DNA Intercalating Agents

Question 1

Dactinomycin MOA

Answer 1

anti-tumor antibiotic

1) intercalates b/w C-G on DNA
2) this complex interferes w/ DNA-dependent RNA pol = inhibition of transcription
3) ss breaks in DNA

Question 2

Dactinomycin USES

Answer 2

Wilm’s tumor, rhabdomyosarcoma, Ewing’s sarcoma

Question 3

Dactinomycin Toxicity

Answer 3

hematopoietic suppression with pancytopenia

Question 4

Anthracycline Antibiotics Names

Answer 4

Daunorubicin, Doxorubicin, Epirubicin, Idarubicin

Question 5

Anthracyclines MOA

Answer 5

1) intercalate b/w DNA base pairs
2) Drug&raquo_space; Superoxide&raquo_space; H2O2 + Fe&raquo_space; Hydroxyl Radical
3) Hydroxyl radical cleaves DNA

Question 6

Daunorubicin USE

Answer 6

AML

Question 7

Idarubicin USE

Answer 7

AML

Question 8

Doxorubicin USE

Answer 8

broad spectrum

sarcomas, breast/lung carcinomas, malignant lymphomas

Question 9

Epirubicin

Answer 9

metastatic breast cancer and gastric cancer

Question 10

Anthracyclines Toxicity

Answer 10

irreversible dose-dependent cardiotoxicity (cardiomyopathy)

Question 11

Bleomycin MOA

Answer 11

2 copper chelating peptides

1) binds to DNA
2) induces ss and ds DNA breaks following oxidation and free radical formation

Question 12

Bleomycin USES

Answer 12

testicular tumors (w/vinblastine OR etoposide)
squamous cell carcinomas and lymphomas

Question 13

Bleomycin Toxicity

Answer 13

pulmonary fibrosis 
cutaneous toxicity (hyperpigmentation, hyperkeratosis, erythema)