full detail antineoplastic

1. ANTINEOPLASTIC AGENT
&
ANTICANCER DRUG
Prepared By:- Miss Anamika Singh

2. INTRODUCTION AND
HISTORY

3. C A N C E R : - C A N C E R I S C H A R A C T E R I Z E D B Y R A P I D A N D
U N C O N T R O L L E D F O R M A T I O N O F A B N O R M A L C E L L
W H I C H M A Y M A S S T O G E T H E R T O F O R M A G R O W T H O R
T U M O R O R P R O L I F E R A T E D T H R O U G H O U T T H E B O D Y
I N I T I A T I N G A B N O R M A L G R O W T H T H E Y O T H E R S I D E .
A N T I – C A N C E R D R U G : - T H E D R U G T H A T A R E U S E D I N
A I N H I B I T I N G T H E A B N O R M A L C E L L G R O W T H O R
K I L L I N G T H E C A N C E R C E L L .
DEFINITION

4. U N C O N T R O L L E D P R O L I F E R A T I O N .
A B N O R M A L N U C L E U S .
L O S S O F A N C H O R A G E .
L O S S O F C O N T A C T I N H I B I T I O N .
F O R M S T U M O R
U N D E R G O E S M E T A S T A S I S .
D E C R E A S E D M U T A T I O N R A T E .
CHARACTERIZED OF CANCER CELL

5. TYPES OF TUMORS

7. SYMPTOMS

8. T O B A C O ( H U M A N S )
S U N L I G H T
I O N I Z I N G R A D I A T I O N
C E R T A I N C H E M I C A L A N D O T H E R S U B S T A N C E
S O M E V I R U S E S A N D B A C T E R I A
C E R T A I N H A R M O N E S
F A M I L Y H I S T O R Y O F C A N C E R
A L C O H O L ( H U M A N S )
P O O R D I E T , L A C K O F P H Y S I C A L A C T I V I T Y
RISK FACTORS

9. T H E M A J O R T Y P E S O F C A N C E R
C A R C I N O M A , S A R C O M A , M E L A N O M A , L Y M P H O M A , L E U K E M I A
.
C A R C I N O M A : -
C A R C I N O M A I S T H E M O S T C O M M O N T Y P E O F C A N C E R . I T
B E G I N S I N T H E E P I T H E L I A L T I S S U E O F T H E S K I N , O R I N T H E
T I S S U E T H A T L I N E S I N T E R N A L O R G A N S , S U C H A S T H E L I V E R
O R K I D N E Y S . C A R C I N O M A S M A Y S P R E A D T O O T H E R P A R T S O F
T H E B O D Y , O R B E C O N F I N E D T O T H E P R I M A R Y L O C A T I O N .
TYPES OF CANCER CELL

10. S A R C O M A : -
A sarcoma is a type of cancer that starts in tissues like bone
or muscle. Bone and soft tissue sarcomas are the main types
of sarcoma. Soft tissue sarcomas can develop in soft tissues
like fat, muscle, nerves, fibrous tissues, blood vessels, or deep
skin tissues

11. M E L A N O M A : -
Melanoma, also known as malignant melanoma, is a type
of skin cancer that develops from the pigment-
producing cells known melanocytes. Melanomas typically
occur in the skin but may rarely occur in the mouth,
intestines or eye (uveal melanoma).

12. L Y M P H O M A : - L Y M P H O M A I S C A N C E R T H A T B E G I N S I N
I N F E C T I O N - F I G H T I N G C E L L S O F T H E I M M U N E S Y S T E M , C A L L E D
L Y M P H O C Y T E S . T H E S E C E L L S A R E I N T H E L Y M P H
N O D E S , S P L E E N , T H Y M U S , B O N E M A R R O W , A N D O T H E R P A R T S
O F T H E B O D Y . W H E N Y O U H A V E L Y M P H O M A , L Y M P H O C Y T E S
C H A N G E A N D G R O W O U T O F C O N T R O L .

13. L E U K E M I A : - L E U K E M I A I S A C A N C E R O F T H E B L O O D C E L L S .
T H E R E A R E S E V E R A L B R O A D C A T E G O R I E S O F B L O O D C E L L S ,
I N C L U D I N G R E D B L O O D C E L L S ( R B C S ) , W H I T E B L O O D C E L L S
( W B C S ) , A N D P L A T E L E T S . G E N E R A L L Y , L E U K E M I A R E F E R S
T O C A N C E R S O F T H E W B C S . W B C S A R E A V I T A L P A R T O F Y O U R
I M M U N E S Y S T E M .

