Antineoplastics

Question 1

Methotrexate

Answer 1

Class: Antimetabolite (S phase specific)
MOA: Inhibits DHFR
Use: Leukemia, Lymphoma, Chorio CA, Sarcoma, abortion, RA, psoriasis, IBD
SE: Myelosuppression (reversal by leucovorin), Teratogen

Question 2

5-Fluoruracil (5FU)

Answer 2

Class: Antimetabolite (S phase specific)
MOA: Pyrimidine analog, inhibits Thymidylate Synthase
Use: Colin CA, Pancreatic CA, basal cell CA
SE: Myelosuppression (rescue with uridine), Photosensitivity

Question 3

Cytarabine

Answer 3

Class: antimetabolite (S phase specific)
MOA: Pyrimidine analog, inhibit DNA Polymerase
Use: Leukemia, lymphoma
SE: Pancytopenia

Question 4

Azathioprine, 6-MP

Answer 4

Class: Antimetabolite (S phase Specific)
MOA; Purine analog, activated by HGPRT, inhibit de novo synthesis of purines
Use: Prevent organ rejection, SLE (azo), Leukemia, IBD
SE: Metabolized by Xanthine oxidase, therefore allopurinol inhibits and causes toxicity (bone marrow suppression)

Question 5

Dactinomycin

Answer 5

Class: Intercalating agent
MOA: intercalates DNA
Use: Wilms tumor, Ewing SA, rhabdosarcoma (childhood tumors)
SE: myelosuppression

Question 6

Doxorubicin, Daunorubicin

Answer 6

Class: Intercalating agent
MOA: intercalates, breaks DNA
Use: Solid tumors, leukemia, lymphoma
SE: CARDIOTOXIC, myelosuppression

Question 7

Bleomycin

Answer 7

Class: Intercalating agent
MOA: Free radicals break DNA
Use: Testicular CA, Hodgkin’s
SE: Pulmonary fibrosis

Question 8

Cyclophosphamide, ifosphamide

Answer 8

Class: Alkylating Agent
MOA: X-Link DNA at guanine (N7), liver activated
Use: Solid tumor, leukemia, brain cancer
SE: Myelosuppression, HEMORRHAGIC CYSTITIS (prevented by MESNA)

Question 9

Nitrosureas (carmustine, lomustine, semustine, streptozocin)

Answer 9

Class: Alkylating Agent
MOA: Crosses BBB, X-links DNA
Use: Brain Tumors
SE: CNS toxicity (convulsions, ataxia)

Question 10

Busulfan

Answer 10

Class: Alkylating Agent
MOA: X-Link DNA
Use: CML
SE: Myelosuprresion, Pulmonary fibrosis, Hyperpigmentation

Question 11

Vincristine, Vinblastine

Answer 11

Class: Microtubule inhibitor
MOA: Vinca Alkaloids bind Beta Tubulin, inhibit polymerization
Use: Solid tumor, L and L
SE: Vincristine-neurotoxic, Vinblastine-Bone marrow suppression

Question 12

Paclitaxel, other taxols

Answer 12

Class: Microtubule inhibitor
MOA: Stabilizes polymers of microtubules, can’t break down in M phase
Use: Ovarian and Breast CA
SE: Myelosuppresion, alopecia

Question 13

Cisplatin, Carboplatin

Answer 13

MOA: X-Link DNA
Use: Testicular, ovary, bladder lung
SE: Nephrotoxic and Ototoxic, amifostine prevents nephrotoxicity

Question 14

Etoposide, teniposide

Answer 14

MOA: Topoisomerase II inhibitor, DNA degrades
Use: Solid Tumors (Testicle and Small cell lung)
SE: Myelosuppresion

Question 15

irnotecan, topotecan

Answer 15

MOA: Inhibit Topoisomerase I, prevent DNA unwinding
Use: Colon CA, ovary and small cell lung
SE: Severe myelosuppresion

Question 16

Hydroxyurea

Answer 16

MOA: Inhibit Ribonucleotide Reductase (dec DNA synthesis in S phase)
Use: Melanoma, CML, SCD (increase HbF)
SE: Bone Marrow suppresion

Question 17

Prednisone, Prednisolone

Answer 17

MOA: Corticosteroid triggers apoptosis
Use: CLL, non hodgkins, immunosuppression
SE: Cushings, osteoporosis

Question 18

Tamoxifen, Raloxifene

Answer 18

MOA: SERM, block binding of Estrogen
Use: Breast CA (Tamoxifen), Raloxifene prevents osteoporosis
SE:Tamoxifen: endometrial agonist may cause CA, Raloxifene: Endometrial antagonist

Question 19

Trastuzumab (Herceptin)

Answer 19

MOA: Her2/Neu antagonist (Tyrosine Kinase receptor(
Use: Her-2 + Breast CA
SE: Cardiotoxicity “HEARTceptin”

Question 20

Imatinib (Gleevac)

Answer 20

MOA: Inhibit Tyrosine Kinase bcr-abl and c-kit
Use: CML (Philadelphia chromosome), GIST
SE: Fluid retention

Question 21

Rituximab

Answer 21

MOA: Binds CD-20 on B cell neoplasm
Use: Non-Hodgkin lymphoma, Rheum Arthritis, ITP
SE: Risk of Multifocal Encephalopathy

Question 22

Vemurafenib

Answer 22

MOA: Inhibit B-Raf kinase of v600E mutation
Use: Malignant Melanoma

Question 23

Bevacizumab

Answer 23

MOA: Mab of VEGF, inhibit angiogenesis
Use: Solid Tumors (CRC and Renal)
SE: Hemorrhage, impairs wound healing