Malignancies

• ALKYLATING AGENTS

  • Carboplatin
  • Chlorambucil
  • Cisplatin
  • Cyclophosphamide
  • Dacarbazine
  • Melphalan
  • Nitrogen mustard
• ALKYLATING AGENTS SIDE EFFECTS

  • Bone marrow depression
  • Amenorrhea in women
  • Azoospermia in men
  • carcinogenesis
• Alkylating Agents

  • First drugs identified to have anticancer activity
  • They are not cell cycle specific, but rather work throughout the cycle. The mechanism of action is to bond with nucleic acids, thereby interfering with their action
• ANTIMETABOLITES

  • Cytarabine
  • Methotrexate
  • 5-Fluorouracil (5-FU)
  • 6-Mercaptopurine
  • 6-Thioguanine
• ANTIMETABOLITES SIDE EFFECTS

  • Gastrointestinal toxicity
  • Acute bone marrow suppression
• Antimetabolites

  • Act by interfering with the synthesis of new nucleic acids.
  • They are cell cycle specific and are much more toxic to proliferating cells but are not associated with delayed bone marrow suppression or carcinogenesis
• ANTITUMOR ANTIBIOTICS

  • Bleomycin
  • Dactinomycin (actinomycin D)
  • Doxorubicin
  • Mithramycin
  • Mitomycin
• ANTITUMOR ANTIBIOTICS SIDE EFFECTS

  • Cardiac toxicity
  • Skin ulceration with extravasation
  • Pulmonary toxicities
  • Bone marrow suppression
  • Increased effects of radiation therapy
• Antitumor Antibiotics

  Derived from microbial fermentation. Antibiotics act on the

  DNA to disrupt DNA and RNA transcription. Although they are not cell cycle specific, the effects of the antibiotics are more pronounced in the S or G2 phase
• HORMONAL AGENTS

  • Corticosteroids
  • Dexamethasone
  • Hydrocortisone
  • Prednisone
  • Antiandrogen
  • Flutamide
  • Antiestrogen
  • Tamoxifen
  • Goserelin acetate (Zoladex)
  • Gonadotropin-releasing hormone
  • Leuprolide
• HORMONAL AGENTS SIDE EFFECTS

  • Hot flashes
  • Depression
  • Loss of libido
  • Increase risk in endometrial cancers.
• Hormonal Agents

  • Act to eliminate or displace natural hormones
  • The most common use is in the treatment of breast cancer when the tumor is positive for estrogen and progesterone receptors.
• An injectable hormone therapy used to treat prostate cancer.


  Lupron
• Clinically manipulate cells by binding to specific intracellular receptors and interacting with DNA to change cellular function.

  Steroid hormones
• NITROSOUREAS

  • Carmustine
  • Lomustine
  • Streptozocin
• NITROSOUREAS SIDE EFFECTS

  • Delayed myelosuppression
  • Gastrointestinal toxicity
  • Delayed nephrotoxicity
• Nitrosoureas


  Not cell cycle specific, but they are lipid soluble and able to

  cross the blood-brain barrier. Their action is similar to that

  of alkylating agents in that they interfere with DNA synthesis.
• PLANT ALKALOID

  • Etoposide
  • Paclitaxel (Taxol)
  • Vinblastine
  • Vincristine
• PLANT ALKALOID SIDE EFFECTS

  • Neurotoxicity,
  • Severe ulceration of the skin (if extravasation occurs)
  • Myelosuppression
• Plant Alkaloid


  Derived from the periwinkle plant. By binding to a substance

  that is needed for mitosis and solute transport, the vinca

  alkaloids stop cell replication in metaphase.
• Chemotherapy Drug Classification

  • Alkylating Agents
  • Antimetabolite
  • Antitumor Antibiotics
  • Hormonal Agents
  • Nitrosoureas
  • Plant Alkaloid