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

General Information of Drug (ID: DMEGAZS)

• Drug Name: PMID24432909C8e Drug Info
• Synonyms: 4cd0; GTPL8137; ZINC98050687; BDBM50448785; NCGC00485046-01; P-355; AWJ

Indication

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

• Cross-matching ID:
  PubChem CID: 72710568
  CAS Number: CAS 1549629-82-4
  TTD Drug ID: DMEGAZS

Molecule-Related Drug Atlas

Drug(s) Targeting Proto-oncogene c-Fer (FER)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PMID22564207C25b	DMBMYKQ	Discovery agent	N.A.	Investigative	[2]

Drug(s) Targeting Proto-oncogene c-Fes (FES)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PMID22564207C25b	DMBMYKQ	Discovery agent	N.A.	Investigative	[2]

Drug(s) Targeting ALK tyrosine kinase receptor (ALK)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Crizotinib	DM4F29C	Non-small-cell lung cancer	2C25.Y	Approved	[3]
Lorlatinib	DMICDLV	Non-small-cell lung cancer	2C25.Y	Approved	[4]
Entrectinib	DMMPTLH	Non-small cell lung cancer	2C25	Approved	[5]
Brigatinib	DM7W94S	Anaplastic large cell lymphoma	2A90.A	Approved	[6]
Ceritinib	DMB920Z	Non-small-cell lung cancer	2C25.Y	Approved	[7]
Alectinib	DMP1I6Y	Lung cancer	2C25.0	Approved	[8]
Ensartinib	DMIKDCQ	Non-small-cell lung cancer	2C25.Y	Phase 3	[9]
PF-06463922	DMKM7EW	Non-small-cell lung cancer	2C25.Y	Phase 2	[10]
AP26113	DMYBQEF	Solid tumour/cancer	2A00-2F9Z	Phase 2	[11]
TPX-0005	DM9FB2T	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[9]

Drug(s) Targeting Proto-oncogene c-Ros (ROS1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Crizotinib	DM4F29C	Non-small-cell lung cancer	2C25.Y	Approved	[3]
Lorlatinib	DMICDLV	Non-small-cell lung cancer	2C25.Y	Approved	[4]
Entrectinib	DMMPTLH	Non-small cell lung cancer	2C25	Approved	[5]
AB-106	DMEW62S	Non-small cell lung cancer	2C25	Phase 2	[12]
TPX-0005	DM9FB2T	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[9]
DS-6051	DM0RD4F	Solid tumour/cancer	2A00-2F9Z	Phase 1	[13]
Carboxamide derivative 4	DMU5GKC	N. A.	N. A.	Patented	[14]
Imidazo[1,2-b]pyridazine derivative 2	DM1JYNW	Solid tumour/cancer	2A00-2F9Z	Patented	[15]
Imidazo[1,2-b]pyridazine derivative 3	DMPDTG0	Solid tumour/cancer	2A00-2F9Z	Patented	[15]
PMID28270010-Compound-Figure21-b	DM6IYAT	Brain metastases	2D50	Patented	[15]

Drug(s) Targeting BDNF/NT-3 growth factors receptor (TrkB)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Entrectinib	DMMPTLH	Non-small cell lung cancer	2C25	Approved	[5]
Larotrectinib	DM26CQR	Solid tumour/cancer	2A00-2F9Z	Approved	[4]
MK-2461	DM21WBH	Alzheimer disease	8A20	Phase 1/2	[16]
PMID28270021-Compound-WO2016054807Example1	DMD5QEL	Chronic pain	MG30	Patented	[17]
PMID28270010-Compound-Figure24-b	DM0QHLK	N. A.	N. A.	Patented	[15]
Pyrrolo[2,3-d]pyrimidine derivative 4	DME0WSR	Chronic pain	MG30	Patented	[17]
3-amino-5-benzyl-substituted indazole derivative 1	DMFDURZ	Chronic pain	MG30	Patented	[17]
PMID28270010-Compound-Figure5-1	DM2YAPJ	N. A.	N. A.	Patented	[15]
PMID28270021-Compound-WO2015042088Example4	DM6KXOQ	Chronic pain	MG30	Patented	[17]
PMID28270010-Compound-Figure5-2	DMK3GRZ	N. A.	N. A.	Patented	[15]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
ALK tyrosine kinase receptor (ALK)	TTPMQSO	ALK_HUMAN	Inhibitor	[1]
BDNF/NT-3 growth factors receptor (TrkB)	TTKN7QR	NTRK2_HUMAN	Inhibitor	[1]
Leukocyte receptor tyrosine kinase (LTK)	TT1JZG6	LTK_HUMAN	Inhibitor	[1]
Proto-oncogene c-Fer (FER)	TTRA9G0	FER_HUMAN	Inhibitor	[1]
Proto-oncogene c-Fes (FES)	TTLBY21	FES_HUMAN	Inhibitor	[1]
Proto-oncogene c-Ros (ROS1)	TTSZ6Y3	ROS1_HUMAN	Inhibitor	[1]

References

• [1] Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib. J Med Chem.> 2014 Feb 27;57(4):1170-87.
• [2] Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase. J Med Chem. 2012 May 24;55(10):4580-93.
• [3] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [4] 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
• [5] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [6] 2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85.
• [7] 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. (Ligand id: 7397).
• [8] CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant. Cancer Cell. 2011 May 17;19(5):679-90.
• [9] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [10] PF-06463922, an ALK/ROS1 Inhibitor, Overcomes Resistance to First and Second Generation ALK Inhibitors in Preclinical Models. Cancer Cell. 2015 Jul 13;28(1):70-81.
• [11] Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
• [12] Clinical pipeline report, company report or official report of AnHeart Therapeutics.
• [13] National Cancer Institute Drug Dictionary (drug id 766123).
• [14] RET kinase inhibitors: a review of recent patents (2012-2015).Expert Opin Ther Pat. 2017 Jan;27(1):91-99.
• [15] Tropomyosin receptor kinase inhibitors: an updated patent review for 2010-2016 - Part I.Expert Opin Ther Pat. 2017 Jun;27(6):733-751.
• [16] MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33.
• [17] Tropomyosin receptor kinase inhibitors: an updated patent review for 2010-2016 - Part II.Expert Opin Ther Pat. 2017 Jul;27(7):831-849.