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

General Information of Drug (ID: DMIVE67)

• Drug Name: TPX-0046 Drug Info

Indication

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

• Cross-matching ID: TTD Drug ID: DMIVE67

Molecule-Related Drug Atlas

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

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[3]
Regorafenib	DMHSY1I	Metastatic colorectal cancer	2B91	Approved	[4]
Ponatinib	DMYGJQO	Acute lymphoblastic leukaemia	2A85	Approved	[4]
Vandetanib	DMRICNP	Solid tumour/cancer	2A00-2F9Z	Approved	[5]
Selpercatinib	DMZR15V	Non-small-cell lung cancer	2C25.Y	Approved	[6]
Pralsetinib	DMWU0I2	Non-small-cell lung cancer	2C25.Y	Approved	[7]
MGCD516	DM752PU	Solid tumour/cancer	2A00-2F9Z	Phase 2/3	[8]
CEP-32496	DMAO04B	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[9]
GSK3179106	DM2KCIP	Inflammatory bowel disease	DD72	Phase 1	[10]
BOS172738	DM9L0D8	Solid tumour/cancer	2A00-2F9Z	Phase 1	[11]

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

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Dasatinib	DMJV2EK	Chronic myelogenous leukaemia	2A20.0	Approved	[5]
Bosutinib	DMTI8YE	Breast cancer	2C60-2C65	Approved	[5]
SKI-758	DMQ8E9R	Ischemia	8B10-8B11	Approved	[12]
Herbimycin A	DM6YWBF	Solid tumour/cancer	2A00-2F9Z	Approved	[13]
Al3818	DM3WP0N	Alveolar soft part sarcoma	2A60-2C35	Phase 3	[9]
CP-868596	DMZIM37	Gastrointestinal cancer	2C11	Phase 3	[9]
Masitinib	DMRSNEU	Amyotrophic lateral sclerosis	8B60.0	Phase 3	[10]
KX-01	DMF0NA9	Actinic keratosis	EK90.0	Phase 3	[14]
Saracatinib	DMBLHGP	Hematologic tumour	2B33.Y	Phase 2	[15]
ISIS-CRP	DMQDUG4	Cardiovascular disease	BA00-BE2Z	Phase 1	[16]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Proto-oncogene c-Ret (RET)	TT4DXQT	RET_HUMAN	Inhibitor	[2]
Proto-oncogene c-Src (SRC)	TT6PKBN	SRC_HUMAN	Inhibitor	[2]

References

• [1] ClinicalTrials.gov (NCT04161391) Study of TPX-0046, A RET/SRC Inhibitor in Adult Subjects With Advanced Solid Tumors Harboring RET Fusions or Mutations. U.S. National Institutes of Health.
• [2] Clinical pipeline report, company report or official report of Turning Point Therapeutics.
• [3] 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.
• [4] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [5] 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.
• [6] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [7] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [8] 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).
• [9] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [10] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [11] National Cancer Institute Drug Dictionary (drug name Zeteletinib).
• [12] 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.
• [13] 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.
• [14] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [15] Novel dual Src/Abl inhibitors for hematologic and solid malignancies.Expert Opin Investig Drugs.2010 Aug;19(8):931-45.
• [16] The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315.