General Information of Drug (ID: DMNE56X)

Drug Name
ABT-263 Drug Info
Synonyms
Navitoclax; ABT 263; S1001_Selleck; ABT263, Navitoclax; 4-(4-{[2-(4-chlorophenyl)-5,5-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-({(1R)-3-morpholin-4-yl-1-[(phenylsulfanyl)methyl]propyl}amino)-3-[(trifluoromethyl)sulfonyl]phenyl}sulfonyl)benzamide
Indication
Disease Entry ICD 11 Status REF
Myelofibrosis 2A20.2 Phase 3 [1]
Relapsed or refractory chronic lymphocytic leukaemia 2A82.0 Phase 2 [2]
Solid tumour/cancer 2A00-2F9Z Discontinued in Phase 2 [3]
Cross-matching ID
PubChem CID
24978538
ChEBI ID
CHEBI:94128
CAS Number
CAS 923564-51-6
TTD Drug ID
DMNE56X
VARIDT Drug ID
DR01365
INTEDE Drug ID
DR1839

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
DME
DOT
Drug Status:
Patented Agent(s)
Clinical Trial Drug(s)
Investigative Drug(s)
Approved Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
PMID27744724-Compound-18 DM73S2C N. A. N. A. Patented [10]
Drug Name Drug ID Indication ICD 11 Highest Status REF
Briciclib DMK7BND Solid tumour/cancer 2A00-2F9Z Phase 1 [11]
4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol DMSKJ1X Discovery agent N.A. Investigative [12]
3,4-di-(4-methoxyphenyl)-1H-pyrrole-2,5-dione DMDO175 Discovery agent N.A. Investigative [13]
3,4-diphenyl-1H-pyrrole-2,5-dione DMPK6YT Discovery agent N.A. Investigative [13]
3-(4-methoxyphenyl)-4-phenyl-1H-pyrrole-2,5-dione DMGC7RY Discovery agent N.A. Investigative [13]
3-(indole-3-yl)-4-phenyl-1H-pyrrole-2,5-dione DM3EV9N Discovery agent N.A. Investigative [13]
7-hydroxycoumarin DMTMNO7 Discovery agent N.A. Investigative [14]
⏷ Show the Full List of 7 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
MCI-186 DM8ZHP1 Amyotrophic lateral sclerosis 8B60.0 Approved [15]
Taxol DMUOT9V Breast cancer 2C60-2C65 Approved [16]
GDC-0199 DMH0QKA Chronic lymphocytic leukaemia 2A82.0 Approved [17]
Taxol/Paraplatin/Herceptin DML6GAN Breast cancer 2C60-2C65 Phase 3 [18]
Oblimersen DM7KI4E Melanoma 2C30 Phase 3 [19]
RG7601 DMDVAFP Chronic lymphocytic leukaemia 2A82.0 Phase 3 [17]
Thymoquinone DMVDTR2 Polycystic ovarian syndrome 5A80.1 Phase 2/3 [20]
Obatoclax DMPF9ZM Solid tumour/cancer 2A00-2F9Z Phase 2 [21]
PI-88/Taxotere DM4FIWC Solid tumour/cancer 2A00-2F9Z Phase 2 [22]
Gossypol DMJWE3I Prostate cancer 2C82.0 Phase 2 [23]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Obatoclax DMPF9ZM Solid tumour/cancer 2A00-2F9Z Phase 2 [21]
APG-1252 DM8O3R9 Small-cell lung cancer 2C25.Y Phase 1/2 [24]
AZD0466 DMWLZI6 Hematologic tumour 2B33.Y Phase 1/2 [25]
PMID27744724-Compound-18 DM73S2C N. A. N. A. Patented [10]
Indole-based analog 2 DM0NEVC N. A. N. A. Patented [10]
PMID27744724-Compound-10 DMFKS2P N. A. N. A. Patented [10]
PMID27744724-Compound-21 DM18UA5 N. A. N. A. Patented [10]
Indole-based analog 3 DMTEYQJ N. A. N. A. Patented [10]
PMID27744724-Compound-26 DM8GOH3 N. A. N. A. Patented [10]
PMID27744724-Compound-27 DMV6MLC N. A. N. A. Patented [10]
⏷ 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 [26]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [27]
Methotrexate DM2TEOL Anterior urethra cancer Approved [28]
Folic Acid DMEMBJC Colorectal carcinoma Approved [29]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [28]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [28]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [30]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [28]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [31]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [32]
⏷ 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 [33]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [34]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [35]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [36]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [37]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [38]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [39]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [40]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [34]
Verapamil DMA7PEW Angina pectoris BA40 Approved [41]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [42]
Gefitinib DM15F0X Colon adenocarcinoma Approved [43]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [44]
Nitric Oxide DM1RBYG Hypertension BA00-BA04 Approved [45]
Etretinate DM2CZFA Keratosis ED56 Approved [46]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [47]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [48]
Lapatinib DM3BH1Y Breast cancer 2C60-2C65 Approved [49]
Quercetin DM3NC4M Obesity 5B81 Approved [50]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [51]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Gelsolin (GSN)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [52]
Selenium DM25CGV N. A. N. A. Approved [53]
