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]
Acute myelogenous leukaemia 2A41 Approved [2]
Langerhans cell histiocytosis Approved [2]
Leukemia Approved [2]
Myelodysplastic syndrome 2A37 Approved [1]
Plasma cell myeloma 2A83.1 Approved [2]
Classic Hodgkin lymphoma Investigative [2]
Therapeutic Class
Anticancer Agents
Cross-matching ID
PubChem CID
119182
ChEBI ID
CHEMBL1750
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)
Clinical Trial Drug(s)
Discontinued Drug(s)
Preclinical Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ampicillin DMHWE7P Acute epiglottitis Approved [7]
Cefazolin DMPDYFR Bacteremia 1A73 Approved [8]
Ceftriaxone DMCEW64 Acute gonococcal cervicitis Approved [9]
Ticarcillin DM4ME02 Aspiration pneumonia Approved [10]
Ciprofloxacin XR DM2NLS9 Acute gonococcal cervicitis Approved [11]
Meropenem DM62UHC Bacterial infection 1A00-1C4Z Approved [9]
Cefadroxil DMMC345 Bacterial infection 1A00-1C4Z Approved [12]
Cephalexin DMD5JU8 Acute otitis media AB00 Approved [13]
Carbenicillin DMLEDNK Infection of the upper and lower urinary tract GC08 Approved [14]
Piperacillin DMTBKF3 Acute gonococcal cervicitis Approved [15]
⏷ 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 [16]
G-207 virus construct DM32AKH Glioma 2A00.0 Phase 1/2 [17]
COH29 DMMEFO0 Solid tumour/cancer 2A00-2F9Z Phase 1 [18]
Didox DM64CAS Solid tumour/cancer 2A00-2F9Z Discontinued in Phase 2 [19]
Trimidox DMY8GDA Solid tumour/cancer 2A00-2F9Z Preclinical [20]
Amidox DM3D0WA N. A. N. A. Terminated [21]
⏷ Show the Full List of 6 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [22]
Methotrexate DM2TEOL Anterior urethra cancer Approved [23]
Folic Acid DMEMBJC Colorectal carcinoma Approved [24]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [25]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [26]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [27]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [28]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [27]
Sulfasalazine DMICA9H Irritable bowel syndrome DD91.0 Approved [29]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [30]
⏷ 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 [31]
Entecavir DM7VTQO Hepatitis B virus infection 1E51.0 Approved [32]
Ribavirin DMEYLH9 Hepatitis C virus infection 1E51.1 Approved [33]
Thioguanine DM7NKEV Acute lymphocytic leukaemia 2B33.3 Approved [31]
Drug Name Drug ID Indication ICD 11 Highest Status REF
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [34]
Mercaptopurine DMTM2IK Acute lymphoblastic leukaemia 2A85 Approved [35]
Cytarabine DMZD5QR Acute lymphoblastic leukaemia 2A85 Approved [36]
Entecavir DM7VTQO Hepatitis B virus infection 1E51.0 Approved [32]
Ribavirin DMEYLH9 Hepatitis C virus infection 1E51.1 Approved [37]
Trifluridine DMG2YBD Herpetic keratitis 1F00.10 Approved [38]
Adenosine DMM2NSK Paroxysmal supraventricular tachycardia BC81.Z Approved [39]
Tecadenoson DM9T6MS Atrial fibrillation BC81.3 Discontinued in Phase 3 [40]
⏷ 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 [35]
Cytarabine DMZD5QR Acute lymphoblastic leukaemia 2A85 Approved [36]
Entecavir DM7VTQO Hepatitis B virus infection 1E51.0 Approved [32]
Trifluridine DMG2YBD Herpetic keratitis 1F00.10 Approved [38]
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 [41]

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 [3]
Ribonucleotide reductase (RIR) TTX09M4 RIR1_HUMAN; RIR2_HUMAN; RIR2B_HUMAN Inhibitor [3]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Equilibrative nucleoside transporter 2 (SLC29A2) DTW78DQ S29A2_HUMAN Substrate [4]
Equilibrative nucleoside transporter 1 (SLC29A1) DTXD1TQ S29A1_HUMAN Substrate [4]
Concentrative Na(+)-nucleoside cotransporter 3 (SLC28A3) DT4YL5R S28A3_HUMAN Substrate [4]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [5]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Deoxycytidine kinase (DCK) Main DME DE9FGNK DCK_HUMAN Substrate [6]

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6802).
