The document provides an overview of various anti-cancer drugs, their classifications, mechanisms of action, and specific applications for different types of cancer. It discusses different categories of cancer and the respective drug choices for treatment, including cell cycle-specific and non-specific agents. Key drug classes include alkylating agents, antimetabolites, vinca alkaloids, and hormonal agents, along with their mechanisms and side effects.

1. ANTI-CANCER DRUGS
SUBMITTED TO; SUBMITTED BY;
Ms. Neelam Painuly Mr. Anupam
Associate Professor M. Pharm(PHARMACOLOGY)
Sopr.Neelam@dbuu.ac.in anupanni111@gmail.com
SoPR, DBUU, Dehradun SoPR, DBUU, Dehradun

2. CONTENTS
 INTRODUCTION
 TYPES OF CANCER
 CELL CYCLE
 CLASSIFICATION OF ANTI-CANCER DRUGS
 DISEASE AND THEIR DRUF OF CHOICE
 REFERENCES
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3. INTRODUCTION
The World Health Organization (WHO) defines the cancer as a wide range of diseases which produces
impact on any body part. The term "metastasis" refers to the unchecked proliferation & dissemination of
aberrant cells to various parts of body via the lymphatic or circulatory systems.
Cancer is a cell disease defined by abnormal, purposeless, progressive, persistent, and uncontrollably
growing tissue.
Cancer cell produce oncoproteins in the absence of growth factor or external stimuli.
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Fig1: Process of cancer cell development.

4. SOPR, DEV BHOOMI UTTARAKHAND UNIVERSITY 4
TYPES OF
CANCER
Carcinoma
Skin cells
and organs
like the
kidney or
liver
cancer.
Sarcoma
Bone,
cartilage,
fat, muscle,
connective
tissue and
supportive
tissue
cancer.
Leukaemia
Bone
marrow
cancer that
results in
an
excessive
quantity of
irregular
blood cells.
Myeloma
and
lymphoma
Immune
system
cancer.
CNS
Cancer
Brain and
Spinal cord
cancer.
Germ cell
Cancer
Testicle and
Ovarian
cancer.

5. Cell Cycle of both Normal as well as Cancer Cells
1. G1 phase (pre-synthetic phase, 40%): Enzyme and other
biological components required for DNA synthesis are
synthesised.
2. S phase (synthetic phase, 39%): The synthesis of DNA occurs.
3. G2 phase (pre-mitotic phase, 19%): biological components
necessary for myosis are synthesised (RNA and protein
synthesis).
4. M phase (mitotic phase, 2.1%): Division of mitotic cells occur.
5. G0 phase (resting phase): Stop division of cells.
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Fig2: Cell Cycle

6. CLASSIFICATION
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ANTI- METABOLITES
TAXANES
CAMPTOTHECINS
ENZYME
HORMONAL AGENTS
ANTIBIOTICS
EPIPODOPHYLLOTOXINS
VINCA ALKALOIDS
ALKYLATING AGENTS
ANTI-CANCER
DRUGS
MISCELLANEOUS
AGENTS

7. CLASSIFICATION OF ANTI-CANCER DRUGS
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1. Alkylating agents
a) Nitrogen Mustered: - Mechlorethamine, Cyclophosphamide, Melphalan, Chlorambucil.
b) Alkyl Sulfonate: - Busulphan.
c) Nitrosoureas: - Carmustine, Lomustine.
d) Platinum-containing compound: - Cisplatin, Carboplatin.
e) Triazene: - Dacarbazine.
2. Antimetabolites
a) Folate antagonists: - Methotrexate.
b) Purine antagonists: - 6-Mercaptopurine, 6-Thioguinine.
c) Pyrimidine antagonists: - 5-Fluorouracil, Cytarabine.

8. 3. Vinca Alkaloid: - Vincristine, Vinblastine.
4. Taxanes: - Paclitaxel, Docetaxel.
5. Epipodophyllotoxins: - Etoposide, Tenoposide.
6. Camptothecins: - Topotecan, Irinotecan.
7. Antibiotics: - Actinomycin, Bleomycin, Mitomycin, Doxorubicin.
8. Enzymes: - L-Asparaginase.
9. Miscellaneous agents: - Hydroxyurea, Imatinib.
10. Hormonal drugs
a) Oestrogen: - Ethnyl estradiol, Fosfestrol.
b) Oestrogen receptor modulator: - Tamoxifen.
c) Aromatase inhibitor: - Anastrozole, Letrozole.
d) Antiandrogen: - Flutamide.
e) Progestin: - Hydroxyprogesterone acetate.
f) Androgen: - Testosterone propionate.
g) GnRH analogue: - Buserelin.
h) Corticosteroids: - Prednisolone.
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9. Anti-Cancer Drugs may be divided into two groups:
1. Cell Cycle Specific (CCS): Act mainly in dividing cell.
2. Cell Cycle Non-Specific (CCNS): Act mainly in dividing cell as well as resting cell.
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Cell Cycle Specific (CCS) Cell Cycle Non-Specific (CCNS)
Antimetabolites Alkylating Agents
Vinca Alkaloids Antibiotics
Taxanes Camptothecins
Epipodophyllotoxins

