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

General Information of Drug (ID: DMCZPH4)

• Drug Name: K-252a analogue Drug Info

Indication

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

• Cross-matching ID:
  PubChem CID: 44400432
  TTD Drug ID: DMCZPH4

Molecule-Related Drug Atlas

Drug(s) Targeting Tropomyosin-related kinase A (TrkA)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Entrectinib	DMMPTLH	Non-small-cell lung cancer	2C25	Approved	[2]
Repotrectinib	DM9FB2T	Non-small-cell lung cancer	2C25	Approved	[3]
Larotrectinib	DM26CQR	Solid tumour/cancer	2A00-2F9Z	Approved	[4]
MIM-D3	DMZHN5B	Alzheimer disease	8A20	Phase 3	[5]
SNA-120	DMPN314	Plaque psoriasis	EA90.0	Phase 2	[6]
CT 327	DMQXL1T	Plaque psoriasis	EA90.0	Phase 2	[7]
ONO-7579	DMXLPYE	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[3]
Altiratinib	DMUJCBT	Solid tumour/cancer	2A00-2F9Z	Phase 1	[8]
PLX7486	DM0IVGU	Pancreatic cancer	2C10	Phase 1	[9]
DS-6051	DM0RD4F	Solid tumour/cancer	2A00-2F9Z	Phase 1	[10]

Drug(s) Targeting Vascular endothelial growth factor receptor 2 (KDR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Sorafenib	DMS8IFC	Adenocarcinoma	2D40	Approved	[11]
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[12]
Regorafenib	DMHSY1I	Gastrointestinal stromal tumour	2B5B	Approved	[13]
Sunitinib	DMCBJSR	Acute undifferentiated leukemia		Approved	[14]
Axitinib	DMGVH6N	Renal cell carcinoma	2C90	Approved	[15]
Vandetanib	DMRICNP	Solid tumour/cancer	2A00-2F9Z	Approved	[16]
Pazopanib HCl	DM6U9CQ	Renal cell carcinoma	2C90	Approved	[17]
Fruquintinib	DMHOSCQ	Colorectal cancer	2B91.Z	Approved	[18]
Cabozantinib	DMIYDT4	Medullary thyroid gland carcinoma		Approved	[19]
Tivozanib	DMUKC5L	Renal cell carcinoma	2C90	Approved	[20]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Tropomyosin-related kinase A (TrkA)	TTTDVOJ	NTRK1_HUMAN	Inhibitor	[1]
Vascular endothelial growth factor receptor 2 (KDR)	TTUTJGQ	VGFR2_HUMAN	Inhibitor	[1]

References

• [1] Synthesis, modeling, and in vitro activity of (3'S)-epi-K-252a analogues. Elucidating the stereochemical requirements of the 3'-sugar alcohol on tr... J Med Chem. 2005 Jun 2;48(11):3776-83.
• [2] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [3] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [4] 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
• [5] Safety and efficacy of MIM-D3 ophthalmic solutions in a randomized, placebo-controlled Phase 2 clinical trial in patients with dry eye. Clin Ophthalmol. 2013; 7: 1275-1285.
• [6] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [7] Topical TrkA Kinase Inhibitor CT327 is an Effective, Novel Therapy for the Treatment of Pruritus due to Psoriasis: Results from Experimental Studies, and Efficacy and Safety of CT327 in a Phase 2b Clinical Trial in Patients with Psoriasis. Acta Derm Venereol. 2015 May;95(5):542-8.
• [8] Tropomyosin receptor kinase inhibitors: an updated patent review for 2010-2016 - Part I.Expert Opin Ther Pat. 2017 Jun;27(6):733-751.
• [9] National Cancer Institute Drug Dictionary (drug id 747694).
• [10] National Cancer Institute Drug Dictionary (drug id 766123).
• [11] Preclinical overview of sorafenib, a multikinase inhibitor that targets both Raf and VEGF and PDGF receptor tyrosine kinase signaling.Mol Cancer Ther.2008 Oct;7(10):3129-40.
• [12] Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. J Med Chem. 2002 Dec 19;45(26):5687-93.
• [13] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [14] 2006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.
• [15] Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
• [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] Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
• [18] Discovery of fruquintinib, a potent and highly selective small molecule inhibitor of VEGFR 1, 2, 3 tyrosine kinases for cancer therapy. Cancer Biol Ther. 2014;15(12):1635-45.
• [19] Clinical pipeline report, company report or official report of Exelixis (2011).
• [20] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services