General Information of Drug (ID: DMRSNEU)

Drug Name
Masitinib Drug Info
Synonyms
Masitinib; 790299-79-5; AB1010; Masatinib; Masitinib (AB1010); Masivet; AB-1010; AB 1010; UNII-M59NC4E26P; Masitinib [INN]; M59NC4E26P; 4-[(4-Methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-thiazolyl]amino]phenyl]benzamide; CHEMBL1908391; CHEBI:63450; Masitinib (INN); N-(4-Methyl-3-((4-(pyridin-3-yl)thiazol-2-yl)amino)phenyl)-4-((4-methylpiperazin-1-yl)methyl)benzamide; Q-201339; C28H30N6OS; N-(4-methyl-3-(4-(pyridin-3-yl)thiazol-2-ylamino)phenyl)-4-((4-methylpiperazin-1-yl)methyl)benzamide
Indication
Disease Entry ICD 11 Status REF
Amyotrophic lateral sclerosis 8B60.0 Phase 3 [1]
Gastrointestinal stromal tumour 2B5B Phase 3 [2]
Metastatic gastric or gastroesophageal junction cancer 2D8Y Phase 3 [1]
Multiple sclerosis 8A40 Phase 3 [3]
Ovarian cancer 2C73 Phase 3 [2]
Pancreatic cancer 2C10 Phase 3 [2]
Cross-matching ID
PubChem CID
10074640
ChEBI ID
CHEMBL63450
CAS Number
CAS 790299-79-5
TTD Drug ID
DMRSNEU

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Patented Agent(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Baricitinib DM4ONW5 Rheumatoid arthritis FA20 Approved [6]
Abrocitinib DM8J29L Atopic dermatitis EA80 Approved [7]
ASP-015K DMZ1UOI Psoriasis vulgaris EA90 Phase 3 [3]
KD019 DMEFW3G Brain metastases 2D50 Phase 2 [2]
LEO 124249 DM7W0JE Asthma CA23 Phase 2 [7]
ATI-502 DM8NODR Alopecia ED70 Phase 2 [7]
TD-1473 DMJG7AY Ulcerative colitis DD71 Phase 1 [3]
Aminotriazolopyridine derivative 1 DMW2LZ0 N. A. N. A. Patented [8]
Imidazo[4,5-c]pyridine derivative 2 DMFDRJT N. A. N. A. Patented [8]
PMID27774824-Compound-Figure11Example1up DMH1W8F N. A. N. A. Patented [8]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting Proto-oncogene c-Src (SRC)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dasatinib DMJV2EK Blast phase chronic myelogenous leukemia, BCR-ABL1 positive Approved [9]
Bosutinib DMTI8YE Blast phase chronic myelogenous leukemia, BCR-ABL1 positive Approved [9]
SKI-758 DMQ8E9R Ischemia 8B10-8B11 Approved [10]
Herbimycin A DM6YWBF Solid tumour/cancer 2A00-2F9Z Approved [11]
AL3818 DM3WP0N Alveolar soft part sarcoma 2A60-2C35 Phase 3 [2]
CP-868596 DMZIM37 Gastrointestinal cancer 2C11 Phase 3 [2]
KX-01 DMF0NA9 Actinic keratosis EK90.0 Phase 3 [7]
Saracatinib DMBLHGP Hematologic tumour 2B33.Y Phase 2 [12]
TPX-0046 DMIVE67 Solid tumour/cancer 2A00-2F9Z Phase 1/2 [13]
ISIS-CRP DMQDUG4 Cardiovascular disease BA00-BE2Z Phase 1 [14]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [15]
Gabapentin DM6T924 Complex partial seizure 8A68.0 Approved [16]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [17]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [18]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [19]
Imiquimod DM1TMA3 Alopecia areata ED70.2 Approved [20]
Prednisone DM2HG4X Acute asthma CA23 Approved [21]
Ciprofloxacin XR DM2NLS9 Acute gonococcal cervicitis Approved [22]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [23]
Methotrexate DM2TEOL Anterior urethra cancer Approved [24]
⏷ 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 [25]
Quercetin DM3NC4M Obesity 5B81 Approved [26]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [27]
Isotretinoin DM4QTBN Acne vulgaris ED80 Approved [28]
Panobinostat DM58WKG Chronic graft versus host disease Approved [29]
Aspirin DM672AH Acute coronary syndrome BA41 Approved [30]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [31]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [32]
Ivermectin DMDBX5F Intestinal strongyloidiasis due to nematode parasite 1F6B Approved [33]
Zoledronate DMIXC7G Adenocarcinoma 2D40 Approved [34]
⏷ 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
Proto-oncogene c-Src (SRC) TT6PKBN SRC_HUMAN Inhibitor [3]
Tyrosine-protein kinase (PTK) TTJSQEF NOUNIPROTAC Inhibitor [2]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Transforming growth factor beta-1 proprotein (TGFB1) OTV5XHVH TGFB1_HUMAN Protein Interaction/Cellular Processes [4]
Tyrosine-protein kinase Lyn (LYN) OTP686K2 LYN_HUMAN Gene/Protein Processing [5]

