General Information of Drug (ID: DMURVE8)

Drug Name
Elacridar Drug Info
Synonyms
Elacridar hydrochloride; 143851-98-3; Elacridar HCl; Elacridar (hydrochloride); gf 120918a; UNII-NX2BHH1A5B; NX2BHH1A5B; Elacridar hydrochloride [USAN]; GF-120918A; Elacridar hydrochloride (USAN); GF 120918; AC1Q3EOG; AC1L55DX; C34H34ClN3O5; SCHEMBL15847793; CHEMBL2074730; AOB5938; MolPort-023-332-877; BCP14056; 7066AA; AKOS016005297; CS-1113; ACN-041487; 4CA-0489; HY-50880; AC-30266; FT-0696337; W-5457; D03968; N-[4-[2-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]-9,10-dihydro-5-methoxy-9-oxo-4-acridinecarboxamide hydro
Indication
Disease Entry ICD 11 Status REF
Solid tumour/cancer 2A00-2F9Z Discontinued in Phase 1 [1]
Cross-matching ID
PubChem CID
119373
CAS Number
CAS 143664-11-3
TTD Drug ID
DMURVE8
VARIDT Drug ID
DR00573

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Clinical Trial Drug(s)
Discontinued Drug(s)
Investigative Drug(s)
Approved Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
EDP-322 DMWTVM1 Bacterial infection 1A00-1C4Z Phase 1 [6]
W-198 DMJ2R69 Solid tumour/cancer 2A00-2F9Z Phase 1 [7]
LY335979 DM2KITF Acute myeloid leukaemia 2A60 Discontinued in Phase 3 [8]
CBT-1 DM097UP Non-small-cell lung cancer 2C25.Y Discontinued in Phase 3 [9]
Biricodar DM65JCM Ovarian cancer 2C73 Discontinued in Phase 2 [10]
Tariquidar DMJG7VP Adrenocortical carcinoma 2D11.Z Discontinued in Phase 2 [11]
ONT-093 DMB8T5U Solid tumour/cancer 2A00-2F9Z Discontinued in Phase 1 [12]
TRISMETHOXYRESVERATROL DM6USPC Discovery agent N.A. Investigative [13]
[1,1':2',1'']-terphenyl-4,3'',5''-triol DMVOY4D Discovery agent N.A. Investigative [13]
XR-9456 DMTUFI1 Discovery agent N.A. Investigative [14]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Flupentixol DM0DJ9O Schizophrenia 6A20 Approved [15]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [16]
Crizotinib DM4F29C Non-small-cell lung cancer 2C25.Y Approved [17]
Lamotrigine DM8SXYG Bipolar disorder 6A60 Approved [18]
Cepharanthine DM9Y5JB N. A. N. A. Approved [19]
Itraconazole DMCR1MV Aspergillosis 1F20 Approved [20]
Clozapine DMFC71L Schizophrenia 6A20 Approved [21]
Midostaurin DMI6E0R Acute myeloid leukaemia 2A60 Approved [22]
Trifluoperazine DMKBYWI Anxiety Approved [23]
Olanzapine DMPFN6Y Bipolar depression Approved [21]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Testosterone DM7HUNW Hot flushes GA30 Approved [24]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [24]
Gefitinib DM15F0X Colon adenocarcinoma Approved [25]
Sunitinib DMCBJSR Acute undifferentiated leukemia Approved [26]
Rosuvastatin DMMIQ7G Arteriosclerosis BD40 Approved [27]
Ciprofloxacin XR DM2NLS9 Acute gonococcal cervicitis Approved [28]
Methotrexate DM2TEOL Anterior urethra cancer Approved [29]
Quercetin DM3NC4M Obesity 5B81 Approved [30]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [31]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [32]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Bile salt export pump (ABCB11)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Glimepiride DM5FSJA Diabetic complication 5A2Y Approved [33]
Ezetimibe DM7A8TW Atherosclerosis BD40 Approved [4]
Glipizide DMZA5PQ Diabetic complication 5A2Y Approved [4]
Bosentan DMIOGBU Pulmonary arterial hypertension BB01.0 Approved [34]
Indinavir DM0T3YH Human immunodeficiency virus infection 1C62 Approved [33]
Ofloxacin DM0VQN3 Acute gonococcal cervicitis Approved [4]
Primidone DM0WX6I Epilepsy 8A60-8A68 Approved [35]
Gefitinib DM15F0X Colon adenocarcinoma Approved [33]
Drospirenone DM1A9W3 Acne vulgaris ED80 Approved [36]
Nitrendipine DM21C09 Hypertension BA00-BA04 Approved [33]
⏷ 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
Multidrug resistance protein 1 (ABCB1) TT3OT40 MDR1_HUMAN Inhibitor [2]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
ATP-dependent translocase ABCB1 (ABCB1) OTEJROBO MDR1_HUMAN Gene/Protein Processing [3]
Bile salt export pump (ABCB11) OTRU7THO ABCBB_HUMAN Gene/Protein Processing [4]
Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2) OTW8V2V1 ABCG2_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 800002537)
2 2-[(3-Methoxyphenylethyl)phenoxy]-based ABCB1 inhibitors: effect of different basic side-chains on their biological properties. J Med Chem. 2008 Dec 11;51(23):7602-13.
