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Heme - Chemo Drugs - Pharm

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S-phase-specific antimetabolite. Folic acid analog that inhibits dihydrofolate
reductase, resulting in ↓ dTMP and therefore ↓ DNA and protein synthesis.
Methotrexate (MTX)
Leukemias, lymphomas, choriocarcinoma, sarcomas. Abortion, ectopic pregnancy,
rheumatoid arthritis, psoriasis.
Methotrexate (MTX)
Myelosuppression, which is reversible with leucovorin (folinic acid) “rescue.”
Macrovesicular fatty change in liver.
Methotrexate (MTX)
S-phase-specific antimetabolite. Pyrimidine analog bioactivated to 5F-dUMP, which
covalently complexes folic acid. This complex inhibits thymidylate synthase, resulting
in ↓ dTMP
5-fluorouracil (5-FU)
Colon cancer and other solid tumors, basal cell carcinoma (topical). Synergy with
MTX.
5-fluorouracil (5-FU)
Myelosuppression, which is NOT reversible with leucovorin; photosensitivity.
5-fluorouracil (5-FU)
Blocks de novo purine synthesis. Activated by HGPRTase.
6-mercaptopurine (6-MP)
Leukemias, lymphomas (not CLL or Hodgkin’s).
6-mercaptopurine (6-MP)
Bone marrow, GI, liver. Metabolized by xanthine oxidase; thus ↑ toxicity with allopurinol.
6-mercaptopurine (6-MP)
Inhibits DNA polymerase.
Cytarabine (ara-C)
AML.
Cytarabine (ara-C)
Leukopenia, thrombocytopenia, megaloblastic anemia.
Cytarabine (ara-C)
Alkylating agents; covalently x-link (interstrand) DNA at guanine N-7. Require
bioactivation by liver.
Cyclophosphamide, ifosfamide
Non-Hodgkin’s lymphoma, breast and ovarian carcinomas. Also immunosuppressants.
Cyclophosphamide, ifosfamide
Myelosuppression; hemorrhagic cystitis, which can be partially prevented with mesna.
Cyclophosphamide, ifosfamide
Names of Nitrosoureas
Carmustine, lomustine, semustine, streptozocin.
Alkylate DNA. Require bioactivation. Cross blood-brain barrier → CNS.
Nitrosoureas

Carmustine, lomustine, semustine, streptozocin.
Brain tumors (including glioblastoma multiforme).
Nitrosoureas

Carmustine, lomustine, semustine, streptozocin.
CNS toxicity (dizziness, ataxia).
Nitrosoureas

Carmustine, lomustine, semustine, streptozocin.
Act like alkylating agents.
Cisplatin, carboplatin
Testicular, bladder, ovary, and lung carcinomas.
Cisplatin, carboplatin
Nephrotoxicity and acoustic nerve damage.
Cisplatin, carboplatin
Alkylates DNA.
Busulfan
CML.
Busulfan
Pulmonary fibrosis, hyperpigmentation.
Busulfan
Generate free radicals and noncovalently intercalate in DNA (creating breaks in DNA
strand to ↓ replication).
Doxorubicin (Adriamycin), daunorubicin
Part of the ABVD combination regimen for Hodgkin’s and for myelomas, sarcomas, and
solid tumors (breast, ovary, lung).
Doxorubicin (Adriamycin), daunorubicin
Cardiotoxicity; also myelosuppression and marked alopecia. Toxic extravasation.
Doxorubicin (Adriamycin), daunorubicin
Intercalates in DNA.
Dactinomycin (actinomycin D)
Wilms’ tumor, Ewing’s sarcoma, rhabdomyosarcoma.
Dactinomycin (actinomycin D)
Myelosuppression.
Dactinomycin (actinomycin D)
Induces formation of free radicals, which cause breaks in DNA strands.
Bleomycin
Testicular cancer, lymphomas (part of the ABVD regimen for Hodgkin’s).
Bleomycin
Pulmonary fibrosis, skin changes, but minimal myelosuppression.
Bleomycin
G2-phase-specific agent that inhibits topoisomerase II and ↑ DNA degradation.
Etoposide (VP-16)
Small cell carcinoma of the lung and prostate, testicular carcinoma.
Etoposide (VP-16)
Myelosuppression, GI irritation, alopecia.
Etoposide (VP-16)
May trigger apoptosis. May even work on nondividing cells.
Prednisone
Most commonly used glucocorticoid in cancer chemotherapy. Used in CLL, Hodgkin’s lymphomas (part of the MOPP regimen). Also an immunosuppressant used in autoimmune diseases.
Prednisone
Cushing-like symptoms; immunosuppression, cataracts, acne, osteoporosis, hypertension, peptic ulcers, hyperglycemia, psychosis.
Prednisone
Estrogen receptor mixed agonist/antagonists (“SERMs”) that block the binding of estrogen to estrogen receptor–positive cells.
Tamoxifen, raloxifene
Breast cancer. Also useful to prevent osteoporosis.
Tamoxifen, raloxifene
_______ may ↑ the risk of endometrial carcinoma via partial agonist effects; “hot flashes.”
Tamoxifen, raloxifene
Monoclonal antibody against HER-2 (erb-B2). Helps kill breast cancer cells that overexpress HER-2, possibly through antibody-dependent cytotoxicity.
Trastuzumab (Herceptin)
Metastatic breast cancer.
Trastuzumab (Herceptin)
Cardiotoxicity.
Trastuzumab (Herceptin)
Myoclonal antibody against the Philadelphia chromosome brc-abl tyrosine kinase.
Imatinib (Gleevec)
CML, GI stromal tumors.
Imatinib (Gleevec)
Fluid retention.
Imatinib (Gleevec)
M-phase-specific alkaloids that bind to tubulin and block polymerization of microtubules so that mitotic spindle cannot form.
Vincristine, vinblastine
Part of the MOPP regimen for lymphoma, Wilms’ tumor,
choriocarcinoma.
(Oncovin [vincristine] is part of MOPP), vinblastine
neurotoxicity (areflexia, peripheral neuritis), paralytic ileus.
Vincristine
Bone marrow suppression
VinBLASTine BLASTs Bone marrow (suppression).
M-phase-specific agents that bind to tubulin and hyperstabilize polymerized microtubules so that mitotic spindle cannot break down (anaphase cannot occur).
Paclitaxel, other taxols
Ovarian and breast carcinomas.
Paclitaxel, other taxols
Myelosuppression and hypersensitivity.
Paclitaxel, other taxols
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