10. ALKYLATING AGENTS
Agents that works by directly damaging the DNA of cancer cell by getting converting to azindinum ion and
bond with the nitrogen atom at 7th position in the guanine of DNA.
These drugs come under CCNS (Cell Cycle Non-Specific Drugs).
 Mechanism of Action:
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11. a) Nitrogen Mustered: - Mechlorethamine, Cyclophosphamide, Melphalan, Chlorambucil.
i. Cyclophosphamide: It is a prodrug and alkylating agent which activated in liver.
 It is effective after metabolism and administered orally and IV route.
 Also have powerful immunosuppressant activity.
 Drug of choice in Lung Cancer.
Mechanism of Action:
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12. ii. Chlorambucil: It is a slow acting alkylating agent.
Drug of choice in lymphatic leukaemia.
Toxicity of chlorambucil is pulmonary fibrosis.
iii. Melphalan: It is a alkylating agent which is treatment of choice for ovarian and testicular cancer.
b) Alkyl Sulfonate: - Busulphan.
Busulphan is a bi-functional methane sulphonic ester that forms transferred cross-linking with DNA results in
cell death.
Drug of choice in myeloid leukaemia.
It depresses bone marrow and have common side effects are hyperuricemia and pigmentation of skin.
c) Nitrosoureas: - Carmustine, Lomustine.
These drugs are highly lipid soluble drugs.
It reaches in high concentration in Blood Brain Barrier (BBB).
Mainly used for Brain Tumours (Drug of choice).
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13. d) Platinum-containing compound: - Cisplatin, Carboplatin.
 Heavy metal complex that shows strong neoplastic action.
i. Cisplatin: It causes nephropathy, emesis and nephrotoxicity.
Mechanism of Action:
ii. Carboplatin: It is a derivative of cisplatin with less Neuro, Nephro and Ototoxicity.
e) Triazene: - Dacarbazine.
 Dacarbazine inhibit RNA and protein synthesis that results in cell death.
 Dacarbazine is a drug of choice in malignant myeloma.
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14. ANTIMETABOLITES
These drugs inhibit the proliferation and development of cancer cells.
 These drugs mimic normal cellular metabolites and integrated into DNA and RNA during the cell cycle, disrupting the
synthesis of nucleic acids and ultimately leading to cell death.
 Therse drugs acts in S phase.
a) Folate antagonists: - Methotrexate (inhibit dihydrofolate reductase).
 Methotrexate drug have anti-neoplastic, immunosuppressant and anti-inflammatory effects.
 Antidote for methotrexate is Folinic Acid.
 Methotrexate shows Hepatotoxicity, Obstructive Nephropathy.
Mechanism of Action:
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15. b) Purine antagonists: - 6-Mercaptopurine, 6-Thioguinine.
 These drugs come under CCS (Cell Cycle Specific Drugs) and acts in S phase.
 Purine antagonists cause Hepatotoxicity.
Mechanism of Action:
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16. c) Pyrimidine antagonists: - 5-Fluorouracil, Cytarabine.
 These drugs come under CCS (Cell Cycle Specific Drugs) and acts in S phase.
i. 5-Fluorouracil: It cause Hand and Foot Syndrome and Neurotoxicity.
Mechanism of Action:
ii. Cytarabine: It cause neurotoxicity.
 Cytarabine is a drug of choice with combination of Idarubicin in Acute Myeloid Leukaemia.
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17. VINCAALKALOIDS
These drugs are cell cycle specific (CCS) and acts in M phase.
Vincristine and Vinblastine are derived from periwinkle plants.
Vinca alkaloid cause Peripheral Neuropathy.
Vinblastine is used to treat leukaemia in children’s and Vincristine is used to treat breast cancer.
Mechanism of Action:
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18. TAXANES
It enhanced stability of microtubule preventing the separation of chromosomes during anaphase.
 It decreases the ability of bone marrow to produce blood cells. e.g., Paclitaxel, Docetaxel.
i. Paclitaxel: It causes peripheral neuropathy and hypersensitivity.
ii. Docetaxel: It causes peripheral neuropathy as well as fluid retention.
EPIPODOPHYLLOTOXINS
Drugs that acts in G2 phase and S phase of cell cycle. e.g., Etoposide, Tenoposide.
Etoposide causes Bone marrow depression and GI side effects.
Mechanism of Action:
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19. CAMPTOTHECINS
