General Information of Drug (ID: DMSQ3AZ)

Drug Name
JNJ-26483327 Drug Info
Synonyms MTKI (cancer), J&J; MTKI (cancer), Johnson & Johnson; Multi-targeted kinase inhibitor (cancer), J&J; Multi-targeted kinase inhibitor (cancer), Johnson & Johnson
Indication
Disease Entry ICD 11 Status REF
Solid tumour/cancer 2A00-2F9Z Phase 1 [1]
Cross-matching ID
TTD Drug ID
DMSQ3AZ

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Investigative Drug(s)
Patented Agent(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tivozanib DMUKC5L Renal cell carcinoma 2C90 Approved [4]
E-3810 DM42PFT Solid tumour/cancer 2A00-2F9Z Phase 3 [5]
Sulfatinib DMPOTM4 Neuroendocrine cancer 2B72.1 Phase 3 [6]
Fruquintinib DMHOSCQ Solid tumour/cancer 2A00-2F9Z Phase 3 [7]
PI-88 DMGZPX6 Hepatocellular carcinoma 2C12.02 Phase 3 [8]
Taberminogene vadenovec DMW5PHL Vascular restinosis BE2Z Phase 3 [9]
ABT-869 DMREDYP Solid tumour/cancer 2A00-2F9Z Phase 3 [10]
MGCD516 DM752PU Solid tumour/cancer 2A00-2F9Z Phase 2/3 [11]
Famitinib DMSFWT7 Solid tumour/cancer 2A00-2F9Z Phase 2 [12]
VATALANIB DMY0UEQ Solid tumour/cancer 2A00-2F9Z Phase 2 [13]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dasatinib DMJV2EK Chronic myelogenous leukaemia 2A20.0 Approved [14]
VX-680 DM93YKJ Solid tumour/cancer 2A00-2F9Z Phase 2 [14]
ISIS-CRP DMQDUG4 Cardiovascular disease BA00-BE2Z Phase 1 [15]
RO-316233 DMAGLPW Discovery agent N.A. Investigative [16]
Bisindolylmaleimide-I DMOQJZC Discovery agent N.A. Investigative [16]
4,5,6,7-tetrabromo-1H-benzo[d][1,2,3]triazole DMN9YOB Discovery agent N.A. Investigative [17]
CI-1040 DMF3DZX Discovery agent N.A. Investigative [16]
AMP-PNP DMTOK1D Discovery agent N.A. Investigative [18]
BMS-536924 DMXJB4N Discovery agent N.A. Investigative [19]
KN-62 DMLZ89P Discovery agent N.A. Investigative [16]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Lapatinib DM3BH1Y Breast cancer 2C60-2C65 Approved [20]
Dacomitinib DMOH8VY Non-small-cell lung cancer 2C25.Y Approved [21]
BIBW 2992 DMTKD7Q Non-small-cell lung cancer 2C25.Y Approved [22]
Merimepodib DM0HS92 Breast cancer 2C60-2C65 Approved [23]
NERATINIB MALEATE DMEDU7B HER2/NEU overexpressing breast cancer 2C60-2C65 Approved [24]
Margetuximab DMKEY6S HER2-positive breast cancer 2C60-2C65 Approved [25]
Trastuzumab DMZQOUX Breast cancer 2C60-2C65 Approved [26]
Tucatinib DMBESUA HER2-positive breast cancer 2C60-2C65 Approved [27]
Pertuzumab DMHJV0X Breast cancer 2C60-2C65 Approved [28]
Masoprocol DMMVNZ0 Prostate cancer 2C82.0 Approved [29]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dasatinib DMJV2EK Chronic myelogenous leukaemia 2A20.0 Approved [14]
Ro-4396686 DM5DMCH Discovery agent N.A. Investigative [30]
PMID15546730C2 DMOPUIH Discovery agent N.A. Investigative [31]
