Specific Chemotherapy Drugs

Chemotherapy started in the early 20th century when scientists observed nitrogen mustards suppressed bone marrow activity.  Early chemotherapy was given as a palliative, but over time the goals adjusted to causing remission or cure.

While the other mainstays of cancer treatment – radiation therapy and surgery – are directed at one portion of the body at a time, chemotherapy is a systemic treatment.  The anti-cancer drugs travel through the body and can attack cancerous cells anywhere.

How would you attack a cancerous cell?  In a body full of trillions of cells, how do you get the cancerous ones and not the healthy ones.  It’s not easy, and devising a method that can kill only malignant cells while leaving normal cells unscathed is a holy grail of cancer.

If we could have the ideal chemotherapy drug, what characteristics would it have?  Some ideas:

  • Would work both to cure cancer and to prevent it
  • Easy to give to patients, avoids needles or extended administration times.  Oral administration in a pill might be ideal
  • Has no negative effect from chronic administration
  • Rapidly shrinks tumor and/or kills cancer cells with no effect on non-cancerous cells.  In other words, has high specificity for cancer.

And what biochemical targets would these drugs aim at?  Perhaps those:

  • High level of expression in neoplastic tissue
  • Important in pathogenesis of cancer
  • Not important in regular functioning of tissue
  • Susceptible to pharmacological disruption
  • If you inhibit the target, you stop or slow the cancer

The earliest antineoplastic compounds aimed at cellular reproduction.  One way malignant cells differ is in that they reproduce more quickly than other cells.  If you send in a drug to disrupt the mitosis (cell dividing) process, you can affect fast-multiplying cancerous cells more than normal cells.  And this is the method by which most chemotherapy drugs have their effects.  Kill the cells while they divide.  We say the drugs are cytotoxic.

Of course the specificity is not even close to perfect, which means many healthy cells are inadvertently killed.   That’s why chemotherapy drugs have severe side effects.

This also explains why side effects show up where they do.  In the cancer-free body some cells multiply faster than others.  Cells in the bone marrow, skin, lining of the digestive system, for instance, grow faster than most cells, and that’s why common side effects include anemia, skin rashes, and nausea.

The cell reproduction cycle is complex and different chemotherapy drugs attack different points in the cycle, so we see somewhat different side effects from different drugs.

This is why chemo nay-sayers say chemo is poison.  The difference between a poison and a medicine is at least partly in the intent of the administrator.

Liver and Kidney damage

The body eliminates foreign substances largely through action of the kidneys and liver.  The liver metabolizes foreign substances – that is – it chemically transforms them to different materials.  If these foreign substances are poisons, the liver might be able to make them non-poisonous, or less poisonous.  The kidneys are super-filters that remove unusual materials from the bloodstream.  When the kidneys function correctly, foreign substances are sent to the urine stream and they exit the body.

Because they are at the front line in the war against poison, the kidneys and liver often take the most damage, and emergency room doctors know to check liver and kidney function when a patient has swallowed something hazardous.  Likewise, liver and kidney damage happens during chemotherapy treatment and is a particular danger if the dose is too high.  The assault on these organs is fundamentally different from the side effects chemotherapy bring; damage to the liver and kidneys is acute and often causes immediate cessation of the cancer treatment.  Further, if the cancer itself damages the liver or kidneys, options for chemotherapy treatment are reduced.

Medicine Trade Name Category Other
Abiraterone Zytiga Antiandrogen
Actinomycin-D Act-D, Cosmegen Antibiotics
Aldesleukin Proleukin Immunostimulant
Alemtuzumab Campath Monoclonal antibody
Alitretinoin Panretin, Toctino Retinoids
Altretamine Hexalen Alkylating agent
Aminoglutethimide Cytadren Aromatase inhibitor
Anastrozole Arimidex Aromatase inhibitor
Arabinosylcytosine Cytarabine Antimetabolite
Arsenic Trioxide Other Might also cause cancer
Asparaginase Elspar, Kidrolase Other
Azacitidine Vidaza Antimetabolite
Bendamustine Treanda Alkylating Agent
Bevacizumab Avastin Monoclonal antibody Angiogenesis inhibitor
Bexarotene Targretin Retinoid
Bicalutamide Casodex Anti-Androgen
Bleomycin Blenoxane Antibiotic
Bortezomib Velcade Kinase Inhibitor
Bosutinib Bosulif Kinase Inhibitor
Brentuximab vedotin Adcetris Monoclonal Antibody
Busulfan Myleran Alkylating Agent
Cabazitaxel Jevtana Taxane
Capecitabine Xeloda Antimetabolite Prodrug of Fluorouracil
Carboplatin Paraplatin Alkylating Agent Platinum compound
Carmustine BiCNU Alkylating Agent
Cetuximab Erbitux MAB
Chlorambucil Leukeran Alkylating Agent
Cisplatin Platinol Alkylating Agent Platinum compound
Cladribine Litak and Movectro Antimetabolite Purine Analog
Crizotinib Xalkori Kinase Inhibitor
Cyclophosphamide Endoxan, Cytoxan, Neosar Alkylating Agent
Cytarabine Cytosar-U Antimetabolite
Dacarbazine DTIC, DTIC-Dome Alkylating Agent
Dasatinib Sprycel Kinase Inhibitor
Daunorubicin DaunoXome, Cerubidine Anthracycline
Decitabine Dacogen Antimetabolite Cytosine Analog
Degarelix Firmagon Antiandrogen
Denileukin diftitox Ontak Other
Docetaxel Taxotere Mitotic Inhibitor
Doxorubicin Adriamycin Anthracycline


