This document discusses various types of anticancer drugs, including their classification, mechanisms of action, and examples. It describes five main classes of anticancer agents: cytotoxic drugs like alkylating agents and antimetabolites that directly kill cancer cells; natural anticancer agents such as vinca alkaloids and taxanes that interfere with cell division; antibiotics that intercalate DNA; miscellaneous agents discovered through random synthesis; and drugs that act on hormones to manipulate the endocrine system and inhibit cancer growth. Recent FDA-approved drugs for various cancer types are also mentioned.

1. Anticancer agent
Submitted by:
Kakadiya Dipesh

2. Content
 What is Cancer?
 Types of Cancer
 Causes and risk factors
 The Classification of Anticancer
Drugs

3. What is Cancer?
Cancer is a disease characterized
by uncontrollable, irreversible,
independent, autonomous,
uncoordinated and relatively
unlimited and abnormal over
growth of tissues.
Cancer spreads by invasion to the
surrounding tissues and by
metastasis to distant sites.

4. Types of Cancer Affected Area
Anal cancer Anus
Breast Cancer Breast
Bladder Cancer Urinary Bladder
Bone marrow Cancer Shafts of long bones
Colon Cancer Colon
Cervical Cancer Cervix
Eye Cancer Eye
Gynecological Cancer Female Reproductive organs
Lung Cancer Lung
Osteo sarcoma metaphyseal region of tubular long bones
Wilms tumour Kidney
Leukemia Blood
Larynx Cancer Larynx
Testicular cancer Testis
Rectal Cancer Rectum

5. Causes and risk factors:
Environment
cigarette smoke
 chemicals
 UV light
 viruses
Metabolic processes
free radicals
 DNA copying and
repair defects
 Inherited genetic mutations

6. The Classification of
Anticancer Drugs
A. Drugs acting directly on cells
(Cytotoxic drugs)
1. Alkylating agents:
o These compounds produce highly
reactive carbonium ion intermediates
which transfer alkyl groups to cellular
macro molecules by forming covalent
bonds.
o Alkylation results in cross linking/
abnormal base pairing/scission of DNA

7. Nitrogen mustard
Breast cancer,
Multiple
myeloma
head and neck carcinomas,
osteogenic sarcoma
Hodgkin’s disease,
T-cell lymphoma
Chronic lymphocytic
leukemia
Multiple myeloma,
Ovarian cancer, Breast
cancer

8. Recent drugs based on Nitrogen mustard
Bestrabucil (phase I trial)
[Chlorambucil derivative]
Bendamustine
Uramustine (Nitrogen mustard+Uracil
Derivative)

9. Ethylenimine
Alkyl sulfonate
Ovarian cancer, Breast
cancer
Lymphoma
Chronic Myeloid
Leukemia

10. Nitrosoureas
Triazine
:- meningeal leukaemias and brain tumours(can
cross BBB)
Malignant melanoma;
Hodgkin's disease.

11. 2. Antimetabolites
o These are analogues related to
normal components of DNA or of
coenzymes involved in nucleic acid
synthesis.
o They competitively inhibit utilization
of the normal substrate or get
themselves incorporated forming
dysfunctional macromolecules.
o Several of the useful drugs used in
antimetabolite therapy are purines,
pyrimidines, folates, and related

12. Folate antagonist
Methotrexate
(NEOTREXATE)
NH
HN
N
O
H2N
CH2CH2
Acute lymphoblastic leukemia,
Lung cancer.
O
NH - CH -(CH2)2COOH
COOH
Pemetrexed

13. Purine antagonist
o These are highly effective antineoplastic
drugs.
oThey are converted in the body to the
corresponding
monoribonucleotides which inhibit the
conversion of inosine monophosphate to
adenine and guanine nucleotides.
N
N
N
N
H
SH
6-mercaptopurine
N
N
N
N
H
SH
H2N
Thioguanine
Childhood acute leukemia Adult acute leukemia

