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

General Information of DTT (ID: TT4DXQT)

• DTT Name: Proto-oncogene c-Ret (RET) DTT Info
• Gene Name: RET

Molecule-Related Drug & Molecule List

6 Approved Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Ponatinib	DMYGJQO	Acute lymphoblastic leukaemia	2A85	Approved	[1]
Pralsetinib	DMWU0I2	Non-small-cell lung cancer	2C25.Y	Approved	[2]
Regorafenib	DMHSY1I	Gastrointestinal stromal tumour	2B5B	Approved	[1]
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[3]
Selpercatinib	DMZR15V	Non-small-cell lung cancer	2C25.Y	Approved	[4]
Vandetanib	DMRICNP	Solid tumour/cancer	2A00-2F9Z	Approved	[5]

7 Clinical Trial Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
MGCD516	DM752PU	Solid tumour/cancer	2A00-2F9Z	Phase 2/3	[6]
CEP-32496	DMAO04B	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[7]
TPX-0046	DMIVE67	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[8]
A400	DMQ0YH2	Aggressive cancer	2A00-2F9Z	Phase 1	[9]
BOS172738	DM9L0D8	Solid tumour/cancer	2A00-2F9Z	Phase 1	[10]
GSK3179106	DM2KCIP	Inflammatory bowel disease	DD72	Phase 1	[11]
tamatinib	DMGANIC	Solid tumour/cancer	2A00-2F9Z	Clinical trial	[12]

30 Patented Agent(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Benzo(b)carbazol-11-one compound 1	DM4VXY1	N. A.	N. A.	Patented	[13]
Benzo(b)carbazol-11-one compound 2	DMGCHW9	N. A.	N. A.	Patented	[13]
Carboxamide derivative 4	DMU5GKC	N. A.	N. A.	Patented	[13]
Dihydropyridine compound 1	DM16M4A	N. A.	N. A.	Patented	[13]
Dihydropyridine compound 2	DM6RGOY	N. A.	N. A.	Patented	[13]
Dihydropyridine compound 3	DMR3AVK	N. A.	N. A.	Patented	[13]
Dihydropyridine compound 4	DMIFZLG	N. A.	N. A.	Patented	[13]
Dihydropyridine compound 5	DMC41TK	N. A.	N. A.	Patented	[13]
Dihydropyridine compound 6	DMEXT6J	N. A.	N. A.	Patented	[13]
Pyrazolo[3,4-d]pyrimidine derivative 5	DMIH0F4	N. A.	N. A.	Patented	[13]
Pyrazolo[3,4-d]pyrimidine derivative 6	DMCTWVY	N. A.	N. A.	Patented	[13]
Pyrazolo[3,4-d]pyrimidine derivative 7	DM4GF58	N. A.	N. A.	Patented	[13]
Pyrazolo[3,4-d]pyrimidine derivative 8	DM89GKE	N. A.	N. A.	Patented	[13]
Pyridine derivative 18	DMBZMYT	N. A.	N. A.	Patented	[13]
Pyridine derivative 19	DMXYT40	N. A.	N. A.	Patented	[13]
Pyridine derivative 20	DMAOF0W	N. A.	N. A.	Patented	[13]
Pyridine derivative 21	DMF3907	N. A.	N. A.	Patented	[13]
Pyridine derivative 22	DMSIERF	N. A.	N. A.	Patented	[13]
Pyrrolo-pyridinone derivative 1	DMK820T	N. A.	N. A.	Patented	[13]
Pyrrolo-pyridinone derivative 2	DM5G67X	N. A.	N. A.	Patented	[13]
Pyrrolo-pyridinone derivative 3	DME1Q3W	N. A.	N. A.	Patented	[13]
Pyrrolo-pyridinone derivative 4	DM2EVJR	N. A.	N. A.	Patented	[13]
Pyrrolo-pyrimidine derivative 2	DMEHYBJ	N. A.	N. A.	Patented	[13]
Pyrrolo-pyrimidine derivative 3	DMKHWN9	N. A.	N. A.	Patented	[13]
Pyrrolo-pyrimidine derivative 4	DMITK03	N. A.	N. A.	Patented	[13]
Pyrrolo-pyrimidine derivative 5	DMVA95G	N. A.	N. A.	Patented	[13]
Pyrrolo-pyrimidine derivative 6	DMGYT81	N. A.	N. A.	Patented	[13]
Quinazoline derivative 14	DMHLJA7	N. A.	N. A.	Patented	[13]
Quinazoline derivative 15	DMD965S	N. A.	N. A.	Patented	[13]
Quinazoline derivative 16	DMQ704Z	N. A.	N. A.	Patented	[13]

1 Discontinued Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
CEP-751	DM956N7	Neurodegenerative disorder	8A20-8A23	Terminated	[14]

9 Investigative Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(E)-3-(4-hydroxybenzylidene)indolin-2-one	DMX4U9L	Discovery agent	N.A.	Investigative	[3]
(Z)-3-((1H-pyrrol-2-yl)methylene)indolin-2-one	DM27WDP	Discovery agent	N.A.	Investigative	[3]
(Z)-5-Amino-3-(4-methoxybenzylidene)indolin-2-one	DMPJAKL	Discovery agent	N.A.	Investigative	[3]
AST-487	DME76KU	Discovery agent	N.A.	Investigative	[15]
GW-559768X	DMGRKT4	Solid tumour/cancer	2A00-2F9Z	Investigative	[6]
ITRI-305	DMWTDS8	Thyroid cancer	2D10	Investigative	[6]
PMID21493067C1d	DMFUQIT	Discovery agent	N.A.	Investigative	[16]
PMID21561767C8h	DMABZH6	Discovery agent	N.A.	Investigative	[17]
TG-100435	DMIR3X2	Discovery agent	N.A.	Investigative	[18]

References

• [1] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [2] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [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. 2020
• [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] 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).
• [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 Turning Point Therapeutics.
• [9] Clinical pipeline report, company report or official report of Klus Pharma
• [10] National Cancer Institute Drug Dictionary (drug name Zeteletinib).
• [11] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [12] 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.
• [13] RET kinase inhibitors: a review of recent patents (2012-2015).Expert Opin Ther Pat. 2017 Jan;27(1):91-99.
• [14] CEP-701 and CEP-751 inhibit constitutively activated RET tyrosine kinase activity and block medullary thyroid carcinoma cell growth. Cancer Res. 2003 Sep 1;63(17):5559-63.
• [15] The RET kinase inhibitor NVP-AST487 blocks growth and calcitonin gene expression through distinct mechanisms in medullary thyroid cancer cells. Cancer Res. 2007 Jul 15;67(14):6956-64.
• [16] In vitro and in vivo evaluation of 6-aminopyrazolyl-pyridine-3-carbonitriles as JAK2 kinase inhibitors. Bioorg Med Chem Lett. 2011 May 15;21(10):2958-61.
• [17] Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant. Bioorg Med Chem Lett. 2011 Jun 15;21(12):3743-8.
• [18] Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinas... Bioorg Med Chem Lett. 2007 Feb 1;17(3):602-8.