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

General Information of Drug (ID: DMFUQIT)

• Drug Name: PMID21493067C1d Drug Info
• Synonyms: GTPL8123; BDBM50343726

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

• Cross-matching ID:
  PubChem CID: 53232451
  TTD Drug ID: DMFUQIT

Molecule-Related Drug Atlas

Drug(s) Targeting Janus kinase 2 (JAK-2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Momelotinib	DMF98Q0	Myelofibrosis	2A20.2	Approved	[2]
Baricitinib	DM4ONW5	Rheumatoid arthritis	FA20	Approved	[3]
Ruxolitinib	DM7Q98D	Essential thrombocythemia	3B63.1Z	Approved	[4]
Pacritinib	DM1T6ZN	Myelofibrosis	2A20.2	Approved	[5]
Fedratinib	DM4ZBK6	Myelofibrosis	2A20.2	Approved	[6]
ITF2357	DMFZBNE	Duchenne dystrophy	8C70	Phase 3	[7]
XL019	DMJ6F5C	Solid tumour/cancer	2A00-2F9Z	Phase 3	[7]
Cerdulatinib	DMSCR2H	B-cell lymphoma	2A86	Phase 2	[8]
CTP-543	DM3SYOK	Alopecia	ED70	Phase 2	[9]
INCB039110	DMD9RV3	Malignant neoplasm	2A00-2F9Z	Phase 2	[10]

Drug(s) Targeting Janus kinase 3 (JAK-3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Tofacitinib	DMBS370	Rheumatoid arthritis	FA20	Approved	[11]
Ritlecitinib	DMYKNME	Alopecia areata	ED70.2	Approved	[12]
ASP-015K	DMZ1UOI	Psoriasis vulgaris	EA90	Phase 3	[13]
VX-509	DM2U3MX	Rheumatoid arthritis	FA20	Phase 2/3	[3]
Cerdulatinib	DMSCR2H	B-cell lymphoma	2A86	Phase 2	[12]
ATI-501	DMTY6OF	Alopecia	ED70	Phase 2	[14]
ATI-502	DM8NODR	Alopecia	ED70	Phase 2	[15]
TD-8236	DMTOMJN	Asthma	CA23	Phase 2	[16]
ALXN2075	DM1BSD8	Non-hodgkin lymphoma	2B33.5	Phase 1/2	[17]
SNA-125	DM8L1GJ	Atopic dermatitis	EA80	Phase 1	[12]

Drug(s) Targeting Muscle-specific kinase receptor (MUSK)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PMID17935989C25	DML8ZBR	Discovery agent	N.A.	Investigative	[18]

Drug(s) Targeting NT-3 growth factor receptor (TrkC)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Entrectinib	DMMPTLH	Non-small-cell lung cancer	2C25	Approved	[19]
Larotrectinib	DM26CQR	Solid tumour/cancer	2A00-2F9Z	Approved	[20]
MK-2461	DM21WBH	Alzheimer disease	8A20	Phase 1/2	[21]
Altiratinib	DMUJCBT	Solid tumour/cancer	2A00-2F9Z	Phase 1	[22]
PMID28270021-Compound-WO2016054807Example1	DMD5QEL	Chronic pain	MG30	Patented	[23]
PMID28270010-Compound-Figure24-b	DM0QHLK	N. A.	N. A.	Patented	[22]
Pyrrolo[2,3-d]pyrimidine derivative 4	DME0WSR	Chronic pain	MG30	Patented	[23]
3-amino-5-benzyl-substituted indazole derivative 1	DMFDURZ	Chronic pain	MG30	Patented	[23]
PMID28270010-Compound-Figure5-1	DM2YAPJ	N. A.	N. A.	Patented	[22]
PMID28270021-Compound-WO2015042088Example4	DM6KXOQ	Chronic pain	MG30	Patented	[23]

Drug(s) Targeting Proto-oncogene c-Ret (RET)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[24]
Regorafenib	DMHSY1I	Gastrointestinal stromal tumour	2B5B	Approved	[11]
Ponatinib	DMYGJQO	Acute lymphoblastic leukaemia	2A85	Approved	[11]
Vandetanib	DMRICNP	Solid tumour/cancer	2A00-2F9Z	Approved	[25]
Selpercatinib	DMZR15V	Non-small-cell lung cancer	2C25.Y	Approved	[26]
Pralsetinib	DMWU0I2	Non-small-cell lung cancer	2C25.Y	Approved	[27]
MGCD516	DM752PU	Solid tumour/cancer	2A00-2F9Z	Phase 2/3	[28]
CEP-32496	DMAO04B	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[29]
TPX-0046	DMIVE67	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[30]
GSK3179106	DM2KCIP	Inflammatory bowel disease	DD72	Phase 1	[9]

