General Information of Drug (ID: DMSTA36)

Drug Name
Intedanib Drug Info
Synonyms
Nintedanib; Vargatef; 656247-17-5; BIBF-1120; BIBF 1120; 928326-83-4; BIBF1120; Nintedanib (BIBF 1120); OFEV; UNII-G6HRD2P839; (Z)-methyl 3-((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenylamino)(phenyl)methylene)-2-oxoindoline-6-carboxylate; G6HRD2P839; CHEBI:85164; 1160294-26-7; Methyl (3z)-3-{[(4-{methyl[(4-Methylpiperazin-1-Yl)acetyl]amino}phenyl)amino](Phenyl)methylidene}-2-Oxo-2,3-Dihydro-1h-Indole-6-Carboxylate
Indication
Disease Entry ICD 11 Status REF
Colorectal cancer 2B91.Z Approved [1]
Idiopathic pulmonary fibrosis CB03.4 Approved [2]
Mesothelioma 2C51.2 Phase 3 [3]
Non-small-cell lung cancer 2C25.Y Phase 3 [4]
Ovarian cancer 2C73 Phase 2 [4]
Cross-matching ID
PubChem CID
135423438
ChEBI ID
CHEBI:85164
CAS Number
CAS 656247-17-5
TTD Drug ID
DMSTA36
VARIDT Drug ID
DR00137

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Patented Agent(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Fruquintinib DMHOSCQ Colorectal cancer 2B91.Z Approved [3]
Sulfatinib DMPOTM4 Neuroendocrine cancer 2B72.1 Phase 3 [3]
KH-902 DM8VO16 Diabetic macular edema 9B71.02 Phase 3 [6]
ABP 938 DM00ACQ Neovascular age-related macular degeneration 9B78.3Z Phase 3 [7]
XL-820 DMMHX9K Solid tumour/cancer 2A00-2F9Z Phase 2 [8]
BAY-57-9352 DMVA5NS Gastric adenocarcinoma 2B72 Phase 2 [9]
X-82 DMW1NKO Age-related macular degeneration 9B75.0 Phase 2 [3]
Vorolanib DMIM1U9 Non-small-cell lung cancer 2C25 Phase 2 [10]
BFH-772 DMVUX1C Psoriasis vulgaris EA90 Phase 2 [11]
ASP-8477 DMBZQS7 Neuropathic pain 8E43.0 Phase 2 [12]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Romiplostim DM3U7SZ Thrombocytopenia 3B64 Approved [13]
Pemigatinib DM819JF Cholangiocarcinoma 2C12.10 Approved [14]
Infigratinib DMNKBEC Cholangiocarcinoma 2C12.10 Approved [15]
E-3810 DM42PFT Solid tumour/cancer 2A00-2F9Z Phase 3 [16]
Sulfatinib DMPOTM4 Neuroendocrine cancer 2B72.1 Phase 3 [17]
ARQ-087 DM02BVQ Intrahepatic cholangiocarcinoma 2C12.10 Phase 3 [18]
AZD4547 DM3827C Solid tumour/cancer 2A00-2F9Z Phase 2/3 [19]
Debio 1347 DMZW50O Solid tumour/cancer 2A00-2F9Z Phase 2 [3]
AM-001 DMGVQI8 Actinic keratosis EK90.0 Phase 2 [20]
FGF-1 DMXMC8I Coronary heart disease BA80.Z Phase 2 [21]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [22]
Pazopanib HCl DM6U9CQ Renal cell carcinoma 2C90 Approved [23]
CT-102 DMB8PF3 Diabetic foot ulcer BD54 Approved [24]
Trapidil DMY67U8 Acute coronary syndrome BA41 Phase 4 [25]
TKI258 DMYLT67 Renal cell carcinoma 2C90 Phase 3 [22]
BAY-57-9352 DMVA5NS Gastric adenocarcinoma 2B72 Phase 2 [22]
X-82 DMW1NKO Age-related macular degeneration 9B75.0 Phase 2 [26]
Vorolanib DMIM1U9 Non-small-cell lung cancer 2C25 Phase 2 [10]
PMID25623274-Compound-WO2014132220C2 DMXEZWP Pulmonary arterial hypertension BB01.0 Patented [27]
PMID25623274-Compound-WO2014132220C1 DMA2IMQ Pulmonary arterial hypertension BB01.0 Patented [27]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [28]
Ponatinib DMYGJQO Acute lymphoblastic leukaemia 2A85 Approved [29]
Midostaurin DMI6E0R Acute myeloid leukaemia 2A60 Approved [22]
Gilteritinib DMTI0ZO Acute myeloid leukaemia 2A60 Approved [30]
Pexidartinib DMS2J0Z Tenosynovial giant cell tumour 2F7B Approved [31]
Pacritinib DM1T6ZN Myelofibrosis 2A20.2 Approved [28]
Quizartinib DM8Y4JS Acute myeloid leukaemia 2A60 Approved [3]
Lestaurtinib DMQ2AIJ Acute myeloid leukaemia 2A60 Approved (orphan drug) [32]
Famitinib DMSFWT7 Solid tumour/cancer 2A00-2F9Z Phase 2 [33]
BMS-690514 DMX302C Chronic pain MG30 Phase 2 [34]
⏷ 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 [35]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [36]
Methotrexate DM2TEOL Anterior urethra cancer Approved [37]
Folic Acid DMEMBJC Colorectal carcinoma Approved [38]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [37]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [37]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [39]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [37]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [40]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [41]
⏷ 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
Fibroblast growth factor receptor 1 (FGFR1) TTRLW2X FGFR1_HUMAN Modulator [1]
Fms-like tyrosine kinase 3 (FLT-3) TTGJCWZ FLT3_HUMAN Inhibitor [1]
Platelet-derived growth factor receptor (PDGFR) TTI2WET NOUNIPROTAC Modulator [1]
Vascular endothelial growth factor receptor (VEGFR) TTVJ1D8 NOUNIPROTAC Modulator [1]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [5]

