General Information of Drug (ID: DMW50NF)

Drug Name
LE-SN38 Drug Info
Synonyms
7-Ethyl-10-hydroxycamptothecin; 86639-52-3; SN-38; SN 38 lactone; 7-Ethyl-10-hydroxy-camptothecin; SN 38; 10-Hydroxy-7-ethylcamptothecin; 7-Ethyl-10-hydroxycamptothecine; SN38; 7-Ethyl-10-hydroxy-20(S)-camptothecin; UNII-0H43101T0J; Captothecin, 7-ethyl-10-hydroxy-; CHEBI:8988; (S)-4,11-Diethyl-4,9-dihydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione; 7-Ethyl-10-hydroxy camptothecin; NSC673596; 0H43101T0J; (+)-7-ETHYL-10-HYDROXYCAMPTOTHECIN; 113015-38-6
Indication
Disease Entry ICD 11 Status REF
Colorectal cancer 2B91.Z Phase 2 [1]
Solid tumour/cancer 2A00-2F9Z Phase 2 [2]
Cross-matching ID
PubChem CID
104842
ChEBI ID
CHEBI:8988
CAS Number
CAS 86639-52-3
TTD Drug ID
DMW50NF
VARIDT Drug ID
DR00161
INTEDE Drug ID
DR0024

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
DME
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Drug(s) Targeting DNA topoisomerase I (TOP1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Irinotecan DMP6SC2 Adenocarcinoma 2D40 Approved [12]
Topotecan DMP6G8T Central nervous system neoplasm Approved [12]
B-Lactams DMR8YD6 Bacterial infection 1A00-1C4Z Approved [13]
Belotecan hydrocholoride DM3SRJZ Small-cell lung cancer 2C25.Y Approved [14]
Topetecan DMAE6LK Small-cell lung cancer 2C25.Y Approved [15]
Karenitecin DMCRGY4 Lung cancer 2C25.0 Phase 3 [16]
Camptothecin DM6CHNJ Solid tumour/cancer 2A00-2F9Z Phase 3 [17]
Exatecan DMCA7FN Solid tumour/cancer 2A00-2F9Z Phase 3 [18]
Edotecarin DM3ZL7D Gastric adenocarcinoma 2B72 Phase 3 [19]
Rubitecan DMDWU1S Human immunodeficiency virus infection 1C62 Phase 3 [20]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [21]
Methotrexate DM2TEOL Anterior urethra cancer Approved [22]
Folic Acid DMEMBJC Colorectal carcinoma Approved [23]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [24]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [25]
Verapamil DMA7PEW Angina pectoris BA40 Approved [5]
Irinotecan DMP6SC2 Adenocarcinoma 2D40 Approved [6]
Glutathione DMAHMT9 Human immunodeficiency virus infection 1C62 Approved [26]
Phenytoin DMNOKBV Epilepsy 8A60-8A68 Approved [27]
Daunorubicin DMQUSBT Acute monocytic leukemia Approved [28]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [29]
Methotrexate DM2TEOL Anterior urethra cancer Approved [30]
Folic Acid DMEMBJC Colorectal carcinoma Approved [31]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [32]
Dinoprostone DMTYOPD Medical abortion JA00.1Z Approved [33]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [34]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [35]
Sulfasalazine DMICA9H Irritable bowel syndrome DD91.0 Approved [36]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [37]
Oxaliplatin DMQNWRD Adenocarcinoma 2D40 Approved [38]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [39]
Methotrexate DM2TEOL Anterior urethra cancer Approved [40]
Folic Acid DMEMBJC Colorectal carcinoma Approved [41]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [42]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [43]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [44]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [45]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [44]
Sulfasalazine DMICA9H Irritable bowel syndrome DD91.0 Approved [46]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [47]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Methotrexate DM2TEOL Anterior urethra cancer Approved [48]
Dinoprostone DMTYOPD Medical abortion JA00.1Z Approved [8]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [49]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [50]
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [49]
Pravastatin DM6A0X7 Adult acute monocytic leukemia Approved [51]
Mycophenolate mofetil DMPQAGE Hepatosplenic T-cell lymphoma Approved [52]
Atorvastatin DMF28YC Acute coronary syndrome BA41 Approved [53]
Cerivastatin DMXCM7H Hyperlipidaemia 5C80 Approved [54]
