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

General Information of Drug (ID: DMNKBEC)

• Drug Name: Infigratinib Drug Info
• Synonyms: BGJ398

Indication

Disease Entry	ICD 11	Status	REF
Cholangiocarcinoma	2C12.10	Approved	[1]
Solid tumour/cancer	2A00-2F9Z	Phase 2	[2]

• Cross-matching ID:
  PubChem CID: 53235510
  ChEBI ID: CHEBI:63451
  CAS Number: CAS 872511-34-7
  TTD Drug ID: DMNKBEC

Molecule-Related Drug Atlas

Drug(s) Targeting Fibroblast growth factor receptor (FGFR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Erdafitinib	DMI782S	Bladder cancer	2C94	Approved	[6]
Futibatinib	DMWM4D0	Intrahepatic cholangiocarcinoma	2C12.10	Approved	[7]
HIF-1alpha	DM4OQRD	Lymphoma	2A80-2A86	Phase 4	[8]
ARQ-087	DM02BVQ	Intrahepatic cholangiocarcinoma	2C12.10	Phase 3	[3]
AZD4547	DM3827C	Solid tumour/cancer	2A00-2F9Z	Phase 2/3	[3]
Debio 1347	DMZW50O	Solid tumour/cancer	2A00-2F9Z	Phase 2	[9]
BAY1163877	DMCSGJ2	Bladder cancer	2C94	Phase 2	[10]
ICP-192	DM524GR	Bladder cancer	2C94	Phase 2	[11]
PRN1371	DMR7BAO	Solid tumour/cancer	2A00-2F9Z	Phase 1	[3]
PD173074	DMP0N4U	Nasopharyngeal carcinoma	2B6B	Investigative	[8]

Drug(s) Targeting Fibroblast growth factor receptor 1 (FGFR1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[12]
Intedanib	DMSTA36	Colorectal cancer	2B91.Z	Approved	[13]
Pemigatinib	DM819JF	Cholangiocarcinoma	2C12.10	Approved	[14]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[15]
Sulfatinib	DMPOTM4	Neuroendocrine cancer	2B72.1	Phase 3	[16]
ARQ-087	DM02BVQ	Intrahepatic cholangiocarcinoma	2C12.10	Phase 3	[17]
AZD4547	DM3827C	Solid tumour/cancer	2A00-2F9Z	Phase 2/3	[18]
Debio 1347	DMZW50O	Solid tumour/cancer	2A00-2F9Z	Phase 2	[3]
AM-001	DMGVQI8	Actinic keratosis	EK90.0	Phase 2	[19]
FGF-1	DMXMC8I	Coronary heart disease	BA80.Z	Phase 2	[20]

Drug(s) Affected By Fibroblast growth factor receptor 3 (FGFR3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Quercetin	DM3NC4M	Obesity	5B81	Approved	[21]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[22]
Isotretinoin	DM4QTBN	Acne vulgaris	ED80	Approved	[23]
Panobinostat	DM58WKG	Chronic graft versus host disease		Approved	[24]
Hydroquinone	DM6AVR4	Melasma	ED60.1	Approved	[25]
Lenalidomide	DM6Q7U4	Adult T-cell leukemia/lymphoma		Approved	[26]
Thalidomide	DM70BU5	Adult T-cell leukemia/lymphoma		Approved	[26]
Marinol	DM70IK5	Anorexia nervosa cachexia	6B80	Approved	[27]
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[28]
Ciclosporin	DMAZJFX	Graft-versus-host disease	4B24	Approved	[29]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Fibroblast growth factor receptor (FGFR)	TT0LF7H	NOUNIPROTAC	Inhibitor	[3]
Fibroblast growth factor receptor 1 (FGFR1)	TTRLW2X	FGFR1_HUMAN	Modulator	[4]

Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
Fibroblast growth factor receptor 3 (FGFR3)	OTSAXDIL	FGFR3_HUMAN	Drug Response	[5]

References

• [1] FDA Approved Drug Products from FDA Official Website. 2021. Application Number: 214622.
• [2] 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: 7877).
• [3] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [4] Pharmacological inhibition of fibroblast growth factor (FGF) receptor signaling ameliorates FGF23-mediated hypophosphatemic rickets. J Bone Miner Res. 2013 Apr;28(4):899-911.
• [5] Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase. J Med Chem. 2011 Oct 27;54(20):7066-83. doi: 10.1021/jm2006222. Epub 2011 Sep 21.
• [6] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [7] TAS-120, a highly potent and selective irreversible FGFR inhibitor, is effective in tumors harboring various FGFR gene abnormalities. Molecular Cancer Therapeutics. 01/2014; 12(11_Supplement):A270-A270.
• [8] Tumor angiogenesis as a therapeutic target. Drug Discov Today. 2001 Oct 1;6(19):1005-1024.
• [9] The fibroblast growth factor receptor genetic status as a potential predictor of the sensitivity to CH5183284/Debio 1347, a novel selective FGFR inhibitor. Mol Cancer Ther. 2014 Nov;13(11):2547-58.
• [10] Preclinical profile of BAY 1163877 - a selective pan-FGFR inhibitor in phase 1 clinical trial. Cancer Research. 10/2014; 74(19 Supplement):1739-1739.
• [11] Clinical pipeline report, company report or official report of InnoCare Pharma.
• [12] Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. J Med Chem. 2002 Dec 19;45(26):5687-93.
• [13] 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
• [14] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [15] 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.
• [16] Clinical pipeline report, company report or official report of Hutchison Medi Pharma.
• [17] 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).
• [18] 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.
• [19] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029917)
• [20] Marimastat as maintenance therapy for patients with advanced gastric cancer: a randomised trial. Br J Cancer. 2002 Jun 17;86(12):1864-70.
• [21] 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.
• [22] Retinoic acid receptor alpha amplifications and retinoic acid sensitivity in breast cancers. Clin Breast Cancer. 2013 Oct;13(5):401-8.
• [23] 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.
• [24] 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.
• [25] Keratinocyte-derived IL-36gama plays a role in hydroquinone-induced chemical leukoderma through inhibition of melanogenesis in human epidermal melanocytes. Arch Toxicol. 2019 Aug;93(8):2307-2320.
• [26] Thalidomide and Its Analogs Differentially Target Fibroblast Growth Factor Receptors: Thalidomide Suppresses FGFR Gene Expression while Pomalidomide Dampens FGFR2 Activity. Chem Res Toxicol. 2019 Apr 15;32(4):589-602. doi: 10.1021/acs.chemrestox.8b00286. Epub 2019 Mar 15.
• [27] THC exposure of human iPSC neurons impacts genes associated with neuropsychiatric disorders. Transl Psychiatry. 2018 Apr 25;8(1):89. doi: 10.1038/s41398-018-0137-3.
• [28] Increased expression of fibroblast growth factor receptor 3 in CD34+ BCR-ABL+ cells from patients with chronic myeloid leukemia. Leukemia. 2003 Dec;17(12):2418-25. doi: 10.1038/sj.leu.2403152.
• [29] Comparison of HepG2 and HepaRG by whole-genome gene expression analysis for the purpose of chemical hazard identification. Toxicol Sci. 2010 May;115(1):66-79.