 3 subclasses of alkylating agents.
Correct Answer(s)
A. Nitrogen Mustards
C. Nitrosureas
D. Platinum Compounds
Explanation
Folate antagonists and Nucleotide analogs are both subclasses of Antimetabolites.
2.
This Nitrogen Mustard will not cross the Blood Brain Barrier (BBB).
Correct Answer(s)
Cyclophosphamide
Explanation
Consequently cyclophosphamide is NOT useful for treating metastasis to the brain.
3.
This alkylating agent has delayed-type bone marrow suppression. Answer as follows: Subclass, Drug.
Correct Answer(s)
Nitrogen mustards, Mechlorethamine
Nitrogen mustard, Mechlorethamine
Explanation
This is the Dose Limiting Toxicity associated with Mechlorethamine usage.
4.
This drug is a bifunctional agent that is used to treat chronic lymphocytic leukemia and non-Hodgkins lymphoma. (Answer as Subclass, Drug)
Correct Answer(s)
Nitrogen mustard, Bendamustine
Nitrogen mustards, Bendamustine
Explanation
Functions as both an alkylator and purine-like antimetabolite.
5.
This drug traps Acrolein and protects from bladder toxicities but has NO anticancer activity.(Answer: Class, Drug)
Correct Answer(s)
Ancillary agents, Mesna
Ancillary agent, Mesna
Explanation
This is often given with cyclophosphamide, a Nitrogen Mustard drug that produces the toxic chemical Acrolein following bioactivation by liver P450 and CYP2B6.
6.
Which of the following are Antimetabolites? (Select all that apply)
Correct Answer(s)
A. Methotrexate
B. Capecitabine
D. Hydroxyurea
E. 5-Fluorouracil
Explanation
Methotexate- Folate antagonist
Capecitabine, 5-Fluorouracil - Nucleotide analogs
Hydroxyurea- other (Blocks ribonucleotide reductase)
7.
Name the 3 Nitrosureas in alphabetical order. (Answer: Drug, Drug, Drug)
Correct Answer(s)
Carmustine, Lomustine, Streptozocin
Explanation
Nitrosureas form interstrand crosslinks. O6 of guanine is the preferred site of attack.
8.
Following treatment with Methotrexate, this drug is used to "rescue" cells. (Class, Drug)
Correct Answer(s)
Ancillary agents, Leucovorin
Ancillary agent, Leucovorin
Explanation
This drug is a reduced form of folic acid. Recall that Methotrexate competitively inhibits Dihydrofolate Reductase, an enzyme required for the continued synthesis of Thymidine (Nucleotide required for DNA synthesis/replication).
9.
This Platinum Compound lacks cross-resistance with the other two platinum compounds.
Correct Answer(s)
Oxaliplatin
Explanation
The other two Platinum Compounds (which are alkylating agents) are Cisplatin and Carboplatin.
10.
Which of the following is commonly used to treat pancreatic islet cell carcinoma and pancreatic adenocarcinoma due to its enhanced uptake by pancreatic beta cells? (Note it is also used to treat colorectal cancer)
Correct Answer
D. Streptozocin
Explanation
Streptozocin is a Nitrosurea, along with Carmustine and Lomustine. Bendamustine is a Nitrogen Mustard. Capecitabine is an antimetabolite- nucleotide analog similar to 5-FU.
11.
The mechanism of action of this drug is as follows:Loses Cl-; forms carbonium ion that attacks nucleophiles.It has a half life of less than 10 minutes following IV injection.Answer: Class, Subclass, Drug
Correct Answer
Alkylating agents, Nitrogen mustards, Mechlorethamine
Alkylating agent, Nitrogen mustard, Mechlorethamine
Explanation
Resistance to this drug is acquired by increasing the inactivation of the drug and decreasing uptake.
Mechlorethamine is highly unstable and reactive. Its half-life is < 10 minutes. It is given via IV injection.
12.
Which of the following drugs are used to treat glioblastomas?
Correct Answer(s)
B. Lomustine
C. Carmustine
D. Temozolomide
Explanation
The more commonly used drug for glioblastomas is Temozolomide (listed as "other alkylators"). Note that Carmustine is a Nitrosurea.
13.
What chemo agent's DLT includes ALL of the following:NephrotoxicityNeurotoxicityOtotoxicityMinimal marrow toxicityAnswer: Class, Subclass, Drug
Correct Answer(s)
Alkylating agents, Platinum compounds, Cisplatin
Alkylating agent, Platinum compound, Cisplatin
Explanation
Cl- diuresis reduces toxicity of Cisplatin. Other side-effects of this drug include Nausea and Vomiting.