CEP-5104 DMV43GY Discovery agent N.A. Investigative [32]
CEP-6331 DMNXBTD Discovery agent N.A. Investigative [32]
JNJ-10198409 DM9GDP5 Discovery agent N.A. Investigative [33]
1-Methoxy-2-[2-(2-Methoxy-Ethoxy]-Ethane DMD7WNV Discovery agent N.A. Investigative [34]
⏷ Show the Full List of 7 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Sorafenib DMS8IFC Hepatocellular carcinoma 2C12.02 Approved [35]
Lapatinib DM3BH1Y Breast cancer 2C60-2C65 Approved [20]
Gefitinib DM15F0X Solid tumour/cancer 2A00-2F9Z Approved [36]
Erlotinib DMCMBHA Non-small-cell lung cancer 2C25.Y Approved [37]
Vandetanib DMRICNP Solid tumour/cancer 2A00-2F9Z Approved [14]
Dacomitinib DMOH8VY Non-small-cell lung cancer 2C25.Y Approved [38]
BIBW 2992 DMTKD7Q Non-small-cell lung cancer 2C25.Y Approved [22]
SKI-758 DMQ8E9R Ischemia 8B10-8B11 Approved [39]
Epidermal growth factor DMVONE6 Vulnerary ND56.Z Approved [38]
Merimepodib DM0HS92 Breast cancer 2C60-2C65 Approved [23]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Bafetinib DM7586F Bone disease FC0Z Phase 2 [40]
Alkynyl-substituted pyrimidinyl-pyrrole derivative 1 DMK7DJ2 N. A. N. A. Patented [41]
NG-25 DMC48D9 Discovery agent N.A. Investigative [42]
PMID17600705C23 DMJFOGW Discovery agent N.A. Investigative [43]
Drug(s) Targeting Yes tyrosine kinase (YES)
Drug Name Drug ID Indication ICD 11 Highest Status REF
TG-100435 DMIR3X2 Discovery agent N.A. Investigative [44]
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dacomitinib DMOH8VY Non-small-cell lung cancer 2C25.Y Approved [21]
RG7388 DMF5GZI Acute myeloid leukaemia 2A60 Phase 3 [45]
CI-1033 DMSI8N3 Lymphoma 2A80-2A86 Phase 2 [14]
JI-101 DMM02VJ Solid tumour/cancer 2A00-2F9Z Phase 2 [46]
PMID24915291C38 DMBXT9J Discovery agent N.A. Investigative [47]
HDS-029 DMLRUVA Discovery agent N.A. Investigative [48]
⏷ Show the Full List of 6 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Epidermal growth factor receptor (EGFR) TTGKNB4 EGFR_HUMAN Inhibitor [2]
Erbb2 tyrosine kinase receptor (HER2) TT6EO5L ERBB2_HUMAN Inhibitor [2]
Erbb4 tyrosine kinase receptor (Erbb-4) TT0JESD ERBB4_HUMAN Inhibitor [2]
Fyn tyrosine protein kinase (FYN) TT2B9KF FYN_HUMAN Inhibitor [3]
LCK tyrosine protein kinase (LCK) TT860QF LCK_HUMAN Inhibitor [2]
Tyrosine-protein kinase Lyn (JTK8) TT1RWNJ LYN_HUMAN Inhibitor [2]
Vascular endothelial growth factor receptor 3 (FLT-4) TTDCBX5 VGFR3_HUMAN Inhibitor [2]
Yes tyrosine kinase (YES) TT0SQ8J YES_HUMAN Inhibitor [2]

References

1 ClinicalTrials.gov (NCT00676299) A Safety and Dose-finding Study of JNJ-26483327, a Drug in Development for Cancer, for Patients With Advanced and/or Refractory Solid Malignancies.. U.S. National Institutes of Health.
