Chemotherapy Drugs I

1. This alkylator is localized to the liver and has an increased half-life. It's DLT includes bone marrow suppression.
ADME: Dose IV
Used to treat Melanoma, Hodgkin's Disease

Answer: Drug

Dacarbazine is listed under the subclass "Other Alkylators".

Explanation

Dacarbazine is listed under the subclass "Other Alkylators".

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2. This Nitrogen Mustard will not cross the Blood Brain Barrier (BBB).

Consequently cyclophosphamide is NOT useful for treating metastasis to the brain.

Explanation

Consequently cyclophosphamide is NOT useful for treating metastasis to the brain.

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3. This Platinum Compound lacks cross-resistance with the other two platinum compounds.

The other two Platinum Compounds (which are alkylating agents) are Cisplatin and Carboplatin.

Explanation

The other two Platinum Compounds (which are alkylating agents) are Cisplatin and Carboplatin.

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5. This drug traps Acrolein and protects from bladder toxicities but has NO anticancer activity.
(Answer: Class, Drug)

This is often given with cyclophosphamide, a Nitrogen Mustard drug that produces the toxic chemical Acrolein following bioactivation by liver P450 and CYP2B6.

Explanation

This is often given with cyclophosphamide, a Nitrogen Mustard drug that produces the toxic chemical Acrolein following bioactivation by liver P450 and CYP2B6.

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6. 5-Fluorouracil is a pyrimidine analog that irreversibly inhibits Thymidylate Synthase. What drug is an analog of 5-FU?

Answer: Drug

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.

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.

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7. Of the following Antimetabolites, which is/are Folate Antagonists?

5-FU

Capecitabine

Cytosine Arabinoside

6-Mercaptopurine

Methotrexate

Recall Methotrexate competitively inhibits Dihidrofolate Reductase, thus inhibiting synthesis of Thymidine.

Explanation

Recall Methotrexate competitively inhibits Dihidrofolate Reductase, thus inhibiting synthesis of Thymidine.

8. What chemo agent's DLT includes ALL of the following:
Nephrotoxicity
Neurotoxicity
Ototoxicity
Minimal marrow toxicity

Answer: Class, Subclass, Drug

Cl- diuresis reduces toxicity of Cisplatin. Other side-effects of this drug include Nausea and Vomiting.

Explanation

Cl- diuresis reduces toxicity of Cisplatin. Other side-effects of this drug include Nausea and Vomiting.

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9. Name the 3 subclasses of alkylating agents.

Nitrogen Mustards

Folate Antagonists

Nitrosureas

Platinum Compounds

Nucleotide Analogs

Folate antagonists and Nucleotide analogs are both subclasses of Antimetabolites.

Explanation

Folate antagonists and Nucleotide analogs are both subclasses of Antimetabolites.

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10. This drug is an Alkylating Agent that is less toxic than cisplatin, but also less active.

Answer: Subclass, Drug

Platinum compounds (Cisplatin, carboplatin, oxaliplatin) generate DNA cross-links.

Explanation

Platinum compounds (Cisplatin, carboplatin, oxaliplatin) generate DNA cross-links.

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11. This drug is activated by HGPRTase, thus resistance is acquired via decreased activity of HGPRTase.

Hydroxyurea

6-Mercaptopurine

Cyclophosphamide

Temozolomide

Dacarbazine

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.

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.

12. Name the 3 Nitrosureas in alphabetical order. (Answer: Drug, Drug, Drug)

Nitrosureas form interstrand crosslinks. O6 of guanine is the preferred site of attack.

Explanation

Nitrosureas form interstrand crosslinks. O6 of guanine is the preferred site of attack.