14. Recent drugs based on purines and related compounds:
N
N
N
N
NH2
Cl
O
HO
HO
Cladribine
N
N
N
N
NH2
O
HO
HO
Vidarabine
OH
N
N
N
N
NH2
O
HO
HO
Clofarabine
F
Cl
N
N
O
HO
HO
Pentostatin
HN
N
OH
N
N
N
N
NH2
O
HO
OH F
O
OH
HO P
O
Fludarabine

15. Pyrimidine antagonist
o Pyrimidine analogues have varied
applications as antineoplastic, antifungal and
antipsoriatic agents.
HN
O
N
H
O
F
5-Fluorouracil
5-Fluorouracil is converted in
the body to the corresponding
nucleotide 5-fluoro-2-
deoxyuridine monophosphate,
which inhibits thymidylate
synthase and blocks the
conversion of deoxyuridilic acid
to deoxythymidylic acid.
This leads to elective failure of
DNA synthesis.
Adenocarcinoma,
Skin cancer

16. Recent drugs

17. 3. Natural anticancer agents:
Vinca alkaloids
o These are mitotic inhibitors, bind to
microtubular protein-'tubulin', prevent its
polymerization and assembly of microtubules,
cause disruption of mitotic spindle and
interfere with cytoskeletal function.
o The chromosomes fail to move apart
during mitosis: metaphase arrest occurs.
o They are cell cycle specific and act in the
mitotic phase.

18. Hodgkin’s disease,
Acute lymphocytic
leukemia,
Lung cancer

19. Taxanes
o First isolated from
bark of Western /
Pacific yew (Taxus
obrIet visif oulsiae)d for treatment
of lung, ovarian and
o Taxanes hyper-sbtarebailiszte csa mncicerro. tubule
structure (freez them). Taxanes binds to the
β subunit of tubulin ,the resulting
microtubule/ Taxanes complex does not
have the ability to disassemble. This
adversely affects cell function because the
shortening and lengthening of microtubules

20. Ovarian cancer, Breast cancer,
Non –small cell lung cancer
Semi-synthetic derivatives

21. Epipodophyllotoxin
Small cell lung cancer, Non-Hodgkin’s
lymphomas,
Kaposi’s sarcoma, Cervical cancer
From Podophyllum
peltarum
May apple
O
O
O
OH
MeO OMe
OMe
O
Podophyllotoxin
HO
O
O
O
O
OO
MeO OMe
OH
O
Etoposide
HO
Affects DNA
topoisomerase II
(not
intercalating)
DNA strand
breakage
Etoposide (Semi-synthetic)
Eposin® Etopofos®
Vepesid®

22. Camptothecin analogues
o First isolated Camptotheca acuminata
(Chinese tree).
o Inhibits DNA topoisomerase II
DNA strand breakag
e
N
N
O
O
OH O
Camptothecin,
toxic, Lead comp.
N
N
O
O
OH O
HO
N
N
N
O
O
OH O
N O
O
N
Topotecan
Hycamtin®
Irinoteca
n
Campto
®
Semisynthetic
Ovarian cancer, Small cell lung cancer

23. 4. Antibiotics
o These are products obtained from
microorganisms and have prominent
antitumour activity.
o Practically all of them intercalate between
DNA strands and interfere with its template
function.
Actinomycin D
Wilms' tumour,
Rhabdomyosarcoma

24. Doxorubicin
Mitoxantrone
Kaposi’s sarcoma,
Small cell lung cancer,
Breast cancer,
Malignant lymphomas
Prostate cancer,
Multiple sclerosis

25. Daunorubicin
Mitomycin
Kaposi’s sarcoma,
Acute myeloid leukemia
Carcinomas of the cervix,
Breast, lung, stomach

26. Recent anticancer antibiotics drugs:
Calicheamicin
(Priclinical
)

27. Kigamicin C ( priclinical)
Lactoquinomycin A

28. o 5. Miscellaneous :
o These drugs have been developed by
random synthesis and testing for anti tumour
activity.
Procarbazine
Hydroxyurea
Hodgkin's disease,
Non-Hodgkin lymphomas,
Oat cell carcinoma of lung
Chronic myeloid leukaemia,
Psoriasis, Polycythaemia

