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

General Information of Drug (ID: DMPHSU8)

• Drug Name: ACTB-1003 Drug Info
• Synonyms: Multi-mode kinase inhibitor (oral, cancer), ACT Biotech; Multi-mode kinase inhibitor (oral, cancer), Bayer

Indication

Disease Entry	ICD 11	Status	REF
Solid tumour/cancer	2A00-2F9Z	Investigative	[1]

• Cross-matching ID:
  PubChem CID: 23653175
  CAS Number: CAS 939805-30-8
  TTD Drug ID: DMPHSU8

Molecule-Related Drug Atlas

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

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[6]
Intedanib	DMSTA36	Colorectal cancer	2B91.Z	Approved	[7]
Pemigatinib	DM819JF	Cholangiocarcinoma	2C12.10	Approved	[8]
Infigratinib	DMNKBEC	Cholangiocarcinoma	2C12.10	Approved	[9]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[10]
Sulfatinib	DMPOTM4	Neuroendocrine cancer	2B72.1	Phase 3	[11]
ARQ-087	DM02BVQ	Intrahepatic cholangiocarcinoma	2C12.10	Phase 3	[2]
AZD4547	DM3827C	Solid tumour/cancer	2A00-2F9Z	Phase 2/3	[12]
Debio 1347	DMZW50O	Solid tumour/cancer	2A00-2F9Z	Phase 2	[13]
AM-001	DMGVQI8	Actinic keratosis	EK90.0	Phase 2	[14]

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	[8]
Interferon Alfa-2a, Recombinant	DMUTZ8S	Chronic HCV-1 infection	1E51.1	Approved	[15]
Palifermin	DM9JOYP	Oral mucositis	DA01.11	Approved	[16]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[10]
Trafermin	DMLKI2B	Periodontitis	DA0C	Phase 3	[17]
Debio 1347	DMZW50O	Solid tumour/cancer	2A00-2F9Z	Phase 2	[13]
LY2874455	DMZ0DMY	Solid tumour/cancer	2A00-2F9Z	Phase 2	[18]
MK-2461	DM21WBH	Alzheimer disease	8A20	Phase 1/2	[19]
AEE-788	DMEOS5K	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[20]
BAY1179470	DM7L91K	Solid tumour/cancer	2A00-2F9Z	Phase 1	[21]

Drug(s) Targeting Fibroblast growth factor receptor 4 (FGFR4)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
INCB62079	DMQO5UF	Liver cancer	2C12	Phase 1/2	[13]
ABC-4	DMA01OF	Solid tumour/cancer	2A00-2F9Z	Investigative	[5]

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	[8]
Trapidil	DMY67U8	Acute coronary syndrome	BA41	Phase 4	[22]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[10]
TKI258	DMYLT67	Renal cell carcinoma	2C90	Phase 3	[20]
BMS-582664	DMDAN8H	Hepatocellular carcinoma	2C12.02	Phase 3	[20]
Debio 1347	DMZW50O	Solid tumour/cancer	2A00-2F9Z	Phase 2	[13]
B-701	DMOMDA4	Bladder cancer	2C94	Phase 2	[23]
Recifercept	DML8N3Y	Achondroplasia	LD24.00	Phase 2	[24]
MK-2461	DM21WBH	Alzheimer disease	8A20	Phase 1/2	[19]
AEE-788	DMEOS5K	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[20]

Drug(s) Targeting Ribosomal protein S6 kinase beta-1 (S6K1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
M2698	DM3PVBJ	Solid tumour/cancer	2A00-2F9Z	Phase 1	[13]
NNI-362	DMPCV65	Alzheimer disease	8A20	Phase 1	[25]
PF-4708671	DMO0892	Ulcerative colitis	DD71	Clinical trial	[26]
PMID27410995-Compound-Figure3c	DMDQMZT	N. A.	N. A.	Patented	[27]
Pyrimido[4,5-d] pyrimidines and pyrido[4,3-d] pyrimidine derivative 1	DM6O2Q9	N. A.	N. A.	Patented	[27]
RO-316233	DMAGLPW	Discovery agent	N.A.	Investigative	[28]
4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol	DMSKJ1X	Discovery agent	N.A.	Investigative	[29]
4,5,6,7-tetrabromo-1H-benzo[d][1,2,3]triazole	DMN9YOB	Discovery agent	N.A.	Investigative	[30]
CI-1040	DMF3DZX	Discovery agent	N.A.	Investigative	[28]
KN-62	DMLZ89P	Discovery agent	N.A.	Investigative	[28]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Fibroblast growth factor receptor 1 (FGFR1)	TTRLW2X	FGFR1_HUMAN	Inhibitor	[2]
Fibroblast growth factor receptor 2 (FGFR2)	TTGJVQM	FGFR2_HUMAN	Inhibitor	[3]
Fibroblast growth factor receptor 3 (FGFR3)	TTST7KB	FGFR3_HUMAN	Inhibitor	[4]
Fibroblast growth factor receptor 4 (FGFR4)	TT5BR7T	FGFR4_HUMAN	Inhibitor	[5]
Ribosomal protein S6 kinase beta-1 (S6K1)	TTG0U4H	KS6B1_HUMAN	Inhibitor	[1]

References

• [1] 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: 1525).
• [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. (Target id: 1808).
• [3] 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: 1809).
• [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: 1810).
• [5] 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: 1811).
• [6] Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. J Med Chem. 2002 Dec 19;45(26):5687-93.
• [7] 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
• [8] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [9] Pharmacological inhibition of fibroblast growth factor (FGF) receptor signaling ameliorates FGF23-mediated hypophosphatemic rickets. J Bone Miner Res. 2013 Apr;28(4):899-911.
• [10] 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.
• [11] Clinical pipeline report, company report or official report of Hutchison Medi Pharma.
• [12] 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.
• [13] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [14] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029917)
• [15] DrugBank: a knowledgebase for drugs, drug actions and drug targets. Nucleic Acids Res. 2008 Jan;36(Database issue):D901-6.
• [16] Keratinocyte growth factor. Expert Opin Biol Ther. 2009 Jun;9(6):779-87.
• [17] Emerging drugs for diabetic foot ulcers. Expert Opin Emerg Drugs. 2006 Nov;11(4):709-24.
• [18] Company report (Eli Lilly) (drug: LY2874455)
• [19] MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33.
• [20] 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.
• [21] National Cancer Institute Drug Dictionary (drug id 751593).
• [22] Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127.
• [23] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [24] 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.
• [25] Novel pharmacotherapy: NNI-362, an allosteric p70S6 kinase stimulator, reverses cognitive and neural regenerative deficits in models of aging and disease. Stem Cell Res Ther. 2021 Jan 13;12(1):59.
• [26] Characterization of PF-4708671, a novel and highly specific inhibitor of p70 ribosomal S6 kinase (S6K1). Biochem J. 2010 Oct 15;431(2):245-55.
• [27] Ribosomal S6 kinase (RSK) modulators: a patent review.Expert Opin Ther Pat. 2016 Sep;26(9):1061-78.
• [28] Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105.
• [29] 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. J Med Chem. 2006 Nov 2;49(22):6500-9.
• [30] Optimization of protein kinase CK2 inhibitors derived from 4,5,6,7-tetrabromobenzimidazole. J Med Chem. 2004 Dec 2;47(25):6239-47.