Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DM7TZL0)

Drug Name
INCB054329 Drug Info
Synonyms
1628607-64-6; (S)-6-(3,5-dimethylisoxazol-4-yl)-3-(pyridin-2-yl)-3,4-dihydro-5-oxa-1,2a-diazaacenaphthylen-2(1H)-one; Q50825078; SCHEMBL16038298; INCB54329; US9624241, Example 14; BDBM318469; INCB-54329; EX-A3126; INCB-054329; NSC816024; s8753; NSC-816024; HY-112504; CS-0046160; INCB054329 pound INCB-054329,INCB-54329 pound(c); CC1=NOC(C)=C1C1=CC=C2C3=C1OC[C@H](C=1N=CC=CC=1)N3C(=O)N2; (4S)-7-(3,5-dimethylisoxazol-4-yl)-4-pyridin-2-yl-4,5-dihydroimidazo[1,5,4-de][1,4]benzoxazin-2(1H)-one
Indication
Disease Entry ICD 11 Status REF
Refractory hematologic malignancy 2A85.5 Phase 1/2 [1]
Solid tumour/cancer 2A00-2F9Z Phase 1/2 [1]
Cross-matching ID
PubChem CID
90410660
TTD Drug ID
DM7TZL0

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Clinical Trial Drug(s)
Approved Drug(s)
Download the Complete Related Drug List
Drug(s) Targeting Bromodomain and extraterminal domain protein (BET)
Drug Name Drug ID Indication ICD 11 Highest Status REF
CPI-0610 DMPXOYJ Myelofibrosis 2A20.2 Phase 3 [4]
ZEN-3694 DM6VQTF Prostate cancer 2C82.0 Phase 2 [5]
OTX-015 DMI8RG1 Acute myeloid leukaemia 2A60 Phase 1/2 [4]
BMS-986158 DM6LDI4 Solid tumour/cancer 2A00-2F9Z Phase 1/2 [4]
INCB057643 DMG65CV Solid tumour/cancer 2A00-2F9Z Phase 1/2 [6]
ODM-207 DMOKVJD Solid tumour/cancer 2A00-2F9Z Phase 1/2 [7]
(+)-JQ1 DM1CZSJ Testicular cancer 2C80 Phase 1 [8]
GSK525762 DMPAWBN Haematological malignancy 2B33.Y Phase 1 [4]
PLX51107 DMXLHVW Haematological malignancy 2B33.Y Phase 1 [4]
BI 894999 DM7W5N2 Solid tumour/cancer 2A00-2F9Z Phase 1 [4]
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Drug(s) Affected By Poly polymerase 1 (PARP1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [9]
Gefitinib DM15F0X Colon adenocarcinoma Approved [10]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [11]
Nitric Oxide DM1RBYG Hypertension BA00-BA04 Approved [12]
Citalopram DM2G9AE Acute coronary syndrome BA41 Approved [13]
Ciprofloxacin XR DM2NLS9 Acute gonococcal cervicitis Approved [14]
Imipramine DM2NUH3 Depression 6A70-6A7Z Approved [13]
Colchicine DM2POTE Acute gout flare FA25.0 Approved [15]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [16]
Methotrexate DM2TEOL Anterior urethra cancer Approved [17]
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Drug(s) Affected By Proliferating cell nuclear antigen (PCNA)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [9]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [18]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [19]
Selenium DM25CGV N. A. N. A. Approved [20]
Methimazole DM25FL8 Hyperthyroidism 5A02 Approved [21]
Ribavirin DMEYLH9 Hepatitis C virus infection 1E51.1 Approved [22]
Meloxicam DM2AR7L Arthritis FA20 Approved [23]
Methotrexate DM2TEOL Anterior urethra cancer Approved [24]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [25]
Epinephrine DM3KJBC Acute asthma CA23 Approved [26]
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Drug(s) Affected By Histone H2AX (H2AX)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [27]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [28]
Selenium DM25CGV N. A. N. A. Approved [29]
Ribavirin DMEYLH9 Hepatitis C virus infection 1E51.1 Approved [30]
Etretinate DM2CZFA Keratosis ED56 Approved [31]
Methotrexate DM2TEOL Anterior urethra cancer Approved [32]
Dactinomycin DM2YGNW Adult kidney Wilms tumor Approved [33]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [34]
Lapatinib DM3BH1Y Breast cancer 2C60-2C65 Approved [35]
Quercetin DM3NC4M Obesity 5B81 Approved [36]
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Drug(s) Affected By G1/S-specific cyclin-E1 (CCNE1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [9]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [37]
Ribavirin DMEYLH9 Hepatitis C virus infection 1E51.1 Approved [22]
Ciprofloxacin XR DM2NLS9 Acute gonococcal cervicitis Approved [14]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [38]
Quercetin DM3NC4M Obesity 5B81 Approved [39]
