Anticancer Drugs (Classification, Clinical Uses, Adverse Effect)

Question 1

Flutamide

Answer 1

• anti androgen
  MOA: compete with testosterone for binding to androgen receptor in prostate gland
• prostate cancer
• AE: increase androgen level (administered with leuprolide), gynecomastia, liver failure

Question 2

Finasteride

Answer 2

5-a-reductase inhibitor
MOA: reduce size of prostate gland
- oral
- prostate cancer
- AE: decrease libido, impotence

Question 2

Leuprolide/Goserelin

Answer 2

- GnRh analogue
MOA: 
1. Act as GnRH receptor agonist
2. inhibit release of FSH and LH
3. Reduce androgen and testosterone synthesis
- SC/IM
- prostate cancer, premenopausal women with advanced BC
- AE: impotence, hot flash, tumor flare

Question 4

Aminogluthatemide/Anastrozole

Answer 4

• aromatase inhibitor
• aminogluthatemide: replace with anastrozole
  MOA: inhibit adrenal synthesis of androgen/estrogen
• early stage BC & Tamoxifen failure of advanced BC
• AE: fragile bone

Question 5

Fulvestrant

Answer 5

• SERD
  MOA: bind to ER and inhibit binding of estrogens (100x more affinity than Tamoxifen)
• IM
• post menopausal women with antiestrogen therapy of metastatic BC
• AE: muscle pain, hot flashes, arthralgia

Question 6

L-asparaginase

Answer 6

• miscellaneous
  MOA:
  1. Hydrolizes asparagine to aspartate& ammonia
  2. Leukemia lacks aspartate
• IV/IM
• ALL
• AE: hypersensitivity, hyperglycemia, CNS toxicity, clotting & bleeding abnormalities

Question 6

Hydroxyurea

Answer 6

- miscellaneous 
MOA: inhibit RNA to DNA (affect S phase)
- oral
- CML, sickle cell disease,
- AE: BMS, GI upset

Question 7

Mechlorethamine

Answer 7

• Alkylating agent
• Hodgkin & non hodgkin lymphoma
• AE: BMS

Question 7

Tamoxifen

Answer 7

-SERM
MOA: Bind to ER and either exert estrogenic or antiestrogenic effect
- oral
- early stage and metastatic BC (preventive for high risk women)
- AE: hot flashes, vision loss, vaginal bleeding, potential to cause endometrial cancer

Question 9

Cyclophosphamide

Answer 9

• Alkylating agent
• ALL, CLL, Nonhodgkin lymphoma, ovarian & breast cancer, neuroblastoma, Wilm’s tumor
• AE: Hematuria

Question 10

Ethinyl estradiol

Answer 10

• estrogens
  MOA:
  1. Block production of LH
  2. Decrease synthesis of androgen in testis
  3. Inhibit growth of prostatic tissue
• prostate cancer
• AE: thromboembolism, MI, strokes, hypercalcemia, impotence, gynecomastia

Question 11

Busulfan

Answer 11

• alkylating agent
• CML
• AE: skin pigmentation, pulmonary fibrosis

Question 13

Procarbazine

Answer 13

• alkylating agent
• hodgkin
• AE: secondary malignancy

Question 14

Medroxyprogesterone acetate

Answer 14

• progestins
  MOA: bind to progesterone receptor
• oral
• breast and endometrial hormone dependent cancer (adjuvant)
• AE: irregular bleeding, breast engorgement, mood swing
  *long term use: increase risk of BC (replace by aromatase inhibitor)

Question 15

Cisplatin&Carboplatin

Answer 15

• alkylating agent
• esophageal, lung, colon, bladder, testicular, ovarian cancer
• AE: Ototoxicity, nephrotoxicity, neurotoxicity

Question 17

Methotrexate (MTX)

Answer 17

• folate antagonist
• ALL, Non hodgkin, BC, lung, bladder cancer, meningeal metastases
• AE: mucositis, GIT toxicity, teratogenic

Question 18

Prednisolone

Answer 18

- glucocorticoids 
MOA:
1. Steroid binds to receptor protein in cancer cells
2. Dissolution of lymphocytes
3. Inhibit growth of mesenchymal tissue
- acute leukaemia & lymphoma
- control side effect chemotherapy

Question 19

6-Mercaptopurine

Answer 19

• purine antagonist
• ALL, CML, non cancer
• AE: hepatotoxicity, GIT upset, hyperuricemia

Question 20

5-Fluorouracil

Answer 20

• pyrimidine antagonist
• colorectal cancer, solid tumor (breast, stomach, liver, pancreas, head, neck)
• AE: mucositis, hand & foot syndrome, neurotoxicity

Question 21

Irinotecan/Topotecan/Etoposide

Answer 21

• topoisomerase inhibitor
  MOA: act in S phase, cell arrest at G2 phase
  : inhibit topoisomerase I (etoposide: II)
• small cell lung cancer (common for all)
• AE: BMS, N&V (common for all)

Question 33

Vincristine

Answer 33

• Vinca alkaloid
• Childhood leukemia, tumor, hodgkin, neuroblastoma
• AE: alopeCia, neurotoxicity & muscle weakness (CNS), constipation

Question 34

Vinblastine

Answer 34

• Vinca alkaloid
• Breast cancer, testicular cancer, hodgkin & non hodgkin
• AE: BMS (everything in vincristine is less common in vinblastine)

Question 35

Paclitaxel/Docetaxel

Answer 35

• Taxane
• breast, ovarian, lung, bladder cancer
• AE: neurotoxicity

Question 36

Actinomycin D

Answer 36

• antibiotics
• IV
• MOA: binds to DNA (inhibit DNA synthesis)
• paediatric tumor, germ cell tumor
• AE: anorexia, pancytooenia, glossitis, oral ulcer, BMS

Question 37

Mitomycin C

Answer 37

MOA: 1. Same like alkylating agent 2. Cell arrest at S phase - IV - SCC of anus (+ 5FU), bladder cancer - AE: HUS, BMS

Question 38

Doxorubicin/Daunorubicin/Idarubicin/Epirubicin

Answer 38

- anthracycline - ALL, hodgkin, solid tumor - AE: cardiotoxicity, MDR, alopecia

Question 39

Bleomycin

Answer 39

- antibiotics MOA: bind and break DNA, cell accumulate at G2 phase - IV/IM/SC - hodgkin & non hodgkin, SCC of skin/cervix/vulva, testicular cancer (+ vinblastine) - AE: pulmonary toxicity, mucocutaneous reaction, alopecia