CHEMOTHERAPEUTIC AGENTS 3.

Injection
4. Arterial
CHEMOTHERAPY 5. Peritoneum/Abdomen
-treatment of cancer by means of chemical 6. Topical
that kill cancer cells CYTOTOXIC AGENTS
ANTI-CANCER DRUGS –drugs that kill cells directly, work by
-destroy cancer cells by stopping their growth interrupting cells at particular places in the
and development. growth cycle.

 Anti-metabolites -cell kill and eventual tumour shrinkage

-Purine analogs CYTOTOXIC T CELLS
-Purine antagonists
-Pyrimidine antagonists – are part of the immune system, which
-Antifolates searches for, finds and destroys cells infected
-Ribonucleotide reductase inhibitors by viruses as well as cancer cells.
 Alkylating Agents
-Platinum-based agents
-Hydrazine
-Oxazaphosphorines
-Nitrogen mustards
 Mitotic Spindle Inhibitors
-Taxanes
-Vinca Alkaloids
 Topoisomerase Inhibiors I and II
 Others
-Proteasome inhibitors
-Enzymes
-Tyrosine kinase inhibitors
-Antibiotics
CELL CYCLE
G0- Resting MCA

G1- Synthesis of components needed for DNA -Disrupts processes related to synthesis of
synthesis DNA or its precursors

S- Synthesis of DNA Cell-Cycle Phase-Specific Drugs:

G2- Synthesis of components needed for  Toxic only to cells that are passing
mitosis through a particular phase of the cell
cycle
M- Mitosis  Cells in “resting” phase (G0) will not
CHEMOTHERAPY DELIVERED VIA: be harmed
 Known as “schedule-dependent
1. Intravenous drugs”
2. Oral
1. Antimetabolites –Methotrexate, 5
Flourouracil
2. Antibiotics – Bleomycin
3. Vinca alkaloids –Vinblastine, Vincristine
G1 PHASE INHIBITORS
CISPLATIN
-binds to the N7 reactive center on purine
residues
-cause DNA damage in cancer cells
-blocks cell division
-results in apoptotic cell death
S INHIBITORS
FLUOROURACIL
-blocks enzyme that converts cytosine
nucleotide in deoxy derivative
-blocks the incorporation of the thymidine
nucleotide into the DNA strand
METHOTREXATE
-inhibition of enzymes responsible for
nucleotide synthesis including dihydrofolate
reductase, thymidylate synthase,
aminoimidazole caboxamide ribonucleotide
transformylase and amido
phosphoribosyltransferase
Drug Class: Immunosuppressants;
Antineoplastics, Antimetabolite,
Immunomodulators.
G2 INHIBITORS
ETOPOSIDE
-inhibits DNA synthesis by forming a complex
with Topoisomerase II and DNA.
-induces breaks in double stranded DNA and
prevents repair by topoisomerase II binding
DNA breaks prevent entry into the mitotic
phase of cell division, and lead to cell death.
MITOTIC INHIBITOR
-plant alkaloids
-stops cell from dividing but can damage cells
in all phases by keeping enzymes from
making proteins needed for cell reproduction
-act during the M phase to prevent cell
division
 Vince Alkaloids- Vinca Rosea
(Periwinkle plant)
 Taxanes- acts during late G2 and M
phase
VINCRISTINE
-inhibition of microtubule formation in
mitotic spindle
-results in an arrest of dividing cells at the
metaphase stage
PACLITAXEL
-defects in mitotic spindle assembly,
chromosome segregation and cell division
ALKYLATING AGENTS
-keeps the cell from reproducing by damaging
its DNA
-works in all phases of the cell cycle
-Bendamustine, Busulfan, Carboplatin,
Carmustine, Chlorambucil
Cell-Cycle Phase-Nonspecific Drugs:
 Act on any phase of the cell cycle,
including G0
 Can increase cell kill when combined
with phase specific drugs
 Among the phase-nonspecific drugs
are the
 alkylating agents and most antitumor
antibiotics
CARBOPLATIN
Drug class - Antineoplastics, Alkylating,
Platinum Analog.
MOA - undergoes activation inside cells and
forms reactive platinum complexes that cause
the intra- and inter-strand cross-linkage of
DNA molecules within the cell. This modifies
the DNA structure and inhibits DNA
synthesis. This may affect a cell in all the
phases of its cycle.
ANTITUMOR ANTIBIOTICS
-treat cancer by affecting the genetic material
within cancerous cells.
-prevents cancer cells from growing and
spreading.
- Antracyclines – Doxorubicin, Epirubicin
BLEOMYCIN
-has antitumor activity
-selectively inhibits the synthesis of DNA
-has major effects in G2 and M phases
DOXORUBICIN
-slows or stops the growth of cancer cells
-blocks Topoisomerase 2