PGX EXAM 3 (SOLVED) QUIZZES & ANS!!
Irinotecan is a prodrug converted to the active SN-38 form by - (ANSWER)carboxylesterases
SN38 is deactivated by _______ in the liver and eliminated by biliary excretion -
(ANSWER)glucuronidated by UDP-glucuronosyltransferases
______ is a contraindication for irinotecan - (ANSWER)major liver impairment
dose reduction if moderate liver impairment
______ and ______ also metabolize irinotecan - (ANSWER)CYP3A4 and 3A5
Irinotecan and its metabolites are actively effused outside the cells by _____ transporters such as -
(ANSWER)ABC
Multidrug resistant protein-1 (MDR1) and Multidrug resistance-associated protein-1 and protein-2
(MRP1 and MRP2)
_______ is a strong UGT1A1 and UGT1A9 inhibitor - (ANSWER)Regorafenib
would inhibit glucoronidation of SN28 and inactivation
_______ polymorphism is the biomarker for ironotecan - (ANSWER)UGT1A1*28
TATA7 polymorphism
______ and ______ are polymorphisms in the coding region (exon 1) for UGT1A1 - (ANSWER)*6 and 27
, PGX EXAM 3 (SOLVED) QUIZZES & ANS!!
which alleles are implicated in Gilbert's syndrome with reduced UGT1A1 function - (ANSWER)*6, 27, 28
what is gilbert's syndrome - (ANSWER)harmless liver condition in which the liver doesn't properly
process bilirubin.
what is the limitation of genetic testing for UGT1A1 in pts about to start irinotecan - (ANSWER)only tests
for TATA box polymorphism and does not detect other genes
5-FU and Capecitabine are inactivated by - (ANSWER)Dihydropyrimidine Dehydrogenase (DPD)
normal DPD function - (ANSWER)Carrying two copies of normal alleles (e.g:*1/1, 1/9A).
low DPD function - (ANSWER)Carrying one functional allele and one non-functional (e.g:*1/2) .
no DPD function - (ANSWER)Carrying two copies of non-functional alleles (e.g: 2/2, 2/13).
DPD deficiency results in - (ANSWER)Exaggerated 5-FU-related toxicities: Neutropenia; Mucositis,
Stomatitis, Diarrhea; Skin rash; Neurologic toxicities; Death.
DPD intermediate metabolizer - (ANSWER)reduce starting dose
DPD poor metabolizer - (ANSWER)avoid 5-FU and capecitabine
_____ and _____ are effective in pts with EGFR expression and *wild type* KRAS and can be used in
colorectal cancer and NSCLC - (ANSWER)Cetuximab and Panitumumab
Irinotecan is a prodrug converted to the active SN-38 form by - (ANSWER)carboxylesterases
SN38 is deactivated by _______ in the liver and eliminated by biliary excretion -
(ANSWER)glucuronidated by UDP-glucuronosyltransferases
______ is a contraindication for irinotecan - (ANSWER)major liver impairment
dose reduction if moderate liver impairment
______ and ______ also metabolize irinotecan - (ANSWER)CYP3A4 and 3A5
Irinotecan and its metabolites are actively effused outside the cells by _____ transporters such as -
(ANSWER)ABC
Multidrug resistant protein-1 (MDR1) and Multidrug resistance-associated protein-1 and protein-2
(MRP1 and MRP2)
_______ is a strong UGT1A1 and UGT1A9 inhibitor - (ANSWER)Regorafenib
would inhibit glucoronidation of SN28 and inactivation
_______ polymorphism is the biomarker for ironotecan - (ANSWER)UGT1A1*28
TATA7 polymorphism
______ and ______ are polymorphisms in the coding region (exon 1) for UGT1A1 - (ANSWER)*6 and 27
, PGX EXAM 3 (SOLVED) QUIZZES & ANS!!
which alleles are implicated in Gilbert's syndrome with reduced UGT1A1 function - (ANSWER)*6, 27, 28
what is gilbert's syndrome - (ANSWER)harmless liver condition in which the liver doesn't properly
process bilirubin.
what is the limitation of genetic testing for UGT1A1 in pts about to start irinotecan - (ANSWER)only tests
for TATA box polymorphism and does not detect other genes
5-FU and Capecitabine are inactivated by - (ANSWER)Dihydropyrimidine Dehydrogenase (DPD)
normal DPD function - (ANSWER)Carrying two copies of normal alleles (e.g:*1/1, 1/9A).
low DPD function - (ANSWER)Carrying one functional allele and one non-functional (e.g:*1/2) .
no DPD function - (ANSWER)Carrying two copies of non-functional alleles (e.g: 2/2, 2/13).
DPD deficiency results in - (ANSWER)Exaggerated 5-FU-related toxicities: Neutropenia; Mucositis,
Stomatitis, Diarrhea; Skin rash; Neurologic toxicities; Death.
DPD intermediate metabolizer - (ANSWER)reduce starting dose
DPD poor metabolizer - (ANSWER)avoid 5-FU and capecitabine
_____ and _____ are effective in pts with EGFR expression and *wild type* KRAS and can be used in
colorectal cancer and NSCLC - (ANSWER)Cetuximab and Panitumumab
