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

General Information of DTT (ID: TTPS3C0)

• DTT Name: Aurora kinase A (AURKA) DTT Info
• Gene Name: AURKA

Molecule-Related Drug & Molecule List

16 Clinical Trial Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
AT9283	DMQ94CT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[1]
MLN8237	DMO8PT9	Solid tumour/cancer	2A00-2F9Z	Phase 3	[2]
ABT-348	DMMZOYN	Haematological malignancy	2B33.Y	Phase 2	[3]
ENMD-2076	DMJZVPB	Acute myeloid leukaemia	2A60	Phase 2	[4]
PHA-739358	DMGYBZI	Prostate cancer	2C82.0	Phase 2	[4]
VX-680	DM93YKJ	Solid tumour/cancer	2A00-2F9Z	Phase 2	[5]
LY3295668	DM8RJTB	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[6]
AMG 900	DMASGXJ	Solid tumour/cancer	2A00-2F9Z	Phase 1	[7]
CYC116	DMUMHXT	Solid tumour/cancer	2A00-2F9Z	Phase 1	[8]
HPP-607	DM5VSZR	Solid tumour/cancer	2A00-2F9Z	Phase 1	[9]
MK-5108	DMFGYKS	Solid tumour/cancer	2A00-2F9Z	Phase 1	[10]
MLN8054	DMUANF3	Solid tumour/cancer	2A00-2F9Z	Phase 1	[5]
R763	DME0CJ9	Haematological malignancy	2B33.Y	Phase 1	[11]
SNS-314	DMAC5F2	Solid tumour/cancer	2A00-2F9Z	Phase 1	[12]
TAS-119	DMJXBVP	Solid tumour/cancer	2A00-2F9Z	Phase 1	[13]
VIC-1911	DMDFC2Y	Solid tumour/cancer	2A00-2F9Z	Phase 1	[14]

1 Discontinued Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PF-03814735	DMO4S6T	Advanced solid tumour	2A00-2F9Z	Discontinued in Phase 1	[4]

9 Investigative Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
2-(1H-pyrazol-3-yl)-1H-benzimidazole	DMHSORL	Discovery agent	N.A.	Investigative	[15]
4-(1H-pyrazol-4-yl)-1H-pyrrolo[2,3-b]pyridine	DM9MPHF	Discovery agent	N.A.	Investigative	[16]
6-bromoindirubin-3-oxime	DM12WYV	Discovery agent	N.A.	Investigative	[17]
7-fluoroindirubin-3-oxime	DMQD34N	Discovery agent	N.A.	Investigative	[17]
Indirubin-3'-monoxime	DMLRQH0	Discovery agent	N.A.	Investigative	[17]
Indirubin-3-acetoxime	DM3UR1E	Discovery agent	N.A.	Investigative	[17]
Indirubin-3-methoxime	DMZ5ODC	Discovery agent	N.A.	Investigative	[17]
Phosphonothreonine	DMTFHPI	Discovery agent	N.A.	Investigative	[18]
ZM-447439	DMFP8WE	Discovery agent	N.A.	Investigative	[19]

References

• [1] A phase I trial of AT9283 (a selective inhibitor of aurora kinases) in children and adolescents with solid tumors: a Cancer Research UK study. Clin Cancer Res. 2015 Jan 15;21(2):267-73.
• [2] Effect of Aurora A kinase inhibitor MLN8237 combined with rituximab on antitumor activity in preclinical B-cell non-Hodgkin's lymphoma models. Journal of Clinical Oncology, 2009:8553.
• [3] Preclinical characterization of ABT-348, a kinase inhibitor targeting the aurora, vascular endothelial growth factor receptor/platelet-derived growth factor receptor, and Src kinase families. J Pharmacol Exp Ther. 2012 Dec;343(3):617-27.
• [4] Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66.
• [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] Aurora A-Selective Inhibitor LY3295668 Leads to Dominant Mitotic Arrest, Apoptosis in Cancer Cells, and Shows Potent Preclinical Antitumor Efficacy. Mol Cancer Ther. 2019 Dec;18(12):2207-2219.
• [7] Preclinical evaluation of AMG 900, a novel potent and highly selective pan-aurora kinase inhibitor with activity in taxane-resistant tumor cell lines. Cancer Res. 2010 Dec 1;70(23):9846-54.
• [8] Clinical pipeline report, company report or official report of Cyclacel.
• [9] 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: 1936).
• [10] A novel c-Met inhibitor, MK8033, synergizes with carboplatin plus paclitaxel to inhibit ovarian cancer cell growth. Oncol Rep. 2013 May;29(5):2011-8.
• [11] Preclinical characterization of Aurora kinase inhibitor R763/AS703569 identified through an image-based phenotypic screen. J Cancer Res Clin Oncol. 2010 Jan;136(1):99-113.
• [12] SNS-314, a pan-Aurora kinase inhibitor, shows potent anti-tumor activity and dosing flexibility in vivo. Cancer Chemother Pharmacol. 2010 Mar;65(4):707-17.
• [13] TAS-119, a selective Aurora A inhibitor, enhanced the antitumor efficacy of taxanes in multiple human tumor cell lines including paclitaxel-resistant cells. Molecular Cancer Therapeutics. 01/2014; 12(11_Supplement):A268-A268.
• [14] Clinical pipeline report, company report or official report of VITRAC Therapeutics.
• [15] The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
• [16] Discovery of a new series of Aurora inhibitors through truncation of GSK1070916. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2552-5.
• [17] An integrated computational approach to the phenomenon of potent and selective inhibition of aurora kinases B and C by a series of 7-substituted in... J Med Chem. 2007 Aug 23;50(17):4027-37.
• [18] How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
• [19] Accurate prediction of the relative potencies of members of a series of kinase inhibitors using molecular docking and MM-GBSA scoring. J Med Chem. 2006 Aug 10;49(16):4805-8.