15. M E C H L O R E T H A M I N E V I N C R I S T I N E
C Y C L O P H O S P H A M I D E E V I N B L A S T I N E
I F O S FA M I D E M E T H O X Y T R AT E
C H L O R A M B U C I L
M E L P H A L A N P R O C A R B A Z I N E
C A R M U S T I N E 6 - M A R C U P T O P U R I N E E T O P O S I D E
L O M U S T I N E F L U D A R A B I N E H Y D R O X Y U R E A
D E C A R B A Z I N E C L A D R I A B I N E L - A S PA R A G I N A S E
T E M O Z O L O M I D E
C I S P L AT I N
1 . 5 - F L U O R O U R A C I L
G E M C I TA B I N E
D A C T I N O M Y C I N C Y T R A B I N E
D O X O R U B I C I N C A PA C I TA B I N E
D A U N O R U B I C I N
B L E O M Y C I N
M I T O M Y C I N - C PA C L I TA X E L
D O C E TA X E L
CLASSIFICATION
Alkylating agent Antimetabolite agent
Folate antagonist
Purine antagonist
Pyramidine
antagonist
Antibiotic Mycin
Taxenes
Vinca Alkaloids
Miscellaneous

16. ONE OF THE FRIGHTENING DEVELOPMENT OF
WORLD WAR I WAS THE PRODUCTION OF CHEMICAL
WARFARE .THESE COMPOUND WERE KNOWN AS THE
NITROGEN MUSTERED GASES
 THE NITROGEN MUSTERED WERE OBSERVED TO
INHIBIT CELL GROWTH SPECIALLY BONE MARROW.
SHORTLY AFTER THE WAR THESE COMPOUND WERE
INVESTIGATED AND SHOWN TO INHIBIT THE
GROWTH OF CANCER CELL.
Alkylating agent

17. M E C H L O R E T H A M I N E : -
U S E S : -
M E C H L O R E T H A M I N E I S U S E D TO T R E AT H O D G K I N ' S
LY M P H O M A ( H O D G K I N ' S D I S E A S E ) A N D C E RTA I N T Y P E S O F N O N -
H O D G K I N ' S LY M P H O M A ( T Y P E S O F C A N C E R T H AT B E G I N I N A
T Y P E O F W H I T E B L O O D C E L L S T H AT N O R M A L LY
F I G H T S I N F E C T I O N ) ; M Y C O S I S F U N G O I D E S ( A T Y P E
O F C A N C E R O F T H E I M M U N E S Y S T E M T H AT F I R S T A P P E A R A S S K I N
R A S H E S ) ;

18. E T H Y L E N E O X I D E I S T R E A T E D W I T H M E T H A N A M I N E . P R O D U C T
S O F O R M E D I S F U R T H E R T R E A T E D W I T H S O C L 2 T O O B T A I N
M E C H L O R E T H A M I N E .
SYNTHESIS OF
MECHLORETHAMINE

19. C Y C L O P H O S P H A M I D E : -
Cyclophosphamide is in a class of medications called alkylating agents.
When cyclophosphamide is used to treat cancer, it works by slowing or
stopping the growth of cancer cells in your body. When
cyclophosphamide is used to treat nephrotic syndrome, it works by
suppressing your body's immune system.
Uses:-
Bioavailability :- 75%
Protein Binding:- >60%
Metabolism :- liver
Excretion :- Kidney
Route of Administration :- injection, mouth