PITAVASTATIN CALCIUM DM1UJO0 Dyslipidemia 5C80-5C81 Approved [51]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Methotrexate DM2TEOL Anterior urethra cancer Approved [55]
Folic Acid DMEMBJC Colorectal carcinoma Approved [56]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [57]
Dinoprostone DMTYOPD Medical abortion JA00.1Z Approved [58]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [5]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [59]
Irinotecan DMP6SC2 Adenocarcinoma 2D40 Approved [60]
Mercaptopurine DMTM2IK Acute lymphoblastic leukaemia 2A85 Approved [61]
Glutathione DMAHMT9 Human immunodeficiency virus infection 1C62 Approved [62]
Ganciclovir DM1MBYQ Cytomegalovirus infection 1D82 Approved [5]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Methotrexate DM2TEOL Anterior urethra cancer Approved [63]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [49]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [64]
Diclofenac DMPIHLS Chronic renal failure GB61.Z Approved [65]
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [49]
Pravastatin DM6A0X7 Adult acute monocytic leukemia Approved [66]
Mycophenolate mofetil DMPQAGE Hepatosplenic T-cell lymphoma Approved [52]
Atorvastatin DMF28YC Acute coronary syndrome BA41 Approved [54]
Erythromycin DM4K7GQ Acne vulgaris ED80 Approved [67]
Cerivastatin DMXCM7H Hyperlipidaemia 5C80 Approved [54]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [68]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [69]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [70]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [71]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [72]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [73]
Mycophenolate mofetil DMPQAGE Hepatosplenic T-cell lymphoma Approved [74]
Metronidazole DMTIVEN Abscess Approved [75]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [76]
Ethanol DMDRQZU Chronic pain MG30 Approved [77]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [78]
Diclofenac DMPIHLS Chronic renal failure GB61.Z Approved [79]
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [80]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [81]
Mycophenolate mofetil DMPQAGE Hepatosplenic T-cell lymphoma Approved [82]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [81]
Ibuprofen DM8VCBE Dysmenorrhea GA34.3 Approved [81]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [83]
Nateglinide DMLK2QH Diabetic complication 5A2Y Approved [81]
Haloperidol DM96SE0 Delirium Approved [81]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
DNA topoisomerase I (TOP1) TTGTQHC TOP1_HUMAN Inhibitor [3]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Multidrug resistance-associated protein 2 (ABCC2) DTFI42L MRP2_HUMAN Substrate [4]
Multidrug resistance-associated protein 4 (ABCC4) DTCSGPB MRP4_HUMAN Substrate [5]
Multidrug resistance-associated protein 1 (ABCC1) DTSYQGK MRP1_HUMAN Substrate [6]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [7]
Organic anion transporting polypeptide 1B1 (SLCO1B1) DT3D8F0 SO1B1_HUMAN Substrate [8]
Organic anion transporting polypeptide 1B3 (SLCO1B3) DT9C1TS SO1B3_HUMAN Substrate [9]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
UDP-glucuronosyltransferase 1A1 (UGT1A1) DEYGVN4 UD11_HUMAN Substrate [10]
UDP-glucuronosyltransferase 1A9 (UGT1A9) DE85D2P UD19_HUMAN Substrate [11]

References

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7 Transport of 7-ethyl-10-hydroxycamptothecin (SN-38) by breast cancer resistance protein ABCG2 in human lung cancer cells. Biochem Biophys Res Commun. 2001 Nov 9;288(4):827-32.
8 Organic anion transporting polypeptide 1B1: a genetically polymorphic transporter of major importance for hepatic drug uptake. Pharmacol Rev. 2011 Mar;63(1):157-81.
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22 Transport of methotrexate (MTX) and folates by multidrug resistance protein (MRP) 3 and MRP1: effect of polyglutamylation on MTX transport. Cancer Res. 2001 Oct 1;61(19):7225-32.
