DNA Intercalating Agents

Question 1

DNA Intercalating Agents General Mechanism

Answer 1

Bind DNA through intercalation between specific bases, blocking DNA, RNA synthesis; cause DNA strands to break and interfere with cell replication; CCNS

Question 2

Dactinomycin (Actinomycin D, Cosmegen) Mech

Answer 2

Intercalates G-C base pairs of DNA,interfering with DNA-dependant RNA polymerase; also causes ssDNA breaks

Question 3

Dactinomycin (Actinomycin D, Cosmegen) Therapeutics

Answer 3

Pediatric tumors (Wilms’ tumor,rhabdomyosarcoma Ewing’s sarcoma); choriocarcinoma in women

Question 4

Dactinomycin (Actinomycin D, Cosmegen) Imp Side effects

Answer 4

Hematopoietic suppression with pancytopenia, Anorexia, nausea, vomiting

Question 5

Daunorubicin (Cerubidine) Mech

Answer 5

Intercalate between DNA base pairs and donate electrons to O2 to form superoxide; superoxide reacts with itself to form H2O2 –> cleaved in the presence of Fe to form OHradical, which cleaves DNA

Question 6

Daunorubicin (Cerubidine) Therapeutics

Answer 6

AML

Question 7

Daunorubicin (Cerubidine) Imp Side effects

Answer 7

Irreversible dose-dependent cardiotoxicity; alopecia. Dexrazoxane is cardio-protective. Myelosuppression(neutropenia), stomatitis, GI disturbances

Question 8

Idarubicin (Idamycin) Mech

Answer 8

Intercalate between DNA base pairs and donate electrons to O2 to form superoxide; superoxide reacts with itself to form H2O2 –> cleaved in the presence of Fe to form OHradical, which cleaves DNA

Question 9

Idarubicin (Idamycin) Therapeutics

Answer 9

AML

Question 10

Idarubicin (Idamycin) Imp Side effects

Answer 10

Irreversible dose-dependent cardiotoxicity; alopecia. Dexrazoxane is cardio-protective. Myelosuppression(neutropenia), stomatitis, GI disturbances

Question 11

Doxorubicin (Adriamicin, Doxil) class

Answer 11

Anthracyclines

Question 12

Doxorubicin (Adriamicin, Doxil) Mech

Answer 12

Intercalate between DNA base pairs and donate electrons to O2 to form superoxide; superoxide reacts with itself to form H2O2 –> cleaved in the presence of Fe to form OHradical, which cleaves DNA

Question 13

Doxorubicin (Adriamicin, Doxil) Therapeutics

Answer 13

Sarcomas, breast and lung carcinomas,malignant lymphomas

Question 14

Doxorubicin (Adriamicin, Doxil) Imp side effects

Answer 14

Irreversible dose-dependent cardiotoxicity; alopecia. Dexrazoxane is cardio-protective. Myelosuppression(neutropenia), stomatitis, GI disturbances

Question 15

Epirubicin (Ellence) Mech

Answer 15

Intercalate between DNA base pairs anddonate electrons to O2 to form superoxide;superoxide reacts with itself to form H2O2 –> cleaved in the presence of Fe to form OHradical, which cleaves DNA

Question 16

Epirubicin (Ellence) Therapeutics

Answer 16

Metastatic breast cancer, gastric cancer

Question 17

Epirubicin (Ellence) Imp side effects

Answer 17

Irreversible dose-dependent cardiotoxicity; alopecia. Dexrazoxane is cardio-protective. Myelosuppression(neutropenia), stomatitis, GI disturbances

Question 18

Bleomycin (Blenoxane) Mech

Answer 18

Acts in G2 phase of cell cycle. Binds to DNA, producing ss- and dsDNA breaks

Question 19

Bleomycin (Blenoxane) Therapeutics

Answer 19

Combination therapy for testicular tumors or Hodgkin’s disease;squamous cell carcinomas and lymphomas

Question 20

Bleomycin (Blenoxane) Imp side effects

Answer 20

Pulmonary toxicity (pulmonaryfibrosis); cutaneous toxicity(hyperpigmentation,hyperkeratosis, erythema);hyperthermia

Question 21

Bleomycin (Blenoxane) Other side effects

Answer 21

Minimally myelo- and immunosuppressive (often usedin combo therapy); headache,nausea, vomiting

Question 22

Bleomycin (Blenoxane) Misc

Answer 22

Dexrazoxane can be used to prevent cardiotoxic effects