Following on from our hugely popular 101 Pharmacology Facts that Every Pharmacy Student Should Know, we’ve come back with a more niche, but no less important, alternative – facts about anticancer drugs.

That’s because the topic of anticancer drugs is quite a complex one.

There are innumerable drug classes, regimens, mechanisms, adverse effects and drug interactions to consider. Add to that the fact that most anticancer drugs are used to tackle a wide diversity of cancers. It can, then, become difficult for pharmacy students to commit this blizzard of facts to memory.

The below 25 facts are by no means intended to be exhaustive, of course. However, they focus on many of the essential, most fundamental facts that students are expected to know. Have an exam on anticancer pharmacology? Memorize the list below right now!

Read the below list multiple times, in conjunction with your study materials, for maximum effect.

  1. Doxorubicin is used to treat cancers such as breast cancer, lymphoma and Kaposi’s sarcoma; it works by intercalating DNA and inhibiting topoisomerase II. Side effects with doxorubicin, a drug nicknamed “red devil” include: red urine discoloration, dilated cardiomyopathy, skin eruptions and typhlitis.
  2. Alkylating agents work by attaching an alkyl group – CnH2n+1 – to the guanine base of DNA, at the #7 nitrogen atom of the purine ring. Classic alkylating agents include cyclophosphamide, melphalan, ifosfamide, lomustine, carmustine, busulfan and chlorambucil.
  3. Think of AM for these alkylating agents:
    – CyclophosphAMide
    – BendAMustine
    – UrAMustine
    – IfosfAMide
    – ChlorAMbucil
  4. Mesna is given to prevent hemorrhagic cystitis in patients taking cyclophosphamide or ifosfamide – it works to detoxify the urotoxic acrolein.
  5. Bleomycin is used to treat cancers such as Hodgkin’s lymphoma, testicular and ovarian cancer – it works to induce breaks in DNA strands. Side effects of bleomycin include:
    – Pulmonary fibrosis (serious risk factor shared with another drug, busulfan)
    – Fever
    – Hyperpigmentation
    – Reynaud’s phenomenon
    – Vomiting
    – Alopecia
    – Rash
  6. Anthracycline anticancer drugs include DED:
    Daunorubicin
    Epirubicin
    Doxorubicin
  7. All anthracycline drugs are linked to cardiotoxicity.