References

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3 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
4 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: 5936).
5 Effects of Ketoconazole and Rifampicin on the Pharmacokinetics of Nintedanib in Healthy Subjects. Eur J Drug Metab Pharmacokinet. 2018 Oct;43(5):533-541.
6 Effects of intravitreal injection of KH902, a vascular endothelial growth factor receptor decoy, on the retinas of streptozotocin-induced diabetic rats. Diabetes Obes Metab. 2012 Jul;14(7):644-53.
7 Clinical pipeline report, company report or official report of Amgen
8 National Cancer Institute Drug Dictionary (drug id 452042).
9 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
10 Vorolanib, an oral VEGFR/PDGFR dual tyrosine kinase inhibitor for treatment of patients with advanced solid tumors: An open-label, phase I dose escalation and dose expansion trial. Chin J Cancer Res. 2021 Feb 28;33(1):103-114.
11 CA patent application no. 841416, Method of selecting therapeutic indications.
12 ClinicalTrials.gov (NCT02065349) A Study Into Pain Relief Given by ASP8477 for Peripheral Neuropathic Pain (Either Post-herpetic Neuralgia or Painful Diabetic Peripheral Neuropathy) and Its Safety. U.S. National Institutes of Health.
13 Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. J Med Chem. 2002 Dec 19;45(26):5687-93.
14 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
15 Pharmacological inhibition of fibroblast growth factor (FGF) receptor signaling ameliorates FGF23-mediated hypophosphatemic rickets. J Bone Miner Res. 2013 Apr;28(4):899-911.
16 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.
17 Clinical pipeline report, company report or official report of Hutchison Medi Pharma.
18 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: 1808).
19 AZD4547: an orally bioavailable, potent, and selective inhibitor of the fibroblast growth factor receptor tyrosine kinase family. Cancer Res. 2012 Apr 15;72(8):2045-56.
20 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029917)
21 Marimastat as maintenance therapy for patients with advanced gastric cancer: a randomised trial. Br J Cancer. 2002 Jun 17;86(12):1864-70.
22 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.
23 Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
24 Emerging drugs for diabetic foot ulcers. Expert Opin Emerg Drugs. 2006 Nov;11(4):709-24.
25 Osteitis fibrosa is mediated by Platelet-Derived Growth Factor-A via a phosphoinositide 3-kinase-dependent signaling pathway in a rat model for chr... Endocrinology. 2008 Nov;149(11):5735-46.
26 National Cancer Institute Drug Dictionary (drug id 695817).
27 Evaluation of WO-2014132220, selective PDGFR inhibitors for the treatment of pulmonary arterial hypertension.Expert Opin Ther Pat. 2015 Apr;25(4):493-9.
28 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: 1807).
29 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
30 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
31 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
32 Lestaurtinib (CEP701) is a JAK2 inhibitor that suppresses JAK2/STAT5 signaling and the proliferation of primary erythroid cells from patients with ... Blood. 2008 Jun 15;111(12):5663-71.
33 Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706.
34 Preclinical pharmacokinetics and in vitro metabolism of BMS-690514, a potent inhibitor of EGFR and VEGFR2. J Pharm Sci. 2010 Aug;99(8):3579-93.
35 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
36 MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
37 Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade. Cancer Lett. 2016 Jan 1;370(1):153-64.
38 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
39 Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
40 Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
41 Association of genetic polymorphisms in the influx transporter SLCO1B3 and the efflux transporter ABCB1 with imatinib pharmacokinetics in patients with chronic myeloid leukemia. Ther Drug Monit. 2011 Apr;33(2):244-50.