General Information of Drug (ID: DMXRU9M)

Drug Name
Valspodar Drug Info
Indication
Disease Entry ICD 11 Status REF
Acute myeloid leukaemia 2A60 Discontinued in Phase 3 [1]
Cross-matching ID
PubChem CID
5281884
ChEBI ID
CHEBI:8985
CAS Number
CAS 121584-18-7
TTD Drug ID
DMXRU9M
VARIDT Drug ID
DR00580

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Investigative Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Benzquinamide DMU4D5Y Nausea MD90 Approved [6]
Curcumin DMQPH29 Solid tumour/cancer 2A00-2F9Z Phase 3 [7]
Ortataxel DM1EK5D Solid tumour/cancer 2A00-2F9Z Phase 2 [8]
MM36 DM6VPIO Atopic dermatitis EA80 Phase 2 [7]
WK-X-34 DMX0ZBC Discovery agent N.A. Investigative [7]
KP772 DMUZSJ2 Discovery agent N.A. Investigative [7]
Chemosensitizers DMYSG9J Discovery agent N.A. Investigative [9]
⏷ Show the Full List of 7 Drug(s)
Drug(s) Targeting Coagulation factor Xa (F10)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Apixaban DM89JLN Thrombosis DB61-GB90 Approved [10]
Rivaroxaban DMQMBZ1 Deep vein thrombosis BD71 Approved [11]
DU-176b DMCIJBH Atrial fibrillation BC81.3 Approved [12]
Emicizumab DM0AQ83 Factor VIII deficiency 3B10 Approved [13]
BETRIXABAN DM2C4RF Venous thromboembolism BD72 Approved [14]
Lmw heparin DMJPD06 Coagulation defect 3B10.0 Approved [15]
Nadroparin calcium DMBNKST Coagulation defect 3B10.0 Approved [16]
Fondaparinux sodium DMWS3FH Deep vein thrombosis BD71 Approved [17]
Danaparoid DM6CLBN Deep venous clot BD71 Approved [18]
Coagulation Factor IX DM8HBJI Haemophilia B 3B11.0 Approved [19]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Transported By P-glycoprotein 1 (ABCB1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Amoxicillin DMUYNEI Acute otitis media AB00 Approved [20]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [21]
Methotrexate DM2TEOL Anterior urethra cancer Approved [4]
Folic Acid DMEMBJC Colorectal carcinoma Approved [22]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [4]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [4]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [23]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [4]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [24]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [25]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Flupentixol DM0DJ9O Schizophrenia 6A20 Approved [26]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [27]
Crizotinib DM4F29C Non-small-cell lung cancer 2C25.Y Approved [28]
Lamotrigine DM8SXYG Bipolar disorder 6A60 Approved [29]
Cepharanthine DM9Y5JB N. A. N. A. Approved [30]
Itraconazole DMCR1MV Aspergillosis 1F20 Approved [31]
Clozapine DMFC71L Schizophrenia 6A20 Approved [32]
Midostaurin DMI6E0R Acute myeloid leukaemia 2A60 Approved [33]
Trifluoperazine DMKBYWI Anxiety Approved [34]
Olanzapine DMPFN6Y Bipolar depression Approved [32]
⏷ 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
Coagulation factor Xa (F10) TTCIHJA FA10_HUMAN Inhibitor [2]
Multidrug resistance protein (MDR) TT0JLSD NOUNIPROTAC Modulator [3]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [4]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
ATP-dependent translocase ABCB1 (ABCB1) OTEJROBO MDR1_HUMAN Gene/Protein Processing [5]

