+

Cancer Pharmacology
Shan Nanji
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Cancer Rx:
Anti-Metabolites
nMethotrexate Inhibits __________________
n Used also for Molar Pregnancies and Rheumatoid Arthritis

n Rescue __________________
n replenishes Folate in the form of Folinic Acid,
which is recognized by the body but NOT by cancer

nara-C/Cytarabine (Pyrimidine Anolog)

n Inhibition of DNA polymerase

nara-A

Shan Nanji - NanjiMD@gmail.com

+ 3

Cancer Rx:
Anti-Metabolites
n6-Mercaptopurine 6-mercap-TOE-purine
n (Purine [thio] analog)
n Decreases de novo purine synthesis
n Activated by HGPRTase, promotes
______________

n6-Thioguanine
n Same as 6-MP
n can be given with allopurinol

n5-Flourouracil 5- FU
n Inhibits __________________
Shan Nanji - NanjiMD@gmail.com
n Rx: Colon Cancer
+ 4

Cancer Rx:
Antitumor Antibiotics
nAdriamycin ATRIA-mycin
MOA:
n Free Radical Formation
n Breaks in DNA

n Can cause __________________

n Rescue __________________

Shan Nanji - NanjiMD@gmail.com

+ 5

Cancer Rx:
Antitumor Antibiotics
nBleomycin
MOA:
n Cause Free Radical Formation
n DNA breaks
n S/E:

n __________________

Shan Nanji - NanjiMD@gmail.com

+ 6

Cancer Rx:
Alkylating Agents
n Cisplatin cis-PLATIN
n MOA:
n DNA Cross-Linking

n Can cause __________________ and __________________

n Rescue __________________

nCyclophosphomide
n Pro-drug: require activation by the liver

n Covalently X-Link DNA at Guanine N-7

n Can Cause __________________

n Rescue __________________
Shan Nanji - NanjiMD@gmail.com
+ 7

Cancer Rx:
Alkylating Agents
nBusulfan
MOA:
n Alkylates DNA

n S/E:
n __________________

nHydroxyurea hyd RoxyuRea

n Inhibits __________________
n can raise HbF in Sickle Cell

nMelphalan
n Rx: Multiple Myeloma

Shan Nanji - NanjiMD@gmail.com

+ 8

Cancer Rx:
Alkylating Agents
nNitrosureas
MOA:
n Require Bioactivation
n S/E:

n __________________

nChlorambucil MC Alkylating agent

Shan Nanji - NanjiMD@gmail.com

+ Cancer Rx: 9

Microtubule Inhibitors
n Vinblastine
n Blocks polymerization therefore mitotic spindle cant form
n S/E:
n Blasts Bone Marrow -> Bone Marrow Suppression

n Vincristine Blocks polymerization so mitotic spindle cant form

n S/E:
n Neurotoxicity (Areflexia, Peripheral Neuritis)
n Paralytic Ileus

n Paclitaxel __________________polymerized microtubules in M-

phase so that mitotic spindle __________________ (anaphase can not
occur)

Shan Nanji - NanjiMD@gmail.com

+ Cancer Rx: 10

SERMS
nTamoxifen/Raloxifene
MOA:
n Receptor __________________ in Breast
n Receptor __________________ in Bone
n S/E:
n Tamoxifen
n Increase Risk __________________
n Hot Flashes
n Raloxifene
n RELAXifeneNo Increased Risk!

Shan Nanji - NanjiMD@gmail.com