Methotrexate DM2TEOL Anterior urethra cancer Approved [54]
Quercetin DM3NC4M Obesity 5B81 Approved [55]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [56]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [57]
Testosterone DM7HUNW Hot flushes GA30 Approved [58]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [58]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [59]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [60]
⏷ Show the Full List of 10 Drug(s)
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 [61]
Gefitinib DM15F0X Colon adenocarcinoma Approved [62]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [63]
Nitric Oxide DM1RBYG Hypertension BA00-BA04 Approved [45]
Citalopram DM2G9AE Acute coronary syndrome BA41 Approved [64]
Ciprofloxacin XR DM2NLS9 Acute gonococcal cervicitis Approved [65]
Imipramine DM2NUH3 Depression 6A70-6A7Z Approved [64]
Colchicine DM2POTE Acute gout flare FA25.0 Approved [66]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [67]
Methotrexate DM2TEOL Anterior urethra cancer Approved [68]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Caspase-3 (CASP3)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Sevoflurane DMC9O43 Anaesthesia 9A78.6 Approved [69]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [70]
Lovastatin DM9OZWQ Arteriosclerosis BD40 Approved [71]
Cidofovir DMA13GD Cytomegalovirus infection 1D82 Approved [72]
Docetaxel DMDI269 Advanced cancer 2A00-2F9Z Approved [73]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [74]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [75]
Mannitol DMSCDY9 Bronchiectasis CA24 Approved [76]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [77]
Aprepitant DM053KT Depression 6A70-6A7Z Approved [78]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Caspase-9 (CASP9)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Lovastatin DM9OZWQ Arteriosclerosis BD40 Approved [79]
Mannitol DMSCDY9 Bronchiectasis CA24 Approved [80]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [61]
Mechlorethamine DM0CVXA Chronic myelogenous leukaemia 2A20.0 Approved [81]
Leuprorelin acetate DM15HAT Prostate cancer 2C82.0 Approved [82]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [83]
Nitric Oxide DM1RBYG Hypertension BA00-BA04 Approved [45]
Meloxicam DM2AR7L Arthritis FA20 Approved [84]
Ciprofloxacin XR DM2NLS9 Acute gonococcal cervicitis Approved [85]
Colchicine DM2POTE Acute gout flare FA25.0 Approved [86]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Nicotine DMWX5CO Lung cancer 2C25.0 Approved [87]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [88]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [89]
Gefitinib DM15F0X Colon adenocarcinoma Approved [90]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [91]
Ribavirin DMEYLH9 Hepatitis C virus infection 1E51.1 Approved [92]
Colchicine DM2POTE Acute gout flare FA25.0 Approved [93]
Quercetin DM3NC4M Obesity 5B81 Approved [94]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [95]
Hydroquinone DM6AVR4 Melasma ED60.1 Approved [96]
⏷ 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
Apoptosis regulator Bcl-2 (BCL-2) TTJGNVC BCL2_HUMAN Inhibitor [4]
Apoptosis regulator Bcl-W (BCL-W) TTQ79W8 B2CL2_HUMAN Inhibitor [4]
Apoptosis regulator Bcl-xL (BCL-xL) TTU1E82 B2CL1_HUMAN Inhibitor [4]
G1/S-specific cyclin-D1 (CCND1) TTFCJ7S CCND1_HUMAN Inhibitor [5]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [6]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) Main DME DE4LYSA CP3A4_HUMAN Substrate [7]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Baculoviral IAP repeat-containing protein 5 (BIRC5) OTILXZYL BIRC5_HUMAN Gene/Protein Processing [8]
Caspase-3 (CASP3) OTIJRBE7 CASP3_HUMAN Protein Interaction/Cellular Processes [9]
Caspase-9 (CASP9) OTD4RFFG CASP9_HUMAN Protein Interaction/Cellular Processes [9]
Gelsolin (GSN) OT4KS2UU GELS_HUMAN Protein Interaction/Cellular Processes [9]
Poly polymerase 1 (PARP1) OT310QSG PARP1_HUMAN Protein Interaction/Cellular Processes [8]
Serine/threonine-protein kinase mTOR (MTOR) OTHH8KU7 MTOR_HUMAN Drug Response [8]

References

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5 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
6 The B-cell lymphoma 2 (BCL2)-inhibitors, ABT-737 and ABT-263, are substrates for P-glycoprotein. Biochem Biophys Res Commun. 2011 May 6;408(2):344-9.
7 Effect of rifampin on the pharmacokinetics, safety and tolerability of navitoclax (ABT-263), a dual inhibitor of Bcl-2 and Bcl-XL , in patients with cancer. J Clin Pharm Ther. 2014 Dec;39(6):680-4.
8 Human breast cancer cells display different sensitivities to ABT-263 based on the level of survivin. Toxicol In Vitro. 2018 Feb;46:229-236. doi: 10.1016/j.tiv.2017.09.023. Epub 2017 Sep 23.
