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SN-38 is an antineoplastic drug. It is the active metabolite of irinotecan (an analog of camptothecin - a topoisomerase I inhibitor) but has 1000 times more activity than irinotecan itself. In vitro cytotoxicity assays show that the potency of SN-38 relative to irinotecan varies from 2- to 2000-fold. SN38 is formed via hydrolysis of irinotecan by carboxylesterases and metabolized via glucuronidation by UGT1A1. SN-38 and its glucuronide are lost into the bile and intestines. It can cause the symptoms of diarrhoea and myelosuppression experienced by ~25% of the patients administered irinotecan.

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  • SN-38 (it)
  • SN-38 (ja)
  • SN-38 (en)
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  • SN-38 (o 7-etil-10-idrossi-camptotecina) è il metabolita attivo dell'irinotecano (un farmaco antineoplastico facente parte della classe della camptotecine, inibitori della topoisomerasi I). È circa 200 volte più attivo rispetto all'irinotecano stesso. (it)
  • SN-38は抗腫瘍効果を有する化合物である。 これはイリノテカンの活性代謝物（カンプトテシン類縁物質 - トポイソメラーゼI阻害剤）であり、イリノテカン自体の1000倍の活性を持つ。In vitro 細胞毒性試験の結果を見ると、SN-38の効力はイリノテカンと比較して2倍から2000倍まで変動する。 SN-38は、カルボキシルエステラーゼによるイリノテカンの加水分解により形成され、UGT1A1によるグルクロン酸抱合により代謝される。 SN-38の代謝不良に繋がるUGT1A1の変異は白人の約10％に存在し、SN-38グルクロニドの形で体から排泄されにくいため、イリノテカンの毒性が上昇する。 SN-38とそのグルクロニドは、胆汁と腸に排泄される。イリノテカンを投与された患者の約25％が経験する下痢および骨髄抑制の症状を引き起こす。 更に、腸管内でSN-38が脱抱合されて再度吸収され腸肝循環するので、下痢が重篤化し易い。 (ja)
  • SN-38 is an antineoplastic drug. It is the active metabolite of irinotecan (an analog of camptothecin - a topoisomerase I inhibitor) but has 1000 times more activity than irinotecan itself. In vitro cytotoxicity assays show that the potency of SN-38 relative to irinotecan varies from 2- to 2000-fold. SN38 is formed via hydrolysis of irinotecan by carboxylesterases and metabolized via glucuronidation by UGT1A1. SN-38 and its glucuronide are lost into the bile and intestines. It can cause the symptoms of diarrhoea and myelosuppression experienced by ~25% of the patients administered irinotecan. (en)
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  • SN-38 is an antineoplastic drug. It is the active metabolite of irinotecan (an analog of camptothecin - a topoisomerase I inhibitor) but has 1000 times more activity than irinotecan itself. In vitro cytotoxicity assays show that the potency of SN-38 relative to irinotecan varies from 2- to 2000-fold. SN38 is formed via hydrolysis of irinotecan by carboxylesterases and metabolized via glucuronidation by UGT1A1. The variant of UGT1A1 in ~10% of Caucasians which leads to poor metabolism of SN-38 predicts irinotecan toxicity, as it is then less easily excreted from the body in its SN-38 glucuronide form. SN-38 and its glucuronide are lost into the bile and intestines. It can cause the symptoms of diarrhoea and myelosuppression experienced by ~25% of the patients administered irinotecan. (en)
  • SN-38 (o 7-etil-10-idrossi-camptotecina) è il metabolita attivo dell'irinotecano (un farmaco antineoplastico facente parte della classe della camptotecine, inibitori della topoisomerasi I). È circa 200 volte più attivo rispetto all'irinotecano stesso. (it)
  • SN-38は抗腫瘍効果を有する化合物である。 これはイリノテカンの活性代謝物（カンプトテシン類縁物質 - トポイソメラーゼI阻害剤）であり、イリノテカン自体の1000倍の活性を持つ。In vitro 細胞毒性試験の結果を見ると、SN-38の効力はイリノテカンと比較して2倍から2000倍まで変動する。 SN-38は、カルボキシルエステラーゼによるイリノテカンの加水分解により形成され、UGT1A1によるグルクロン酸抱合により代謝される。 SN-38の代謝不良に繋がるUGT1A1の変異は白人の約10％に存在し、SN-38グルクロニドの形で体から排泄されにくいため、イリノテカンの毒性が上昇する。 SN-38とそのグルクロニドは、胆汁と腸に排泄される。イリノテカンを投与された患者の約25％が経験する下痢および骨髄抑制の症状を引き起こす。 更に、腸管内でSN-38が脱抱合されて再度吸収され腸肝循環するので、下痢が重篤化し易い。 (ja)
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alternative name
  • 7-Ethyl-10-hydroxycamptothecin (en)
IUPAC name
  • (4S)-4,11-Diethyl-4,9-dihydroxy-1,4-dihydro-3H,14H-pyrano[3′,4′:6,7]indolizino[1,2-b]quinoline-3,14-dione (en)
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