Anticancer drugs

Question 1

What are the 6 classes of anticancer drugs?

Answer 1

• Alkylating Agents
• Antimetabolites
• Natural Products
• Antitumor Antibiotics
• Hormonal Agents
• Miscellaneous

Question 2

What is the largest and most diverse class of anticancer drugs?

Answer 2

Alkylating Agents

Question 3

What is the MOA of alkylating anticancer drugs?

Answer 3

Either alkylate DNA or interfere by crosslinking (platinum compounds)

Question 4

What are the 4 groups of alkylating agents?

Answer 4

• Nitrogen Mustards
• Nitrosureas
• Alkyl Sulfonate
• Platinum Analogs

Question 5

What are the 2 nitrogen mustards?

Answer 5

Cyclophosphamide and Chlorambucil

Question 6

What are the 2 platinum analogs?

Answer 6

Cisplatin, carboplatin

Question 7

What are the 3 antimetabolites?

Answer 7

Methotrexate, 6-Mercaptopurine (6-MP), 5 Fluorouracil (5-FU)

Question 8

What are the 2 plant-based anticancer drugs?

Answer 8

Vincristine, Paclitaxel (Taxol)

Question 9

What are the 3 antitumor antibiotics?

Answer 9

Dactinomycin, Doxorubicin, Bleomycin

Question 10

What are the 3 anticancer Hormonal Agents?

Answer 10

Corticosteroids, Tamoxifen, Fulvestrant

Question 11

What is the MOA of -ibs anticancer drugs? What is one example?

Answer 11

Inhibitors of growth factors receptors
Imatinib

Question 12

What is the MOA of -mabs anticancer drugs? What are 2 examples?

Answer 12

Bind to specific receptors to inhibit proliferation; Trastuzumab, Rituximab

Question 13

What are the pharmacokinetics of Cisplatin?

Answer 13

• Highly bound to plasma proteins
• Concentrates in kidney, intestine, testes
• Poorly penetrates BBB
• Slowly excreted in urine

Question 14

Compare Cisplatin and Carboplatin

Answer 14

Carboplatin – better tolerated but not as effective as Cisplatin

Question 15

What are the uses for Cisplatin?

Answer 15

• Testicular cancer (85% - 95 % curative )
• Ovarian cancer
• Other solid tumors: lung, esophagus, gastric

Question 16

What is the MOA of Cisplatin?

Answer 16

Cisplatin enters cells → forms highly reactive platinum complexes → intra-strand and inter-strand cross links → DNA damage → inhibits cell proliferation

Question 17

What is the MOA of methotrexate?

Answer 17

Inhibits dihydrofolate reductase (DHFR) – Interferes with DNA/RNA synthesis

Question 18

What are the cytotoxic actions of methotrexate?

Answer 18

• Predominant on bone marrow
• Ulceration of intestinal mucosa
• Crosses placenta interferes with embryogenesis - fetal malformations and death

Question 19

Describe the immunosuppressive action of methotrexate

Answer 19

Prevents clonal expansion of B & T lymphocytes

Question 20

Describe the anti-inflammatory action of methotrexate

Answer 20

Interferes with release of inflammatory cytokines

Question 21

Proto-oncogenes versus Tumor Suppressors

Answer 21

Proto-oncogenes: a gene that helps cells grow and divide normally, but can mutate into an oncogene that causes cancer

Tumor suppressor genes: anti-oncogenes, genes that regulate cell division and replication to prevent cancer

Question 22

Carcinoma

Answer 22

Epithelial origin

Question 23

sarcoma

Answer 23

Connective tissue or muscle

Question 24

leukemias and lymphomas

Answer 24

Immune cells

Question 25

What are the 3 types of chemo?

Answer 25

Primary, neoadjuvant, adjuvant

Question 26

Differentiate between primary, neoadjuvant, adjuvant chemotherapy

Answer 26

Primary - primary treatment is chemotherapy
Neoadjuvant - chemo before and after surgery
Adjuvant - chemo after surgery

Question 27

What are the toxic effects of chemo?

Answer 27

Attacks rapidly dividing cells:
- Nausea & Vomiting, Bone marrow depression, Alopecia, Abortion, fetal death, teratogenicity, Carcinogenicity, Immunosuppression