Anticancer Agents

Question 1

A semi-synthetic analogue of camptotechin given intravenously and is a prodrug used in combination with fluorouracil and folinic acid for the treatment of advanced colorectal cancer.

Answer 1

Irinotecan

Question 2

An antisense drug designed to inhibit the mRNA molecules that code for proteins which suppress apoptosis.

Answer 2

Oblimersen (Antisense therapy)

Question 3

A natural product that reacts with nucleophiles to produce diradial species. Its reaction with DNA ultimately leads to cutting of the DNA chains.

Answer 3

Calicheamicin (Chain cutters)

Question 4

It is the most commonly used alkylating agent in cancer chemotherapy. The metabolism of which produces acrolein which is toxic to the bladder and kidneys.

Answer 4

Cyclophosphamide

Question 5

An alkylating agent that can cause intrastrand cross-linking preferred over Cisplatin for the intravenous treatment of advances ovarian tumors because it has less severe side effects.

Answer 5

Carboplatin

Question 6

A thiopurine prodrug which is converted to its correspondong monophosphate that inhibits purine synthesis.

Answer 6

6-mercaptopurine

Question 7

An anti-metabolite that is very similar in structure to the natural folates differing only in additional amino acids and methyl groups. It inhibits the enyme dihydrofolate reductase which is responsible in maintaining levels of the enzyme cofactor tetrahydrofolate.

Answer 7

Methorexate

Question 8

This drug acts as a prodrug for a suicide inhibitor. It is converted in the body to the fluorinated analogue of 2’-deoxyuridylic acid monophosphate which then combines with the enzyme thymidylate synthase and the cofactor.

Answer 8

5-fluorouracil

Question 9

An anti-leukemia drug isolated from Streptomyces antibioticus and is a powerful inhibitor of Adenosine deaminase.

Answer 9

Pentostatin

Question 10

A prodrug analogue of 2’-deoxycytidine which inhibits DNA polymerases.

Answer 10

Cytarabine

Question 11

Glucocorticoids for anti-cancer therapy (2)

Answer 11

• prednisolone
• prednisone

Question 12

Oestrogens for anti-cancer therapy. They inhibit the production of luteinizing hormone (LH) to decrease testosterone synthesis. (3).

Answer 12

• Ethinylestradiol (oestradiol derivative)
• Diethylstilbestrol (non-steroidal estrogen)
• Fosfestrol (diphosphate prodrug of diethylstilbestrol)

Question 13

Progestins for anti-cancer therapy (2).

Answer 13

• Medroxyprogesterone acetate
• Megesterol acetate

Question 14

Androgens for anti-cancer therapy (2).

Answer 14

• Fluoxymesterone
• Testosterone propionate

Question 15

A decapeptide analogue of the luteinizing hormone-releasing hormone designed to be more resistant to peptidase degradation.

Answer 15

Goserelin

Question 16

A reversible competitive inhibitor of the enzyme aromatase (breast cancer). The design of which is based on the structure of aminoglutethimide.

Answer 16

Anastrozole

Question 17

This mode of therapy involves an antibody which has catalytic activity designed to activate a prodrug.

Answer 17

Antibody-directed abzyme prodrug (ADAPT)

Question 18

This mode of therapy involves the delivery of a gene that codes for an enzyme capable of activating an anticancer prodrug into a cancer cell.

Answer 18

Gene-directed enzyme producing therapy

(GDEPT)

Question 19

This involves the irradiation of tumors containing porphyrin phososensitizers resulting to the production of reactive oxygen species whicha re fatal to the cell.

Answer 19

Photodynamic Therapy

Question 20

This therapy involves an antibody-enzyme conjugate that is targeted to specific cancer cells. Once the antibody has becpme attached to the outer surface of cancer cells, a prodrug is administered which is activated by the enzyme at the tumor site.

Answer 20

Antibody-directed enzyme producing therapy (ADAPT)