14.
This drug is activated by HGPRTase, thus resistance is acquired via decreased activity of HGPRTase.
Correct Answer
B. 6-Mercaptopurine
Explanation
Note that some of the above drugs require some sort of bioactivation:
Cyclophosphamide via liver P450 and CYP2B6.
Temozolomide is metabolized to 5-amino-imidizole-4-carboxamide.
15.
The following Alkylating Agent has a high oil-to-water partition coefficient, thus bone marrow suppression from it may persist due to storage in adipose tissue and liver. Answer: Subclass, Drug
Correct Answer
Nitrosureas, Carmustine
Nitrosurea, Carmustine
Explanation
Resistance to Carmustine is acquired by increased DNA repair. It is used to treat glioblastomas and brain tumors.
16.
Which drug has the following characteristics:Mechanism: Inhibits DNA polymerase alpha causing termination of DNA synthesisResistance: Cytidine deaminase detoxificationToxicity: Potent myelosuppressive, neurotoxicity with renal impairmentADME: Sensitive to dosing scheduleOther: Combo therapy for leukemias
Correct Answer
C. Cytosine Arabinoside
Explanation
Note that Bendamustine (A nitrosurea) is also used to treat certain types of Leukemias.
17.
This drug is an Alkylating Agent that is less toxic than cisplatin, but also less active.Answer: Subclass, Drug
Correct Answer
Platinum Compounds, Carboplatin
Platinum Compound, Carboplatin
Explanation
Platinum compounds (Cisplatin, carboplatin, oxaliplatin) generate DNA cross-links.
18.
Of the following Antimetabolites, which is/are Folate Antagonists?
Correct Answer
E. Methotrexate
Explanation
Recall Methotrexate competitively inhibits Dihidrofolate Reductase, thus inhibiting synthesis of Thymidine.
19.
This alkylator is localized to the liver and has an increased half-life. It's DLT includes bone marrow suppression.ADME: Dose IVUsed to treat Melanoma, Hodgkin's DiseaseAnswer: Drug
Correct Answer
Dacarbazine
Explanation
Dacarbazine is listed under the subclass "Other Alkylators".
20.
5-Fluorouracil is a pyrimidine analog that irreversibly inhibits Thymidylate Synthase. What drug is an analog of 5-FU?Answer: Drug
Correct Answer
Capecitabine
Explanation
ADME: Oral dosing, generates 5-FU in tumor cells
Used to treat: Metastatic breast cancer. Also injected into hepatic artery for treatment of colon carcinoma metastasis to the liver.
21.
What drug fits the following criteria:Lacks cross-resistance with other alkylating agents.Toxicity: Secondary leukemia or lung cancerDLT: PneumonitisADME: Oral, non-cell cycle phase specificAnswer: Drug
Correct Answer
Procarbazine
Explanation
Procarbazine is listed under the subclass "Other Alkylators".
22.
Resistance to which of the following drugs is due to cellular acquisition of Aldehyde Oxidase?
Correct Answer
B. Cyclophosphamide
23.
A patient is recieving ongoing treatment for gliobastoma. Select all of the following that could be used to treat this tumor.
Correct Answer(s)
B. Carmustine
C. Lomustine
E. Temozolomide
24.
Patients with a deficiency in Dihydrothymidine Dehydrogenase can have a fatal interaction with which of the following drugs:
Correct Answer
B. 5-Fluorouracil
25.
There is a risk of secondary neoplasia, bone marrow suppression, as well as birth defects associated with which chemotherapy drug that is commonly used to treat chronic and acute myelogenous leukemia (CML and AML):
Correct Answer
A. Hydroxyurea
26.
A patient is being treated for Hodgekins disease. More than one of the following drugs are commonly used to treat patients with this condition. Which ones are they?
Correct Answer(s)
C. Dacarbazine
D. Methotrexate
27.
Which of the following is administered orally due to the fact that it is readily absorbed by the GI tract?
Correct Answer
D. Lomustine
28.
Name, in alphabetical order, the 4 drugs that fit the following criteria:Class: AntimetabolitesSublcass: Nucleotide AnalogsAlphabetize drugs with numbers by the first letter after the number and a hyphen, i.e. 8-Drug.
Correct Answer
Capecitabine, Cytosine Arabinoside, 5-Fluorouracil, 6-Mercaptopurine
29.
This chemo drug is commonly used to treat small-cell and non small-cell lung cancers as well as ovarian cancer.
Correct Answer
Carboplatin
carboplatin