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

General Information of Drug (ID: DMC2IJN)

• Drug Name: TPX-0022 Drug Info
• Synonyms: CSF1R-IN-2; SCHEMBL20694441; TPX0022; NSC820832; NSC-820832; HY-111787; CS-0091874; 2271119-26-5

Indication

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

• Cross-matching ID:
  PubChem CID: 137455315
  TTD Drug ID: DMC2IJN

Molecule-Related Drug Atlas

Drug(s) Targeting Macrophage colony-stimulating factor 1 receptor (CSF1R)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Pexidartinib	DMS2J0Z	Tenosynovial giant cell tumour	2F7B	Approved	[3]
Sulfatinib	DMPOTM4	Neuroendocrine cancer	2B72.1	Phase 3	[4]
ARRY-382	DM0VGDC	Solid tumour/cancer	2A00-2F9Z	Phase 2	[4]
BLZ-945	DMG1LVA	Amyotrophic lateral sclerosis	8B60.0	Phase 2	[4]
Cabiralizumab	DMGE058	Pancreatic cancer	2C10	Phase 2	[5]
AMB-05X	DM958C5	Idiopathic pulmonary fibrosis	CB03.4	Phase 2	[6]
FPA-008	DM3ZN6Y	Autoimmune diabetes	5A10	Phase 1/2	[7]
DCC-3014	DMHW289	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[4]
DCC-3014	DMHW289	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[8]
PLX7486	DM0IVGU	Pancreatic cancer	2C10	Phase 1	[4]

Drug(s) Targeting Proto-oncogene c-Met (MET)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Crizotinib	DM4F29C	Non-small-cell lung cancer	2C25.Y	Approved	[9]
Cabozantinib	DMIYDT4	Medullary thyroid gland carcinoma		Approved	[10]
Amivantamab	DMZ7AMY	Non-small-cell lung cancer	2C25	Approved	[11]
Capmatinib	DMYCXKL	Non-small-cell lung cancer	2C25.Y	Approved	[12]
Tepotinib	DMUQ0E8	Non-small-cell lung cancer	2C25	Approved	[13]
RG3638	DMTQJE0	Gastric adenocarcinoma	2B72	Phase 3	[14]
Savolitinib	DMALFKX	Renal cell carcinoma	2C90	Phase 3	[4]
Beperminogene perplasmid	DM6RWBN	Critical limb ischemia	BD4Y	Phase 3	[15]
Tivantinib	DMNVP8Q	Hepatocellular carcinoma	2C12.02	Phase 3	[16]
MGCD516	DM752PU	Solid tumour/cancer	2A00-2F9Z	Phase 2/3	[14]

Drug(s) Targeting Proto-oncogene c-Src (SRC)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Dasatinib	DMJV2EK	Blast phase chronic myelogenous leukemia, BCR-ABL1 positive		Approved	[17]
Bosutinib	DMTI8YE	Blast phase chronic myelogenous leukemia, BCR-ABL1 positive		Approved	[17]
SKI-758	DMQ8E9R	Ischemia	8B10-8B11	Approved	[18]
Herbimycin A	DM6YWBF	Solid tumour/cancer	2A00-2F9Z	Approved	[19]
AL3818	DM3WP0N	Alveolar soft part sarcoma	2A60-2C35	Phase 3	[4]
CP-868596	DMZIM37	Gastrointestinal cancer	2C11	Phase 3	[4]
Masitinib	DMRSNEU	Amyotrophic lateral sclerosis	8B60.0	Phase 3	[20]
KX-01	DMF0NA9	Actinic keratosis	EK90.0	Phase 3	[21]
Saracatinib	DMBLHGP	Hematologic tumour	2B33.Y	Phase 2	[22]
TPX-0046	DMIVE67	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[23]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Macrophage colony-stimulating factor 1 receptor (CSF1R)	TT7MRDV	CSF1R_HUMAN	Inhibitor	[2]
Proto-oncogene c-Met (MET)	TTNDSF4	MET_HUMAN	Inhibitor	[2]
Proto-oncogene c-Src (SRC)	TT6PKBN	SRC_HUMAN	Inhibitor	[2]

References

• [1] ClinicalTrials.gov (NCT03993873) Phase 1 Study of TPX-0022, a MET/CSF1R/SRC Inhibitor, in Patients With Advanced Solid Tumors Harboring Genetic Alterations in MET. U.S. National Institutes of Health.
• [2] Clinical pipeline report, company report or official report of Turning Point Therapeutics.
• [3] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [4] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [5] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [6] Clinical pipeline report, company report or official report of AmMax Bio
• [7] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [8] Clinical pipeline report, company report or official report of Deciphera Pharmaceuticals.
• [9] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [10] Clinical pipeline report, company report or official report of Exelixis (2011).
• [11] Antitumor Activity of Amivantamab (JNJ-61186372), an EGFR-MET Bispecific Antibody, in Diverse Models of EGFR Exon 20 Insertion-Driven NSCLC. Cancer Discov. 2020 Aug;10(8):1194-1209.
• [12] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [13] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2021
• [14] 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: 1815).
• [15] Beperminogene perplasmid for the treatment of critical limb ischemia. Expert Rev Cardiovasc Ther. 2014 Oct;12(10):1145-56.
• [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. (Ligand id: 7948).
• [17] 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.
• [18] Synthesis and Src kinase inhibitory activity of a series of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-7-furyl-3-quinolinecarbonitriles. J Med Chem. 2006 Dec 28;49(26):7868-76.
• [19] In vivo antitumor activity of herbimycin A, a tyrosine kinase inhibitor, targeted against BCR/ABL oncoprotein in mice bearing BCR/ABL-transfected cells. Leuk Res. 1994 Nov;18(11):867-73.
• [20] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [21] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [22] Novel dual Src/Abl inhibitors for hematologic and solid malignancies.Expert Opin Investig Drugs.2010 Aug;19(8):931-45.
• [23] Clinical pipeline report, company report or official report of Turning Point Therapeutics.