20. MECHANISUM OF ACTION
CYCLOPHOSPHAMIDE

21. SYNTHESIS OF
CYCLOPHOSPHAMIDE

22. I F O S FA M I D E : -
U S E S : - I F O S FA M I D E I S U S E D TO T R E AT VAR I O US C A NC E R S ( S U C H
A S T E ST I C UL A R C A NC E R ) . I T W O R K S B Y S LO W I N G O R S TO PP I N G
T H E G R O W T H O F C A N C E R C E L L S .
M E TA B O L I S M : - L I V E R
E X C R E T I O N : - R E N A L
U S E S : - T H I S M E D I C A T I O N I S U S E D T O T R E A T C E R T A I N T Y P E S
O F C A N C E R ( S U C H A S L E U K E M I A , L Y M P H O M A ) .
C H L O R A M B U C I L B E L O N G S T O A C L A S S O F D R U G S K N O W N A S
A L K Y L A T I N G A G E N T S . I T W O R K S B Y S L O W I N G O R S T O P P I N G T H E
G R O W T H O F C A N C E R C E L L S .
Bioavailability :- 100%
Protein Binding:- 60%
Metabolism :- Hepatic
Excretion :- Renal
Route of Administration :- Intravenously
CHLORAMBUCIL :-

23. SYNTHESIS OF
CHLORAMBUCIL

24. M E L P H A L A N : -
Bioavailability :- 25-89%
Protein Binding:- 30%
Metabolism :- Hepatic
Excretion :- kidney
Route of Administration :- Intravenously, Mouth
Uses:- Melphalan is used to treat multiple myeloma (a type of cancer of the
bone marrow). Melphalan is also used to treat a certain type of ovarian
cancer (cancer that begins in the female reproductive organs where eggs
are formed). Melphalan is in a class of medications called alkylating agents.
CARMUSTINE :-
This medication is used to treat certain types
of cancer (including multiple myeloma, brain tumor, Hodgkin's
disease, non-Hodgkin's lymphoma). Carmustine belongs to a class of
drugs known as alkylating agents. It works by slowing or stopping the
growth of cancer cells.
Uses:-

25. L O M U S T I N E : -
Bioavailability :- 100%
Protein Binding:- 90%
Metabolism :- Hepatic
Excretion :- Renal
Route of Administration :- oral
Uses:- Lomustine is used to treat certain types of brain tumors. Lomustine is also
used with other medications to treat Hodgkin's lymphoma (Hodgkin's
disease) that has not improved or that has worsened after treatment with
other medications. Lomustine is in a class of medications called alkylating
agents.
DECARBAZINE :-
Bioavailability :- 100%
Protein Binding:- 90%
Metabolism :- Hepatic
Excretion :- kidney
Route of Administration :- Intravenously,
Uses:-
Dacarbazine is used to treat certain types of cancer, such as skin
cancer and Hodgkin's disease. It is a cancer chemotherapy drug
that is used to slow or stop cancer cell growth.

26. MYCIN WAS AN EARLY BACKWARD
CHAINING EXPERT SYSTEM THAT USED ARTIFICIAL
INTELLIGENCE TO IDENTIFY BACTERIA CAUSING
SEVERE INFECTIONS, SUCH
AS BACTEREMIA AND MENINGITIS, AND TO
RECOMMEND ANTIBIOTICS, WITH THE DOSAGE
ADJUSTED FOR PATIENT'S BODY WEIGHT — THE
NAME DERIVED FROM THE ANTIBIOTICS
THEMSELVES, AS MANY ANTIBIOTICS HAVE THE
SUFFIX "-MYCIN". THE MYCIN SYSTEM WAS ALSO
USED FOR THE DIAGNOSIS OF BLOOD CLOTTING
DISEASES. MYCIN WAS DEVELOPED OVER FIVE OR
SIX YEARS IN THE EARLY 1970S AT STANFORD
UNIVERSITY
Antibiotic Mycin

27. DACTINOMYCIN :-
U S E S : - Dactinomycin may also be used to treat certain types of cancerous
tumors that are located in a specific area of the body. Dactinomycin is a
type of antibiotic that is only used in cancer chemotherapy. It works
by slowing or stopping the growth of cancer cells in your body
DOXORUBICIN
U S E S : -
Doxorubicin is used in combination with other
medications to treat certain types of bladder,
breast, lung, stomach, and ovarian cancer;
Hodgkin's lymphoma (Hodgkin's disease) and
non-Hodgkin's lymphoma (cancer that begins in
the cells of the immune system); and certain types
of leukemia (cancer of the white blood cells ...

