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

General Information of Drug (ID: DMGANIC)

• Drug Name: tamatinib Drug Info
• Synonyms: R 406; R-406; R406 free base

Indication

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

• Cross-matching ID:
  PubChem CID: 11213558
  ChEBI ID: CHEBI:91348
  CAS Number: CAS 841290-80-0
  TTD Drug ID: DMGANIC

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	Gastrointestinal stromal tumour	2B5B	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]
TPX-0046	DMIVE67	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[10]
GSK3179106	DM2KCIP	Inflammatory bowel disease	DD72	Phase 1	[11]

Drug(s) Targeting Tyrosine-protein kinase SYK (SYK)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Fostamatinib	DM6AUHV	Immune thrombocytopenic purpura	3B64.13	Approved	[12]
Fostamatinib disodium	DM3274D	Thrombocytopenia	3B64	Phase 3	[13]
Cerdulatinib	DMSCR2H	B-cell lymphoma	2A86	Phase 2	[14]
TAK-659	DMJH3U0	Diffuse large B-cell lymphoma	2A81	Phase 2	[15]
GS-9876	DM9Q2B6	Cutaneous lupus erythematosus	EB5Z	Phase 2	[11]
GS-9973	DMKWCTR	Acute myeloid leukaemia	2A60	Phase 2	[16]
Cevidoplenib	DM9QU5G	Rheumatoid arthritis	FA20	Phase 2	[17]
HM43239	DMV1SDA	Acute myeloid leukaemia	2A60	Phase 1/2	[18]
ALXN2075	DM1BSD8	Non-hodgkin lymphoma	2B33.5	Phase 1/2	[19]
SKI-O-703	DMTSKXR	Rheumatoid arthritis	FA20	Phase 1	[11]

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	[1]
Tyrosine-protein kinase SYK (SYK)	TTOU65C	KSYK_HUMAN	Inhibitor	[2]

References

• [1] Developmental toxicity associated with receptor tyrosine kinase Ret inhibition in reproductive toxicity testing. Birth Defects Res A Clin Mol Teratol. 2009 Feb;85(2):130-6.
• [2] Pharmacophore modeling study based on known spleen tyrosine kinase inhibitors together with virtual screening for identifying novel inhibitors. Bioorg Med Chem Lett. 2009 Apr 1;19(7):1944-9.
• [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 Turning Point Therapeutics.
• [11] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [12] 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: 2230).
• [13] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [14] Company report (Portola Pharmaceuticals)
• [15] J Clin Oncol 32:5s, 2014 (suppl; abstr 8580).
• [16] An open-label phase 2 trial of entospletinib (GS-9973), a selective spleen tyrosine kinase inhibitor, in chronic lymphocytic leukemia. Blood. 2015 Apr 9;125(15):2336-43.
• [17] A novel selective spleen tyrosine kinase inhibitor SKI-O-703 (cevidoplenib) ameliorates lupus nephritis and serum-induced arthritis in murine models. Clin Exp Immunol. 2023 Mar 8;211(1):31-45.
• [18] Clinical pipeline report, company report or official report of Hanmi Pharmaceutical.
• [19] 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.