Alkylating agents |
Cyclophosphamide | Forms DNA cross-links, resulting in inhibition of DNA synthesis and function | Breast cancer, ovarian cancer, non-Hodgkin's lymphoma, chronic lymphocytic leukemia, neuroblastoma | Nausea and vomiting | Myelosuppression, alopecia, hemorrhagic cystitis |
Other major alkylating agents: Mechlorethamine, procarbazine, busulfan carmustine, lomustine, dacarbazine Platinum analogs: Cisplatin, carboplatin, oxaliplatin |
Antimetabolites |
Methotrexate | Inhibits DHFR, resulting in inhibition of synthesis of thymidylate, purine nucleotides, serine, and methionine | Breast cancer, head and neck cancer, primary CNS lymphoma, non-Hodgkin's lymphoma, bladder cancer, choriocarcinoma | Mucositis, diarrhea | Myelosuppression |
6-Mercaptopurine | Inhibits de novo purine synthesis | Acute myelogenous leukemia | Nausea and vomiting | Myelosuppression, immunosuppression, hepatotoxicity |
5-Fluorouracil | Inhibits thymidylate synthase, and its metabolites are incorporated into RNA and DNA, all resulting in inhibition of DNA synthesis and function and in RNA processing | GI cancers, breast cancer, head and neck cancer, hepatocellular cancer | Nausea, mucositis, diarrhea | Myelosuppression, neurotoxicity |
Other antimetabolites: Cytarabine, gemcitabine |
Vinca alkaloids |
Vincristine | Interferes with microtubule function, resulting in impaired mitosis | Acute lymphocytic leukemia, Hodgkin's and non-Hodgkin's lymphoma, Wilms' tumor, neuroblastoma | None | Neurotoxicity with peripheral neuropathy, paralytic ileus, myelosuppression, alopecia, inappropriate ADH secretion |
Other vinca alkaloids: Vinblastine, vinorelbine |
Podophyllotoxins |
Etoposide | Inhibits topoisomerase II, resulting in DNA damage | Lung cancer, non-Hodgkin's lymphoma, gastric cancer | Nausea, vomiting | Alopecia, myelosuppression |
Other podophyllotoxins: Teniposide |
Camptothecins |
Topotecan | Inhibits topoisomerase I, resulting in DNA damage | Small cell lung cancer, ovarian cancer | Nausea, vomiting, diarrhea | Myelosuppression |
Other camptothecins: Irinotecan |
Taxanes |
Paclitaxel | Interferes with microtubule function, resulting in impaired mitosis | Breast, lung, ovarian, gastroesophageal, prostate, bladder, and head and neck cancers | Nausea, vomiting, hypotension, arrhythmias, hypersensitivity | Myelosuppression, peripheral sensory neuropathy |
Other taxanes: Docetaxel |
Anthracyclines |
Doxorubicin | Oxygen free radicals bind to DNA causing strand breakage; inhibits topoisomerase II; intercalates into DNA | Lymphomas, myelomas, sarcomas, and breast, lung, ovarian and thyroid cancers | Nausea, arrhythmias | Alopecia, myelosuppression, cardiomyopathy, myelosuppression |
Other anthracyclines: Daunorubicin, idarubicin, epirubicin, mitoxantrone Other antitumor antibiotics: Bleomycin, mitomycin |
Tyrosine kinase inhibitors |
Imatinib | Inhibits bcr-abl tyrosine kinase and other receptor tyrosine kinases | Chronic myelogenous leukemia, gastrointestinal stromal tumor | Nausea, vomiting | Fluid retention with ankle and periorbital edema, diarrhea, myalgias, congestive heart failure |
Other tyrosine kinase inhibitors: Dasatinib, nilotinib, sorafenib*, sunitinib*, and pazopanib* |
Growth factor receptor inhibitors |
Trastuzumab | Inhibits the binding of EGF to the HER-2/neu growth receptor | HER-2/neu receptor + breast cancer | Nausea, vomiting, chills, fever, headache | Cardiac dysfunction |
Other growth factor receptor inhibitors: Cetuximab, panitumumab, gefitinib, erlotinib |
Vascular endothelial growth factor (VEGF) inhibitors |
Bevacizumab | Inhibits binding of VEGF to its receptor, resulting in inhibition of tumor vascularization | Colorectal, breast, non-small cell lung, and renal cancer | Hypertensin, infusion reaction | Arterial thromboembolic events, gastrointestinal perforations, wound healing complications, proteinuria |
Proteasome Inhibitors |
Bortezomib | Reversibly inhibits chymotrypsin-like activity of the 26S proteasome | Multiple myeloma | Hypotension, edema, GI upset | Peripheral neuropathy, cardiac dysfunction, |
Hormone agonists |
Prednisone | See Chapter 39 | | | |
Hormone antagonists |
Tamoxifen | See Chapter 40 | | | |
Other hormonal antagonists: Aromatase inhibitors, GnRH agonist and antagonists, androgen receptor antagonists (see Chapter 40) |