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1. Anti-Neoplastics

2. 
Antimetabolites
◦
◦
◦
◦

Methotrexate
5-FU
Mercaptopurine
Azathioprine
Alkylating Agents
◦
◦
◦
◦

Cyclophosphamide
Cisplatin
Chlorambucil
Carmustine
Cytotoxic Antibiotics
◦
◦
◦
◦

Doxorubicin
Dactinomycin
Daunorubicin
Bleomycin
Natural Products
◦
◦
◦
◦
Vincristine
Vinblastine
Etoposide
Paclitaxel

3. 
Hormones

◦ Tamoxifen
◦ Anastrazole
◦ Prednisone

◦ Azathioprine
◦ Prednisolone
◦ Cyclosporine
Monoclonal Ab
◦ Trastuzumab
◦ Rituximab
Immunosuppressant
s

Others
◦ Asparaginase
◦ Imatinib Mesylate
◦ Hydroxyurea

4. 
S phase
◦ Methotrexate  blocks dihydrofolate reductase
◦ 5 – FU  inhibits thymidylate synthase
◦ Mercaptopurine  inhibits purine nucleotide
interconversions
◦ Hydroxyurea  inhibits ribonucleotide
reductase
◦ Pentostatin  inhibits adenosine deaminase
Drugs acting at Cell Cycle phases

5. 
G2 phase

M phase

G1 phase

Between S and G2
◦ Bleomycin  fragments DNA
◦ Vincristine & Vinblastine binds tubulin & blocks MT
polymerization
◦ Paclitaxel  prevents MT depolymerization; promotes
polymerization
◦ Dactinomycin  binds DNA & inhibits DNA-dependent
RNA synthesis
◦ Etoposide  interferes with topo II
◦ Dactinomycin
Drugs acting at Cell Cycle phases

6. 
High dose of tx for a short period of time
to reduce burden on cells
What is an induction regime?

7. 




Used for cancers with low percentage of
mitotic cells
Cyclophosphamide, busulphan,
chlorambucil
Doxorubicin, daunorubicin, dactinomycin
Cisplatin
Recruitment: initial use of CCNS drugs
achieves a significant log kill which causes
more cells in Go to go into G1; then CCS
drugs are given
CCNS – Cell cycle nonspecific
drugs

8. Drug/irradiation kills a constant
proportion of cells in population, not
fixed number of cancer cells
 One log kill = 90% decrease in cell pop
 3 log kill = 99.9% decrease
 Smaller tumor will have greater portion of
cells killed than larger tumor but they
regrow quicker between cycles of therapy

Log – Kill concept

9. Cyclophosphamide
 Methotrexate
 5-FU

Breast Cancer Combo

10. Doxorubicin
 Methotrexate
 5-FU

Pancreatic Cancer Combo

11. Cisplatin
 Paclitaxel

Ovarian Cancer Combo

12. Cisplatin
 Vinblastine
 Bleomycin

Testicular Cancer Combo

13. 




Cyclophosphamide
Doxorubicin
Vincristine
Prednisone
Rituximab
Non Hodgkin’s Lymphoma Combo

14. 



Mechlorethamine
Vincristine
Prednisone
Procarbazine




Doxorubicin
Bleomycin
Vinblastine
Dacarbazine
Hodgkin’s Disease Combo

15. 







Cytarabine
Capecitabine
Carmustine
Etoposide
Topotecan
Fulvestrant
Flutamide &
Finasteride
Leuprolide



Rituximab
Hydroxyurea
Imatinib Mesylate
Drugs w/ features you must know

16. Antimetabolite
 DOC for AML
 MoA: blocks DNA strand elongation
 Neurotoxic

Cytarabine

17. Stabilizes the topo II – DNA complex
causing dsDNA breaks during DNA
replication
 Dose limiting leukopenia
 Treat first time and metastatic testicular
cancer
 may cause AML!!

