This document classifies and describes various anticancer drugs, including cytotoxic drugs like alkylating agents, platinum coordination drugs like cisplatin, antimetabolites, microtubule damaging agents like vincristine and vinblastine, topoisomerase inhibitors, antibiotics, targeted drugs, hormonal drugs, and miscellaneous drugs. It provides details on the mechanisms of action, uses, doses, and common side effects of representative drugs from each class, such as how cisplatin causes DNA cross-linking, how vinca alkaloids inhibit microtubule assembly, and how paclitaxel and docetaxel inhibit beta-tubulin.

1. Anticancer drugs
Dr. S. Parasuraman
Faculty of Pharmacy,
AIMST.

2. Classification of anticancer agents
Cytotoxic drugs
1. Alkylating agents
2. Platinum coordination: Cisplatin, Carboplatin, Oxaliplatin
3. Antimetabolites
4. Microtubule damaging agents: Vincristine, Vinblastine,
Vinorelbine, Paclitaxel, Docetaxel
5. Topoisomerase-2 inhibitor: Etoposide
6. Topoisomerase-1 inhibitor: Topotecan, Irinotecan
7. Antibiotics: Actinomycin D, Doxorubicin, Daunorubicin,
Epirubicin, Bleomycins, Mitomycin C.
8. Miscellaneous: Hydroxyurea, L-Asparaginase, Tretinoin,
Arsenic trioxide

3. Classification of anticancer agents
Targeted drugs
1.
2.
3.
4.
5.
Tyrosine proteinkinase inhibitors: Imatinib, Nilotinib
EGF receptor inhibitor: Gefitinib, Erlotinib
Angiogenesis inhibitors: Bevacizumab
Proteasome inhibitor: Bortezomib
Unarmed monoclonal antibody: Rituximab, Trastuzumab

4. Classification of anticancer agents
Hormonal drugs
1.
2.
3.
4.
5.
6.
7.
8.
9.
Glucocorticods: Prednisolone
Estrogens: Fosfestrol, ethinylestradiol
Selective estrogen receptor modulators: Tamoxifen
Selective estrogen receptor down: Fulvestrant
Aromatase inhibitors: Letrozole, Anastrozole
Antiandrogen: Flutamide
5-α reductase inhibitor: Finasteride
GnRH analogues: Nafarelin, Triotorelin
Progestins: Hydroxyprogesterone acetate

5. Platinum coordination
Cisplatin:
• Cisplatin hydrolysed intracellularly to produce a highly
reactive moiety which causes cross linking of DNA.
• Effect is resemble those of alkylating agents and
radiation.
• Bound to plasma proteins, penetrates tissues and is
slowly excreted unchanged in urine with t½ of about 72
hr.
• Very effective in metastatic testicular and ovarian
carcinoma. Widely used in many solid tumours like lung,
bladder, esophageal, gastric, hepatic, head and neck
carcinomas.
• Dose: 50-100 mg/m2

6. Microtubule damaging agents
Vinca alkaloids (Vincristine & vinblastine):
•
MoA:
–
–
•
Inhibits microtubular protein and prevents polymerization and
assembly of microtubules and cause disruption of mototic
spindle and interfere with cytoskeletal function.
Cell cycle specific, acts on MITOTIC phase.
Use:
–
Administered in combination with other drugs. Used in POMP
regimen for leukemia and the MOPP regimen for Hodgkin
lymphoma
– Vinca alkaloids are used in the treatment of acute
lymphoblastic leukemia in children, Wilms tumor, Ewing
soft-tissue sarcoma, and Hodgkin and non-Hodgkin
lymphomas as well as some other rapidly proliferating
neoplasms.