References

1 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
2 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
3 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
4 Additive cell protective and oxidative stress reducing effects of combined treatment with cromolyn sodium and masitinib on MPTP-induced toxicity in SH-SY5Y neuroblastoma cells. Chem Biol Interact. 2022 Feb 25;354:109808. doi: 10.1016/j.cbi.2022.109808. Epub 2022 Jan 7.
5 Masitinib (AB1010), a potent and selective tyrosine kinase inhibitor targeting KIT. PLoS One. 2009 Sep 30;4(9):e7258. doi: 10.1371/journal.pone.0007258.
6 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
7 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
8 Inhibitors of JAK-family kinases: an update on the patent literature 2013-2015, part 1.Expert Opin Ther Pat. 2017 Feb;27(2):127-143.
9 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.
10 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.
11 In vivo antitumor activity of herbimycin A, a tyrosine kinase inhibitor, targeted against BCR/ABL oncoprotein in mice bearing BCR/ABL-transfected cells. Leuk Res. 1994 Nov;18(11):867-73.
12 Novel dual Src/Abl inhibitors for hematologic and solid malignancies.Expert Opin Investig Drugs.2010 Aug;19(8):931-45.
13 Clinical pipeline report, company report or official report of Turning Point Therapeutics.
14 The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315.
15 Oxidative stress in kidney transplant patients with calcineurin inhibitor-induced hypertension: effect of ramipril. J Cardiovasc Pharmacol. 2002 Oct;40(4):625-31.
16 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.
17 Transcriptomic Analysis of Stem Cells Treated with Moringin or Cannabidiol: Analogies and Differences in Inflammation Pathways. Int J Mol Sci. 2019 Nov 30;20(23):6039. doi: 10.3390/ijms20236039.
18 Antiestrogens induce transforming growth factor beta-mediated immunosuppression in breast cancer. Cancer Res. 2010 Feb 15;70(4):1314-22. doi: 10.1158/0008-5472.CAN-09-3292. Epub 2010 Feb 9.
19 PPAR-alpha ligands inhibit H2O2-mediated activation of transforming growth factor-beta1 in human mesangial cells. Antioxid Redox Signal. 2002 Dec;4(6):877-84. doi: 10.1089/152308602762197416.
20 Cannabidiol selectively modulates interleukin (IL)-1 and IL-6 production in toll-like receptor activated human peripheral blood monocytes. Toxicology. 2021 Dec;464:153016. doi: 10.1016/j.tox.2021.153016. Epub 2021 Nov 2.
21 Cytokine abnormalities in a patient with eosinophilic fasciitis. Ann Allergy Asthma Immunol. 2003 Apr;90(4):452-5. doi: 10.1016/S1081-1206(10)61832-7.
22 Ciprofloxacin decreases survival in HT-29 cells via the induction of TGF-beta1 secretion and enhances the anti-proliferative effect of 5-fluorouracil. Br J Pharmacol. 2009 Jun;157(3):362-70. doi: 10.1111/j.1476-5381.2009.00161.x. Epub 2009 Apr 9.
23 Enhanced apoptosis and transforming growth factor-beta1 expression in colorectal adenomas and carcinomas after Sulindac therapy. Dis Colon Rectum. 2001 Jul;44(7):1008-15. doi: 10.1007/BF02235490.
24 The contribution of methotrexate exposure and host factors on transcriptional variance in human liver. Toxicol Sci. 2007 Jun;97(2):582-94.
25 DNA methylome-wide alterations associated with estrogen receptor-dependent effects of bisphenols in breast cancer. Clin Epigenetics. 2019 Oct 10;11(1):138. doi: 10.1186/s13148-019-0725-y.
26 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.
27 Development of a neural teratogenicity test based on human embryonic stem cells: response to retinoic acid exposure. Toxicol Sci. 2011 Dec;124(2):370-7.
28 Temporal changes in gene expression in the skin of patients treated with isotretinoin provide insight into its mechanism of action. Dermatoendocrinol. 2009 May;1(3):177-87.
29 A transcriptome-based classifier to identify developmental toxicants by stem cell testing: design, validation and optimization for histone deacetylase inhibitors. Arch Toxicol. 2015 Sep;89(9):1599-618.
30 Expression profile analysis of human peripheral blood mononuclear cells in response to aspirin. Arch Immunol Ther Exp (Warsz). 2005 Mar-Apr;53(2):151-8.
31 Comparison of the gene expression profiles of monocytic versus granulocytic lineages of HL-60 leukemia cell differentiation by DNA microarray analysis. Life Sci. 2003 Aug 15;73(13):1705-19. doi: 10.1016/s0024-3205(03)00515-0.
32 Human embryonic stem cell-derived test systems for developmental neurotoxicity: a transcriptomics approach. Arch Toxicol. 2013 Jan;87(1):123-43.
33 Quantitative proteomics reveals a broad-spectrum antiviral property of ivermectin, benefiting for COVID-19 treatment. J Cell Physiol. 2021 Apr;236(4):2959-2975. doi: 10.1002/jcp.30055. Epub 2020 Sep 22.
34 Interleukin-19 as a translational indicator of renal injury. Arch Toxicol. 2015 Jan;89(1):101-6.