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Anticancer Drugs 1 Classic Cytotoxic Agents

Method

Alkylating Agents

Antimetabolites

Insert alkyl group


(carbonium ion) into DNA
structure, causing covalent
crosslinking between
guanine bases

Affects pathway
involving folate (replace
w methotrexate) OR
affect pyrimidine OR
purine base. (Folate
impt for cell division)

Stress in DNA leading to


breaks and apoptosis
QUESTION EOS: Alkyl
group..
Affects
Cycle
Specificity
Limitations

Common
Adverse
Effects

DNA Structure
Cycle non-specific

Plant Alkaloids
Mitotic poison
Inhibits microtubule
formation (No mitotic
spindles) AND
inhibit
topoisomerase

Blocks synthesising of
new strand making
molecule non-functional

Cell cycle paralysed


OR supercoils
forms, molecule
non-functional

DNA replication
S-phase inhibitors

DNA rep/mitosis
S and M phase

Hormonal
Agents/Antagonists
Prostate
Breast cancer
Leukaemia/lym
a) Antiandrogens:
a) Selective oestrogen
phoma
Prevent androgen
receptor modulator:
(Blood borne
interaction (no growth Deny sex hormone
cancers)
factor)
b) Aromatase inhibitors Use of
b) Gonadrotrophin-RH preventing fat cells
glucocorticoids
analogues: Increase
from making oestrogen that cause cell
production of
lysis in high
androgen until
doses
negative feedback
shuts it down
(LH/FSH)
Tumour growth, reduce cancer cells
M phase??

Cytotoxic Antibiotics (Unrelated to the rest?) Binds to DNA and topoisomerase


Post-menapausal
Cushings
- Too toxic for use in infectious disease therapy
syndrome &
osteoporosis
- Cost/benefit ratio different in cancer
- Inhibits transcription and translation processes, cycle non-specific
Rapidly dividing normal cell populations (Epithelial/stable tissue)
- Inflammation of GIT lining
- Developing of sores, skin necrosis, blistering
- Loss of hair follicles
Nausea, vomiting
Low WBC count (infection vulnerable), low RBC (anaemia), low platelets (clotting issues)
Damage to gametes (infertility), growth impairment (children)
Organ toxicity
- Heart: Arrhythmia (irregular heartbeat); Kidneys: Renal failure (low drug excretion, dosage problems); Nervous system: Paresthesias
(tingling, burning, numbness); Urinary bladder (Damage lining, bleeding)
Effects go away after drug use stops

Alkylating agents

Antimetabolites

Plant Alkaloids

Hormonal agents

Cytotoxic antibiotics

Cyclophosphamide,
ifosfamide (causes urinary
bladder bleeding),
cisplatin (testicular cancer)

Methotrexate, 5-flurouracil
(RNA uracil)

Vinca alkaloids
Vinblastine, vinorelbine
Etiposide (mandrake)
M-cycle specific
Taxanes
Paclitaxel, docetaxel

Glucocorticoids:
Cortisol & prednisolone

Doxirubicin, mitomycin,
daunorubicin

Tamoxifen (SERM:
Selective Oestrogen
receptor modulator)
Inhibits oestrogen

Anticancer Drugs 1 Classic Cytotoxic Agents


receptors
Anastrozole (aromatase
inhibitor)
- Adipocytes:
Converts sex
hormone
precursor to
oestrogen
- Only works on
post menopausal
women
-taxel/-ine
G0 phase: Cell is virtually unresponsive to drug

-cin/-rubicin

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