This slides show you the antineoplastic or anticancer drugs and their etiology and in this slide we can see the mechanism of some antineoplastic drugs.

1. Antineoplastic Drugs

2. What is antineoplastic drug?
 Antineoplastic drugs are the type of drugs that are used to
treat malignant diseases like cancer. Drugs contain chemicals
that kill rapidly divided cells.
 Other names for antineoplastic drugs are anticancer,
chemotherapy, chemo, cytotoxic, or hazardous drugs.

3. Characteristics of cancer
cells
• Persistent cell proliferation
• Invasive growth
• Metastasis

4. • Genetics
• Viruses
• Occupational and environmental change
• Radiation
Etiology of cancer Genetic
mutations
Oncogenes
Tumor suppressor gene
Telomeres
Abnormal karyotype
Viruses
Immune system dysfunction
Ionizing radiation
• 1.Direct ionization
• 2.Secondary effectors

5. Genesis of cancer
Decreased expression of tumor suppressor
genes:P54, Rb1
Proto-oncogenes converted to oncogenes
sis, erbB, ras, myc gene for cyclin C
Alteration of gene expression
Metastasis
Angiogenesis
Invasion of nearby tissue by tumor cells
Production of metalloproteinases
Secondary tumor development
Decreased apoptosis,
alterations in telomerase
Uncontrolled cell proliferation,
dedifferentiation
Other factors
Inherited mutations
Acquired mutations
Chemicals, viruses, irradiation
Primary tumor development

6. Problems associated with chemotherapy
Decrease the amount of drug reuptake
Decrease
Increase the amount of drug removed by
cancer cells
Increase
Decrease or alteration in target molecule
sensitivity
Decrease
Increase in DNA repair ability of the cell
Increase

7. DNA
Deoxyribonucleotide
Ribonucleotides
Pyrimidine synthesis
Purine synthesis
RNA
Enzymes
Proteins
Microtubules
PENTOSTATIN
Inhibit adenosine
deaminase
6-MERCAPTOPURINE
6-THIOGUANINE
Inhibit purine synthesis
Inhibit nucleotide
interconversions
METHOTREXATE
Inhibit purine synthesis
Inhibit DNA polymerase
CRISANTASPASE
Deaminates asparagine
Inhibit protein synthesis
5-FLUOROURACIL
Inhibit
topoisomerase II
CAMPOTHECINS
DOXORUBICIN
Cross-link DNA
ALKYLATING AGENT
Damage DNA and
prevent repair
BLEOMYCINS
Inhibit RNA function
CYTARABINE
Inhibit DTMP synthesis
Inhibit DTMP synthesis
Inhibit RNA synthesis
Inhibit function of
microtubules
VINCA ALKALOIDS
DACTINOMYCIN
Intercalates in DNA
Inhibit
topoisomerase II
Inhibit RNA synthesis
Main site of action of cytotoxic agents:

8. Alkylating agents
Nitrogen Mustards
e.g.
Meclorethamine,
Cyclophosphamide
Nitrosoureas e.g.
Carmustine
Triazines e.g.
Dacarbazine

9. Nitrogen Mustards
e.g. Meclorethamine,
Mechanism of action

10. Folate antagonist
e.g. Methotrexate
Mechanism of action
Structure of folic acid & methotrexate
Antimetabolites

11. Purine antagonists
e.g.
6-Mercaptopurine &
6-Thioguanine
Mechanism of action
Antimetabolites

12. Pyrimidine
antagonists
e.g.
5-fluorouracil
Mechanism of action
Antimetabolites

13. Cancer therapy
Block
angiogenesis
Halt
neoplastic
cell division
Prevention
of
metastasis
Removal
via surgery
Destroy
neoplastic
cells
Different therapies or combinations
of treatments with chemotherapy

14. Bone marrow depression
Immediate adverse effects
Psychiatric morbidity
Teratogenicity
Carcinogenicity
Adverse effects of
anticancer drugs

15. THANK YOU
Any question??