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

General Information of Drug (ID: DM02BVQ)

• Drug Name: ARQ-087 Drug Info

Indication

Disease Entry	ICD 11	Status	REF
Intrahepatic cholangiocarcinoma	2C12.10	Phase 3	[1]
Cholangiocarcinoma	2C12.10	Phase 2	[2]
Solid tumour/cancer	2A00-2F9Z	Phase 1	[3]

• Cross-matching ID:
  PubChem CID: 46834118
  CAS Number: CAS 1234356-69-4
  TTD Drug ID: DM02BVQ

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	[5]
HIF-1alpha	DM4OQRD	Lymphoma	2A80-2A86	Phase 4	[6]
TAS-120	DMWM4D0	Cholangiocarcinoma	2C12.10	Phase 3	[7]
BGJ398	DMNKBEC	Cholangiocarcinoma	2C12.10	Phase 3	[1]
AZD4547	DM3827C	Solid tumour/cancer	2A00-2F9Z	Phase 2/3	[1]
Debio 1347	DMZW50O	Solid tumour/cancer	2A00-2F9Z	Phase 2	[8]
BAY1163877	DMCSGJ2	Bladder cancer	2C94	Phase 2	[9]
ICP-192	DM524GR	Bladder cancer	2C94	Phase 2	[10]
PRN1371	DMR7BAO	Solid tumour/cancer	2A00-2F9Z	Phase 1	[1]
PD173074	DMP0N4U	Nasopharyngeal carcinoma	2B6B	Investigative	[6]

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

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[11]
Intedanib	DMSTA36	Colorectal cancer	2B91.Z	Approved	[12]
Pemigatinib	DM819JF	Cholangiocarcinoma	2C12.10	Approved	[13]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[14]
Sulfatinib	DMPOTM4	Neuroendocrine cancer	2B72.1	Phase 3	[15]
Rosiglitazone + metformin	DMPIDXT	Diabetic complication	5A2Y	Phase 3	[16]
BGJ398	DMNKBEC	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	[1]
AM-001	DMGVQI8	Actinic keratosis	EK90.0	Phase 2	[19]

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	Antagonist	[1]
Fibroblast growth factor receptor 1 (FGFR1)	TTRLW2X	FGFR1_HUMAN	Inhibitor	[4]

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] ClinicalTrials.gov (NCT01752920) Phase 1 Dose Escalation Study of ARQ 087 in Adult Subjects With Advanced Solid Tumors. U.S. National Institutes of Health.
• [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. (Target id: 1808).
• [5] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [6] Tumor angiogenesis as a therapeutic target. Drug Discov Today. 2001 Oct 1;6(19):1005-1024.
• [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] 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.
• [9] Preclinical profile of BAY 1163877 - a selective pan-FGFR inhibitor in phase 1 clinical trial. Cancer Research. 10/2014; 74(19 Supplement):1739-1739.
• [10] Clinical pipeline report, company report or official report of InnoCare Pharma.
• [11] Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. J Med Chem. 2002 Dec 19;45(26):5687-93.
• [12] 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
• [13] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [14] 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.
• [15] Clinical pipeline report, company report or official report of Hutchison Medi Pharma.
• [16] 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.
• [17] Pharmacological inhibition of fibroblast growth factor (FGF) receptor signaling ameliorates FGF23-mediated hypophosphatemic rickets. J Bone Miner Res. 2013 Apr;28(4):899-911.
• [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)