Fluoxetine DM3PD2C Bipolar depression Approved [40]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [41]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [42]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [43]
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Drug(s) Affected By Breast cancer type 1 susceptibility protein (BRCA1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [9]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [44]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [45]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [46]
Methotrexate DM2TEOL Anterior urethra cancer Approved [24]
Quercetin DM3NC4M Obesity 5B81 Approved [47]
Furazolidone DM3P6V7 Diarrhea ME05.1 Approved [48]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [49]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [50]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [51]
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Drug(s) Affected By Cyclin-dependent kinase inhibitor 1 (CDKN1A)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [52]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [53]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [54]
Gefitinib DM15F0X Colon adenocarcinoma Approved [55]
Talazoparib DM1KS78 Breast cancer 2C60-2C65 Approved [56]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [57]
Etretinate DM2CZFA Keratosis ED56 Approved [58]
Prednisone DM2HG4X Acute asthma CA23 Approved [59]
Ciprofloxacin XR DM2NLS9 Acute gonococcal cervicitis Approved [14]
Colchicine DM2POTE Acute gout flare FA25.0 Approved [60]
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Drug(s) Affected By Proliferation marker protein Ki-67 (MKI67)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Levonorgestrel DM1DP7T Atypical endometrial hyperplasia Approved [61]
Methotrexate DM2TEOL Anterior urethra cancer Approved [62]
Quercetin DM3NC4M Obesity 5B81 Approved [63]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [49]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [64]
Remdesivir DMBFZ6L Coronavirus Disease 2019 (COVID-19) 1D6Y Approved [65]
Chlorpromazine DMBGZI3 Acute intermittent hepatic porphyria 5C58.11 Approved [66]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [67]
Thalidomide DM70BU5 Adult T-cell leukemia/lymphoma Approved [68]
Marinol DM70IK5 Anorexia nervosa cachexia 6B80 Approved [69]
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Drug(s) Affected By DNA repair protein RAD51 homolog 1 (RAD51)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [70]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [71]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [72]
Dactinomycin DM2YGNW Adult kidney Wilms tumor Approved [73]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [49]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [74]
Testosterone DM7HUNW Hot flushes GA30 Approved [75]
Quizartinib DM8Y4JS Acute myeloid leukaemia 2A60 Approved [76]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [75]
Leflunomide DMR8ONJ Arthritis FA20 Approved [77]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas
Download the Complete Interaction Atlas for Visualization in Cytoscape

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Bromodomain and extraterminal domain protein (BET) TTE4BSY NOUNIPROTAC Inhibitor [2]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Breast cancer type 1 susceptibility protein (BRCA1) OT5BN6VH BRCA1_HUMAN Gene/Protein Processing [3]
Cyclin-dependent kinase inhibitor 1 (CDKN1A) OTQWHCZE CDN1A_HUMAN Gene/Protein Processing [3]
DNA repair protein RAD51 homolog 1 (RAD51) OTNVWGC1 RAD51_HUMAN Gene/Protein Processing [3]
G1/S-specific cyclin-E1 (CCNE1) OTLD7UID CCNE1_HUMAN Gene/Protein Processing [3]
Histone H2AX (H2AX) OT18UX57 H2AX_HUMAN Gene/Protein Processing [3]
Poly polymerase 1 (PARP1) OT310QSG PARP1_HUMAN Protein Interaction/Cellular Processes [3]
Proliferating cell nuclear antigen (PCNA) OTHZ1RIA PCNA_HUMAN Gene/Protein Processing [3]
Proliferation marker protein Ki-67 (MKI67) OTA8N1QI KI67_HUMAN Gene/Protein Processing [3]

