Anand Antineoplastic

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CANCER & ANTINEOPLASTIC                AGENTS

Trivedi Anand K. M.Sc Biotechnology 4th Sem. Shree M.& N. Virani Science College.

Contents ◆ ◆ ◆ ◆ ◆ ◆ ◆ ◆ ◆ ◆

Introduction Cancer treatment Antineoplastic agents Classification of antineoplastic agents Approches for antineoplastic agents Mechanism of antineoplastic agents Major classes of antineoplastic agents Adverse effects Conclution References

Introduction ◆



Cancer (medical term: malignant  neoplasm)  is  a  class  of  diseases  in which a group of cells display  uncontrolled  growth  ,  invasion  (intrusion  on  and  destruction  of  adjacent tissues). Two types of tumor: Benign tumor ◆ Malignant tumor ◆

Antineoplastic Agents ◆



Antineoplastics are Chemotheraputic Agents. The choice of which antineoplastic to use depends on what the cell type of the tumor is, and on its site of growth. Antineoplastic agents have more of an effect on the tumor cells than normal cells because of their rapid growth.

Cancer Treatments ◆

Possible treatments include: ◆ Treatment of choice depends on type of cancer, it’s location, 

invasion process, patient’s state of health. ◆ Surgery ◆ Antineoplastic agents or Chemotherapeutic agents. ◆ Radiation ◆ Immunotherapy

Antineoplastic Agents??.. ◆ ◆ ◆ ◆ ◆ ◆ ◆ ◆ ◆ ◆ ◆ ◆ ◆ ◆

A N T I N E O P L A S T I C

: Anticancer drugs cause : Nausea and vomiting : Treatment regimen must be followed : Individualized dosage : New drugs appear on the market : Exposure time kept to a minimum : Only a physician can administer : Protect  yourself : Look, listen, and learn : Assessment of laboratory tests : Safe dosage based on weight : Toxicities : Inform patients : Classification of agents

Classification of Antineoplastic Agents ◆

On  the  basis  of  antineoplastic  action  on  the  phase  of  proliferation cycle, drugs are classified as:



Cell  cycle  non­specific  agents:  (phase  non­specific  agents, 



Cell  cycle  specific  agents:  (phase  specific  agents,  CCSA).  (e.g. 

CCNSA) (e.g. Alkylating agents and antitumor antibiotics.)  ◆ Act in all proliferating phases. ◆ Effects are stronger.  Antimetabolites, and plant alkaloids)  ◆ just act on specific phases of the cell cycle  ◆ effects are comparatively weaker. 

Approches for Antineoplastic agent on Cells Most antineoplastic drugs act on the proliferating cycle of cell. ◆ ◆ ◆ ◆ ◆

Destruction of DNA or inhibition of DNA duplication  e.g. alkylating agents, mitomycin C  Inhibition of nucleic acid (DNA and RNA) synthesis  e.g. 5­fluorouracil, 6­mercaptopurine, methotrexate, cytarabine, etc. Interfering with the transcription to inhibit RNA synthesis  e.g. dactinomycin, dauoruicin, and doxorubicin Inhibition of protein synthesis  e.g. vinca alkaloids, epipodophylotoxins, and paclitaxel  Interfering with hormone balance e.g. adrenal corticosteroids, estrogens, tamoxifen etc. 

Mechanism of Antineoplastic Agents

Major Classes of Antineoplastic  Agents ◆  Alkalyting agent ◆  Antimetabolites ◆  Enzymetic agents  ◆  Antitumor antibiotics ◆  Plant alkaloids ◆  Hormonal agents ◆

Miscellaneous agents

Alkylating Agents ◆

In general these are used to treat many types of leukamia (“Hematological  malignancies”). ◆

All alkylating agents are phase­nonspecific. ◆ kill rapidly proliferating cells, also kill non­proliferating cells.  Examples:  Mechlorethamine  ◆ the first drug used in the treatment of cancer and At present, it is mainly used for  Hodgkin's disease and non­Hodgkin's lymphomas.  Cyclophosphamide  ◆ Most widely used in clinical therapy for treatment of cancer at present.  ◆ It has no antineoplastic action outside the body and must be activated in the liver ◆

◆ ◆



There follows either cross­linking of the two strands of DNA, preventing replication,  or DNA breakage.

