DGIdb - 7-ETHYL-10-HYDROXYCAMPTOTHECIN Drug Record

7-ETHYL-10-HYDROXYCAMPTOTHECIN chembl:CHEMBL837 Antineoplastic

Alternate Names:

7-ETHYL-10-HYDROXYCAMPTOTHECIN
NK-012
NK012
IRINOTECAN RELATED COMPOUND B
NK 012
SN 38
SN-38
7-ETHYL-10-HYDROXY-CAMPTOTHECIN
IT-141

Drug Info:

Drug Type	small molecule
Drug Groups	investigational
Drug Categories	alkaloids
Drug Categories	antineoplastic agents
Drug Categories	cytochrome p-450 cyp3a inhibitors
Drug Categories	cytochrome p-450 cyp3a substrates
Drug Categories	cytochrome p-450 cyp3a4 inhibitors
Drug Categories	cytochrome p-450 cyp3a4 inhibitors (strength unknown)
Drug Categories	cytochrome p-450 cyp3a4 substrates
Drug Categories	cytochrome p-450 enzyme inhibitors
Drug Categories	cytochrome p-450 substrates
Drug Categories	enzyme inhibitors
Drug Categories	topoisomerase i inhibitors
Drug Categories	topoisomerase inhibitors

(1 More Sources)

Publications:

Wang MJ et al., 2014, Design, synthesis, mechanisms of action, and toxicity of novel 20(s)-sulfonylamidine derivatives of camptothecin as potent antitumor agents., J Med Chem
Luo Y et al., 2012, Synthesis and biological evaluation of new homocamptothecin analogs., Eur J Med Chem
Parrino B et al., 2015, Water-soluble isoindolo[2,1-a]quinoxalin-6-imines: in vitro antiproliferative activity and molecular mechanism(s) of action., Eur J Med Chem
Cananzi S et al., 2011, Synthesis and topoisomerase I inhibitory activity of a novel diazaindeno[2,1-b]phenanthrene analogue of Lamellarin D., Bioorg Med Chem
Guerrant W et al., 2013, Dual-acting histone deacetylase-topoisomerase I inhibitors., Bioorg Med Chem Lett
Clericuzio M et al., 2006, Cucurbitane triterpenes from the fruiting bodies and cultivated mycelia of Leucopaxillus gentianeus., J Nat Prod
Samorì C et al., 2009, Semisynthesis, biological activity, and molecular modeling studies of C-ring-modified camptothecins., J Med Chem
Wang L et al., 2015, Design, synthesis and biological evaluation of novel homocamptothecin analogues as potent antitumor agents., Bioorg Med Chem
Han JY et al., 2006, Comprehensive analysis of UGT1A polymorphisms predictive for pharmacokinetics and treatment outcome in patients with non-small-cell lung cancer treated with irinotecan and cisplatin., J Clin Oncol
Wang H et al., 2014, Association analysis of UGT1A genotype and haplotype with SN-38 glucuronidation in human livers., Pharmacogenomics
Gagné JF et al., 2002, Common human UGT1A polymorphisms and the altered metabolism of irinotecan active metabolite 7-ethyl-10-hydroxycamptothecin (SN-38)., Mol Pharmacol
Han JY et al., 2009, Integrated pharmacogenetic prediction of irinotecan pharmacokinetics and toxicity in patients with advanced non-small cell lung cancer., Lung Cancer
Li M et al., 2018, ABC transporter polymorphisms are associated with irinotecan pharmacokinetics and neutropenia., Pharmacogenomics J
Kim KP et al., 2015, A phase I study of UGT1A1 28/6 genotype-directed dosing of irinotecan (CPT-11) in Korean patients with metastatic colorectal cancer receiving FOLFIRI., Oncology
Cecchin E et al., 2009, Predictive role of the UGT1A1, UGT1A7, and UGT1A9 genetic variants and their haplotypes on the outcome of metastatic colorectal cancer patients treated with fluorouracil, leucovorin, and irinotecan., J Clin Oncol
Ramesh et al., 2010, Irinotecan and its active metabolite, SN-38: review of bioanalytical methods and recent update from clinical pharmacology perspectives., Biomed. Chromatogr.
Stewart CF et al., 2007, UGT1A1 promoter genotype correlates with SN-38 pharmacokinetics, but not severe toxicity in patients receiving low-dose irinotecan., J Clin Oncol
Mbatchi LC et al., 2016, Effect of Single Nucleotide Polymorphisms in the Xenobiotic-sensing Receptors NR1I2 and NR1I3 on the Pharmacokinetics and Toxicity of Irinotecan in Colorectal Cancer Patients., Clin Pharmacokinet
Lankisch TO et al., 2008, Gilbert's Syndrome and irinotecan toxicity: combination with UDP-glucuronosyltransferase 1A7 variants increases risk., Cancer Epidemiol Biomarkers Prev
Jada SR et al., 2007, Role of UGT1A16, UGT1A128 and ABCG2 c.421C>A polymorphisms in irinotecan-induced neutropenia in Asian cancer patients., Cancer Sci
Lankisch TO et al., 2006, Gilbert's disease and atazanavir: from phenotype to UDP-glucuronosyltransferase haplotype., Hepatology
de Jong FA et al., 2007, Irinotecan-induced diarrhea: functional significance of the polymorphic ABCC2 transporter protein., Clin Pharmacol Ther
Kishi S et al., 2004, Effects of prednisone and genetic polymorphisms on etoposide disposition in children with acute lymphoblastic leukemia., Blood
Kawato Y et al., 1991, Intracellular roles of SN-38, a metabolite of the camptothecin derivative CPT-11, in the antitumor effect of CPT-11., Cancer Res
Obradovic M et al., 2008, Cost-effectiveness of UGT1A1 genotyping in second-line, high-dose, once every 3 weeks irinotecan monotherapy treatment of colorectal cancer., Pharmacogenomics
Danoff TM et al., 2004, A Gilbert's syndrome UGT1A1 variant confers susceptibility to tranilast-induced hyperbilirubinemia., Pharmacogenomics J
Hu ZY et al., 2010, Dose-dependent association between UGT1A1*28 genotype and irinotecan-induced neutropenia: low doses also increase risk., Clin Cancer Res
Onoue M et al., 2009, UGT1A1*6 polymorphism is most predictive of severe neutropenia induced by irinotecan in Japanese cancer patients., Int J Clin Oncol
Hoskins JM et al., 2007, UGT1A1*28 genotype and irinotecan-induced neutropenia: dose matters., J Natl Cancer Inst
Kemp DC et al., 2002, Characterization of raloxifene glucuronidation in vitro: contribution of intestinal metabolism to presystemic clearance., Drug Metab Dispos
Iyer L et al., 2002, UGT1A1*28 polymorphism as a determinant of irinotecan disposition and toxicity., Pharmacogenomics J
Sai K et al., 2004, UGT1A1 haplotypes associated with reduced glucuronidation and increased serum bilirubin in irinotecan-administered Japanese patients with cancer., Clin Pharmacol Ther
Ciotti M et al., 1999, Glucuronidation of 7-ethyl-10-hydroxycamptothecin (SN-38) by the human UDP-glucuronosyltransferases encoded at the UGT1 locus., Biochem Biophys Res Commun
de Jong FA et al., 2006, Prophylaxis of irinotecan-induced diarrhea with neomycin and potential role for UGT1A1*28 genotype screening: a double-blind, randomized, placebo-controlled study., Oncologist
Innocenti F et al., 2004, Genetic variants in the UDP-glucuronosyltransferase 1A1 gene predict the risk of severe neutropenia of irinotecan., J Clin Oncol
Guillemette C et al., 2000, Structural heterogeneity at the UDP-glucuronosyltransferase 1 locus: functional consequences of three novel missense mutations in the human UGT1A7 gene., Pharmacogenetics