  8. Dexrazoxane is a cardioprotective agent used to protect against the cardiotoxic effects of anthracycline anticancer drugs.
  9. Indications of daunorubicin – the acute and the c(k)hronic:
    Acute myeloid leukemia
    Acute lymphocytic leukemia
    Chronic myelogenous leukemia
    Kaposi’s sarcoma
  10. Cisplatin treats a very wide variety of cancers – from bladder to testicular (highly effective) to brain tumors – it works to interfere with DNA replication. Side effects with cisplatin include:
    – Nephrotoxicity
    – Hearing loss
    – Bone marrow suppression
    – Vomiting
    – Electrolyte disturbances
  11. Anticancer microtubule inhibitors – the taxanes and vinca alkaloids:
    Taxanes
    – Paclitaxel
    – Docetaxel
    Vinca alkaloids
    – Vincristine
    – Vinblastine
    – Vindesine
  12. Anticancer topoisomerase inhibitors work by effecting either topoisomerase I or topoisomerase II:
    Topo I
    – Irinotecan
    – Topotecan
    Topo II
    – Etoposide
    – Teniposide
    – Daunorubicin
    – Doxorubicin
    – Mitoxantrone
  13. Tamoxifen is used to treat and prevent breast cancer; an antagonist at the ER receptor in breast tissue. Effects of tamoxifen:
    – Increased risk of uterine cancer
    – Decreased bone breakdown
    – Irregular periods
    – Weight loss
    – Hot flashes
  14. Monoclonal antibodies are increasingly used to treat a wide variety of cancers:
    Rituximab: works against the protein CD20 to treat hematological cancers such as non-Hodgkin’s lymphoma and chronic lymphocytic leukemia.
    Bevacizumab: is an angiogenesis inhibitor, slowing the growth of new blood vessels. It is used to treat renal-cell carcinoma, glioblastoma, lung cancer and colon cancer.
    Cetuximab: is an epidermal growth factor receptor (EGFR) inhibitor. It is used to treat colorectal cancer and head and neck cancer.
    Trastuzumab: is used to treat HER2-positive breast cancer. It works by inhibiting the HER2 pathway, a pathway responsible for the cell growth and division in breast tissue.
    Alemtuzumab: works by binding to CD52, a binding that makes lymphocytes a target for destruction. It is used to treat chronic lymphocytic leukemia (CLL) and T-cell lymphoma.
  15. Bicalutamide is an antiandrogen drug used primarily in the treatment of prostate cancer. However, the drug is not used alone. Instead, it’s used alongside a GnRH analogue – such as leuprorelin or buserelin.
  16. Exemestane, a member of the aromatase class of medicines, is primarily used in the treatment of breast cancer, particularly breast cancer that has proved invasive despite other therapies having been used.
  17. Capecitabine is used in the treatment of colorectal cancer, colon cancer and breast cancer. Capecitabine is converted into 5-fluorouracil in the body; 5-FU being a medicine that is itself used to treat a wide variety of cancers – colon, rectum, stomach, breast and pancreas. 5-FU works as an antimetabolite – blocking the action of thymidylate synthase and, in effect, the production of DNA.
  18. How do we remember that capecitabine treats colorectal and colon cancer?
    Capecitabine
    Colon cancer
    Colorectal cancer
  19. Pemetrexed is used in the treatment of two main conditions:
    – Non-small cell lung cancer
    – Mesothelioma (combined with cisplatin)
    Pemetrexed is also an antimetabolite medicine, preventing formation of purine and pyrimidine nucleotides (and so production of DNA) – by inhibiting thymidylate synthase and dihydrofolate reductase, among others.
    Recall the 5 Ps: Pemetrexed Prevents Purine and Pyrimidine Production.
  20. Dacarbazine is used to treat malignant melanoma (skin cancer) and Hodgkin’s disease. It works by methylating guanine, one of the four bases of DNA – meaning cell division becomes impossible.
  21. Prednisone is widely used in anticancer regimens. For example, it is often used alongside mitoxantrone in the treatment of prostate cancer (albeit a second-line treatment).
  22. However, prednisone also comes with clinical value in the treatment of HAM:
    Hodgkin’s lymphoma
    Acute lymphoblastic leukemia
    Multiple myeloma

  23. Imatinib is an anticancer drug used to treat the following conditions (CAGE):
    Chronic myelogenous leukemia (CML)
    Acute lymphocytic leukemia (ALL)
    Gastrointestinal stromal tumor (GIST)
    Imatinib works by stopping the Bcl-Abl tyrosine kinase – slowing growth of cancer cells or inducing programmed cell death; B – ImatinibBcl-Abl.
  24. Indications for carmustine and lomustine, drugs that belong to the alkylating agent family of chemotherapy drugs, include:
    – Brain tumors
    – Lymphoma (Hodgkin and non-Hodgkin)
    Carmustine is also used to treat multiple myeloma.
  25. ThioTEPA is also an alkylating agent; a drug combined with other treatments to tackle breast, ovarian and bladder cancers, among others. The main side effect is bone marrow suppression. In some cases, liver and lung toxicity occur.
  26. Methotrexate was originally used as a chemotherapy drug. It is used to treat a wide variety of cancers – breast, head and neck, skin and lung, among others. It works as an antimetabolite of the antifolate class – inhibiting dihydrofolate reductase (DHFR) production, an enzyme needed to catalyse production of tetrahydrofolate. In this way, methotrexate inhibits synthesis of DNA, RNA and thymidylates (due to its effect on folic acid).
  27. Anticancer pharmacology terms:
    Carcinogen: any substance that promotes carcinogenesis, the development of cancer.
    Cancer: takes its name from the Greek karkinos, meaning crab or crab-like – referring to the shape of veins from a sliced tumor. Cancer refers to the abnormal growth of cells.
    Benign tumors do not spread, whereas malignant/metastatic cancer spread.
    Apoptosis: cancer cells do not undergo programmed cell death, or apoptosis. This means they are able to grow and spread further around the body.

Want to learn more about the pharmacology of anticancer drugs – their indications, mechanisms, adverse effects, drug interactions and other clinical considerations? Join our member’s area today – our resources contain everything you need to know not only to master anticancer pharmacology but also every other major drug class, too.