Natural Products (anti-cancer) Flashcards
(29 cards)
Inhibits tubulin polymerization?
Enhance tubulin polymerization & prevent depolymerization ?
Inhibits tubulin polymerization? Vinca alkaloids
Engave tubulun polymerization & prevent depolymerization ? Taxanes
inhibit the process of tubulin polymerization,
which disrupts assembly of microtubules?
A) taxanes
B) epidophyllotoxins
C) vinca alkaloids
C) vinca alkaloids
Vincristine
Vinblastine
Viorelbine
All vinca alkaloids are cell cycle specific
They inhibits mitosis acting on …
A) S phase
B) M phase
C) G phase
B) M phase
Vincristine
C. CNS = neurotoxicity for both autonomic and peripheral neuropathy
Cisplatin (platinum compounds) is only periheral neurotoxicity
Vinblastine
B. Bone marrow suppression (myelosuppression)
Vinorelbine
Myelosuppression with neutropenia
Taxanes
Paclitaxel. Hyperseinsitivity
Docetaxel
Cabazitaxel
Ixabepilone
Eribulin. Block G2-M phase
Hypersensitivity reactions may be observed
reduced by premedication with dexamethasone, and diphenhydramine.
Paclitaxel
An albumin-bound paclitaxel nanoparticle formulation (nab-paclitaxel or Abraxane) is
not associated with HSRs
Nab-paclitaxel is indicated for pancreatic cancers.
Same as folfox (oxaliplatin)
poor substrate for the multidrug resistance
P-glycoprotein efflux pump and may, therefore, be useful for treating multidrug-resistant
tumors
A) Docetaxel
B) Cabazitaxel
C) Ixabepilone
D) Eribulin
B) Cabazitaxel
binds directly to βtubulin subunits on microtubules, leading to inhibition
of normal microtubule dynamics.
A) Docetaxel
B) Cabazitaxel
C) Ixabepilone
D) Eribulin
C) Ixabepilone
Oral bioavailability is about 50%, requiring oral dosage to be twice that of IV dosage.
Up to 30–50% of an administered dose of drug is excreted in the urine
Etoposide
forms a complex with topoisomerase II, the enzyme responsible for cutting
and religating double stranded DNA
Etoposide
G2-S phase
cell cycle specific
A) eribuln
B) camptothecin
C)bleomycin
D) etoposide
D) etoposide. (G2-S)
A) eribuln. (G2-M)
B) camptothecin (G2-M)
C)bleomycin (G2-M)
inhibit the activity of topoisomerase I (topo
I), the key enzyme responsible for cutting and re-ligating single DNA strands.
They are G2-M phase cell cycle specific.
A) eribuln
B) camptothecin
C)bleomycin
D) etoposide
Topo 1 and G2-M
B) camptothecin
prodrug that is converted mainly in the liver by the carboxylesterase
enzyme to govitecan, the SN-38 metabolite that is 1000-fold more potent as an
inhibitor of topo I than the parent compound
Hint: “can” family.
A) irinotecan
B) topotecan
C) deruxtecan
A) irinotecan
conjugated with trastuzumab to form an antibody drug conjugate (ADC).
The activity of this molecule is dependent on HER expression and not on HER2 gene
amplification
Hint: “can” family.
A) irinotecan
B) topotecan
C) deruxtecan (the most potent)
C) deruxtecan ( the most potent)
Myelosuppression and diarrhea (early and late) are adverse events.
Early diarrhea treated with atropine
Late diarrhea leads to electrolyte imbalance & dehydration
Hint: “can” family.
A) irinotecan
B) topotecan
C) deruxtecan (the most potent)
A) irinotecan
Anthraxycline is given?
IM
IV
Topical
Oral
IV
Anthracycline is cell cycle specific?
Nooooo its CCNS
NON-SPECIFIC
Anthracyclines S.E?
Q. Radiation recall reaction ? Anthracycline
Myelosuppression
Cardiotoxicity
Rubin
Mitoxantrone
Doxorubicin
Daunorubicin
Idarubicin
Epirubicin
Mitoxantrone
A blue discoloration of the fingernails, sclera, and urine is observed 1–2 days after drug
administration.
S.E of drug?
Hint: Anthracycline family
So rubin or Mitoxantrone
A) Doxorubicin
B) Daunorubicin
C) Idarubicin
D) Mitoxantrone
D) Mitoxantrone
Dilated cardiomyopathy, HF
Drug xx —> approved to prevent
or reduce anthracycline-induced cardiotoxicity in women with metastatic breast
cancer
A) dexamethasone
B )Diphenhydramine
C) dextrazoxane
C) dextrazoxane
Dexamethasone & Diphenhydramine for hypersensitivity reaction of paclitaxel