23 Folate concentration dependent transport activity of the Multidrug Resistance Protein 1 (ABCC1). Biochem Pharmacol. 2004 Apr 15;67(8):1541-8.
24 Hammerhead ribozyme against gamma-glutamylcysteine synthetase sensitizes human colonic cancer cells to cisplatin by down-regulating both the glutathione synthesis and the expression of multidrug resistance proteins. Cancer Gene Ther. 2001 Oct;8(10):803-14.
25 Multidrug resistance-associated protein-1 functional activity in Calu-3 cells. J Pharmacol Exp Ther. 2001 Sep;298(3):1199-205.
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27 Evaluation of transport of common antiepileptic drugs by human multidrug resistance-associated proteins (MRP1, 2 and 5) that are overexpressed in pharmacoresistant epilepsy. Neuropharmacology. 2010 Jun;58(7):1019-32.
28 Vinblastine and sulfinpyrazone export by the multidrug resistance protein MRP2 is associated with glutathione export. Br J Cancer. 2000 Aug;83(3):375-83.
29 Involvement of the drug transporters p glycoprotein and multidrug resistance-associated protein Mrp2 in telithromycin transport. Antimicrob Agents Chemother. 2006 Jan;50(1):80-7.
30 Dose-dependent disposition of methotrexate in Abcc2 and Abcc3 gene knockout murine models. Drug Metab Dispos. 2011 Nov;39(11):2155-61.
31 Mammalian multidrug-resistance proteins (MRPs). Essays Biochem. 2011 Sep 7;50(1):179-207.
32 Enhancing chemosensitivity in oral squamous cell carcinoma by lentivirus vector-mediated RNA interference targeting EGFR and MRP2. Oncol Lett. 2016 Sep;12(3):2107-2114.
33 Multidrug resistance associated protein 2 mediates transport of prostaglandin E2. Liver Int. 2006 Apr;26(3):362-8.
34 Lentivirus-mediated RNAi silencing targeting ABCC2 increasing the sensitivity of a human nasopharyngeal carcinoma cell line against cisplatin. J Transl Med. 2008 Oct 4;6:55.
35 Effect of acetaminophen on expression and activity of rat liver multidrug resistance-associated protein 2 and P-glycoprotein. Biochem Pharmacol. 2004 Aug 15;68(4):791-8.
36 Small intestinal efflux mediated by MRP2 and BCRP shifts sulfasalazine intestinal permeability from high to low, enabling its colonic targeting. Am J Physiol Gastrointest Liver Physiol. 2009 Aug;297(2):G371-7.
37 Delineating the contribution of secretory transporters in the efflux of etoposide using Madin-Darby canine kidney (MDCK) cells overexpressing P-glycoprotein (Pgp), multidrug resistance-associated protein (MRP1), and canalicular multispecific organic anion transporter (cMOAT). Drug Metab Dispos. 2002 Apr;30(4):457-63.
38 Multidrug Resistance-Associated Protein 2 (MRP2) Mediated Transport of Oxaliplatin-Derived Platinum in Membrane Vesicles. PLoS One. 2015 Jul 1;10(7):e0130727.
39 Doxorubicin transport by RALBP1 and ABCG2 in lung and breast cancer. Int J Oncol. 2007 Mar;30(3):717-25.
40 Wild-type breast cancer resistance protein (BCRP/ABCG2) is a methotrexate polyglutamate transporter. Cancer Res. 2003 Sep 1;63(17):5538-43.
41 The effect of low pH on breast cancer resistance protein (ABCG2)-mediated transport of methotrexate, 7-hydroxymethotrexate, methotrexate diglutamate, folic acid, mitoxantrone, topotecan, and resveratrol in in vitro drug transport models. Mol Pharmacol. 2007 Jan;71(1):240-9.
42 Role of BCRP as a biomarker for predicting resistance to 5-fluorouracil in breast cancer. Cancer Chemother Pharmacol. 2009 May;63(6):1103-10.
43 Inhibiting the function of ABCB1 and ABCG2 by the EGFR tyrosine kinase inhibitor AG1478. Biochem Pharmacol. 2009 Mar 1;77(5):781-93.