7-ETHYL-10-HYDROXYCAMPTOTHECIN UGT1A1

Interaction Score: 1.46

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25427841 16636344 19364970 19852077 17577039 27116457 18349289 17627617 12181437 17058217 17185998 12969965 1651156 18466101 14647407 20562211 19390945 17728214 12019197 18221820 11990381 15179405 10381366 16951398 15007088 11037804

Sources:
PharmGKB
7-ETHYL-10-HYDROXYCAMPTOTHECIN CES2

Interaction Score: 1.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
7-ETHYL-10-HYDROXYCAMPTOTHECIN UGT1A9

Interaction Score: 0.55

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16636344 24897286 12181437 18221820

Sources:
PharmGKB
7-ETHYL-10-HYDROXYCAMPTOTHECIN TOP1

Interaction Score: 0.25

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25003995 22647222 25768699 21783369 23622981 17190463 19530720 25835359

Sources:
DTC PharmGKB TTD DrugBank
7-ETHYL-10-HYDROXYCAMPTOTHECIN UGT1A10

Interaction Score: 0.21

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
7-ETHYL-10-HYDROXYCAMPTOTHECIN UGT1A8

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
7-ETHYL-10-HYDROXYCAMPTOTHECIN UGT1A6

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
7-ETHYL-10-HYDROXYCAMPTOTHECIN UGT1A3

Interaction Score: 0.15

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
7-ETHYL-10-HYDROXYCAMPTOTHECIN UGT1A4

Interaction Score: 0.15

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
7-ETHYL-10-HYDROXYCAMPTOTHECIN HDAC11