29. Cisplatin
Carboplatin
Imatinib
Metastatic testicular
and
Ovarian carcinoma
Squamous carcinoma of
head
and neck,
Small cell lung cancer,
Seminoma
chronic myeloid
leukaemia

30. Recent drugs
Gefitinib
Erlotinib
Crizotinib
Non-
Small
Cell lung
cancer
(PROTEIN
KINASE
INHIBITORS)
Oxaliplatin
Ovarian
carcinoma,
Seminoma

31. B. Drugs acting on Hormones
o It involves the manipulation of the
endocrine system through exogenous
administration of specific hormones,
particularly steroid hormones, or drugs which
inhibit the production or activity of such
hoorBmeocnaeuss.e steroid hormones are powerful
drivers of gene expression in certain cancer
cells, changing the levels or activity of certain
hormones can cause certain cancers to cease
growing, or even undergo cell death.

32. 1. Corticosteroids :
o Corticosteroids are strong anti-inflammatory
drugs.
o They are used to reduce swelling that
causes cancer pain.
Examples

33. Prednisolone
palliation of lymphomas
and leukemias
Dexamethasone
haematological
malignancies

34. 2. Estrogens
o The agonist is occasionally used to treat
prostate cancer through suppression of
testosterone production.
Fosfestrol
carcinoma
prostate
Ethinylestradiol

35. 3. Selective estrogen receptor
modulators
o Acts by selective antagonism of the
estrogen receptor.
Breast
cancer
Toremifene Tamoxifen

36. 4. Selective estrogen receptor down
regulators
o Estrogen receptor down regulators blocks
the effects of estrogen in breast tissue.
Fulvestrant
Metastatic
breast
cancer

37. 5. Aromatase inhibitors
o Aromatase is the enzyme that synthesizes
estrogen.
o Aromatase inhibitors (AIs) are a class of
drugs used in the treatment of breast cancer
and ovarian cancer in postmenopausal
women.
o As breast and ovarian cancers require
estrogen to grow, Aromatase inhibitors are
taken to either block the production of
estrogen or block the action of estrogen on

38. Letrozole
Anastrozole
Breast cancer
Breast cancer

39. Exemestane
Early stage of breast cancer
Recent drug
Aminoglutethimide Vorozole

40. 6. Antiandrogen
o Antiandrogens, or androgen antagonists,
first discovered in the 1960s, prevent
androgens from expressing their biological
effects on responsive tissues.
o Antiandrogens alter the androgen pathway
by blocking the appropriate receptors,
competing for binding sites on the cell's
surface, or affecting androgen production.
o Antiandrogens are most frequently used to
treat prostate cancer.

41. Flutamide Bicalutamide
Nilutamide Finasteride

42. development status of antiandrogen drugs:

45. Recently Approved Drugs by FDA
Drugs Uses
2014
Belinostat Peripheral T-cell lymphoma
Ramucirumab Gastric cancer
Ibrutinib Chronic lymphocytic leukemia
Idelalisib Relapsed Chronic lymphocytic leukemia
Ceritinib Non-small cell lung Cancer

46. Drugs Uses
2013
Obinutuzumab Chronic lymphocytic leukemia
Afatinib Metastatic non-small cell lung cancer
Ibrutinib Mantle cell lymphoma
Trametinib Metastatic melanoma
Pomalidomide Relapsed and refractory multiple myeloma
Lenalidomide Mantle cell lymphoma
Regorafenib Gastrointestinal stromal tumor
Dabrafenib Metastatic melanoma
Denosumab Prostate cancer

47. References
1. Wilson and Gisvold's textbook of organic medicinal and
pharmaceutical
chemistry, Twelfth Edition, Charles Owens wilson, Ole
Gisvold
2. Essentials of Medical Pharmacology, Sixth Edition, K.D
TRIPATHI
3. Foye’s Principles of medicinal chemistry, Sixth Edition,
Thomas L.
Lemke, David A. Williams
http://www.fda.gov/drugs/informationondrugs/approveddr
ugs/ ucm279174.htm
4.