Exam 1 Table Flashcards
5-fluorouracil (5-FU) target
Thymidylate synthase - blocks uracil to thymine conversion
5-fluorouracil (5-FU) drug class
Anti-metabolite; uridine analog
5-fluorouracil (5-FU) cell cycle phase
S
5-fluorouracil (5-FU) dose limiting side effect
Myelosuppression
5-fluorouracil (5-FU) rescue drug
Thymidine
5-fluorouracil (5-FU) synergy drug
Leucovorate
5-fluorouracil (5-FU) unique resistance mechanisms
-Downregulation of activating enzymes that convert 5-FU to fd-UMP
-Upregulation of thymidylate synthase
5-fluorouracil (5-FU) genetic testing
~5% of the population has gene polymorphisms that result in a deficiency of the enzyme dihydropyrimidine dehydrogenase (DPD) which breaks down 5-FU
Cytarabine target
Converted to Ara-CTP intracellularly -> competitive inhibitor of DNA polymerase alpha
Cytarabine drug class
Anti-metabolite; cytosine analog
Cytarabine cell cycle phase
S
Cytarabine indication
-Leukemia
-Lymphoma
Cytarabine dose limiting side effect
Myelosuppression
Cytarabine synergy drug
Tetrahydrouridine because of inhibition of cytidine deaminase
Cytarabine unique resistance mechanisms
-Downregulation of activating enzymes
-Upregulation of cytidine deaminases
-Downregulation of influx transporters
6-mercaptopurine (6-MP) target
Blocks multiple enzymes in de novo purine biosynthesis
6-mercaptopurine (6-MP) drug class
Antimetabolite; purine analog, thio-analog of adenine
6-mercaptopurine (6-MP) cell cycle phase
S
6-mercaptopurine (6-MP) dose limiting side effects
Hematologic toxicity, myelosuppression
6-mercaptopurine (6-MP) drug interactions
Allopurinol increases 6-MP toxicity
6-mercaptopurine (6-MP) unique resistance mechanisms
Loss of HGPRT (activating enzyme)
6-mercaptopurine (6-MP) genetic testing
TPMT polymorphism loss of function - (TPMT inactivates 6-MP) - dose adjustment needed
Methotrexate target
DHFR inhibitor
Methotrexate drug class
Antimetabolite, antifolate