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. 2013 Jun 21;21(1):15–25. doi: 10.1038/cdd.2013.67

Table 1. Biochemical and biological properties of conventional antineoplastic drugs.

Class Examples Biochemical activity Biological effects Use in clinical oncology
Antimetabolites 5-Fluorouracil Analog of pyrimidine nucleoside Perturbation of RNA and DNA synthesis Colorectal cancer, pancreatic cancer
  Gemcitabine     Non-small cell lung cancer, pancreatic cancer, bladder cancer, breast cancer
  Methotrexate Inhibits dihydrofolate reductase Reduction of folates required for DNA synthesis Breast, head and neck, leukemia, lymphoma, lung, osteosarcoma, bladder and trophoblastic neoplasms
Alkylating agents Cyclophosphamide Adds an alkyl group to DNA Inhibition of DNA replication Lymphomas, leukemias, brain tumors
  Dacarbazine     Metastatic melanoma, Hodgkin's lymphoma
  Melphalan     Multiple myeloma, ovarian cancer, malignant melanoma
Anthracyclines Doxorubicin Intercalates base pairs of nucleic acids Inhibition of RNA and DNA synthesis Leukemias, Hodgkin's lymphoma, bladder cancer, breast, stomach, lung, ovaries, thyroid, soft-tissue sarcoma, multiple myeloma
Antimicrotubule agents Vinblastine Binds tubulin, thereby inhibiting the assembly of microtubules M-phase-specific cell cycle arrest by disrupting microtubule assembly Hodgkin's lymphoma, non-small cell lung cancer, breast cancer, head and neck cancer, and testicular cancer
Platinum compounds Cisplatin Crosslinks DNA strands Inhibition of DNA replication and transcription Head and neck, lung and ovarian carcinomas, lymphomas, germ cell tumors
  Oxaliplatin     Colorectal cancer
Taxanes Paclitaxel Stabilizes GDP-bound tubulin in microtubules Inhibition of mitosis Lung, ovarian, breast, head and neck cancer, advanced forms of Kaposi's sarcoma
  Docetaxel     Breast, ovarian, prostate and non-small cell lung cancer
Topoisomerase inhibitors Irinotecan Interferes with type I topoisomerases inducing DNA strands breaks Cell cycle arrest and apoptosis Colorectal cancer
  Etoposide phosphate Interferes with type II topoisomerases inducing DNA strands breaks   Kaposi's and Ewing's sarcomas, certain leukemias, lung, ovarian, gastrointestinal cancers, glioblastoma multiforme
  Mitoxantrone     Metastatic breast cancer, acute myeloid leukemia and non-Hodgkin's lymphoma