General Information of Drug (ID: DMCVJ86)

Drug Name
Clofarabine Drug Info
Synonyms
CAFdA; CFB; Clofarabina; Clofarabinum; Clofarex; Clolar; Evoltra; Clofarabine [USAN]; Clolar (TN); Evoltra (TN); Clofarabine (USAN/INN); Clolar, Evoltra, Clofarabine; Cl-F-Ara-A; (2R,3R,4S,5R)-5-(6-amino-2-chloropurin-9-yl)-4-fluoro-2-(hydroxymethyl)oxolan-3-ol; 2-Chloro-9-(2-deoxy-2-fluoro-b-D-arabinofuranosyl)-9H-purin-6-amine; 2-Chloro-9-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl)-9H-purin-6-amine; 2-Chloro-9-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl)adenine; 2-Cl-2'-F-araA; 2-chloro-9-(2'-deoxy-2'-fluoro-beta-D-arabinofuranosyl)adenine; 3S211048
Indication
Disease Entry ICD 11 Status REF
Acute lymphoblastic leukaemia 2A85 Approved [1] , [2] , [3] , [4]
Myelodysplastic syndrome 2A37 Approved [1] , [2] , [3] , [4]
Therapeutic Class
Anticancer Agents
Cross-matching ID
PubChem CID
119182
ChEBI ID
CHEBI:681569
CAS Number
CAS 123318-82-1
TTD Drug ID
DMCVJ86
VARIDT Drug ID
DR01330
INTEDE Drug ID
DR1773

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
DME
Drug Status:
Approved Drug(s)
Discontinued Drug(s)
Clinical Trial Drug(s)
Preclinical Drug(s)
Drug(s) Metabolized By Deoxycytidine kinase (DCK)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cladribine DM3JDRP Hairy cell leukaemia 2A82.2 Approved [9]
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Solid tumour/cancer 2A00-2F9Z Approved [10]
Methotrexate DM2TEOL leukaemia 2A60-2B33 Approved [11]
Folic acid DMEMBJC Folate-deficiency anemia 3A02.Y Approved [12]
Fluorouracil DMUM7HZ Solid tumour/cancer 2A00-2F9Z Approved [13]
Cisplatin DMRHGI9 Solid tumour/cancer 2A00-2F9Z Approved [14]
Progesterone DMUY35B Premature labour JB00 Approved [15]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [16]
Estradiol DMUNTE3 Breast cancer 2C60-2C65 Approved [15]
Sulfasalazine DMICA9H Irritable bowel syndrome DD91.0 Approved [17]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [18]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Mercaptopurine DMTM2IK Acute lymphoblastic leukaemia 2A85 Approved [19]
Entecavir DM7VTQO Hepatitis B virus infection 1E51.0 Approved [20]
Ribavirin DMEYLH9 Hepatitis C virus infection 1E51.1 Approved [21]
Thioguanine DM7NKEV Acute myeloid leukaemia 2A60 Approved [19]
Drug Name Drug ID Indication ICD 11 Highest Status REF
Fluorouracil DMUM7HZ Solid tumour/cancer 2A00-2F9Z Approved [22]
Mercaptopurine DMTM2IK Acute lymphoblastic leukaemia 2A85 Approved [23]
Cytarabine DMZD5QR Acute lymphoblastic leukaemia 2A85 Approved [24]
Entecavir DM7VTQO Hepatitis B virus infection 1E51.0 Approved [20]
Ribavirin DMEYLH9 Hepatitis C virus infection 1E51.1 Approved [25]
Trifluridine DMG2YBD Virus infection 1A24-1D9Z Approved [26]
Adenosine DMM2NSK Paroxysmal supraventricular tachycardia BC81.Z Approved [27]
Tecadenoson DM9T6MS Atrial fibrillation BC81.3 Discontinued in Phase 3 [28]
⏷ Show the Full List of 8 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Mercaptopurine DMTM2IK Acute lymphoblastic leukaemia 2A85 Approved [23]
Cytarabine DMZD5QR Acute lymphoblastic leukaemia 2A85 Approved [24]
Entecavir DM7VTQO Hepatitis B virus infection 1E51.0 Approved [20]
Trifluridine DMG2YBD Virus infection 1A24-1D9Z Approved [26]
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ampicillin DMHWE7P Bacterial infection 1A00-1C4Z Approved [29]
Cefazolin DMPDYFR Bacterial infection 1A00-1C4Z Approved [30]
Ceftriaxone DMCEW64 Bacterial infection 1A00-1C4Z Approved [31]
Ticarcillin DM4ME02 Bacterial infection 1A00-1C4Z Approved [32]
Ciprofloxacin XR DM2NLS9 Bacterial infection 1A00-1C4Z Approved [33]