44 Sterol transport by the human breast cancer resistance protein (ABCG2) expressed in Lactococcus lactis. J Biol Chem. 2003 Jun 6;278(23):20645-51.
45 The phytoestrogen genistein enhances multidrug resistance in breast cancer cell lines by translational regulation of ABC transporters. Cancer Lett. 2016 Jun 28;376(1):165-72.
46 Curcumin inhibits the activity of ABCG2/BCRP1, a multidrug resistance-linked ABC drug transporter in mice. Pharm Res. 2009 Feb;26(2):480-7.
47 Imatinib mesylate (STI571) is a substrate for the breast cancer resistance protein (BCRP)/ABCG2 drug pump. Blood. 2004 Nov 1;104(9):2940-2.
48 Preclinical Mouse Models To Study Human OATP1B1- and OATP1B3-Mediated Drug-Drug Interactions in Vivo. Mol Pharm. 2015 Dec 7;12(12):4259-69.
49 Contribution of OATP1B1 and OATP1B3 to the disposition of sorafenib and sorafenib-glucuronide. Clin Cancer Res. 2013 Mar 15;19(6):1458-66.
50 Identification of drugs and drug metabolites as substrates of multidrug resistance protein 2 (MRP2) using triple-transfected MDCK-OATP1B1-UGT1A1-MRP2 cells. Br J Pharmacol. 2012 Mar;165(6):1836-1847.
51 The effect of SLCO1B1*15 on the disposition of pravastatin and pitavastatin is substrate dependent: the contribution of transporting activity changes by SLCO1B1*15. Pharmacogenet Genomics. 2008 May;18(5):424-33.
52 Influence of SLCO1B1, 1B3, 2B1 and ABCC2 genetic polymorphisms on mycophenolic acid pharmacokinetics in Japanese renal transplant recipients. Eur J Clin Pharmacol. 2007 Dec;63(12):1161-9.
53 Rifampicin alters atorvastatin plasma concentration on the basis of SLCO1B1 521T>C polymorphism. Clin Chim Acta. 2009 Jul;405(1-2):49-52.
54 FDA Drug Development and Drug Interactions
55 Interaction of nonsteroidal anti-inflammatory drugs with multidrug resistance protein (MRP) 2/ABCC2- and MRP4/ABCC4-mediated methotrexate transport. J Pharmacol Exp Ther. 2007 Jan;320(1):229-35.
56 Analysis of methotrexate and folate transport by multidrug resistance protein 4 (ABCC4): MRP4 is a component of the methotrexate efflux system. Cancer Res. 2002 Jun 1;62(11):3144-50.
57 ATP-binding cassette C transporters in human pancreatic carcinoma cell lines. Upregulation in 5-fluorouracil-resistant cells. Pancreatology. 2009;9(1-2):136-44.
58 The human multidrug resistance protein MRP4 functions as a prostaglandin efflux transporter and is inhibited by nonsteroidal antiinflammatory drugs. Proc Natl Acad Sci U S A. 2003 Aug 5;100(16):9244-9.
59 Steroid and bile acid conjugates are substrates of human multidrug-resistance protein (MRP) 4 (ATP-binding cassette C4). Biochem J. 2003 Apr 15;371(Pt 2):361-7.
60 P-glycoprotein, but not multidrug resistance protein 4, plays a role in the systemic clearance of irinotecan and SN-38 in mice. Drug Metab Lett. 2010 Dec;4(4):195-201.
61 Polymorphisms in multidrug resistance-associated protein gene 4 is associated with outcome in childhood acute lymphoblastic leukemia. Blood. 2009 Aug 13;114(7):1383-6.
62 Role of glutathione in the multidrug resistance protein 4 (MRP4/ABCC4)-mediated efflux of cAMP and resistance to purine analogues. Biochem J. 2002 Feb 1;361(Pt 3):497-503.
63 LST-2, a human liver-specific organic anion transporter, determines methotrexate sensitivity in gastrointestinal cancers. Gastroenterology. 2001 Jun;120(7):1689-99.