28. U S E S : -
B I O AVA I L A B I L I T Y : - 1 0 0 %
P R O T E I N B I N D I N G : - 9 0 %
M E TA B O L I S M : - H E PAT I C
E X C R E T I O N : - R E N A L
R O U T E O F A D M I N I S T R AT I O N : - O R A L
DAUNORUBICIN :-
Bioavailability :- 100%
Protein Binding:- 90%
Metabolism :- Hepatic
Excretion :- Renal
Route of Administration :- oral
Daunorubicin is also used with other chemotherapy drugs to treat a
certain type of acute lymphocytic leukemia (ALL; a type of cancer of
the white blood cells). Daunorubicin is in a class of medications called
anthracyclines. It works by slowing or stopping the growth
of cancer cells in your body.
BLEOMYCIN :-

29. A DRUG THAT IS SIMILAR ENOUGH TO A NATURAL
CHEMICAL TO PARTICIPATE IN A NORMAL BIOCHEMICAL
REACTION IN CELLS BUT DIFFERENT ENOUGH TO
INTERFERE WITH THE NORMAL DIVISION AND
FUNCTIONS OF CELLS. SO NAMED BECAUSE THE DRUG
INHIBITS A NORMAL METABOLIC PROCESS. EXAMPLES OF
ANTIMETABOLITES INCLUDE 6-
MERCAPTOPURINE (6MP), METHOTREXATE,
AND HYDROXYUREA .
ANTIMETABOLITE
AGENT

30. F O L A T E A N T A G O N I S T
METHOXYTRATE :-
Bioavailability :- 60%
Protein Binding:- 50%
Metabolism :- Hepatic
Excretion :- Renal
Route of Administration :- oral
Uses:-
Methotrexate is in a class of medications called antimetabolites.
Methotrexate treats cancer by slowing the growth of cancer cells.
Methotrexate treats psoriasis by slowing the growth of skin cells to stop
scales from forming. Methotrexate may treat rheumatoid arthritis by
decreasing the activity of the immune system.

31. SYNTHESIS

32. MECHANISUM OF ACTION
Methotrexate

33. STRUCTURE ACTIVITY
RELEATIONSHIP

34. M E R C A P T O P U R I N E ( 6 - M P ) , S O L D U N D E R T H E B R A N D N A M E
P U R I N E T H O L A M O N G O T H E R S , I S A M E D I C A T I O N U S E D F O R
C A N C E R A N D A U T O I M M U N E D I S E A S E S . S P E C I F I C A L L Y I T I S
U S E D T O T R E A T A C U T E L Y M P H O C Y T I C L E U K E M I A ( A L L ) ,
C H R O N I C M Y E L O I D L E U K E M I A ( C M L ) , C R O H N ' S D I S E A S E , A N D
U L C E R A T I V E C O L I T I S .
PURINE ANTAGONIST
6-MARCUPTOPURINE :-

35. SYNTHESIS

36. U S E S : - F L U D A R A B I N E I S U S E D F O R : T R E A T M E N T O F C H R O N I C
L Y M P H O C Y T I C L E U K E M I A ( C L L ) , I N C L U D I N G C L L T H A T H A S
N O T R E S P O N D E D T O O R R E O C C U R R E D A F T E R S T A N D A R D
T H E R A P Y . S A L V A G E T H E R A P Y F O R N O N - H O D G K I N ' S L Y M P H O M A
A N D A C U T E L E U K E M I A S .
C L A D R I B I N E I S U S E D T O T R E A T H A I R Y C E L L L E U K E M I A ( C A N C E R O F
A C E R T A I N T Y P E O F W H I T E B L O O D C E L L ) . C L A D R I B I N E I S I N A C L A S S
O F M E D I C A T I O N S K N O W N A S P U R I N E A N A L O G S . I T W O R K S B Y
S T O P P I N G O R S L O W I N G T H E G R O W T H O F C A N C E R C E L L S .
FLUDARABINE :-
Bioavailability :- 55%
Protein Binding:- 29%
Metabolism :- Hepatic
Excretion :- Kidney
Route of Administration :- oral
CLADRIABINE
USES:-

37. PYRAMIDINE
ANTAGONIST
5-FLUOROURACIL :- Bioavailability :- 28-100%
Protein Binding:- 8-15%
Metabolism :- Hepatic
Excretion :- Kidney
Route of Administration :- IV, Topical
U S E S : - Fluorouracil (5-FU), sold under the brand name Adrucil among others, is
a medication used to treat cancer. By injection into a vein it is used
for colon cancer, esophageal cancer, stomach cancer,
pancreatic cancer, breast cancer, and cervical cancer.