Meropenem DM62UHC Bacterial infection 1A00-1C4Z Approved [31]
Cefadroxil DMMC345 Bacterial infection 1A00-1C4Z Approved [34]
Cephalexin DMD5JU8 Bacterial infection 1A00-1C4Z Approved [35]
Carbenicillin DMLEDNK Infection of the upper and lower urinary tract GC08 Approved [36]
Piperacillin DMTBKF3 Bacterial infection 1A00-1C4Z Approved [37]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
CPX-POM DMK7DFM Bladder cancer 2C94 Phase 2 [38]
G-207 virus construct DM32AKH Glioma 2A00.0 Phase 1/2 [39]
COH29 DMMEFO0 Solid tumour/cancer 2A00-2F9Z Phase 1 [40]
Didox DM64CAS Solid tumour/cancer 2A00-2F9Z Discontinued in Phase 2 [41]
Trimidox DMY8GDA Solid tumour/cancer 2A00-2F9Z Preclinical [42]
Amidox DM3D0WA N. A. N. A. Terminated [43]
⏷ Show the Full List of 6 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Bacterial Penicillin binding protein (Bact PBP) TTJP4SM NOUNIPROTAC Binder [5]
Ribonucleotide reductase (RIR) TTX09M4 RIR1_HUMAN; RIR2_HUMAN; RIR2B_HUMAN Inhibitor [5]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Equilibrative nucleoside transporter 2 (SLC29A2) DTW78DQ S29A2_HUMAN Substrate [6]
Equilibrative nucleoside transporter 1 (SLC29A1) DTXD1TQ S29A1_HUMAN Substrate [6]
Concentrative Na(+)-nucleoside cotransporter 3 (SLC28A3) DT4YL5R S28A3_HUMAN Substrate [6]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [7]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Deoxycytidine kinase (DCK) Main DME DE9FGNK DCK_HUMAN Substrate [8]

References

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2 2004 approvals: the demise of the blockbuster. Nat Rev Drug Discov. 2005 Feb;4(2):93-4.
3 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
4 Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77.
5 Clofarabine: past, present, and future. Leuk Lymphoma. 2007 Oct;48(10):1922-30.
6 Cytarabine-resistant leukemia cells are moderately sensitive to clofarabine in vitro. Anticancer Res. 2014 Apr;34(4):1657-62.
7 Contribution of the drug transporter ABCG2 (breast cancer resistance protein) to resistance against anticancer nucleosides. Mol Cancer Ther. 2008 Sep;7(9):3092-102.
8 FDA label of Belinostat. The 2020 official website of the U.S. Food and Drug Administration.
9 Potential mechanisms of action related to the efficacy and safety of cladribine. Mult Scler Relat Disord. 2019 May;30:176-186.
10 Doxorubicin transport by RALBP1 and ABCG2 in lung and breast cancer. Int J Oncol. 2007 Mar;30(3):717-25.
11 Wild-type breast cancer resistance protein (BCRP/ABCG2) is a methotrexate polyglutamate transporter. Cancer Res. 2003 Sep 1;63(17):5538-43.
12 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.
13 Role of BCRP as a biomarker for predicting resistance to 5-fluorouracil in breast cancer. Cancer Chemother Pharmacol. 2009 May;63(6):1103-10.
14 Inhibiting the function of ABCB1 and ABCG2 by the EGFR tyrosine kinase inhibitor AG1478. Biochem Pharmacol. 2009 Mar 1;77(5):781-93.
15 Sterol transport by the human breast cancer resistance protein (ABCG2) expressed in Lactococcus lactis. J Biol Chem. 2003 Jun 6;278(23):20645-51.
16 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.
17 Curcumin inhibits the activity of ABCG2/BCRP1, a multidrug resistance-linked ABC drug transporter in mice. Pharm Res. 2009 Feb;26(2):480-7.
18 Imatinib mesylate (STI571) is a substrate for the breast cancer resistance protein (BCRP)/ABCG2 drug pump. Blood. 2004 Nov 1;104(9):2940-2.
19 Involvement of the concentrative nucleoside transporter 3 and equilibrative nucleoside transporter 2 in the resistance of T-lymphoblastic cell lines to thiopurines. Biochem Biophys Res Commun. 2006 Apr 28;343(1):208-15.
