Review Note
Last Update: 08/30/2023 12:42 AM
Current Deck: ACMS Study Guide Deck::A. Cancers
PublishedCurrently Published Content
Front
Treatment of AKs
Back
5-fluorouracil (5FU)
◦ Antimetabolite
◦ Pyrimidine antagonist
◦ Blocks conversion of dUMP to dTMP in the synthesis of DNA and RNA
through thymidylate synthetase
◦ Toxicity due to systemic drug absorption rare, but serious side effects
(e.g., cardiac ischemia, enterotoxicity) reported in patients with inherited
deficiency of dihydropyrimidine dehydrogenase
• Imiquimod
▪ Toll-like receptor 7 agonist (TLR7) and lesser extent 8 (TLR8)
induces interferon, Th1-type immunity
• Ingenol mebutate
◦ Derived from Euphorbia peplus plant (radium weed) Mechanism of action unknown but causes activation of protein C kinase
immediate cell necrosis (not apoptosis), neutrophils and inflammation at
site of application
• Diclofenac
◦ Blocks cyclooxygenases and prostaglandins E2 synthesis
◦ Pro-apoptotic and anti-angiogenic
◦ But long treatment cycle and lower clearance rates
• PDT
◦ FDA approved for AKs but off-label for NMSC
◦ Methyl aminolevulinate and aminolevulinic acid are photosensitizers
◦ Protoporphyrin IX accumulates intracellularly
◦ Protoporphyrin IX maximally absorbs at UV wavelength of 400-420 nm
(Soret band); also, at the red (635 nm)
◦ Antimetabolite
◦ Pyrimidine antagonist
◦ Blocks conversion of dUMP to dTMP in the synthesis of DNA and RNA
through thymidylate synthetase
◦ Toxicity due to systemic drug absorption rare, but serious side effects
(e.g., cardiac ischemia, enterotoxicity) reported in patients with inherited
deficiency of dihydropyrimidine dehydrogenase
• Imiquimod
▪ Toll-like receptor 7 agonist (TLR7) and lesser extent 8 (TLR8)
induces interferon, Th1-type immunity
• Ingenol mebutate
◦ Derived from Euphorbia peplus plant (radium weed) Mechanism of action unknown but causes activation of protein C kinase
immediate cell necrosis (not apoptosis), neutrophils and inflammation at
site of application
• Diclofenac
◦ Blocks cyclooxygenases and prostaglandins E2 synthesis
◦ Pro-apoptotic and anti-angiogenic
◦ But long treatment cycle and lower clearance rates
• PDT
◦ FDA approved for AKs but off-label for NMSC
◦ Methyl aminolevulinate and aminolevulinic acid are photosensitizers
◦ Protoporphyrin IX accumulates intracellularly
◦ Protoporphyrin IX maximally absorbs at UV wavelength of 400-420 nm
(Soret band); also, at the red (635 nm)
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