3 Human organic anion-transporting polypeptide OATP-A (SLC21A3) acts in concert with P-glycoprotein and multidrug resistance protein 2 in the vectorial transport of Saquinavir in Hep G2 cells. Mol Pharm. 2004 Jan 12;1(1):49-56.
4 Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11). Toxicol Sci. 2013 Dec;136(2):328-43.
5 Flavonoid structure-activity studies identify 6-prenylchrysin and tectochrysin as potent and specific inhibitors of breast cancer resistance protein ABCG2. Cancer Res. 2005 Jun 1;65(11):4852-60.
6 In vitro activities of the novel bicyclolides modithromycin (EDP-420, EP-013420, S-013420) and EDP-322 against MDR clinical Neisseria gonorrhoeae isolates and international reference strains. J Antimicrob Chemother. 2015 Jan;70(1):173-7.
7 Mechanisms of tetrandrine and 5-bromotetrandrine in reversing multidrug resistance may relate to down-regulation of multidrug resistance associated protein 7 expression. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2012 Jun;20(3):558-63.
8 A Phase I trial of a potent P-glycoprotein inhibitor, zosuquidar trihydrochloride (LY335979), administered intravenously in combination with doxoru... Clin Cancer Res. 2004 May 15;10(10):3265-72.
9 A pharmacodynamic study of the P-glycoprotein antagonist CBT-1 in combination with paclitaxel in solid tumors. Oncologist.2012;17(4):512.
10 ClinicalTrials.gov (NCT00003847) VX-710, Doxorubicin, and Vincristine for the Treatment of Patients With Recurrent Small Cell Lung Cancer. U.S. National Institutes of Health.
11 Inhibition of P-glycoprotein (ABCB1)- and multidrug resistance-associated protein 1 (ABCC1)-mediated transport by the orally administered inhibitor, CBT-1((R)).Biochem Pharmacol.2008 Mar 15;75(6):1302-12.
12 A phase I pharmacokinetic study of the P-glycoprotein inhibitor, ONT-093, in combination with paclitaxel in patients with advanced cancer. Invest New Drugs. 2005 Aug;23(4):311-5.
13 Identification of a terphenyl derivative that blocks the cell cycle in the G0-G1 phase and induces differentiation in leukemia cells. J Med Chem. 2006 May 18;49(10):3012-8.
14 Functional assay and structure-activity relationships of new third-generation P-glycoprotein inhibitors. Bioorg Med Chem. 2008 Mar 1;16(5):2448-62.
15 Characteristics of P388/VMDRC.04, a simple, sensitive model for studying P-glycoprotein antagonists. Cancer Res. 1994 Feb 1;54(3):730-7.
16 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.
17 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.
18 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.
19 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.
20 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.
21 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.
22 Actions of the selective protein kinase C inhibitor PKC412 on B-chronic lymphocytic leukemia cells in vitro. Haematologica. 2002 Feb;87(2):167-76.
23 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.
24 Localization of breast cancer resistance protein (Bcrp) in endocrine organs and inhibition of its transport activity by steroid hormones. Cell Tissue Res. 2012 Aug;349(2):551-63. doi: 10.1007/s00441-012-1417-5. Epub 2012 May 13.
25 Pharmacogenetics of ABCG2 and adverse reactions to gefitinib. J Natl Cancer Inst. 2006 Dec 6;98(23):1739-42.
26 ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
27 ABCG2 polymorphism is associated with the low-density lipoprotein cholesterol response to rosuvastatin. Clin Pharmacol Ther. 2010 May;87(5):558-62.
28 Ciprofloxacin mediates cancer stem cell phenotypes in lung cancer cells through caveolin-1-dependent mechanism. Chem Biol Interact. 2016 Apr 25;250:1-11.
29 Proteomic identification of differentially expressed proteins associated with the multiple drug resistance in methotrexate-resistant human breast cancer cells. Int J Oncol. 2014 Jul;45(1):448-58.
30 Activation of beta-catenin signalling by GSK-3 inhibition increases p-glycoprotein expression in brain endothelial cells. J Neurochem. 2008 Aug;106(4):1855-65. doi: 10.1111/j.1471-4159.2008.05537.x. Epub 2008 Jul 4.
31 Differential gene expression in human hepatocyte cell lines exposed to the antiretroviral agent zidovudine. Arch Toxicol. 2014 Mar;88(3):609-23. doi: 10.1007/s00204-013-1169-3. Epub 2013 Nov 30.
32 Chronic imatinib mesylate exposure leads to reduced intracellular drug accumulation by induction of the ABCG2 (BCRP) and ABCB1 (MDR1) drug transport pumps. Cancer Biol Ther. 2005 Jul;4(7):747-52.
33 Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development. Toxicol Sci. 2010 Dec; 118(2):485-500.
34 Omics-based responses induced by bosentan in human hepatoma HepaRG cell cultures. Arch Toxicol. 2018 Jun;92(6):1939-1952.
35 Evaluating the Role of Multidrug Resistance Protein 3 (MDR3) Inhibition in Predicting Drug-Induced Liver Injury Using 125 Pharmaceuticals. Chem Res Toxicol. 2017 May 15;30(5):1219-1229. doi: 10.1021/acs.chemrestox.7b00048. Epub 2017 May 4.
36 A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. Toxicol Sci. 2013 Nov;136(1):216-41.