2 National Cancer Institute Drug Dictionary (drug id 596693).
3 National Cancer Institute Drug Dictionary (drug id 596693).
4 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services
5 E-3810 is a potent dual inhibitor of VEGFR and FGFR that exerts antitumor activity in multiple preclinical models. Cancer Res. 2011 Feb 15;71(4):1396-405.
6 Clinical pipeline report, company report or official report of Hutchison Medi Pharma.
7 Discovery of fruquintinib, a potent and highly selective small molecule inhibitor of VEGFR 1, 2, 3 tyrosine kinases for cancer therapy. Cancer Biol Ther. 2014;15(12):1635-45.
8 Company report (Medigen)
9 Advances in kinase targeting: current clinical use and clinical trials. Trends Pharmacol Sci. 2014 Nov;35(11):604-20.
10 Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor. Mol Cancer Ther. 2006 Apr;5(4):995-1006.
11 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: 1814).
12 Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706.
13 Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors. J Med Chem. 2005 Mar 10;48(5):1610-9.
14 A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.
15 The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315.
16 Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105.
17 Optimization of protein kinase CK2 inhibitors derived from 4,5,6,7-tetrabromobenzimidazole. J Med Chem. 2004 Dec 2;47(25):6239-47.
18 The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
19 Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitum... J Med Chem. 2005 Sep 8;48(18):5639-43.
20 Triple negative breast cancer--current status and prospective targeted treatment based on HER1 (EGFR), TOP2A and C-MYC gene assessment. Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub. 2009 Mar;153(1):13-7.
21 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. (Ligand id: 7422).
22 Boehringer Ingelheim. Product Development Pipeline. June 2 2009.
23 Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
24 2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85.
25 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
26 Her2/neu is not a commonly expressed therapeutic target in melanoma -- a large cohort tissue microarray study. Melanoma Res. 2004 Jun;14(3):207-10.
27 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
28 Clinical pipeline report, company report or official report of Roche (2009).
29 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
30 Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1950-3.
31 Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56(Lck) inhibitors. Bioorg Med Chem Lett. 2004 Dec 20;14(24):6061-6.
32 Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-linea... J Med Chem. 2008 Sep 25;51(18):5680-9.
33 (6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad ant... J Med Chem. 2005 Dec 29;48(26):8163-73.
34 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
35 Nasopharyngeal carcinoma: Current treatment options and future directions. J Nasopharyng Carcinoma, 2014, 1(16): e16.
36 Gefitinib ('Iressa', ZD1839) and new epidermal growth factor receptor inhibitors. Br J Cancer. 2004 Feb 9;90(3):566-72.
37 Quantitative prediction of fold resistance for inhibitors of EGFR. Biochemistry. 2009 Sep 8;48(35):8435-48.
38 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: 1797).
39 Synthesis and Src kinase inhibitory activity of a series of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-7-furyl-3-quinolinecarbonitriles. J Med Chem. 2006 Dec 28;49(26):7868-76.
40 Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
41 Inhibitors of JAK-family kinases: an update on the patent literature 2013-2015, part 2.Expert Opin Ther Pat. 2017 Feb;27(2):145-161.
42 Discovery of type II inhibitors of TGFbeta-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2). J Med Chem. 2015 Jan 8;58(1):183-96.
43 N-4-Pyrimidinyl-1H-indazol-4-amine inhibitors of Lck: indazoles as phenol isosteres with improved pharmacokinetics. Bioorg Med Chem Lett. 2007 Aug 1;17(15):4363-8.
44 Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinas... Bioorg Med Chem Lett. 2007 Feb 1;17(3):602-8.
45 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: 1799).
46 A pilot study of JI-101, an inhibitor of VEGFR-2, PDGFR-, and EphB4 receptors, in combination with everolimus and as a single agent in an ovarian cancer expansion cohort.Invest New Drugs.2015 Dec;33(6):1217-24.
47 Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity. J Med Chem. 2014 Jun 26;57(12):5112-28.
48 Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB... J Med Chem. 2006 Feb 23;49(4):1475-85.