[3] Drugs for Cancer (pp. 3-4)

1. Plant Alkaloids

2. Antibiotic Anticancer Agents

3. Alkylating Agents

4. Hormonal Agents

5. Antimetabolites

6. Miscellaneous Anticancer Drugs

General Types of Anti-Cancer Drugs

• Alopecia

• Bone marrow suppression

• Fatigue

Common Side Effects of Cancer Treatment

• Vinca Alkaloids

• Taxanes

• Podophyllotoxins

• Camptothecins

These are groups of drugs classified as Plant Alkaloids used as treatment for Cancer.

Vinca rosea (Cataranthus roseus)

Periwinkle plant

Source for Vinca Alkaloids

M-Phase specific; binds to microtubules, forming a drug-tubulin complex

What is the of Vinca alkaloids?

Terminates the formation of microtubules by promoting depolymerization and preventing “rescue” of microtubules.

What is the action of the drug-tubulin complex formed with Vinca alkaloids?

Vinblastine

This agent is a Vinca alkaloid, indicated/used for the treatment of Testicular cancer.

• Vinblastine

• Vincristine

What are the anti-cancer agents classified as Vinca alkaloids?

Vincristine

This agent is a Vinca alkaloid, indicated/used for the treatment of the following conditions:

• Hodgkin’s lymphoma

• Wilm’s tumor

Bone marrow suppression

What is the major side-effect of Vinblastine?

Neurotoxicity

What is the major side-effect of Vincristine?

Western yew (Taxus brevifolia)

European yew (Taxus baccata)

What are the sources of Taxanes?

• M-Phase specific; enhances tubulin polymerization

• Blocks dynamic instability by stabilizing GDP-bound tubulin in microtubule

• This leads to weak polymers and clogged microtubules, inhibiting cancer cell division.

What is the MOA of Taxanes?

• Paclitaxel

• Docataxel

What are the anti-cancer. agents classified as Taxanes?

Paclitaxel

This anti-cancer drug under Taxanes is indicated/used for the treatment of the following conditions:

• Ovarian cancer

• Advanced breast cancer

• Neutropenia

• Thromocytopenia

• Peripheral neuropathy

What are the adverse effects of Paclitaxel?

Docataxel

This anti-cancer drug is indicated/used for the treatment of advanced breast cancer and has an adverse effect of bone marrow suppression.

Root of mayapple (Podophyllum peltatum)

Source of Podophyllotoxins

Inhibits topoisomerase II

What is the MOA of Podophyllotoxins?

Topoisomerase

These are enzymes that break, unwind, and reseal tangled DNA strands for DNA replication and RNA transcription.

Topoisomerase I

This enzyme acts on 1 strand only.

Topoisomerase II

This enzyme acts on both strands for DNA.

• Etoposide

• Teniposide

These are the anti-cancer agents classified as Podophyllotoxins.

Etoposide

This anti-cancer drug under Podophyllotoxins is indicated/used for the following conditions:

• Monocytic leukemia

• Testicular cancer

• Lung carcinoma

Teniposide

This anti-cancer agent under Podophyllotoxins is indicated/used for the treatment of Lymphomas.

• Hematopoietic toxicity

• Lymphoid system toxicity

What are the general, major side effects of Podophyllotoxins?

Camptotheca acuminata

“Happy tree, CA tree, Tree of life”

What is the source of Camptothecins?

Inhibit topoisomerase I

What is the MOA of Camptothecin?

• Topotecan

• Irinotecan

What are the two agents classified as Camptothecins?

Topotecan

This anti-cancer agent under Camptothecins is indicated/used for the treatment of the following conditions:

• Metastatic ovarian cancer

• Cisplatin-resistant neoplasms

• Neutropenia

• Thrombocytopenia

• Anemiaq

What are the major adverse effects of Topotecan?

Irinotecan

This is a prodrug that is metabolized into SN-38, which is an active topoisomerase I inhibitor.

• Colon cancer

• Rectal cancer

What are the indications/uses for Irinotecan?

Myelosuppresion

What is the major adverse effect of Irinotecan?