General Information of Drug (ID: DMP79A1)

Drug Name
Macitentan Drug Info
Synonyms
Macitentan; 441798-33-0; Opsumit; ACT-064992; ACT 064992; UNII-Z9K9Y9WMVL; ACT064992; Z9K9Y9WMVL; N-[5-(4-Bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-propylsulfamide; N-(5-(4-Bromophenyl)-6-(2-((5-bromo-2-pyrimidinyl)oxy)ethoxy)-4-pyrimidinyl)-N'-propylsulfamide; CHEBI:76607; Actelion-1; Macitentan [USAN:INN]; macitentanum; zlchem 5; Opsumit (TN); Macitentan (JAN/USAN); (non-labelled)Macitentan-d7; MLS006011174; C19H20Br2N6O4S; SCHEMBL1445625; GTPL7352; CHEMBL2103873; ZLA0005; EX-A544; DTXSID50196063
Indication
Disease Entry ICD 11 Status REF
Cardiovascular disease BA00-BE2Z Approved [1]
Cross-matching ID
PubChem CID
16004692
ChEBI ID
CHEBI:76607
CAS Number
CAS 441798-33-0
TTD Drug ID
DMP79A1
INTEDE Drug ID
DR0998
ACDINA Drug ID
D00382

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DME
DOT
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
Bosentan DMIOGBU Pulmonary arterial hypertension BB01.0 Approved [5]
Ambrisentan DMD1QXW Pulmonary arterial hypertension BB01.0 Approved [6]
Sparsentan DMMP51W IgA nephropathy MF8Y Approved [7]
LU302146 DMMJVXZ Pulmonary hypertension BB01 Approved [8]
Atrasentan DMM74PK Diabetic nephropathy GB61.Z Phase 3 [9]
Clazosentan DMQSBX4 Cerebral vasospasm BA85.Z Phase 3 [10]
PF-1228305 DMS1EQ7 Pulmonary hypertension BB01 Phase 3 [11]
Darusentan DMN8DQH Hypotension BA20-BA21 Phase 3 [12]
BQ-123 DM0MO8I Pulmonary arterial hypertension BB01.0 Phase 2 [13]
FR139317 DMEL5SV Hypertension BA00-BA04 Phase 2 [14]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Bosentan DMIOGBU Pulmonary arterial hypertension BB01.0 Approved [5]
BQ788 DM6KRLW Acute kidney injury GB60 Phase 3 [15]
PD-145065 DMWVBTQ Hypertension BA00-BA04 Phase 2 [16]
SPI-1620 DMNPRMC Solid tumour/cancer 2A00-2F9Z Phase 2 [17]
ENB003 DMK2B3S Melanoma 2C30 Phase 1/2 [18]
J-104132 DM5E6MK Pulmonary arterial hypertension BB01.0 Discontinued in Phase 2 [19]
ENRASENTAN DM05F1Z Pulmonary arterial hypertension BB01.0 Discontinued in Phase 2 [20]
SB-209670 DMJYW80 Arrhythmia BC9Z Discontinued in Phase 2 [21]
ET-1 DMA85ND N. A. N. A. Phase 0 [22]
PD142893 DMFA27N N. A. N. A. Terminated [23]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Cytochrome P450 3A4 (CYP3A4)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [24]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [25]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [26]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [27]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [28]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [29]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [30]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [31]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [25]
Verapamil DMA7PEW Angina pectoris BA40 Approved [32]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Mephenytoin 4-hydroxylase (CYP2C19)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Amoxicillin DMUYNEI Acute otitis media AB00 Approved [33]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [34]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [35]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [36]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [37]
Verapamil DMA7PEW Angina pectoris BA40 Approved [38]
Diclofenac DMPIHLS Chronic renal failure GB61.Z Approved [39]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [40]
Quinine DMSWYF5 Malaria 1F40-1F45 Approved [41]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [42]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Paclitaxel DMLB81S Breast carcinoma Approved [43]
Methotrexate DM2TEOL Anterior urethra cancer Approved [44]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [45]
Calcipotriol DM03CP7 Psoriasis EA90 Approved [46]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [47]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [48]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [49]
Prednisone DM2HG4X Acute asthma CA23 Approved [50]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [51]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [52]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Flupentixol DM0DJ9O Schizophrenia 6A20 Approved [53]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [54]
Crizotinib DM4F29C Non-small-cell lung cancer 2C25.Y Approved [55]
Lamotrigine DM8SXYG Bipolar disorder 6A60 Approved [56]
Cepharanthine DM9Y5JB N. A. N. A. Approved [57]
Itraconazole DMCR1MV Aspergillosis 1F20 Approved [58]
Clozapine DMFC71L Schizophrenia 6A20 Approved [59]
Midostaurin DMI6E0R Acute myeloid leukaemia 2A60 Approved [60]
Trifluoperazine DMKBYWI Anxiety Approved [61]
Olanzapine DMPFN6Y Bipolar depression Approved [59]
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Drug Name Drug ID Indication ICD 11 Highest Status REF
Clavulanate DM2FGRT Bacteremia 1A73 Approved [62]
obeticholic acid DM3Q1SM Primary biliary cholangitis DB96.1 Approved [63]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [64]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [65]
Nefazodone DM4ZS8M Major depressive disorder 6A70.3 Approved [66]
Rifampicin DM5DSFZ Non-insulin dependent diabetes 5A11 Approved [67]
Cholic Acid DM7OKQV Cholelithiasis DC11 Approved [68]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [69]
Lindane DMB8CNL Infestations of lice and scabies 1G00.Z Approved [70]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [71]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Lopinavir DMITQS0 Human immunodeficiency virus infection 1C62 Approved [72]
Sulfinpyrazone DMEV954 Gout FA25 Approved [73]
Probenecid DMMFWOJ Acute gonococcal cervicitis Approved [74]
Docetaxel DMDI269 Advanced cancer 2A00-2F9Z Approved [75]
Methotrexate DM2TEOL Anterior urethra cancer Approved [76]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [77]
Cholic Acid DM7OKQV Cholelithiasis DC11 Approved [68]
Epirubicin DMPDW6T Solid tumour/cancer 2A00-2F9Z Approved [78]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [43]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [79]
⏷ 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
Endothelin A receptor (EDNRA) TTKRD0G EDNRA_HUMAN Modulator [2]
Endothelin B receptor (EDNRB) TT3ZTGU EDNRB_HUMAN Modulator [2]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) Main DME DE4LYSA CP3A4_HUMAN Substrate [3]
Mephenytoin 4-hydroxylase (CYP2C19) Main DME DEGTFWK CP2CJ_HUMAN Substrate [3]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
ATP-binding cassette sub-family C member 2 (ABCC2) OTJSIGV5 MRP2_HUMAN Gene/Protein Processing [4]
ATP-binding cassette sub-family C member 3 (ABCC3) OTC3IJV4 MRP3_HUMAN Gene/Protein Processing [4]
ATP-dependent translocase ABCB1 (ABCB1) OTEJROBO MDR1_HUMAN Gene/Protein Processing [4]
Hepatic sodium/bile acid cotransporter (SLC10A1) OTUJVMCL NTCP_HUMAN Gene/Protein Processing [4]

