chemotherapy agents

Question 1

Doxorubicin and Bleomycin belongs to which class of chemotherapy agents?

Answer 1

DNA intercalating drugs

Question 2

What is the mechanism of action of doxorubicin?

Answer 2

• Formation of free radicals –> DNA BREAKAGE
• Inhibition of topoisomerase 2 -> Increase DNA degradation (dsDNA breaks) and decrease DNA replication.
  -DNA intercalation

Question 3

What are the main clinical uses of doxorubicin?

Answer 3

-Breast cancer
-Metastic solid tumors
-Lymphomas
-kaposi Sarcoma
-Leukemias

Question 4

What are the most common adverse effects of doxorubicin?

Answer 4

-Dilated cardiomyopathy (often irreversible)
-Acute toxicity: Nausea and vomiting
-Delayed toxicity: Alopecia, cardiotoxicity, myelosupression

Question 5

Bleomycin mechanism of action:

Answer 5

-Induces formation of free radicals –> Breakage of DNA strand–> cell cycle arrest at G2 phase and M phase

Question 6

Clinical uses of Bleomycin?

Answer 6

-SCC of the head and neck
-Testicular cancer
-Hodkin and non-Hodkin Lymphoma

Question 7

Bleomycin Adverse Effects:

Answer 7

-Pulmonary Fibrosis
-Alopecia
-Myelosuppression
-Acute toxicity: Fever, allergic rxns
-Skin Hyperpigmentation

Question 8

Etiposide and Teniposide are classified as:?

Answer 8

DNA Topoisomerase II inhibitors

Question 9

What is the mechanism of action of Etoposide and Teniposide?

Answer 9

Inhibits topoisomerase II

Question 10

What are the clinical uses of Etoposide and Teniposide?

Answer 10

-Small cell lung cancer
-Testicular carcinoma
-non Hodking Lymphoma

Question 11

Adverse effects of Etoposide and Teniposide:

Answer 11

-Myelosuppression
-Alopecia
-Acute toxicity: Mild nausea and vomiting
-Delayed toxicity: Alopecia, myelosuppression

Question 12

Irinotecan and Topotecan are classified as?

Answer 12

Topoisomerase I inhibitors

Question 13

MoA of Irinotecan and Topotecan:

Answer 13

Inhibit topoisoomerase I “TecONE’

Question 14

Clinical uses of Irinotecan and Topotecan?

Answer 14

-Colon
Breasts, Ovarian, Small cell lung cancer

Question 15

What are the most common adverse effects of Irinotecan and Topotecone?

Answer 15

-Severe myelosuppression
-Diarrhea
-Acute toxicity: Diarrhea, nausea and vomiting
-Delayed toxicity: Myelosuppression

Question 16

Vincristine/Vinablastine (Vinca alkaloids) and Panclitaxel/Docetaxel (Taxanes) are classified as:

Answer 16

Mitotic inhibitors

Question 17

Vincristine and Vinblastine Mechanism of action:

Answer 17

Bind B-tubulin and inhibits its polymerization into microtubules –> Prevention of mitotic spindle formation

Question 18

Clinical uses of Vinblastine and Vincristine?

Answer 18

-Solid tumors
- Hematologic cancers (ALL and Hodking and non-Hodking)

Question 19

Adverse effects of Vincristine:

Answer 19

-Neurotoxicity: (areflexia, peripheral neuropathy)
-Constipation (paralytic ileum)

Question 20

Vinblastine Adverse Effects:

Answer 20

-Myelosuppression
-Acute toxicity: Usual well tolerated
-Delayed toxicity: Alopecia, mild myelosuppression, neurotoxicity

Question 21

Paclitaxel and Docetaxel MoA:

Answer 21

Hyperstabilize polymerized microtubules –> Prevent mitotic spindle breakdown

Question 22

Paclitaxel and Docetaxel Target:

Answer 22

-Tubulin beta chain-1 inhibitor
-Apoptosis regulator BCL-2 inhibitor

Question 23

Clinical uses of Paclitaxel and Docetaxel:

Answer 23

Varoius tumors (e.g., OVARIAN and breast carcinoma)

Question 24

Paclitaxel and Docetaxel Adverse Effects:

Answer 24

Myelosuppression, neuropathy, Hypersensitivity

Acute toxicity: Usually well tolerated
Delayed toxicity: Alopecia, Mild myelosuppression, Neurotoxicity

Question 25

Imatinib is a:

Answer 25

Small molecule inhibitor (Tyrosine Kinase Inhibitor)

Question 26

Imatinib MoA:

Answer 26

Tyrosine-kinase inhibitor that inhibits BCR-ABL tyrosine kinase (the constitutive Philadelphia chromosome abnormality in CML.

Question 27

Imatinib clinical uses:

Answer 27

-CML -ALL -Malignant Gastrointestinal stromal tumors

Question 28

Imatinib Adverse Effects:

Answer 28

-Myelosuppression -↑ LFTs -Edema -Myalgias

Question 29

Bortezominab and Carfilzominab are?

Answer 29

Proteasome inhibitors

Question 30

Bortezominab and Carfilzominab MoA:

Answer 30

The drug prevents the degradation and recycling of proteins by the proteasome of cancer cells, leading to protein accumulation and cell death.

Question 31

Bortezominab and Carfilzominab Clinical uses:

Answer 31

-Multiple myeloma -Mantle cell Lymphoma

Question 32

Rituximab and Cetuximab are which type of cancer therapy?

Answer 32

Anticancer monoclonal antibodies

Question 33

Adverse Effects of Bortezominab and Carfilzominab:

Answer 33

-Peripheral neuropathy -Herpes zoster reactivation

Question 34

Rituximab MoA:

Answer 34

Work against extracellular targets to neutralize them or to promote immune system recognition. Eliminated by macrophages (not cleared by kidneys or liver) Target: CD20 antigen

Question 35

Clinical uses of Rituximab:

Answer 35

-Non-Hodking Lymphoma -Chronic Lymphocytic Leukemia -Rheumatic Arthritis in combination with methotrexate -Granulomatosis with Polyangitis, etc.

Question 36

Adverse reactions of rituximab:

Answer 36

Infusion reaction due to cytokine release following interaction of rituximab with its target on B cells

Question 37

Cetuximab MoA:

Answer 37

Binds to the epidermal growth factor receptor (EGFr) on both normal and tumor cells Target: EGFR

Question 38

Cetuximab Clinical Use:

Answer 38

Binds to the epidermal growth factor receptor (EGFr) on both normal and tumor cells

Question 39

Adverse effects of cetuximab

Answer 39

-Rash -Elevated LFTs -Diarrhea