18. ANTI-NEOPLASTIC AGENTS

Anti-neoplastic agents, also called anticancer or chemotherapy drugs, are medicines used to treat different types of cancers. Cancer cells divide rapidly and uncontrollably, forming tumors and spreading to other parts of the body. Anti-cancer drugs work by slowing or stopping the growth of these abnormal cells.

What Is Cancer?

Cancer occurs when normal cells undergo genetic changes and begin to multiply beyond control. They invade nearby tissues and may spread (metastasize) to distant organs. Because cancer cells divide faster than most normal cells, chemotherapy targets these rapidly growing cells.

General Mechanisms of Anti-Cancer Drugs

Anti-neoplastic drugs act through different mechanisms:

  • Damaging cancer cell DNA
  • Blocking DNA or RNA synthesis
  • Preventing cell division (mitosis)
  • Inhibiting enzymes needed for cancer growth
  • Triggering cancer cell death (apoptosis)

Classification of Anti-Neoplastic Agents

1. Alkylating Agents

These drugs add alkyl groups to DNA, making it impossible for cancer cells to replicate.

Examples: Cyclophosphamide, Chlorambucil, Melphalan, Busulfan.

Uses: Leukemia, lymphomas, breast cancer.

2. Antimetabolites

Antimetabolites resemble natural molecules needed for DNA synthesis but block cell division when incorporated into DNA/RNA.

Examples:

  • Methotrexate – folate antagonist
  • 5-Fluorouracil (5-FU) – pyrimidine analog
  • Cytarabine – used in leukemia

3. Antibiotic Anti-Cancer Agents

These are not typical antibiotics used for infections; instead, they inhibit DNA replication in cancer cells.

Examples: Doxorubicin, Bleomycin, Mitomycin.

Uses: Solid tumors and blood cancers.

4. Plant Alkaloids

Derived from plants, these agents interfere with mitotic spindle formation and block cell division.

Examples:

  • Vincristine and Vinblastine – act on microtubules
  • Paclitaxel (Taxol) – stabilizes microtubules

5. Hormones and Hormonal Antagonists

Some tumors depend on hormones to grow; these drugs block hormone production or action.

  • Anti-estrogens: Tamoxifen
  • Aromatase inhibitors: Anastrozole
  • Anti-androgens: Flutamide
  • Corticosteroids: Prednisolone

6. Enzyme Inhibitors

These drugs block enzymes critical for cancer growth.

  • Topoisomerase inhibitors: Etoposide, Topotecan
  • Tyrosine kinase inhibitors: Imatinib

7. Miscellaneous Agents

Drugs with unique mechanisms.

  • Hydroxyurea – inhibits DNA synthesis
  • Procarbazine – disrupts DNA function

Drug Profiles

Cyclophosphamide

Class: Alkylating agent.

Mechanism: Forms cross-links in DNA, preventing cell division.

Uses: Breast cancer, lymphomas, autoimmune diseases.

Methotrexate

Class: Antimetabolite (folate antagonist).

Mechanism: Inhibits dihydrofolate reductase, blocking DNA synthesis.

Uses: Leukemia, breast cancer, choriocarcinoma.

5-Fluorouracil (5-FU)

Mechanism: Inhibits thymidylate synthase, preventing DNA formation.

Uses: Colon cancer, breast cancer.

Doxorubicin

Class: Anti-cancer antibiotic.

Mechanism: Intercalates DNA and produces free radicals.

Uses: Many solid tumors and leukemias.

Vincristine

Class: Plant alkaloid.

Mechanism: Prevents spindle formation in mitosis.

Uses: Leukemia, lymphoma.

Paclitaxel

Mechanism: Stabilizes microtubules, blocking cell division.

Uses: Breast and ovarian cancer.


General Adverse Effects of Anti-Cancer Drugs

Because chemotherapy targets rapidly dividing cells, it also affects fast-growing normal tissues.

  • Hair loss (alopecia)
  • Bone marrow suppression
  • Nausea and vomiting
  • Mouth ulcers
  • Infections due to low immunity

Drug-Specific Side Effects

  • Doxorubicin: Heart toxicity
  • Bleomycin: Lung fibrosis
  • Vincristine: Nerve toxicity

Detailed Notes:

For PDF style full-color notes, open the complete study material below:

Share your love