Drugs that acts in G2 phase and S phase of cell cycle. e.g., Topotecan, Irinotecan.
 These are used in Ovarian, Lungs, Colorectal cancer.
Mechanism of Action: Camptothecins binds to topoisomerase-I (a nuclear enzyme that replicate DNA and transcription)
complex and inhibit the resealing of DNA, thus produce cell death.
ANTIBIOTICS
All these drugs produce direct action on DNA & they act by blocking the transcription of DNA.
e.g., Actinomycin, Bleomycin, Mitomycin, Doxorubicin.
i. Actinomycin: It administered through IV route.
Mechanism of Action: Actinomycin also produces direct action of DNA & they act by blocking the transcription of DNA.
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20. ii. Bleomycin: A mixture of glycopeptide antibiotics.
 It acts on G2 phase and M phase of cell cycle.
 It also crosses BBB (Blood Brain Barrier), so it is used to treat Brain cancer.
 Bleomycin is given as a drug of choice with combination of Cisplatin and Etoposide to treat testis cancer.
ii. Mitomycin: It causes cross-linking of DNA and generates free radicals which damage DNA.
iii. Doxorubicin: It causes Cardiotoxicity.
Mechanism of Action:
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21. ENZYME
Enzyme is isolated from bacteria specially ecoli.
It is a necessary amino acid for the production of proteins. e.g., L-Asparaginase.
 Cancer cells lack of this enzyme.
 It causes toxicity of Hypersensitivity, Hyperglycaemia, Haemorrhage.
Mechanism of Action:
Normal cells can synthesize asparagine because they contain asparagine synthase.
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22. MISCELLANEOUS AGENTS
It acts on S phase of cell cycle (CCS drugs).
e.g., Hydroxyurea, Imatinib.
Mechanism of Action: Hydroxyurea interferes with the conversion of RBC to DNA by inhibiting ribonucleoside
diphosphate reductase, this results in inhibition of DNA synthesis.
HORMONALAGENTS
These agents are non-cytotoxic but it modifies the growth of hormones dependent tumour.
a) Oestrogen: - These are physically antagonist of androgen; hence oestrogen is used to antagonise the effect of androgen.
 Widely used in Prostate cancer.
 e.g., Ethnyl estradiol, Fosfestrol.
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23. b) Oestrogen receptor modulator: - It is a compound that can interact with oestrogen receptors
in the body and modulate their activities.
These can act as either agonist (activating the receptor) or antagonist (blocking the receptor) of
oestrogen receptors, depending on the specific tissue type.
 E.g., Tamoxifen i.e. highly effective in Breast cancer.
c) Aromatase inhibitor: - These are used in the post-monophasic menstrual cycle to treat
hormone-dependent breast cancer. e.g., Anastrozole, Letrozole.
d) Antiandrogen: - It antagonizes the androgen action on prostate cancer. E.g., Flutamide.
e) Progestin: - Used to treat endometrium cancer. e.g., Hydroxyprogesterone acetate.
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24. f) Androgen: - e.g., Testosterone propionate.
Testosterone propionate is an injectable medication that is used as hormone replacement therapy in
men with less testosterone levels and female breast cancer.
g) GnRH analogue: - These drugs produce arising LH (Luteinizing hormone) and FSH (Follicle
stimulating hormone).
These are effective in advance prosthetic & breast cancer.
e.g., Buserelin.
h) Corticosteroids: - It produces feeling of well-being and it suppress the hypersensitivity
reactions.
These drugs having anti-inflammatory activity and it decreases Glaucoma.
e.g., Prednisolone.
Mechanism of Action: Prednisolone interfere with the cell cycle of activated lymphoid cells.
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25. Diseases and their Drug of Choice
Diseases Drug of Choice
Brain Tumour Nitrosourea
Lung Cancer Cyclophosphamide
Ovarian and Testicular Cancer Melphalan
Acute Myeloid Leukaemia Cytarebine + Idarabicin
Testis Cancer Bleomycin + Cisplatin + Etoposide
Myeloid Leukaemia Busulfan
Breast Cancer Tamoxifen
Prostate Cancer Oestrogen
Lymphatic Leukaemia Chlorambucil
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26. REFERENCES
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27. THANK YOU
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