Antineoplastic agents

[email protected]
L.Gopi

1. PREPARED BY
L.GOPI, B. Pharm
AADHI BHAGAWAN college of pharmacy, RANTHAM

2. These are the agents which inhibit the development of
neoplasm, a new & abnormal growth (cancer cells) (or) modify their
growth.
CLASSIFICATION:
A.Alkylating agents:
These are subdivided into four classes such as:
Nitrogen mustards (or) Mustards
Methanesulphonates
Ethylenimines
Nitrosoureas
ANTINEOPLASTIC AGENTS

3. B. Antimetabolites:
1.FolateAntagonist: E.g: Methotrexate(Mtx)
2.PurineAntagonists:
E.g: 6-Mercaptopurine (6-MP), 6-Thioguanine (6-TG), Azathiopurine&
Fludarabine.
A. Alkylating agents
1. Nitrogen Mustard
Cyclophosphamide,
Chlorambucil,
Ifosfamide,
Methlorethamine
Melphalan.
2. Methanesulphonates: Busulphan
3. Ethylenimines: Triethylenemelamine&
Triethylenethiophosphoramide
4. Nitrosoureas Carmustine& Lomustine

4. 3.PyrimidineAntagonist:
E.g: 5-Flurouracil (5-FU),
Cytarabine(cytosine arabinoside)
4.AminoacidAntagonist:
E.g: Azascrine
C. Antibiotics:
E.g: Dactinomycine& Daunorubin
D. Plant Products:
1.Imides & Amides:
E.g: Colchicine& Narciclasine
2. Tertiary Amine:

5. 3. Heterocylicamines:
E.g: Camptothecin, HydroxyCamptothecin& MethoxyCaprotothecin.
4.Lactone:
E.g: Podophyllotoxin& DeoxyPodophyllotoxin
5.Glycoside:
E.g: Mithramycin(Aureolicacid) & β-Solamarine
E. Miscellaneous Compounds
E.g: Cisplatin, ImidazoletriazinesHycantheone& Pipobroman
F. Hormones:
E.g: Megestrol; Mitotaneand Testolactone
G. Immunotherapy:
E.g: Interferon-σ,2a.

6. NITROGEN MUSTARDS
1. MECHLORETHAMINE:
Structure:
C.N:
Syn:
M.OA:
Agents have groups that form covalent bond with cell substitutents
a carboniumion is the intermediate. Most have two alkylatinggps
(Bifunctional) can crosslink two nucleophilicsites such as the N7 of
Guanine in DNA.
ALKYLATING AGENTS

7. &thymine, leading to substitution of AT for GC (or) chain breakage.
All alkylatingagents depress bone marrow function & cause
gastrointestionaldisturbances.
With prlongeduse, two further unwanted effect occurs.
a) Depression of Gametogenesisin men.
b) Increased risk of acute non-lympholyticleukaemia& other
malignancies.
Use: Used in the treatment for mytosisfungoides& Lymphomas.
2. MELPHANAN
Structure:
C.N:

8. SYN:

9. M.O.A:
Serves as a Primary Immunosuppressive drugs.
USE:
Very effective in preventing the reoccurenceof cancer in
premenopansalwomen.
3. CYCLOPHOSPHAMIDE:
Structure:
C.N:
Syn:

10. Use:
Effective against acute leukemia, chronic lymphocytic leukemia & multiple
myeloma.
4. CHLORAMBUCIL:
Structure:
C.N:
Syn:

11. USE:
2. METHANESULPHONATES
Busulphan
Structure:
C.N:
Syn:

12. M.O.A:
Non-specific phase
Almost negligible action on rapidly prloiferativetissues other than
bone marrow.
At relatively lower dose level granulo-cytopoesismay be
suppressed & without causing any effect on erythropoises.
USE:
Used in the treatment for Granuocyticleukemeia.

13. 3. ETHYLENIMINES

14. SYN:
USE:
M.O.A:

15. 4. NITROSOUREAS

16. USE:
Possesses the potential to cross BBB.
Employed specifically for brain tumour& other tumours,
for instance leukemias, which have metastasized to the
brain.
Combination of Carmustine& prednisone used for the
treatment of multiple mycloma
Used for the treatment of lymphomas & Hodgkin’s
Disease.
Used for the treatment of Glioblastoma

17. U
USE:

18. 1. FOLATE ANTAGONIST
METHOTREXATE
C.N:
SYN:
ANTIMETOBOLITES

19. USE:
M.O.A:
2. PURINE ANTAGONIST:
a)6-MERCAPTOPURINE:
C.N: O-Mercapto-6-Purine

20. SYN:
M.O.A:
USE:

21. 2. AZATHIOPURINE
C.N: 6-[1-Methyl-4-nitromidazole-5 yl] thio] purine
SYN:
USE:

22. 3. PYRIMIDINE ANTAGONIST:

24. M.O.A:
a)Fluorouracil;
b)Cytarabine:
4. AMINOACID ANTAGONIST:

25. M.O.A:
The ‘drug’ is believed to be a glutamine antagonist that specifically inhiits
purinebiosynthesis and thus may exert antitumouractivity.
C. ANTIBIOTICS

26. USE:
Useful in the treatment of acute lymphoblastic leukemia in
children. It is normally employed in combination therapy, for instance :
with cytosine arabinosidein the treatment of myclogenousleukemia ; with
cytarabinein the treatment of non-lymphoblastic leukemia in adult.

27. M.O.A:
Dactinomycin
Inhibits the DNA-dependent RNA-polymerase. Interestingly, the drug also
significantly potentiates radiation recall (otherwise known as ‘radiotherapy’).
It also serves as a secondary (efferent) immunosuppressive agent.
does not pass the blood-brain barrier (BBB).
DaunorubicinHydrochloride
intercalates into DNA, inhibits topoisomeraseII, yields oxygen radicals,
and ultimately inhibits DNA synthesis. It can invariably prevent and check cell
division in doses that virtually fail tointerferedirectly with the nucleic acid
synthesis.

28. HORMONES