Anticancer Drugs

ANTICANCER DRUGS
ANTIMETABOLITES
Methotrexate Fluorouracil-5

ANTIBIOTICS
Doxorubicin Daunorubicin

ALKYLATING AGENTS
Ifosfamide Cyclophosphamide

MICROTUBULE INHIBITORS
Vincristine Vinorelbine Vinblastine

STEROID HORMONES AND

THEIR ANTAGONISTS
Prednisone
 Principles of Cancer
Chemotherapy
• Ideally, anticancer drugs should interfere
only with cellular process that are unique to
malignant cells. Unfortunately, most
currently available anticancer drugs do not
specifically recognize neoplastic cells but,
rather, affect all proliferating cells- both
normal and abnormal.
 Antimetabolites
• Antimetabolites are structurally related to
normal compound within the cell.

• Methotrexate
Methorexate is structurally related to folic acid, and
act as an antagonist of that vitamin by inhibiting
dihydrofolate reductaes – the enzyme that
convert folic acid to its active, coenzyme form,
tetrahydrofolic acid (FH ).
 Methotrexate
• Therapeutic uses: MTX, usually in
combination with other drugs, is effective
against acute lymphoma in children, breast
cancer, and head and neck carcinomas. In
addition, low- dose MTX is effective as a
single agent certain inflammatory diseases,
such as severe psoriasis and rheumatoid
arthitis
 Methotrexate
• Adverse effects:
1. Commonly observed toxicities: to nausea,
vomiting and diarrhea,.
2. Renal damage: Alkalinization of the urine
and hydration help to prevent this
problem.
3. Hepatic function: MTX may lead to
fibrosis or cirrhosis Hepatotixic agent.
 Methotrexate
4. Pulmonary toxicity
5. Neurologic toxicities
6. Contraindications: Because MTX is
teratogenic in experimental animals and is
an abortifacient, it should be avoided in
pregnancy.
 Alkylating Agents
• Alkylation of DNA is probably the crucial
cytotoxic reaction that is lethal to the tumor
cell. They are used in combination with
other agents to treat a wide variety of
lymphatic and solid cancers.
• Cyclophosphamide
 Cyclophosphamide and
Ifosfamide
• These drugs are very closely related
mustard agents that share most of the
same toxicities
1. Mechanism of action: Cyclophosphamide
is the most commonly used alklating
agent. Both cyclophosphamide and
ifosfamide
 Steroid Hormones and Their
Antagonists
• Prednisone is a potent, synthetic, anti-
inflammatory corticosteroid with less
mineralocorticoid activity than cortisol.
• For patient with acute lymphocytic
leukemia.
 Prednisone
• Mechanism of action: prednisone itself is
inactive, and must first be reduced to
prednisolone.
• Adverse effects: prednisone has many of
the adverse effects associated with
glucocorticoids. It can predispose to
infection (due to its immunosuppressant
action) and to ulcers and pancreatitis.