Etoposide

18. Oral prodrug  converted to 5-FU
 MoA: inhibits thymidylate synthase
 Useful for paclitaxel and doxorubicin –
resistant pts with colorectal or metastatic
breast cancers

Capecitabine

19. Alkylating agent; nitrosoureas
 Most alkylating agents taken up by active
transport but nitrosoureas taken up by
passive transport
 Liphopilic & passes BBB  CNS Toxicity
 Used for CNS cancers that are metastatic
 malignant astrocytoma

Carmustine

20. Unique topo I inhibitor, preventing
religation of bits of helices 
accumulation of single stranded breaks in
DNA
 Dose limiting neutropenia

Topotecan

21. Antiestrogen for hormone-sensitive
tumors
 Give to post-menopausal women who are
resistant to tamoxifen

Fulvestrant

22. Flutamide is a nonsteroidal androgen
antagonist which inhibits the translocation
of steroid receptors to the nucleus
 Finasteride is a 5-alpha reductase
inhibitor which inhibits synthesis of
dihydrotestosterone
 Both used to treat prostate cancer

Flutamide & Finestiride

23. GnRH analog which acts as a partial
agonist at GnRH receptors
 When administered in constant doses to
maintain stable blood levels, it inhibits the
release of LH and FSH
 Used in tx of prostate cancer

Leuprolide

24. 
This is an unconjugated chimeric
(murine/human) antiCD20 monoclonal
antibody which binds to the CD20 antigen
on follicular B cells in Non Hodgkins
lymphoma
Rituximab

25. Inhibits ribonucleotide reductase 
ribonucleotides to deoxyribonucleotides
 Used for myeloproliferative disorders

Hydroxyurea

26. 
Inhibits bcr-abl tyrosine kinase found in
chronic myelocytic leukemia (CML)
Imatinib Mesylate

27. Methotrexate (CCS  works during S
phase)
 Uses

◦
◦
◦
◦
◦

Solid tumors such as choriocarcinoma
Osteogenic sarcoma
Acute Lymphoblastic Leukemia (ALL)
Psoriasis
Abortifacient
Looks like folate  take up by cells readily
Antimetabolites

28. Inhibits dihydrofolate Reductase
 This enzyme reduces folate to
tetrahydrofolate which is a one carbon
unit carrier used in synthesis of purines
and pyrimidines which are part of DNA
and RNA  cell replication
 ANTIDOTE: Leucovorin  folinic acid
rescue

◦ Host cells are rescued while cancer cells die
MoA of Methotrexate

29. Nephrotoxicity
 Myelosuppression

◦ Neutropenia, thrombocytopenia, mucositis,
diarrhea, and GI ulceration (oral)
◦ G-CSF can counteract leukopenia

Pulmonary toxicity and hepatotoxicity
(long term)
Methotrexate Toxicity

30. 
Pyrimidine analogs
◦ 5 – FU
◦ Capecitabine  5-FU
◦ Cytarabine

5 – FU
◦ MoA: inihibit thymidylate synthase
◦ Uses: colon, breast, rectal, gastric, pancreatic
cancer
◦ Capecitabine is same but one of the newest
drugs for pancreatic cancer
Other Antimetabolites

31. 




Anorexia, nausea
Alopecia
Stomatitis and diarrhea
Myelosuppression (less for capecitaine)
Maculopapular rash

Resistance develops when
thymidylate synthase becomes less
sensitive to the drug
Toxicity of 5-FU and
Antimetabolites

32. 




Azathioprine, Mercaptopurine
MoA: as nucleotides they inhibit
phosphoribosylpyrophosphate (PRPP) synthetase
 reduction in PRPP
They also inhibit PRPP amidotransferase 
reduction in phosphoribosylamine
Block de novo PURINE synthesis and
salvage pathways
Toxicity:
◦
◦
◦
◦
Bone marrow suppression
Leukopenia
Hyperuricemia (Mercaptopurine)
Hepatotoxicity
Purine Analogs

33. 
Pentostatin
◦ Uses: Hairy Cell Leukemia
◦ MoA: blocks adenosine deaminase 
impairment of DNA replication and cell division
◦ Toxicity: Myelosuppression
Purine analogs

34. Cyclophosphamide (ifosphamide also)
 Busulphan
 Carmustine (nitrosoureas)

Alkylating Agents

35. 
MoA: prodrug converted in liver to active
nitrogen mustard (nephrotoxic) and
acrolein (causes cystitis)  interferes with
transcription and translation and causes
increased ADH secretion (water
reabsorption leading to hyponatremia
results)
◦ Drug is given with high water load