9 BCL2/BCL-X(L) inhibition induces apoptosis, disrupts cellular calcium homeostasis, and prevents platelet activation. Blood. 2011 Jun 30;117(26):7145-54. doi: 10.1182/blood-2011-03-344812. Epub 2011 May 11.
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42 mTOR inhibition reverses acquired endocrine therapy resistance of breast cancer cells at the cell proliferation and gene-expression levels. Cancer Sci. 2008 Oct;99(10):1992-2003. doi: 10.1111/j.1349-7006.2008.00955.x.
43 Leptomycin B reduces primary and acquired resistance of gefitinib in lung cancer cells. Toxicol Appl Pharmacol. 2017 Nov 15;335:16-27. doi: 10.1016/j.taap.2017.09.017. Epub 2017 Sep 21.
44 Assessment of the cytotoxic, genotoxic, and apoptotic potential of flurbiprofen in HeLa and HepG2 cell lines. J Biochem Mol Toxicol. 2021 Jun;35(6):1-11. doi: 10.1002/jbt.22770. Epub 2021 Mar 11.
45 Apoptotic signaling pathways induced by nitric oxide in human lymphoblastoid cells expressing wild-type or mutant p53. Cancer Res. 2004 May 1;64(9):3022-9. doi: 10.1158/0008-5472.can-03-1880.
46 Bexarotene activates the p53/p73 pathway in human cutaneous T-cell lymphoma. Br J Dermatol. 2009 Mar;160(3):519-26. doi: 10.1111/j.1365-2133.2008.08931.x. Epub 2008 Nov 25.
47 Expression profile analysis of colon cancer cells in response to sulindac or aspirin. Biochem Biophys Res Commun. 2002 Mar 29;292(2):498-512.
48 Apoptotic induction by simvastatin in human lung cancer A549 cells via Akt signaling dependent down-regulation of survivin. Invest New Drugs. 2011 Oct;29(5):945-52. doi: 10.1007/s10637-010-9450-2. Epub 2010 May 13.
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50 Quercetin inhibit human SW480 colon cancer growth in association with inhibition of cyclin D1 and survivin expression through Wnt/beta-catenin signaling pathway. Cancer Invest. 2009 Jul;27(6):604-12. doi: 10.1080/07357900802337191.
51 Troglitazone sensitizes tumor cells to TRAIL-induced apoptosis via down-regulation of FLIP and Survivin. Apoptosis. 2006 Sep;11(9):1503-12. doi: 10.1007/s10495-006-8896-3.
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53 Selenium and vitamin E: cell type- and intervention-specific tissue effects in prostate cancer. J Natl Cancer Inst. 2009 Mar 4;101(5):306-20.
54 Functional gene expression profile underlying methotrexate-induced senescence in human colon cancer cells. Tumour Biol. 2011 Oct;32(5):965-76.
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56 Species-specific toxicity of diclofenac and troglitazone in primary human and rat hepatocytes. Chem Biol Interact. 2009 Apr 15;179(1):17-24.
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61 Cannabidiol enhances cytotoxicity of anti-cancer drugs in human head and neck squamous cell carcinoma. Sci Rep. 2020 Nov 26;10(1):20622. doi: 10.1038/s41598-020-77674-y.
62 Evidence of securin-mediated resistance to gefitinib-induced apoptosis in human cancer cells. Chem Biol Interact. 2013 Apr 25;203(2):412-22. doi: 10.1016/j.cbi.2013.03.011. Epub 2013 Mar 22.
63 Cigarette smoke and asbestos activate poly-ADP-ribose polymerase in alveolar epithelial cells. J Investig Med. 2001 Jan;49(1):68-76. doi: 10.2310/6650.2001.34092.
64 The antidepressants imipramine, clomipramine, and citalopram induce apoptosis in human acute myeloid leukemia HL-60 cells via caspase-3 activation. J Biochem Mol Toxicol. 1999;13(6):338-47. doi: 10.1002/(sici)1099-0461(1999)13:6<338::aid-jbt8>3.0.co;2-7.
65 Ciprofloxacin mediated cell growth inhibition, S/G2-M cell cycle arrest, and apoptosis in a human transitional cell carcinoma of the bladder cell line. Clin Cancer Res. 2000 Mar;6(3):891-900.
66 Investigation of molecular mechanisms underlying the antiproliferative effects of colchicine against PC3 prostate cancer cells. Toxicol In Vitro. 2021 Jun;73:105138. doi: 10.1016/j.tiv.2021.105138. Epub 2021 Mar 6.
67 Sulindac enhances adenoviral vector expressing mda-7/IL-24-mediated apoptosis in human lung cancer. Mol Cancer Ther. 2005 Feb;4(2):291-304.
68 Methotrexate induces poly(ADP-ribose) polymerase-dependent, caspase 3-independent apoptosis in subsets of proliferating CD4+ T cells. Clin Exp Immunol. 2007 May;148(2):288-95. doi: 10.1111/j.1365-2249.2007.03335.x. Epub 2007 Feb 7.
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