2 Clofarabine FDA Label
3 Clofarabine: past, present, and future. Leuk Lymphoma. 2007 Oct;48(10):1922-30.
4 Cytarabine-resistant leukemia cells are moderately sensitive to clofarabine in vitro. Anticancer Res. 2014 Apr;34(4):1657-62.
5 Contribution of the drug transporter ABCG2 (breast cancer resistance protein) to resistance against anticancer nucleosides. Mol Cancer Ther. 2008 Sep;7(9):3092-102.
6 FDA label of Belinostat. The 2020 official website of the U.S. Food and Drug Administration.
7 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.
8 Bacteriological characteristics of Staphylococcus aureus isolates from humans and bulk milk. J Dairy Sci. 2008 Feb;91(2):564-9.
9 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
10 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.
11 Emerging drugs for bacterial urinary tract infections. Expert Opin Emerg Drugs. 2005 May;10(2):275-98.
12 Penicillin-binding protein sensitive to cephalexin in sporulation of Bacillus cereus. Microbiol Res. 1997 Sep;152(3):227-32.
13 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.
14 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.
15 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.
16 Preclinical Pharmacokinetics of Fosciclopirox, a Novel Treatment of Urothelial Cancers, in Rats and Dogs. J Pharmacol Exp Ther. 2019 Aug;370(2):148-159.
17 Anti-tumor effect of oncolytic herpes simplex virus G47delta on human nasopharyngeal carcinoma. Chin J Cancer. 2011 Dec;30(12):831-41.
18 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
19 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.
20 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.
21 Metabolism of the new ribonucleotide reductase inhibitor amidox in the isolated perfused rat liver. Anticancer Res. 2000 Sep- Oct;20(5B):3521-6.
22 Doxorubicin transport by RALBP1 and ABCG2 in lung and breast cancer. Int J Oncol. 2007 Mar;30(3):717-25.
23 Wild-type breast cancer resistance protein (BCRP/ABCG2) is a methotrexate polyglutamate transporter. Cancer Res. 2003 Sep 1;63(17):5538-43.
24 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.
25 Role of BCRP as a biomarker for predicting resistance to 5-fluorouracil in breast cancer. Cancer Chemother Pharmacol. 2009 May;63(6):1103-10.
26 Inhibiting the function of ABCB1 and ABCG2 by the EGFR tyrosine kinase inhibitor AG1478. Biochem Pharmacol. 2009 Mar 1;77(5):781-93.
27 Sterol transport by the human breast cancer resistance protein (ABCG2) expressed in Lactococcus lactis. J Biol Chem. 2003 Jun 6;278(23):20645-51.
28 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.
29 Curcumin inhibits the activity of ABCG2/BCRP1, a multidrug resistance-linked ABC drug transporter in mice. Pharm Res. 2009 Feb;26(2):480-7.
30 Imatinib mesylate (STI571) is a substrate for the breast cancer resistance protein (BCRP)/ABCG2 drug pump. Blood. 2004 Nov 1;104(9):2940-2.
31 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.
32 Multiple SLC and ABC Transporters Contribute to the Placental Transfer of Entecavir. Drug Metab Dispos. 2017 Mar;45(3):269-278.
33 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.
34 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.
35 PharmGKB: A worldwide resource for pharmacogenomic information. Wiley Interdiscip Rev Syst Biol Med. 2018 Jul;10(4):e1417. (ID: PA2040)
36 FLT3 is implicated in cytarabine transport by human equilibrative nucleoside transporter 1 in pediatric acute leukemia. Oncotarget. 2016 Aug 2;7(31):49786-49799.
37 Effects of dipyridamole coadministration on the pharmacokinetics of ribavirin in healthy volunteers. Drug Metab Pharmacokinet. 2013;28(5):406-10.
38 Lonsurf, INN-trifluridine/tipiracil.
39 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.
40 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.
41 Potential mechanisms of action related to the efficacy and safety of cladribine. Mult Scler Relat Disord. 2019 May;30:176-186.