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

General Information of Drug (ID: DMZW50O)

• Drug Name: Debio 1347 Drug Info

Indication

Disease Entry	ICD 11	Status	REF
Solid tumour/cancer	2A00-2F9Z	Phase 2	[1]
Breast cancer	2C60-2C65	Phase 1/2	[2]

• Cross-matching ID:
  PubChem CID: 66555680
  CAS Number: CAS 1265229-25-1
  TTD Drug ID: DMZW50O

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	[4]
HIF-1alpha	DM4OQRD	Lymphoma	2A80-2A86	Phase 4	[5]
TAS-120	DMWM4D0	Cholangiocarcinoma	2C12.10	Phase 3	[6]
BGJ398	DMNKBEC	Cholangiocarcinoma	2C12.10	Phase 3	[2]
ARQ-087	DM02BVQ	Intrahepatic cholangiocarcinoma	2C12.10	Phase 3	[2]
AZD4547	DM3827C	Solid tumour/cancer	2A00-2F9Z	Phase 2/3	[2]
BAY1163877	DMCSGJ2	Bladder cancer	2C94	Phase 2	[7]
ICP-192	DM524GR	Bladder cancer	2C94	Phase 2	[8]
PRN1371	DMR7BAO	Solid tumour/cancer	2A00-2F9Z	Phase 1	[2]
PD173074	DMP0N4U	Nasopharyngeal carcinoma	2B6B	Investigative	[5]

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

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[9]
Intedanib	DMSTA36	Colorectal cancer	2B91.Z	Approved	[10]
Pemigatinib	DM819JF	Cholangiocarcinoma	2C12.10	Approved	[11]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[12]
Sulfatinib	DMPOTM4	Neuroendocrine cancer	2B72.1	Phase 3	[13]
Rosiglitazone + metformin	DMPIDXT	Diabetic complication	5A2Y	Phase 3	[14]
BGJ398	DMNKBEC	Cholangiocarcinoma	2C12.10	Phase 3	[15]
ARQ-087	DM02BVQ	Intrahepatic cholangiocarcinoma	2C12.10	Phase 3	[16]
AZD4547	DM3827C	Solid tumour/cancer	2A00-2F9Z	Phase 2/3	[17]
AM-001	DMGVQI8	Actinic keratosis	EK90.0	Phase 2	[18]

Drug(s) Targeting Fibroblast growth factor receptor 2 (FGFR2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Pemigatinib	DM819JF	Cholangiocarcinoma	2C12.10	Approved	[11]
Interferon Alfa-2a, Recombinant	DMUTZ8S	Chronic HCV-1 infection	1E51.1	Approved	[19]
Palifermin	DM9JOYP	Oral mucositis	DA01.11	Approved	[20]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[12]
Trafermin	DMLKI2B	Periodontitis	DA0C	Phase 3	[21]
LY2874455	DMZ0DMY	Solid tumour/cancer	2A00-2F9Z	Phase 2	[22]
MK-2461	DM21WBH	Alzheimer disease	8A20	Phase 1/2	[23]
AEE-788	DMEOS5K	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[14]
BAY1179470	DM7L91K	Solid tumour/cancer	2A00-2F9Z	Phase 1	[24]
Alofanib	DMIEKTF	Gastric adenocarcinoma	2B72	Phase 1	[25]

Drug(s) Targeting Fibroblast growth factor receptor 3 (FGFR3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Pemigatinib	DM819JF	Cholangiocarcinoma	2C12.10	Approved	[11]
Trapidil	DMY67U8	Acute coronary syndrome	BA41	Phase 4	[26]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[12]
TKI258	DMYLT67	Renal cell carcinoma	2C90	Phase 3	[14]
BMS-582664	DMDAN8H	Hepatocellular carcinoma	2C12.02	Phase 3	[14]
B-701	DMOMDA4	Bladder cancer	2C94	Phase 2	[27]
Recifercept	DML8N3Y	Achondroplasia	LD24.00	Phase 2	[28]
MK-2461	DM21WBH	Alzheimer disease	8A20	Phase 1/2	[23]
AEE-788	DMEOS5K	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[14]
Anti-FGFR3	DM6QENU	Multiple myeloma	2A83	Phase 1	[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	Modulator	[3]
Fibroblast growth factor receptor 1 (FGFR1)	TTRLW2X	FGFR1_HUMAN	Inhibitor	[2]
Fibroblast growth factor receptor 2 (FGFR2)	TTGJVQM	FGFR2_HUMAN	Inhibitor	[2]
Fibroblast growth factor receptor 3 (FGFR3)	TTST7KB	FGFR3_HUMAN	Inhibitor	[2]

References

• [1] ClinicalTrials.gov (NCT03834220) Basket Trial in Solid Tumors Harboring a Fusion of FGFR1, FGFR2 or FGFR3- (FUZE Clinical Trial). U.S. National Institutes of Health.
• [2] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [3] 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.
• [4] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [5] Tumor angiogenesis as a therapeutic target. Drug Discov Today. 2001 Oct 1;6(19):1005-1024.
• [6] 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.
• [7] Preclinical profile of BAY 1163877 - a selective pan-FGFR inhibitor in phase 1 clinical trial. Cancer Research. 10/2014; 74(19 Supplement):1739-1739.
• [8] Clinical pipeline report, company report or official report of InnoCare Pharma.
• [9] Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. J Med Chem. 2002 Dec 19;45(26):5687-93.
• [10] 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
• [11] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [12] 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.
• [13] Clinical pipeline report, company report or official report of Hutchison Medi Pharma.
• [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] 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] 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).
• [17] 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.
• [18] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029917)
• [19] DrugBank: a knowledgebase for drugs, drug actions and drug targets. Nucleic Acids Res. 2008 Jan;36(Database issue):D901-6.
• [20] Keratinocyte growth factor. Expert Opin Biol Ther. 2009 Jun;9(6):779-87.
• [21] Emerging drugs for diabetic foot ulcers. Expert Opin Emerg Drugs. 2006 Nov;11(4):709-24.
• [22] Company report (Eli Lilly) (drug: LY2874455)
• [23] MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33.
• [24] National Cancer Institute Drug Dictionary (drug id 751593).
• [25] Corrigendum to 'Targeting FGFR2 with alofanib (RPT835) shows potent activity in tumour models' [Eur J Cancer 61 (2016) 20-28]. Eur J Cancer. 2017 Jan;70:156.
• [26] Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127.
• [27] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [28] In vitro and in vivo characterization of Recifercept, a soluble fibroblast growth factor receptor 3, as treatment for achondroplasia. PLoS One. 2020 Dec 28;15(12):e0244368.
• [29] Clinical pipeline report, company report or official report of Genentech (2011).