64 Effect of pregnane X receptor ligands on transport mediated by human OATP1B1 and OATP1B3. Eur J Pharmacol. 2008 Apr 14;584(1):57-65.
65 Influence of non-steroidal anti-inflammatory drugs on organic anion transporting polypeptide (OATP) 1B1- and OATP1B3-mediated drug transport. Drug Metab Dispos. 2011 Jun;39(6):1047-53.
66 Relevance of conserved lysine and arginine residues in transmembrane helices for the transport activity of organic anion transporting polypeptide 1B3. Br J Pharmacol. 2010 Feb 1;159(3):698-708.
67 Impact of OATP transporters on pharmacokinetics. Br J Pharmacol. 2009 Oct;158(3):693-705.
68 Functional significance of UDP-glucuronosyltransferase variants in the metabolism of active tamoxifen metabolites. Cancer Res. 2009 Mar 1;69(5):1892-900.
69 Functional characterization of human and cynomolgus monkey UDP-glucuronosyltransferase 1A1 enzymes. Life Sci. 2010 Aug 14;87(7-8):261-8.
70 Effect of UDP-glucuronosyltransferase (UGT) 1A polymorphism (rs8330 and rs10929303) on glucuronidation status of acetaminophen. Dose Response. 2017 Sep 11;15(3):1559325817723731.
71 UDP-glucuronosyltransferase 1A1 is the principal enzyme responsible for etoposide glucuronidation in human liver and intestinal microsomes: structural characterization of phenolic and alcoholic glucuronides of etoposide and estimation of enzyme kinetics. Drug Metab Dispos. 2007 Mar;35(3):371-80.
72 Interindividual variability in pharmacokinetics of generic nucleoside reverse transcriptase inhibitors in TB/HIV-coinfected Ghanaian patients: UGT2B7*1c is associated with faster zidovudine clearance and glucuronidation. J Clin Pharmacol. 2009 Sep;49(9):1079-90.
73 Effect of aging on glucuronidation of valproic acid in human liver microsomes and the role of UDP-glucuronosyltransferase UGT1A4, UGT1A8, and UGT1A10. Drug Metab Dispos. 2009 Jan;37(1):229-36.
74 Characterization of rat intestinal microsomal UDP-glucuronosyltransferase activity toward mycophenolic acid. Drug Metab Dispos. 2006 Sep;34(9):1632-9.
75 Drug-drug interactions for UDP-glucuronosyltransferase substrates: a pharmacokinetic explanation for typically observed low exposure (AUCi/AUC) ratios. Drug Metab Dispos. 2004 Nov;32(11):1201-8.
76 Substrate-dependent modulation of UDP-glucuronosyltransferase 1A1 (UGT1A1) by propofol in recombinant human UGT1A1 and human liver microsomes. Basic Clin Pharmacol Toxicol. 2007 Sep;101(3):211-4.
77 Identification and preliminary characterization of UDP-glucuronosyltransferases catalyzing formation of ethyl glucuronide. Anal Bioanal Chem. 2014 Apr;406(9-10):2325-32.
78 Polymorphic expression of UGT1A9 is associated with variable acetaminophen glucuronidation in neonates: a population pharmacokinetic and pharmacogenetic study. Clin Pharmacokinet. 2018 Oct;57(10):1325-1336.
79 Glucuronidation of nonsteroidal anti-inflammatory drugs: identifying the enzymes responsible in human liver microsomes. Drug Metab Dispos. 2005 Jul;33(7):1027-35.
80 Pharmacokinetic interaction involving sorafenib and the calcium-channel blocker felodipine in a patient with hepatocellular carcinoma. Invest New Drugs. 2011 Dec;29(6):1511-4.
81 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
82 The evolution of population pharmacokinetic models to describe the enterohepatic recycling of mycophenolic acid in solid organ transplantation and autoimmune disease. Clin Pharmacokinet. 2011 Jan;50(1):1-24.
83 The UDP-glucuronosyltransferase 1A9 enzyme is a peroxisome proliferator-activated receptor alpha and gamma target gene. J Biol Chem. 2003 Apr 18;278(16):13975-83.