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CHEMOTHERAPY OF ANTICANCER
AGENTS
BY
HARSHIT JADAV
NIPER-AHMEDABAD
WHAT IS CELL CYCLE???
WHAT IS CANCER???
• Cancer is a term used for diseases in which
abnormal cells divide without control and
are able to invade other tissues. Cancer cells
can spread to other parts of the body
through the blood and lymph systems
TYPES OF CANCER
• Carcinoma - cancer that begins in the skin or in tissues that line or cover
internal organs. There are a number of subtypes of carcinoma,
including adenocarcinoma basal cell carcinoma, squamous cell carcinoma
and transitional cell carcinoma.
• Sarcoma - cancer that begins in bone, cartilage, fat, muscle, blood vessels,
or other connective or supportive tissue.
• Leukemia - cancer that starts in blood-forming tissue such as the bone
marrow and causes large numbers of abnormal blood cells to be produced
and enter the blood.
• Lymphoma and myeloma - cancers that begin in the cells of the immune
system
TYPES OF TUMORS
• Not all tumors are cancerous; tumors can be benign or
malignant.
• Benign tumors aren't cancerous. They can often be
removed, and, in most cases, they do not come back. Cells
in benign tumors do not spread to other parts of the body.
• Malignant tumors are cancerous. Cells in these tumors can
invade nearby tissues and spread to other parts of the
body. The spread of cancer from one part of the body to
another is called metastasis.
10
Cancer Therapeutic Modalities (classical)
1. Surgery
2. Radiation
3. Chemotherapy
1/3 of patients without metastasis
Respond to surgery and radiation.
If diagnosed at early stage,
close to 50% cancer
could be cured.
50% patients will undergo chemotherapy,
to remove micrometastasis. However,
chemotherapy is able to cure only about 10-15%
of all cancer patients.
Antineoplastic Agent
a. Cell Cycle Specific (CCS) agents
b. Cell Cycle Non-Specific (CCNS)
agents
c. Miscellaneous (e.g., antibodies)
agents
12
G0 = resting phase
G1 = pre-replicative phase
G2 = post-replicative phase
S = DNA synthesis
M = mitosis or cell division
M
S
G G2 1 Hydrocortisone
Vincristine,Vinblastine
G0
Cyclophosphamide
Bleomycin
Actinomycin D
Actinomycin D
5-Fluorouracil
Cytosine arabinoside
Methotrexate
6-Mercaptopurine
6-Thioguanine
Purine antagonists
Methotrexate
Cyclophosphamide
5-Fluorouracil
Cytosine arabinoside
Daunomycin
Paclitaxel, Docetaxel
resting
Cell cycle specificity of Anti-Neoplastic Agents
NOW CONCENTRATE
ON WHITE BOARD…
ENJOY THE CANCER…
CLASSIFICATION
1. ALKYLATING AGENTS
• A. Nitrogen Mustards: Cyclophosphamide,.
Chlorambucil, Melphalan,
• B. Alkyl Sulfonate: Busulfan
• C. Nitrosoureas : Carmustine,
Lomustine,semustine
• D. Ethylenimines: Thiotepa
• E. Triazenes : Dacarbazine
2. Antimetabolites
•A. Folate antagonist: methotrexate and
gemcitabine
•B. Purine analogues: thioguanine,
mercaptopurine, pentostatin
•C. Pyrimidine analogues: fluorouracil,
cytarabine
• 3. Plant-derived products : vinca alkaloids(
vincristine, vinblastine) epipodophyllotoxins (
etoposide) taxanes: (paclitaxel)
• 4. Antibiotics : doxorubicin , daunorubicin ,
bleomycin, mitomycin, dactinomycin
• 5. Hormones and related drugs : tamoxifen
estramustine, flutamide , progestins
• 6. Miscellaneous agent : hydroxyurea, cisplatin ,
mitoxantrone, levamisole, interferon alfa and
aldesleukin.
•7. Drugs that alters hormonal milieu
1. Glucocorticoids: Prednisolon, Prednisone
2. Estrogen: Diethylstilbestreol
3. Anti-estrogen: Tamoxifen
4. Androgen: Testosteron
5. Progestin: Medroxy Progesteron Acetate
8. Monoclonal Antibodies
1. Trantuzumab
2. Rituximab
3. Imatinib
MECHANISM OF ACTION: ALKYLATING AGENT
• Alkylating agents exert their cytotoxic effects via transfer
of their alkyl groups to various cellular constituents.
• Alkylations of DNA within the nucleus probably represent
the major interactions that lead to cell death.
• The major site of alkylation within DNA is the n7 position
of guanine; however, other bases are also alkylated to
lesser degrees, including n1 and n3 of adenine, n3 of
cytosine, and o6 of guanine
MOA: ANTI METABOLITES
• Antimetabolites are drugs that are
structurally related to naturally occurring
compounds, such as vitamins, amino acids,
and nucleotides. These drugs can compete
for binding sites on enzymes or can
themselves become incorporated into DNA
or RNA and thus interfere with cell growth
and proliferation.