References

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55 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.
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66 Robustness testing and optimization of an adverse outcome pathway on cholestatic liver injury. Arch Toxicol. 2020 Apr;94(4):1151-1172. doi: 10.1007/s00204-020-02691-9. Epub 2020 Mar 10.
67 Differential regulation of sinusoidal and canalicular hepatic drug transporter expression by xenobiotics activating drug-sensing receptors in primary human hepatocytes. Drug Metab Dispos. 2006 Oct;34(10):1756-63. doi: 10.1124/dmd.106.010033. Epub 2006 Jul 12.
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70 Regulation of hepatic drug transporter activity and expression by organochlorine pesticides. J Biochem Mol Toxicol. 2014 Mar;28(3):119-28.
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75 Association of genetic polymorphisms in SLCO1B3 and ABCC2 with docetaxel-induced leukopenia. Cancer Sci. 2008 May;99(5):967-72.
76 Methotrexate normalizes up-regulated folate pathway genes in rheumatoid arthritis. Arthritis Rheum. 2013 Nov;65(11):2791-802.
77 In vitro study of transporters involved in intestinal absorption of inorganic arsenic. Chem Res Toxicol. 2012 Feb 20;25(2):446-53. doi: 10.1021/tx200491f. Epub 2012 Jan 26.
78 Co-encapsulation of chrysophsin-1 and epirubicin in PEGylated liposomes circumvents multidrug resistance in HeLa cells. Chem Biol Interact. 2015 Dec 5;242:13-23. doi: 10.1016/j.cbi.2015.08.023. Epub 2015 Sep 1.
79 Gene expression analysis of precision-cut human liver slices indicates stable expression of ADME-Tox related genes. Toxicol Appl Pharmacol. 2011 May 15;253(1):57-69.