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ANTINEOPLASTIC
AGENTS
BY
KENCHA SWATHI
ASSISTANT PROFESSOR
BANGALORE
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INTRODUCTION
• A neoplasm or tumour is an abnormal mass of tissue ,the growth of which
exceeds and is uncoordinated with that of the normal tissue and continues
in the same manner after cessation of the stimuli which have initiated it.
• A malignant tumour grows rapidly and continuously.
• Malignant tumours invade and destroy neighbouring tissues.
• Better understanding of the tumour biology shows tremendous growth of
cancer research,cancer chemotherapy and leads to evolution of
antineoplastic agents.
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CAUSES OFTUMOUR
• GENETIC FACTORS
• CHEMICAL CARCINOGENS
• POLYCYCLIC HYDROCARBON CARCINOGENS
• RADIATIONS
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TYPES OF CANCER
• Ten different types of cancer may be cured with the aid of chemotherapy
1.Leukemia in children (Blood cancer)
2.Hodgkin’s disease( Affects immune system)
3.Ewing’s sarcoma ( Bone,arms or pelvis)
4.Choriocarcinoma in women(Uterus or womb)
5.Testicular carcinoma
6.Retinoblastoma in children(Eye cancer)
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FACTORS AFFECTING CANCER
1.Age incidence: Bone cancer in 10-12 years
2.Sex Incidence: Cervical cancer in women
3.Geographical Incidence: Mouth and tongue cancer in india
4. Ethnic incidence: Penile carcinoma
5.Radiation Incidence: Radiologists suffer from leukemia.
6.Hormone Incidence: Breast cancer occurs becoz of over
production of estrogens.
7.Environment Incidence: Lung cancer in cigarette smokers.
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CLASSIFICATION
Antineoplastic drugs are classified as:
1.Alkylating agents: Mechlorethamine,Cyclophosphamide,Melphalan,
Chlorambucil,Busulfan,Thiotepa
2.Antimetabolites: Mercaptopurine,Thioguanine,Fluorouracil,Floxuridine,
Cytarabine,Methotrexate,Azathioprine
3.Antibiotics: Dactinomycin,Daunorubicin,Doxorubicin,Bleomycin
4.Plant products: Etoposide,Vinblastin,Vincristine
5.Miscellaneous drugs: Cisplatin,Mitotane
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MECHLORETHAMINE
Uses: Effective in Hodgkin’s disease
Drug of choice for the treatment of Mycosis fungoides and
lymphomas.
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CYCLOPHOSPHAMIDE
Uses:To treat Acute leukemia.
To treat chronic lymphocytic leukemia.
To control Burkitt’s lymphoma and multiple myelenoma.
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MELPHALAN
Uses: Effective in preventing the reoccurrence of cancer in premenopausal
women.
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CHLORAMBUCIL
Uses: Used to treat leukemia,lymphoma.
To stop the growth of cancer cells.
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BUSULFAN
Uses: Busulfan shows action on rapidly proliferative tissues.
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THIOTEPA
Uses: Used to prevent rejection of stem cell transplant
To treat bladder cancer
To stop the growth of cancer cells.
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MOA OF ALKYLATINGAGENTS
• Drugs attaches an alkyl group to DNA.
• The alkyl group is attached to the guanine base of DNA,7th nitrogen atom of the
purine ring.
• Drug +
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Alkylation
CLASSIFICATIONOF ANTIMETABOLITES
Antimetabolites are subclassified as:
1.Folate antagonists – Methotrexate
2.Purine antagonists – Mercaptopurine,Thioguanine,Azathioprine
3.Pyrimidine antagonists – Fluorouracil ,Floxuridine,cytarabine
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MERCAPTOPURINE
Uses:Inhibits othoimmune encephalomyletis and thyroiditis.
To treat childhood leukemia
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THIOGUANINE
Uses:To treat acute nonlymphocytic leukemia.
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FLUOROURACIL
Uses:To treat breast cancer,colorectal cancer,stomach cancer,pancreatic
cancer and skin cancer.
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FLOXURIDINE
Uses:To treat cancer of GIT(stomach and intestines) and that has spread to
liver.
It works by stopping or slowing the growth of cancer cells in body.
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CYTARABINE
Uses:Cytarabine is used alone or in combination with other drugs for the
treatment of leukemia(cancer ofWBC),acute myeloid leukemia,acute
lymphocytic leukemia.
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METHOTREXATE
Uses:To treat lymphoblastic leukemia.
To treat lung cancer
To treat breast cancer and epidermoid cancer.
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AZATHIOPRINE
Uses: Azathioprine is used to prevent organ rejection in patients who have
received kidney transplant.It allows functioning of new kidney properly.
To treat rheumatoid arthritis
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MOA OF ANTIMETABOLITES
• Drugs that interfere with one or more enzymes which are necessary for
DNA synthesis.
• They affect DNA synthesis by acting as a substitute to the actual
metabolites that would be used in the normal metabolism.
• Some drugs inhibit folate reductase enzyme during the synthesis of folic
acid.
• Inhibition of folic acid forms abnormal DNA or RNA.
• Finally Proteins cannot form by translation.
• This leads to cell-death or stopping the growth of cancer related cells or
tissues.
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ANTIBIOTICS-DACTINOMYCIN
Uses:To treat adenocarcinoma.
To treat Rhabdomyosarcoma in children(Injury of muscles or death of
muscle fibres)
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DAUNORUBICIN
Uses: It is used in combination with other drugs for treating acute
lymphocytic leukemia.
It works by stopping or slowing the growth of cancer cells.
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DOXORUBICIN
Uses: Doxorubicin is used to treat bladder cancer,lung,breast,stomach and ovarian
cancers.
Used to treat various types of leukemia.
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BLEOMYCIN
Uses:To treat squamous cell cancer,testicular cancer and ovarian cancer.
Used to treat malignant pleural effusion(storage of fluid in the space between
lungs lining and the chest wall)
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MOA OF ANTIBIOTICS
• Drugs specifically inhibits the DNA dependant RNA polymerase.
• This enzyme synthesizes RNA from a DNA template and it inhibits transcription.
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ETOPOSIDE
Uses:To treat lung cancer, testicular cancer, glioblastoma(Cancer of brain or spinal
cord),leukemia,Kaposi’s sarcoma(Cancer that causes lesions under the skin lining)
and Ewing’s sarcoma(Cancer that grows in bone or tissue around the bone)
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VINBLASTINE
Uses:To treat Hodgkin’s neuroblastoma,breast tumour and mycosis
fungoides.
In the treatment of Myeloblastic leukemia in children.
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VINCRISTINE
Uses:To treat acute leukemia in
children,neuroblastoma,Rhabdomyosarcoma(cancer occurs in skeletal muscle or
bladder or uterus)
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MOA OF PLANT PRODUCTS
• The drug interferes with the assembly of the microtubules,by effectively
combining with tubulin,thereby causing a mitotic arrest in the metaphase.
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CISPLATIN
Uses:To treat testicular cancer,ovarian cancer and other solid tumours like lung
cancer,esophageal cancer and gastric cancer.
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MITOTANE
Uses:It is used to treat cancer of adrenal glands that cannot be treated by
surgery.
It stops or slows the growth of cancer cells.
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SYNTHESISOF MECHLORETHAMINE
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SYNTHESISOF METHOTREXATE
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ROUTE -I
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ROUTE-II
SYNTHESISOF MERCAPTOPURINE
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ROUTE-I
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ROUTE-II
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