38. GEMCITABINE
U S E S : - Gemcitabine is used to treat certain types
of cancer (including breast, lung,
ovarian, pancreatic). It is
a chemotherapy drug that works by
slowing or stopping the growth
of cancer cells.

39. MECHANISUM OF ACTION
GEMICTABINE

40. A TYPE OF DRUG THAT BLOCKS CELL
GROWTH BY STOPPING MITOSIS (CELL
DIVISION). TAXANES INTERFERE WITH
MICROTUBULES (CELLULAR STRUCTURES
THAT HELP MOVE CHROMOSOMES DURING
MITOSIS). THEY ARE USED TO TREAT
CANCER. A TAXANE IS A TYPE OF MITOTIC
INHIBITOR AND A TYPE OF
ANTIMICROTUBULE AGENT.
Taxenes

41. PACLITAXEL :-
Bioavailability :- 65%
Protein Binding:- 89-98%
Metabolism :- Hepatic
Excretion :- Kidney
Route of Administration :- IV, Topical
Paclitaxel Is Used For: Treatment of breast, ovarian, lung,
bladder, prostate, melanoma, esophageal, as well as other types
of solid tumor cancers. It has also been used in Kaposi's
sarcoma.
U S E S : -

42. A TYPE OF DRUG THAT BLOCKS CELL GROWTH BY
STOPPING MITOSIS (CELL DIVISION). VINCA
ALKALOIDS INTERFERE WITH MICROTUBULES
(CELLULAR STRUCTURES THAT HELP MOVE
CHROMOSOMES DURING MITOSIS). THEY ARE
USED TO TREAT CANCER. A VINCA ALKALOID IS A
TYPE OF MITOTIC INHIBITOR AND A TYPE OF
ANTIMICROTUBULE AGENT.
Vinca Alkaloids

43. VINCRISTINE :-
Bioavailability :- Not rellably absorbed in GI Track
Protein Binding:- 44%
Metabolism :- Hepatic
Excretion :- Kidney
Route of Administration :- IV
U S E S : - Cancers treated with Vincristine include: acute leukemia, Hodgkin's
and non- Hodgkin's lymphom,neuroblastoma, rhabdomyosarcoma,
Ewing's sarcoma, Wilms' tumor, multiple myeloma, chronic leukemias,
thyroid cancer, brain tumors.
It is also used to treat some blood disorders.

44. VINBLASTINE :-
Bioavailability :- NA
Protein Binding:- 24%
Metabolism :- Hepatic
Excretion :- Kidney
Route of Administration :- IV
Vinblastine is used in combination with other chemotherapy drugs
to treat Hodgkin's lymphoma (Hodgkin's disease) and non-
Hodgkin's lymphoma (types of cancer that begin in a type of
white blood cell that normally fights infection), and cancer of the
testicles.
U S E S : -

45. MISCELLANEOUS
PROCARBAZINE :-
U S E S : - Procarbazine is used in combination with other medications to treat
certain types of Hodgkins disease (types of cancer that begin in a type
of white blood cells that normally fights infection). Procarbazine is in a
class of medications called alkylating agents.
HYDROXYUREA
U S E S : - Hydroxyurea (Hydrea) is used alone or with other
medications or radiation therapy to treat a certain
type of chronic myelogenous leukemia (CML;
a type of cancer of the white blood cells) and
certain types of head and
neck cancer (including cancer of the mouth,
cheek, tongue, throat, tonsils, and sinuses).

46. BONE NARROW TOXICITY DECRESED LEUCOSIDES
PRODUCTION AND THUS DECRESED RESISTANCE TO
INFECTION.
IMPARED WOUND HEALING
LOSS OF HAIR
DAMAGE TO GASTROINTESTINAL EPITHELIUM.
DEPRESSION OF GROWTH IN CHILDREN
STERILITY
TERETOGENICITY
TOXIC EFFECT OF
ANTICANCER DRUG

47. ACUTE TOXICITY
VOMATING
ALLERGY REACTION
ARRHYTHMIAS
DELAYED EFFECT
MUCOSITIES
ALOPECIA
BONE NARROW SUPPRESSION
CHRONIC TOXICITY
HEART
KIDNEY
LIVER
LUNG

48. TREATMENT OF CANCER