Medicine Trade Name Category Other
Epirubicin Ellence Anthracycline
Erlotinib Tarceva Kinase Inhibitor
Estramustine Estracit Alkylating Agent
Etoposide Eposin, Vepesid Topoisomerase inhibitor
Everolimus Zortress mTOR inhibitor
Exemestane Aromasin Aromatase Inhibitor
Filgrastim Neupogen Other
Fludarabine Phosphate Fludara Other
Fulvestrant Faslodex SERD
Gefitinib Iressa Kinase Inhibitor
Gemcitabine Gemzar Antimetabolite Nucleoside analog
Gemtuzumab ozogamicin Mylotarg Monoclonal antibody
Goserelin Zoladex Hormone agonist
Ibritumomab Zevalin Monoclonal antibody
Idarubicin Idamycin Anthracycline
Ifosfamide Mitoxana, Ifex Alkylating Agent
Imatinib Gleevec Kinase Inhibitor
Irinotecan Camptosa Topoisomerase inhibitor
Isotretinoin Roaccutane Retinoid
Ixabepilone Azaepothilone B Mitotic Inhibitor
Lapatinib Tykerb Kinase Inhibitor
L-asparaginase Elspar Other can be given as an intramuscular, subcutaneous, or intravenous injection
Lenalidomide Revlimid Other Angiogenesis inhibitor
Letrozole Femara Aromatase Inhibitor


Medicine Trade Name Category Other
Leucovorin Antimetabolite Same as Folinic acid
Leuprolide Viadur, Eligard Hormone Suppresant
Lomustine CeeNu Alkylating Agent
L-Sarcolysin Alkeran Alkylating Agent
Mechlorethamine Mustargen Alkylating Agent
Melphalan Alkeran Alkylating Agent
Mercaptopurine Purinethol Antimetabolite
Methotrexate MTX Antimetabolite Antifolate
Mitomycin Antibiotic
Mitoxantrone Topoisomerase inhibitor
Nelarabine Arranon Antimetabolite
Nilotinib Tasigna Kinase inhibitor
Nilutamide Nilandron, Anandron Anti-androgen
Nitrogen Mustard Alkylating Agent A class of drugs
Ofatumumab Arzerra Monoclonal antibody
Oxaliplatin Eloxatin Alkylating Agent Platinum compound


Medicine Trade Name Category Other
Paclitaxel Taxol Mitotic Inhibitor
Panitumumab Vectibix Monoclonal antibody
Pazopanib Votrient Kinase Inhibitor
Pegaspargase Oncaspar Other
Pegfilgrastim Neulasta Other
Pemetrexed Alimta Antimetabolite Antifolate
Pentostatin Nipent Antimetabolite deoxycoformycin
Phenylalanine Mustard Alkeran Alkylating Agent
Pralatrexate Folotyn Antifolate
Prednisolone corticosteroid Mostly used for other diseases
Prednisone corticosteroid Mostly used for other diseases
Procarbazine Matulane Antimetabolite


Medicine Trade Names Category Other
Raltitrexed Tomudex Antimetabolite Antifolate
Rituximab Rituxan, MabThera Monoclonal antibody
Sorafenib Nexavar Kinase Inhibitor
Streptozocin Zanosar Alkylating agent
Sunitinib Sutent, SU11248 Kinase Inhibitor
Tamoxifen Nolvadex, Istubal, and Valodex Aromatase inhibitor
Temozolomide Temodar, Temodal Alkylating agent
Temsirolimus Torisel Kinase Inhibitor
Teniposide Vumon, VM-26 Other
Thalidomide Thalomid Other
Thioguanine Tabloid Antimetabolites
Thiotepa Thioplex Alkylating agent
Topotecan Hycamtin Topoisomerase inhibitor
Toremifene Fareston SERM
Tositumomab Bexxar Monoclonal antibody
Trastuzumab Herceptin Monoclonal antibody
Valrubicin Valstar Anthracycline
Tretinonin Vesanoid Retinoid
Vinblastine Velban Vinca Alkaloid
Vincristine Vincasar Pfs Vinca Alkaloid
Vindesine Vinca Alkaloid
Vinorelbine Navelbine Vinca Alkaloid
Vorinostat Zolinza HDAC inhibitor


Popular combination regimens for chemotherapy.

The economics and market structure of the chemotherapy industry.