Cancer Drugs

Front 1

Methotrexate

Back 1

MOA:
- folic acid analog
- inhibits dihydrofolate reductase
- decreased dTMP -> decreased DNA and protein synthesis

Indication:
- leukemias
- lymphomas
- choriocarcinomas
- sarcomas
- abortion, ectopic pregnancy
- RA
- psoriasis

Hint 1

Toxicity:
- myelosuppression -> leucovorin (folinic acid) rescue
- macrovesicular fatty change in liver
- mucositis
- teratogenic

Front 2

5-fluorouracil (5FU)

Back 2

MOA:
- pyrimidine analog
- bioactivated to 5F-dUMP which complexes covalently with folic acid
- inhibits thymidylate synthase -> low dTMP -> low DNA and protein synthesis

Indication:
- colon cancer and other solid tumors
- basal cell carcinoma (topical)
- synergy with MTX

Hint 2

Toxicity:
- myelosuppression ("overdose" rescue with thymidine)
- photosensitivity

Front 3

6-Mercaptopurine (6MP)

Back 3

MOA:
- purine (thiol) analog
- decreases de novo purine synthesis
- activated by HGPRTase

Indication:
- leukemias, lymphomas (not CLL or Hodkin's)

Hint 3

Toxicity:
- bone marrow, GI, liver
- metabolized by xanthine oxidase and TPMT
- increased toxicity with allopurinol

Front 4

6-thioguanine (6-TG)

Back 4

MOA:
- purine (thiol) analog that decreases de novo purine synthesis

Indications:
- ALL

Hint 4

Toxicity:
- bone marrow suppression
- liver
- can be given with allopurinol (unlike 6-MP)

Front 5

Cytarabine (ara-C)

Back 5

MOA:
- pyrimidine antagonist
- inhibits DNA polymerase

Indication:
- AML, ALL, high-grade non-Hodgkin's lymphoma

Hint 5

Toxicity:
- leukopenia
- thrombocytopenia
- megaloblastic anemia

Front 6

Cladribine

Back 6

MOA:
- purine analog
- resistant to adenosine deamine degradation -> high levels inside of cells
- incorporated into DNA -> strand breaks
- good CNS penetration
- excreted unchanged in urine

Indication:
- HLL (hairy)

Front 7

Daptomycin

(actinomycin D)

Back 7

MOA:
- intercalates in DNA

Indications:
- Wilm's tumor, Ewing's sarcoma, rhabdomyosarcoma

Hint 7

Toxicity:
- myelosuppression

Front 8

Doxorubicin (adriamycin), daunorubicin

Back 8

MOA:
- generate free radicals
- noncovalently intercalate in DNA -> breaks in DNA
- decreased replication

Indication:
- Hodgkin's
- myeloma
- sarcoma
- solid tumors (breast, ovar, lung)

Hint 8

Toxicity:
- cardiotoxicity (dexrazoxane = Fe chelator to prevent cardiotoxicity)
- myelosuppression
- alopecia
- toxic to tissues with extravasation

Front 9

Bleomycin

Back 9

MOA:
- induces free radical formation
- breaks in DNA

Indication:
- testicular cancer
- Hodgkin's lymphoma

Hint 9

Toxicity:
- pulmonary fibrosis
- skin changes
- minimal myelosuppression

Front 10

Etoposide (TP-16), teniposide

Back 10

MOA:
- inhibits topoisomerase II
- increases DNA degradation

Indication:
- small cell carcinoma of the lung and prostate
- testicular carcinoma

Hint 10

Toxicity:
- myelosuppression
- GI irritation
- alopecia

Front 11

Cyclophosphamide, ifosfamide

Back 11

MOA:
- alkylating agent
- covalently crosslink (interstrand) DNA at guanine N-7
- require bioactivation by liver

Indication:
- Non-Hodgkin's lymphoma
- breast and ovarian carcinoma
- also immunosuppressants

Hint 11

Toxicity:
- myelosuppression
- hemorrhagic cystitis (MESNA to prevent)

Front 12

Nitrosoureas

carmustine, lomustine, semustine, streptozocin

Back 12

MOA:
- alkylating agents
- require bioactivation (hydroxylation)
- cross BBB -> CNS

Indication:
- brain tumors (including GBM)

Hint 12

Toxicity:
- CNS toxicity (dizziness, ataxia)

Front 13

Busulfan

Back 13

MOA:
- alkylates DNA

Indication:
- CML
- also used to ablate bone marrow before BM transplant

Hint 13

Toxicity:
- pulmonary fibrosis
- hyperpigmentation

Front 14

Vincristine, vinblastine

Back 14

MOA:
- alkaloids that bind to tubulin in M-phase and block polymerization of MT
-> mitotic spindle cannot form

Indications:
- Hodgkin's lymphoma
- Wilm's tumor
- choriocarcinoma

Hint 14

Toxicity:
- vincristine: neurotoxicity (areflexia, peripheral neuritis), paralytic ileus

- vinblastine: bone marrow suppression

Front 15

Paclitaxel, other taxols

Back 15

MOA:
- hyperstabilize polymerized MT in M-phase
-> mitotic spindle cannot break down
-> anaphase cannot occur

Indications:
- ovarian and breast carcinomas

Hint 15

Toxicity:
- myelosuppression
- hypersensitivity

Front 16

Cisplatin, carboplatin

Back 16

MOA:
- crosslink DNA

Indications:
- testicular, bladder, ovary and lung carcinomas

Hint 16

Toxicity:
- nephrotoxicity
- acoustic nerve damage

Front 17

Hydroxyurea

Back 17

MOA:
- inhibits ribonucleotide reductase
- decreases DNA synthesis (S-phase specific)

Indications:
- melanoma, CML
- sickle cell dz -> upregulates HbF expression

Hint 17

Toxicity:
- myelosuppression
- GI upset

Front 18

Prednisone

Back 18

MOA:
- may trigger apoptosis
- may even work on non-dividing cells

Indications:
- CLL, Hodgkin's lymphoma
- immunosuppressant used in autoimmune dz

Hint 18

Toxicity:
- Cushing-like sx, acne
- immunosuppression
- cataracts
- osteoporosis
- HTN
- peptic ulcers
- hyperglycemia
- psychosis

Front 19

Tamoxifen, raloxifene

Back 19

MOA:
- SERMs
- receptor antagonist in breast and agonists in bone
- block binding of estrogen to ER-positive cells

Indication:
- breast cancer
- also useful in prevention of osteoporosis

Hint 19

Toxicity:
- hot flashes
- tamoxifen: may increase risk for endometrial cancer via partial agonist effect (raloxifene endometrial antagonist)

Front 20

Trastuzumab (herceptin)

Back 20

MOA:
- monoclonal Ab against HER-2 (erb-B2)
- helps kill breast cancer cells that overexpress HER-2, possibly via Ab-dependent cytotoxicity

Indications:
- metastatic breast cancer

Hint 20

Toxicity:
- cardiotoxicity

Front 21

Imatinib (gleevec)

Back 21

MOA:
- inhibitor of bcr-abl kinase

Indication:
- CML, GI stromal cancer

Hint 21

Toxicity:
- fluid retention

Front 22

Rituximab

Back 22

MOA:
- monoclonal Ab against CD20, found on most B-cell neoplasms

Hint 22

Indication:
- Non-Hodgkin's lymphoma
- RA (with MTX)

Front 23

Filgrastim

Back 23

MOA:
- G-CSF analog for patients with neutropenia