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23622981

Sources:
DTC
7-ETHYL-10-HYDROXYCAMPTOTHECIN HDAC9

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23622981

Sources:
DTC
7-ETHYL-10-HYDROXYCAMPTOTHECIN HDAC10

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23622981

Sources:
DTC
7-ETHYL-10-HYDROXYCAMPTOTHECIN HDAC7

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23622981

Sources:
DTC
7-ETHYL-10-HYDROXYCAMPTOTHECIN HDAC5

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23622981

Sources:
DTC
7-ETHYL-10-HYDROXYCAMPTOTHECIN HDAC4

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23622981

Sources:
DTC
7-ETHYL-10-HYDROXYCAMPTOTHECIN HDAC3

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23622981

Sources:
DTC
7-ETHYL-10-HYDROXYCAMPTOTHECIN HDAC6

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23622981

Sources:
DTC
7-ETHYL-10-HYDROXYCAMPTOTHECIN CES1

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
7-ETHYL-10-HYDROXYCAMPTOTHECIN HDAC8

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23622981

Sources:
DTC
7-ETHYL-10-HYDROXYCAMPTOTHECIN HDAC2

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23622981

Sources:
DTC
7-ETHYL-10-HYDROXYCAMPTOTHECIN HDAC1

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23622981

Sources:
DTC
7-ETHYL-10-HYDROXYCAMPTOTHECIN ABCC1

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
27845419

Sources:
PharmGKB
7-ETHYL-10-HYDROXYCAMPTOTHECIN SLCO1B1

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18221820

Sources:
PharmGKB
7-ETHYL-10-HYDROXYCAMPTOTHECIN BCHE

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
7-ETHYL-10-HYDROXYCAMPTOTHECIN ABCC2

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
7-ETHYL-10-HYDROXYCAMPTOTHECIN ABCG2

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
7-ETHYL-10-HYDROXYCAMPTOTHECIN ABCB1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB

DrugBank: DB05482
- Version: 5.1.7
Alternate Names:

86639-52-3 CAS Number

NeoLipid Camptosar Drug Brand

CHEMBL837 ChEMBL ID

Drug Info:

Drug Type small molecule

Drug Groups investigational

Drug Categories alkaloids

Publications:

DTC: 7-ETHYL-10-HYDROXY-CAMPTOTHECIN

Version: 02-September-2020

Alternate Names:

CHEMBL837 ChEMBL Drug ID

Drug Info:

Publications:

Guerrant W et al., 2013, Dual-acting histone deacetylase-topoisomerase I inhibitors., Bioorg Med Chem Lett

Wang MJ et al., 2014, Design, synthesis, mechanisms of action, and toxicity of novel 20(s)-sulfonylamidine derivatives of camptothecin as potent antitumor agents., J Med Chem

Luo Y et al., 2012, Synthesis and biological evaluation of new homocamptothecin analogs., Eur J Med Chem

PharmGKB: SN-38

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Han JY et al., 2009, Integrated pharmacogenetic prediction of irinotecan pharmacokinetics and toxicity in patients with advanced non-small cell lung cancer., Lung Cancer

Kim KP et al., 2015, A phase I study of UGT1A1 28/6 genotype-directed dosing of irinotecan (CPT-11) in Korean patients with metastatic colorectal cancer receiving FOLFIRI., Oncology

Han JY et al., 2006, Comprehensive analysis of UGT1A polymorphisms predictive for pharmacokinetics and treatment outcome in patients with non-small-cell lung cancer treated with irinotecan and cisplatin., J Clin Oncol

TTD: IT-141
- Version: 2020.06.01
Alternate Names:

D0K6QU TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL837
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:

86639-52-3	CAS Number
NeoLipid Camptosar	Drug Brand
CHEMBL837	ChEMBL ID

7-ETHYL-10-HYDROXYCAMPTOTHECIN Drug Record

7-ETHYL-10-HYDROXYCAMPTOTHECIN chembl:CHEMBL837 Antineoplastic

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 25427841 16636344 19364970 19852077 17577039 27116457 18349289 17627617 12181437 17058217 17185998 12969965 1651156 18466101 14647407 20562211 19390945 17728214 12019197 18221820 11990381 15179405 10381366 16951398 15007088 11037804

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16636344 24897286 12181437 18221820

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 25003995 22647222 25768699 21783369 23622981 17190463 19530720 25835359

Sources: DTC PharmGKB TTD DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23622981

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23622981

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23622981

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23622981

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23622981

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23622981

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23622981

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23622981

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23622981

Interaction Types & Directionality:

n/a

PMIDs:
25427841 16636344 19364970 19852077 17577039 27116457 18349289 17627617 12181437 17058217 17185998 12969965 1651156 18466101 14647407 20562211 19390945 17728214 12019197 18221820 11990381 15179405 10381366 16951398 15007088 11037804

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
16636344 24897286 12181437 18221820

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
25003995 22647222 25768699 21783369 23622981 17190463 19530720 25835359

Sources:
DTC PharmGKB TTD DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
23622981

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
23622981

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
23622981

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
23622981

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
23622981

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
23622981

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
23622981

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
23622981

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
23622981

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
23622981

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
23622981

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
27845419

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
18221820

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found