References

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2 The Novel Bromodomain and Extraterminal Domain Inhibitor INCB054329 Induces Vulnerabilities in Myeloma Cells That Inform Rational Combination Strategies. Clin Cancer Res. 2019 Jan 1;25(1):300-311.
3 The BET inhibitor INCB054329 reduces homologous recombination efficiency and augments PARP inhibitor activity in ovarian cancer. Gynecol Oncol. 2018 Jun;149(3):575-584. doi: 10.1016/j.ygyno.2018.03.049. Epub 2018 Mar 20.
4 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
5 Clinical pipeline report, company report or official report of Zenith Epigenetics.
6 Development of 2 Bromodomain and Extraterminal Inhibitors With Distinct Pharmacokinetic and Pharmacodynamic Profiles for the Treatment of Advanced Malignancies. Clin Cancer Res. 2020 Mar 15;26(6):1247-1257.
7 First-in-human Phase 1 open label study of the BET inhibitor ODM-207 in patients with selected solid tumours. Br J Cancer. 2020 Dec;123(12):1730-1736.
8 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
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38 Sulindac induces specific degradation of the HPV oncoprotein E7 and causes growth arrest and apoptosis in cervical carcinoma cells. Cancer Lett. 2007 Jan 8;245(1-2):103-11. doi: 10.1016/j.canlet.2005.12.034. Epub 2006 Feb 20.
39 Comparison of phenotypic and transcriptomic effects of false-positive genotoxins, true genotoxins and non-genotoxins using HepG2 cells. Mutagenesis. 2011 Sep;26(5):593-604.
40 Fluoxetine mediates G0/G1 arrest by inducing functional inhibition of cyclin dependent kinase subunit (CKS)1. Biochem Pharmacol. 2008 May 15;75(10):1924-34. doi: 10.1016/j.bcp.2008.02.013. Epub 2008 Feb 17.
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68 Thalidomide suppresses angiogenesis and immune evasion via lncRNA FGD5-AS1/miR-454-3p/ZEB1 axis-mediated VEGFA expression and PD-1/PD-L1 checkpoint in NSCLC. Chem Biol Interact. 2021 Nov 1;349:109652. doi: 10.1016/j.cbi.2021.109652. Epub 2021 Sep 11.
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72 Propolis alleviates 4-aminobiphenyl-induced oxidative DNA damage by inhibition of CYP2E1 expression in human liver cells. Environ Toxicol. 2021 Aug;36(8):1504-1513. doi: 10.1002/tox.23147. Epub 2021 Apr 13.
73 Unpredicted Downregulation of RAD51 Suggests Genome Instability Induced by Tetrachlorobenzoquinone. Chem Res Toxicol. 2016 Dec 19;29(12):2184-2193. doi: 10.1021/acs.chemrestox.6b00369. Epub 2016 Nov 21.
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75 Effects of 1alpha,25 dihydroxyvitamin D3 and testosterone on miRNA and mRNA expression in LNCaP cells. Mol Cancer. 2011 May 18;10:58.
76 Inhibitors of class I HDACs and of FLT3 combine synergistically against leukemia cells with mutant FLT3. Arch Toxicol. 2022 Jan;96(1):177-193. doi: 10.1007/s00204-021-03174-1. Epub 2021 Oct 19.
77 Endoplasmic reticulum stress and MAPK signaling pathway activation underlie leflunomide-induced toxicity in HepG2 Cells. Toxicology. 2017 Dec 1;392:11-21.