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	[31]
Trapidil	DMY67U8	Acute coronary syndrome	BA41	Phase 4	[32]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[33]
TKI258	DMYLT67	Renal cell carcinoma	2C90	Phase 3	[25]
BMS-582664	DMDAN8H	Hepatocellular carcinoma	2C12.02	Phase 3	[25]
Debio 1347	DMZW50O	Solid tumour/cancer	2A00-2F9Z	Phase 2	[29]
B-701	DMOMDA4	Bladder cancer	2C94	Phase 2	[34]
Recifercept	DML8N3Y	Achondroplasia	LD24.00	Phase 2	[35]
MK-2461	DM21WBH	Alzheimer disease	8A20	Phase 1/2	[21]
AEE-788	DMEOS5K	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[25]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Fibroblast growth factor receptor 3 (FGFR3)	TTST7KB	FGFR3_HUMAN	Inhibitor	[1]
Janus kinase 2 (JAK-2)	TTRMX3V	JAK2_HUMAN	Inhibitor	[1]
Janus kinase 3 (JAK-3)	TTT7PJU	JAK3_HUMAN	Inhibitor	[1]
Muscle-specific kinase receptor (MUSK)	TT6SA0X	MUSK_HUMAN	Inhibitor	[1]
NT-3 growth factor receptor (TrkC)	TTXABCW	NTRK3_HUMAN	Inhibitor	[1]
Proto-oncogene c-Ret (RET)	TT4DXQT	RET_HUMAN	Inhibitor	[1]

References

• [1] In vitro and in vivo evaluation of 6-aminopyrazolyl-pyridine-3-carbonitriles as JAK2 kinase inhibitors. Bioorg Med Chem Lett. 2011 May 15;21(10):2958-61.
• [2] Genetic determinants of response and survival in momelotinib-treated patients with myelofibrosis.Leukemia.2015 Mar;29(3):741-4.
• [3] Selective JAK inhibitors in development for rheumatoid arthritis. Expert Opin Investig Drugs. 2014 Aug;23(8):1067-77.
• [4] 2011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.
• [5] National Cancer Institute Drug Dictionary (drug id 609888).
• [6] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [7] Emerging drugs for the therapy of primary and post essential thrombocythemia, post polycythemia vera myelofibrosis. Expert Opin Emerg Drugs. 2009 Sep;14(3):471-9.
• [8] Company report (Portola Pharmaceuticals)
• [9] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [10] 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: 2048).
• [11] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [12] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [13] 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: 2049).
• [14] Clinical pipeline report, company report or official report of Aclaris Therapeutics.
• [15] ClinicalTrials.gov (NCT03759340) ATI-502 Topical Solution for the Treatment of Alopecia Areata (AA), Alopecia Universalis (AU) and Alopecia Totalis (AT). U.S. National Institutes of Health.
• [16] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2023. Adis Insight
• [17] The Dual Syk/JAK Inhibitor Cerdulatinib Antagonizes B-cell Receptor and Microenvironmental Signaling in Chronic Lymphocytic Leukemia. Clin Cancer Res. 2017 May 1;23(9):2313-2324.
• [18] Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and prelimina... Bioorg Med Chem Lett. 2007 Dec 1;17(23):6593-601.
• [19] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [20] 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
• [21] MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33.
• [22] Tropomyosin receptor kinase inhibitors: an updated patent review for 2010-2016 - Part I.Expert Opin Ther Pat. 2017 Jun;27(6):733-751.
• [23] Tropomyosin receptor kinase inhibitors: an updated patent review for 2010-2016 - Part II.Expert Opin Ther Pat. 2017 Jul;27(7):831-849.
• [24] Synthesis, structure-activity relationship and crystallographic studies of 3-substituted indolin-2-one RET inhibitors. Bioorg Med Chem. 2010 Feb 15;18(4):1482-96.
• [25] 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.
• [26] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [27] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [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: 2185).
• [29] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [30] Clinical pipeline report, company report or official report of Turning Point Therapeutics.
• [31] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [32] Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127.
• [33] 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.
• [34] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [35] 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.