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13. Patients with a deficiency in Dihydrothymidine Dehydrogenase can have a fatal interaction with which of the following drugs:

Methotrexate

5-Fluorouracil

Hydroxyurea

Cytosine Arabinoside

Oxaliplatin

14. Which drug has the following characteristics:

Mechanism: Inhibits DNA polymerase alpha causing termination of DNA synthesis
Resistance: Cytidine deaminase detoxification
Toxicity: Potent myelosuppressive, neurotoxicity with renal impairment
ADME: Sensitive to dosing schedule
Other: Combo therapy for leukemias

Bendamustine

5-Fluorouracil

Cytosine Arabinoside

6-Mercaptopurine

Leucovorin

Note that Bendamustine (A nitrosurea) is also used to treat certain types of Leukemias.

Explanation

Note that Bendamustine (A nitrosurea) is also used to treat certain types of Leukemias.

15. Following treatment with Methotrexate, this drug is used to "rescue" cells. (Class, Drug)

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).

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).

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16. Resistance to which of the following drugs is due to cellular acquisition of Aldehyde Oxidase?

Mechlorethamine

Cyclophosphamide

Bendamustine

Carmustine

Lomustine

17. 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)

Carmustine

Bendamustine

Capecitabine

Streptozocin

Lomustine

Streptozocin is a Nitrosurea, along with Carmustine and Lomustine. Bendamustine is a Nitrogen Mustard. Capecitabine is an antimetabolite- nucleotide analog similar to 5-FU.

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.

18. 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

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

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

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19. 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

Resistance to Carmustine is acquired by increased DNA repair. It is used to treat glioblastomas and brain tumors.

Explanation

Resistance to Carmustine is acquired by increased DNA repair. It is used to treat glioblastomas and brain tumors.

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20. What drug fits the following criteria:

Lacks cross-resistance with other alkylating agents.
Toxicity: Secondary leukemia or lung cancer
DLT: Pneumonitis
ADME: Oral, non-cell cycle phase specific

Answer: Drug

Procarbazine is listed under the subclass "Other Alkylators".

Explanation

Procarbazine is listed under the subclass "Other Alkylators".

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21. A patient is recieving ongoing treatment for gliobastoma. Select all of the following that could be used to treat this tumor.

Cyclophosphamide

Carmustine

Lomustine

Dacarbazine

Temozolomide

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22. This drug is a bifunctional agent that is used to treat chronic lymphocytic leukemia and non-Hodgkins lymphoma. (Answer as Subclass, Drug)

Functions as both an alkylator and purine-like antimetabolite.

Explanation

Functions as both an alkylator and purine-like antimetabolite.

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23. This alkylating agent has delayed-type bone marrow suppression. Answer as follows: Subclass, Drug.

This is the Dose Limiting Toxicity associated with Mechlorethamine usage.

Explanation

This is the Dose Limiting Toxicity associated with Mechlorethamine usage.

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24. Which of the following drugs are used to treat glioblastomas?

Cyclophosphamide

Lomustine

Carmustine

Temozolomide

Dacarbazine

The more commonly used drug for glioblastomas is Temozolomide (listed as "other alkylators"). Note that Carmustine is a Nitrosurea.

Explanation

The more commonly used drug for glioblastomas is Temozolomide (listed as "other alkylators"). Note that Carmustine is a Nitrosurea.

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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):

Hydroxyurea

Cytosine Arabinoside

6-Mercaptopurine

Bendomustine

Carmustine

26. Which of the following is administered orally due to the fact that it is readily absorbed by the GI tract?

5-FU

Mechlorethamine

Carmustine

Lomustine

Dacarbazine

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28. Which of the following are Antimetabolites? (Select all that apply)

Methotrexate

Capecitabine

Dacarbazine

Hydroxyurea

5-Fluorouracil

Methotexate- Folate antagonist
Capecitabine, 5-Fluorouracil - Nucleotide analogs
Hydroxyurea- other (Blocks ribonucleotide reductase)

Explanation

Methotexate- Folate antagonist
Capecitabine, 5-Fluorouracil - Nucleotide analogs
Hydroxyurea- other (Blocks ribonucleotide reductase)

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29. 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?

Bendamustine

Procarbazine

Dacarbazine

Methotrexate

5-FU

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