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Classification of anti cancer agents

  • 2. WHAT IS CELL CYCLE???
  • 3.
  • 4. WHAT IS CANCER??? • Cancer is a term used for diseases in which abnormal cells divide without control and are able to invade other tissues. Cancer cells can spread to other parts of the body through the blood and lymph systems
  • 5.
  • 6. TYPES OF CANCER • Carcinoma - cancer that begins in the skin or in tissues that line or cover internal organs. There are a number of subtypes of carcinoma, including adenocarcinoma basal cell carcinoma, squamous cell carcinoma and transitional cell carcinoma. • Sarcoma - cancer that begins in bone, cartilage, fat, muscle, blood vessels, or other connective or supportive tissue. • Leukemia - cancer that starts in blood-forming tissue such as the bone marrow and causes large numbers of abnormal blood cells to be produced and enter the blood. • Lymphoma and myeloma - cancers that begin in the cells of the immune system
  • 7.
  • 8.
  • 9. TYPES OF TUMORS • Not all tumors are cancerous; tumors can be benign or malignant. • Benign tumors aren't cancerous. They can often be removed, and, in most cases, they do not come back. Cells in benign tumors do not spread to other parts of the body. • Malignant tumors are cancerous. Cells in these tumors can invade nearby tissues and spread to other parts of the body. The spread of cancer from one part of the body to another is called metastasis.
  • 10. 10 Cancer Therapeutic Modalities (classical) 1. Surgery 2. Radiation 3. Chemotherapy 1/3 of patients without metastasis Respond to surgery and radiation. If diagnosed at early stage, close to 50% cancer could be cured. 50% patients will undergo chemotherapy, to remove micrometastasis. However, chemotherapy is able to cure only about 10-15% of all cancer patients.
  • 11. Antineoplastic Agent a. Cell Cycle Specific (CCS) agents b. Cell Cycle Non-Specific (CCNS) agents c. Miscellaneous (e.g., antibodies) agents
  • 12. 12 G0 = resting phase G1 = pre-replicative phase G2 = post-replicative phase S = DNA synthesis M = mitosis or cell division M S G G2 1 Hydrocortisone Vincristine,Vinblastine G0 Cyclophosphamide Bleomycin Actinomycin D Actinomycin D 5-Fluorouracil Cytosine arabinoside Methotrexate 6-Mercaptopurine 6-Thioguanine Purine antagonists Methotrexate Cyclophosphamide 5-Fluorouracil Cytosine arabinoside Daunomycin Paclitaxel, Docetaxel resting Cell cycle specificity of Anti-Neoplastic Agents
  • 13. NOW CONCENTRATE ON WHITE BOARD… ENJOY THE CANCER…
  • 14. CLASSIFICATION 1. ALKYLATING AGENTS • A. Nitrogen Mustards: Cyclophosphamide,. Chlorambucil, Melphalan, • B. Alkyl Sulfonate: Busulfan • C. Nitrosoureas : Carmustine, Lomustine,semustine • D. Ethylenimines: Thiotepa • E. Triazenes : Dacarbazine
  • 15. 2. Antimetabolites •A. Folate antagonist: methotrexate and gemcitabine •B. Purine analogues: thioguanine, mercaptopurine, pentostatin •C. Pyrimidine analogues: fluorouracil, cytarabine
  • 16. • 3. Plant-derived products : vinca alkaloids( vincristine, vinblastine) epipodophyllotoxins ( etoposide) taxanes: (paclitaxel) • 4. Antibiotics : doxorubicin , daunorubicin , bleomycin, mitomycin, dactinomycin • 5. Hormones and related drugs : tamoxifen estramustine, flutamide , progestins • 6. Miscellaneous agent : hydroxyurea, cisplatin , mitoxantrone, levamisole, interferon alfa and aldesleukin.
  • 17. •7. Drugs that alters hormonal milieu 1. Glucocorticoids: Prednisolon, Prednisone 2. Estrogen: Diethylstilbestreol 3. Anti-estrogen: Tamoxifen 4. Androgen: Testosteron 5. Progestin: Medroxy Progesteron Acetate
  • 18. 8. Monoclonal Antibodies 1. Trantuzumab 2. Rituximab 3. Imatinib
  • 19. MECHANISM OF ACTION: ALKYLATING AGENT • Alkylating agents exert their cytotoxic effects via transfer of their alkyl groups to various cellular constituents. • Alkylations of DNA within the nucleus probably represent the major interactions that lead to cell death. • The major site of alkylation within DNA is the n7 position of guanine; however, other bases are also alkylated to lesser degrees, including n1 and n3 of adenine, n3 of cytosine, and o6 of guanine
  • 20. MOA: ANTI METABOLITES • Antimetabolites are drugs that are structurally related to naturally occurring compounds, such as vitamins, amino acids, and nucleotides. These drugs can compete for binding sites on enzymes or can themselves become incorporated into DNA or RNA and thus interfere with cell growth and proliferation.