ANTIDOTE: Mesna
ADH antidote: Demeclocycline
Cyclophosphamide

36. 
Uses

Toxicity
◦
◦
◦
◦
Hodgkin’s disease
Lymphomas, myeloma
Leukemia
Ovarian & breast tumors
◦ Myelosuppression
◦ Permanent amenorrhea and azoospermia
◦ Renal and bladder toxicity (hemorrhagic cystitis
& hematuria)
◦ Alopecia
◦ Cardiotoxic at high doses
Cyclophosphamide Use and
Toxicity

37. MoA: cross-links DNA strands by
covalently bonding guanine residues 
prevents DNA replication & transcription
 Use: CML
 Toxicity:

◦ Busulphan Lung - pulmonary fibrosis
◦ Busulphan tan – hyper pigmentation
Busulphan

38. 
Some success in treating malignant
gliomas (multiforme glioblastoma 
thought to be incurable)
Temozolamide

39. Doxorubicin
 Daunorubicin
 Dactinomycin
 Bleomycin


All CCNS mostly
Cytotoxic Antibiotics

40. 
MoA:
◦ Intercalates DNA and is topo II block/poison
◦ Increases radicals
◦ Causes extravasation  ulcers and
inflammation

USES:
◦ Breast, ovarian, bladder tumors – Solid tumors
◦ Bronchogenic carcinoma
◦ Lymphoma and leukemia
Doxorubicin

41. 






Cardiomyopathy
Colors urine red
Stomatitis
Alopecia
Anemia, leukemia
ANTIDOTE for radicals: Dimethyl Sulphoxide
ANTIDOTE for cardiomyopathy: Dexrazoxane
Doxorubicin Toxicity

42. Similar to doxorubicin
 Use: LEUKEMIA

Daunorubicin

43. MoA: binds DNA Helix  prevents
transcription of DNA by RNA polymerase
 USES

◦
◦
◦
◦

Rhabdomyosarcoma
Wilm’s tumor in children
Ewing’s Tumor
Kaposi’s sarcoma
Toxicity: Pancytopenia
Dactinomycin

44. MoA: fragments DNA via free radicals 
cells accumulate in G2 phase
 USES

◦
◦
◦
◦

Lymphomas
SCC
Testicular carcinoma
Choriocarcinoma
Toxicity: Pulmonary Fibrosis,
hyperpigmentation
Bleomycin

45. Vinca alkaloids: Vincristine and
Vinblastine
 Epidophyllotoxins: Etoposide
 Camptothecins: Topotecan
 Taxanes: Paclitaxel

Natural Products

46. MoA: bind tubulin and prevent MT
assembly; act in M phase
 Vincristine (Neurotoxic—peripheral
neuropathy, loss of deep tendon
reflexes)

◦ Use: Hodgkin’s disease, rhabdomyosarcoma,
lymphomas, leukemia, neuroblastoma

Vinblastine (reversibly myelotoxic)
◦ Use: Hodgkin’s, testicular carcinoma

Resistance assoc/ MDR gene mutation
Vinca Alkaloids

47. MoA: stabilizes topo II-DNA complex 
dsDNA breaks
 Specific for late S and early G2 phases
 Uses: testicular carcinoma (less toxic than
other natural products), Hodgkin’s disease
 Toxicity:

◦ Leukopenia; hepatic and renal toxicity at high
dose
◦ May cause AML!!!
Epidophyllotoxins - ETOPOSIDE

48. MoA: inhibit MT disassembly 
abnormal/dysfunctional spindles
 Uses

◦ Advanced ovarian cancer w/ cisplatin
◦ Metastatic ovarian or breast cancer

Toxicity
◦ Hypersensitivity reactions
◦ Neutropenia
◦ Peripheral neuropathy & muscle pain
Taxane - Paclitaxel

49. Estrogens
 Antiestrogens

◦ Tamoxifen
◦ Fulvestrant
◦ Anastrazole
Androgens
 Antiandrogens

◦ Flutamide
◦ Finasteride
Hormonal Chemotherapy

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