References

1 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001281)
2 Non-hemostatic activity of coagulation factor Xa: potential implications for various diseases. Curr Opin Pharmacol. 2001 Apr;1(2):169-75.
3 Intracellular levels of two cyclosporin derivatives valspodar (PSC 833) and cyclosporin a closely associated with multidrug resistance-modulating activity in sublines of human colorectal adenocarcinoma HCT-15. Jpn J Cancer Res. 2001 Oct;92(10):1116-26.
4 Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade. Cancer Lett. 2016 Jan 1;370(1):153-64.
5 Selective inhibition of human cytochrome P450 3A4 by N-[2(R)-hydroxy-1(S)-indanyl]-5-[2(S)-(1, 1-dimethylethylaminocarbonyl)-4-[(furo[2, 3-b]pyridin-5-yl)methyl]piperazin-1-yl]-4(S)-hydroxy-2(R)-phenylmethy lpentanamide and P-glycoprotein by valspodar in gene transfectant systems. Drug Metab Dispos. 2000 Oct;28(10):1238-43.
6 Benzquinamide inhibits P-glycoprotein mediated drug efflux and potentiates anticancer agent cytotoxicity in multidrug resistant cells. Oncol Res. 1992;4(8-9):359-65.
7 Thiazolides: a new class of antiviral drugs. Expert Opin Drug Metab Toxicol. 2009 Jun;5(6):667-74.
8 Clinical pipeline report, company report or official report of Spectrum Phamaceuticals (2009).
9 P-glycoprotein as a drug target in the treatment of multidrug resistant cancer. Curr Drug Targets. 2000 Jul;1(1):85-99.
10 Pfizer. Product Development Pipeline. March 31 2009.
11 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
12 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. (Target id: 2359).
13 2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85.
14 Company report (Portola)
15 Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77.
16 Serum zinc concentrations: contamination from laboratory equipment. JPEN J Parenter Enteral Nutr. 1979 May-Jun;3(3):179-81.
17 Biochemistry and clinical pharmacology of new anticoagulant agents. Pathophysiol Haemost Thromb. 2002 Sep-Dec;32(5-6):218-24.
18 Effect of factor X inhibition on coagulation activation and cytokine induction in human systemic inflammation. J Infect Dis. 2002 Nov 1;186(9):1270-6.
19 Haemophilia B: Christmas disease. Expert Opin Pharmacother. 2005 Aug;6(9):1517-24.
20 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
21 MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
22 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
23 Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
24 Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
25 Association of genetic polymorphisms in the influx transporter SLCO1B3 and the efflux transporter ABCB1 with imatinib pharmacokinetics in patients with chronic myeloid leukemia. Ther Drug Monit. 2011 Apr;33(2):244-50.
26 Characteristics of P388/VMDRC.04, a simple, sensitive model for studying P-glycoprotein antagonists. Cancer Res. 1994 Feb 1;54(3):730-7.
27 Michaelis-Menten kinetic analysis of drugs of abuse to estimate their affinity to human P-glycoprotein. Toxicol Lett. 2013 Feb 27;217(2):137-42. doi: 10.1016/j.toxlet.2012.12.012. Epub 2012 Dec 27.
28 Editor's Highlight: PlacentalDisposition and Effects of Crizotinib: An Ex Vivo Study in the Isolated Dual-Side Perfused Human Cotyledon. Toxicol Sci. 2017 Jun 1;157(2):500-509. doi: 10.1093/toxsci/kfx063.
29 Functional evaluation of polymorphisms in the human ABCB1 gene and the impact on clinical responses of antiepileptic drugs. Pharmacogenet Genomics. 2008 May;18(5):390-402. doi: 10.1097/FPC.0b013e3282f85e36.
30 Cepharanthine potently enhances the sensitivity of anticancer agents in K562 cells. Cancer Sci. 2005 Jun;96(6):372-6. doi: 10.1111/j.1349-7006.2005.00057.x.
31 Clinical pharmacokinetic monitoring of itraconazole is warranted in only a subset of patients. Ther Drug Monit. 2005 Jun;27(3):322-33. doi: 10.1097/01.ftd.0000150135.22645.ea.
32 Evaluation of antipsychotic drugs as inhibitors of multidrug resistance transporter P-glycoprotein. Psychopharmacology (Berl). 2006 Sep;187(4):415-23. doi: 10.1007/s00213-006-0437-9. Epub 2006 Jun 30.
33 Actions of the selective protein kinase C inhibitor PKC412 on B-chronic lymphocytic leukemia cells in vitro. Haematologica. 2002 Feb;87(2):167-76.
34 Characterization of the ATPase activity of the Mr 170,000 to 180,000 membrane glycoprotein (P-glycoprotein) associated with multidrug resistance in K562/ADM cells. Cancer Res. 1988 Sep 1;48(17):4926-32.