Antimetabolites Agents ◆ ◆ ◆ ◆

These are purine and pyrimidine analogues. Interfere with the metabolic process of the cell, preventing cell reproduction. Only act on dividing cells and are most effective in treating rapidly proliferating malignant cells Example: ◆ ◆

6-Merceptopurine:Inhibit purine biosynthesis, causing inhibition of biosynthesis of nucleic acid. Treatment in leukamia. 5-flurouracil

Example of Antimetabolites

Enzymatic Agents ◆ ◆

The enzymes which act as antineoplastic agents. Inter,feres with DNA synthesis by inhibiting the DNA enzyme topoisomerase I. ◆ ◆ ◆ ◆

L-asparaginase is an example of an enzyme used in the treatment of cancer. L-asparaginase works by hydrolyzing asparagines into aspartic acid and ammonia. Cancer cells need an exogenous source of asparagine for survival; normal cell can synthesize asparagine. Side effects of L-asparaginase include pain at the injection site, hypotension, and diarrhea.

Antitumor Antibiotics Certain antibiotics have an antineoplastic effect ◆ Act by interfering with one or more stages of RNA and DNA synthesis ◆ Interfere with a malignant cell’s ability to grow and reproduce ◆

Hormonal Agents ◆

Used to treat tumors; capable of suppressing the growth of certain tissues of the body without causing cytotoxic effects on healthy neighboring cells. ◆

◆ ◆ ◆ ◆

Adrenocortical steroids to inhibit the growth of cancers of lymphoid tissue and blood. Oestrogen antagonists ( tamoxifen ) is indicated for breast cancer. Oestrogen is used for prostatic cancers. Testosterone: treatment in testicular cancer. Progesterone: Use in metastatic carcinoma.

Immuno suppresors ◆



In immuno therapy use immunosuppresor which is act as antineoplastic agents. Treatment of disease by stimulation of the body’s immune system. Uses the body’s own immune defense system to attack the cancer. Immunosuppressive drugs work by interfering with one of the stages of the cell cycle or by affecting cell messengers ◆ ◆



Cyclosporine inhibits the proliferation of T-lymphocytes; used for managing KCS in dogs and immune-mediated skin disorders Azathioprine affects cells in the S phase of the cell cycle and also inhibits T- and B-lymphocytes; used mainly in dogs for immunemediated disease Cyclophosphamide interferes with DNA and RNA replication, disrupting nucleic acid function; has been used for immune-mediated diseases

Plant Alkaloids ◆





Affects rapidly growing cells . Inhibits the cell division – mitosis. Treatment of: ◆ Lymphomas ◆ Leukemias ◆ Breast cancer and bladder carcinoma.

May apple

Taxus brevifolia

Vinca rosea

Miscellaneous agents ◆

Examples: Hydroxyurea ◆ Hydroxyurea

inhibits ribonucleotide reductase. inhibition of DNA synthesis. ◆ It is CCS agent, specific for the cells of S phase ◆ The major adverse effect of this drug is bone marrow depression.

Adverse effects Interfere with vital cells functioning and kill or destroy malignant cells ◆ Normal, healthy cells may also be destroyed ◆ Most agents are cytotoxic, mutagenic, and carcinogenic ◆ Nausea and vomiting ◆ Diarrhea andAnemia & Malnutrition ◆ Hair loss and Memory loss and Weight loss or gain ◆

Conclusion Now a days, there are number of natural and artificial antineoplastic agents which are used for curing some malignant diseases but still there are some serious diseases like AIDS and certain neurological disorders which are uncurable. So, further research should be carried out for those diseases and antineoplastic agents can be potent source in the research.

References ◆

Websites:◆ ◆ ◆



www.medical online.com www.cancer.org www.cancer.com/antineoplastic agents

Reviews:◆





Joensuu H. (2008). “Systemic chemotherapy and antineoplastic agents for cancer: from weapon to treatment”. Lancet Oncol. 9 (3): 304. Tannock IF, Ahles TA, Ganz PA, Van Dam FS (June 2004). “Cognitive impairment associated with chemotherapy and antineoplastic agents for cancer: report of a workshop”. J. Clin. Oncol. 22 (11): 2233–9. Goodman LS, Wintrobe MM, Dameshek W, Goodman MJ, Gilman A, McLennan MT. (1946). “Nitrogen mustard therapy”. JAMA 132: 26–32.

Thank You

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