20 Multiple SLC and ABC Transporters Contribute to the Placental Transfer of Entecavir. Drug Metab Dispos. 2017 Mar;45(3):269-278.
21 Kinetic study of anti-viral ribavirin uptake mediated by hCNT3 and hENT1 in Xenopus laevis oocytes. Biophys Chem. 2010 Mar;147(1-2):59-65.
22 Human equilibrative nucleoside transporter 1, as a predictor of 5-fluorouracil resistance in human pancreatic cancer. Anticancer Res. 2007 Jul-Aug;27(4B):2241-9.
23 PharmGKB: A worldwide resource for pharmacogenomic information. Wiley Interdiscip Rev Syst Biol Med. 2018 Jul;10(4):e1417. (ID: PA2040)
24 FLT3 is implicated in cytarabine transport by human equilibrative nucleoside transporter 1 in pediatric acute leukemia. Oncotarget. 2016 Aug 2;7(31):49786-49799.
25 Effects of dipyridamole coadministration on the pharmacokinetics of ribavirin in healthy volunteers. Drug Metab Pharmacokinet. 2013;28(5):406-10.
26 Lonsurf, INN-trifluridine/tipiracil.
27 Nitric oxide reduces adenosine transporter ENT1 gene (SLC29A1) promoter activity in human fetal endothelium from gestational diabetes. J Cell Physiol. 2006 Aug;208(2):451-60.
28 Transport of A1 adenosine receptor agonist tecadenoson by human and mouse nucleoside transporters: evidence for blood-brain barrier transport by murine equilibrative nucleoside transporter 1 mENT1. Drug Metab Dispos. 2013 Apr;41(4):916-22.
29 Effects of amino acid alterations in penicillin-binding proteins (PBPs) 1a, 2b, and 2x on PBP affinities of penicillin, ampicillin, amoxicillin, cefditoren, cefuroxime, cefprozil, and cefaclor in 18 clinical isolates of penicillin-susceptible, -intermediate, and -resistant pneumococci. Antimicrob Agents Chemother. 2002 May;46(5):1273-80.
30 Bacteriological characteristics of Staphylococcus aureus isolates from humans and bulk milk. J Dairy Sci. 2008 Feb;91(2):564-9.
31 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
32 Activities of antibiotics against methicillin-resistant Staphylococcus aureus with particular reference to synergetic effect between ticarcillin and fosfomycin on penicillinase non-producing methicillin-resistant S. aureus. Jpn J Antibiot. 1993 Jun;46(6):421-7.
33 Emerging drugs for bacterial urinary tract infections. Expert Opin Emerg Drugs. 2005 May;10(2):275-98.
34 Penicillin-binding protein sensitive to cephalexin in sporulation of Bacillus cereus. Microbiol Res. 1997 Sep;152(3):227-32.
35 Relationship between penicillin-binding protein patterns and beta-lactamases in clinical isolates of Bacteroides fragilis with different susceptibility to beta-lactam antibiotics. J Med Microbiol. 2004 Mar;53(Pt 3):213-21.
36 Resistance of Pseudomonas aeruginosa to cefsulodin: modification of penicillin-binding protein 3 and mapping of its chromosomal gene. J Antimicrob Chemother. 1990 Apr;25(4):513-23.
37 In vitro antienterococcal activity explains associations between exposures to antimicrobial agents and risk of colonization by multiresistant enter... J Infect Dis. 2004 Dec 15;190(12):2162-6.
38 Preclinical Pharmacokinetics of Fosciclopirox, a Novel Treatment of Urothelial Cancers, in Rats and Dogs. J Pharmacol Exp Ther. 2019 Aug;370(2):148-159.
39 Anti-tumor effect of oncolytic herpes simplex virus G47delta on human nasopharyngeal carcinoma. Chin J Cancer. 2011 Dec;30(12):831-41.
40 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
41 Didox (a novel ribonucleotide reductase inhibitor) overcomes Bcl-2 mediated radiation resistance in prostate cancer cell line PC-3. Cancer Biol Ther. 2002 Sep-Oct;1(5):539-45.
42 Suppression of retrovirus-induced immunodeficiency disease (murine AIDS) by trimidox and didox: novel ribonucleotide reductase inhibitors with less bone marrow toxicity than hydroxyurea. Antiviral Res. 2002 Nov;56(2):167-81.
43 Metabolism of the new ribonucleotide reductase inhibitor amidox in the isolated perfused rat liver. Anticancer Res. 2000 Sep- Oct;20(5B):3521-6.