Cancer drugs: Antineoplastic medications

Cell cycle specific drugs (CCS)

- Drugs that are cytotoxic during a specific cell cycle phase
- Used to treat a variety of solid and circulating tumors
- Classes of drugs:
o Antimetabolites
o Mitotic inhibitors
o Alkaloid topoisomerase II inhibitors
o Topoisomerase I inhibitors
o Antineoplastic enzymes

Antimetabolites:
Action:
- antagonizing the actions of key cellular metabolites. More specifically, antimetabolites inhibit cellular
growth by interfering with the synthesis or actions of compounds critical to cellular reproduction: the
vitamin folic acid, purines, and pyrimidines.
Indications:
- Used in combination with other drugs to treat various types of cancer, such as solid tumors and some
hematologic cancers
o Acute and chronic lymphocytic leukemias
o Colon, rectal, breast, stomach, lung, pancreatic cancers
- Oral and topical forms may be used for low-dose maintenance and palliative cancer therapy
Adverse effects:
- hair loss, nausea and vomiting, myelosuppression
- metabolic toxicity also includes tumor lysis syndrome (a common post chemotherapy condition) this is
associated with rapidly growing hematologic malignances
o it may include hyperphosphatemia, hyperkalemia, and hypocalcemia
o hyperuricemia can lead to nephropathy, and hemodialysis may be required in serve cases
- Palmar-plantar dysesthesia or paresthesia (hand foot syndrome)

Antimetabolite drugs:
Folate (folic acid) antagonists
- Methotrexate (MTX)
o Results in DNA not being produced and the cell dying
o Also used to treat psoriasis and rheumatoid arthritis
Immunosuppression and anti-inflammatory properties
o Rescue drug: leucovorin (wellcovorin)
Purine Antagonists
- Cladribine (Leustatin)
o Not cell cycle specific interrupts the synthesis of DNA and RNA
o Treatment of hairy cell leukemia
Pyrimidine antagonists
- Capecitabine (Xeloda) oral
o Inhibits production for DNA synthesis leading to chain termination
o Indicated for metastatic breast and colon cancer
- Cytarabine (Ara-C, Cytostar-U)
- Fluorouracil (5-FU, Adrucil)
Mitotic inhibitors:
- Vinca alkaloids:
- Natural products obtained from the periwinkle plants
o Vinblastine (Velban)
o Vincristine (Oncovin)
Only available in injectable form
Most significant neurotoxin in its class
Dilute in 25 ml of fluid and NEVER dispensed via syringe
o Vinorelbine (Navelbine)
- Taxanes:
- Semisynthetic drugs from mandrake (mayapple) plant and other drugs obtained from the yew tree
o doxetaxel (Taxotere) (European yew tree: needles)
o Paclitaxel (Taxol) (western pacific yew tree: bark)
water insoluble (hydrophobic) and put into a solution containing oil rather than water
only available in injectable form
Indications:
- used in combination therapies
o the use of multiple use of antineoplastic drugs can cause neutropenia and infection, due to
additive bone marrow suppression
- solid and hematologic tumors

Adverse effects:
- hair loss, nausea and vomiting, myelosuppression
- liver, kidney, and lung toxicities
- neuropathic constipation
- extravasation (vinca alkaloids are vesicants)
o antidotes can be used