7. Microtubule damaging agents
Vinca alkaloids (Vincristine & vinblastine):
•
MoA:

8. Microtubule damaging agents
Vinca alkaloids (Vincristine & vinblastine):
•
Resistance:
–
•
Pharmacokinetics:
–
–
–
•
Resistant cells have enhanced efflux of vinca alkaloids via Pglycoprotein in the cell membrane.
IV administration has rapid cytotoxic effects and cell destruction.
Metabolized in the liver by the CYP450 pathway.
Excreted in bile and feces.
Adverse effects:
–
–
phlebitis or cellulitis, if the drugs extravasate during injection
Nausea, vomiting, diarrhea, and alopecia
– Myelosuppressant, Inappropriate ADH secreaction.
• Dose:
–
–
Vincristine 1.5-5 mg/m2 BSA
Vinblastine 0.1-0.15mmg/kg i.v. weekly X 3 doses

9. Taxanes
Paclitaxel, Docetaxel:
• Paclitaxel is a diterpin taxane obtained from bark of the
Western yew tree.
• Paclitaxel has shown good activity against advanced ovarian
cancer and metastatic breast cancer.
• Docetaxel effective in breast and ovarian cancer.
• Both the drugs active in the G2/M phase of the cell cycle and
inhibiting the beta tubulin.
• Paclitaxel used for metastatic breast cancer after failure of first
line chemotherapy and relapse cases.
• Docetaxel effective in breast and ovarian cancer refractory to
first line drug.
• Dose: Paclitaxel – 135-175 mg/m2 i.v; Docetaxel 20-120 mg/vial
inj

10. Antibiotics
Drug
Actinomycin D
Use
• Very potent antineoplastic
drug, highly efficacious in
Wilms' tumour and
rhabdomyosarcoma
• Mtx resistant
choriocarcinoma
Daunorubicin
Doxorubicin
Epirubicin
ADR
vomiting,
stomatitis,
diarrhoea,
erythema and
desquamation of
skin, alopecia
Dose
15 µg/kg i.v.
daily for 5
days
• effective in many solid
tumours
• capable of causing breaks
in DNA strands by
activating topoisomerase II
and generating quinone
type free radicals
Marrow depression, Daunorubicin
alopecia, stomatitis, : 20 mg/vial
vomiting and local
inj
tissue damage
Doxorubicin:
60-75 mg/m2
• Newer drugs similar to
doxorubicin
Adj. therap. For
breast cancer, GIT,
bladder cancer
Dose: 60-90
mg/m2

11. Antibiotics
Drug
Mitomycin C
Use
• highly toxic drug is used
only in resistant cancers of
stomach, cervix, colon,
rectum, bladder, etc.
• kills cells in G1-M phases
ADR
Dose
Bone marrow and
• 10 mg/m2
g.i.t are the primary
BSA
targets of toxicity.

12. Miscellaneous
Drug
Use
ADR
Dose
Hydroxyurea
blocks the conversion of Myelosuppressio
ribonucleotides to
n is the major
deoxyribonucleotides by toxicity
inhibiting the enzyme
ribonucleoside
diphosphate
reductase- interferes
with DNA synthesis
(active in s phase)
20-30 mg/kg daily or
80 rng/kg twice
weekly
L-Asparaginase
The enzyme Lasparaginase (from E.
coli) degrades
L-asparagine to Laspartic acid, depriving
leukaemic cells of an
essential metabolite
Dose: SG-200 KU/kg
i.v. daily for 2-4
weeks
liver damage,
allergic reactions,
anaphylaxis

13. Miscellaneous
Drug
Use
Tretinoin
• Trans-retinoic acid, a
form of vit. A.
• Degradation of PLLRARα fusion gene.
Arsenic trioxide
• Traditional poison for
ages.
• Used for Acute
Promyelocytic
Leukemia (APL)
ADR
Dose
Dryness of skin,
eye, nose,
mouth, prutitus,
epistaxis, rise in
serum lipids and
intraocular
pressure.
Most important
ADR is ‘retinoic
acid syndrome’
Nausea, fatigue,
sensory
disturbances,
effusions,
hyperglycemia, QT
prolongation, A-V
block.

14. Thank you