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

General Information of Drug (ID: DM8RJTB)

• Drug Name: LY3295668 Drug Info
• Synonyms: 1919888-06-4; (2R,4R)-1-(3-Chloro-2-fluorobenzyl)-4-((3-fluoro-6-((5-methyl-1H-pyrazol-3-yl)amino)pyridin-2-yl)methyl)-2-methylpiperidine-4-carboxylic acid; AK-01; LY-3295668; (2R,4R)-1-[(3-chloro-2-fluorophenyl)methyl]-4-({3-fluoro-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyridin-2-yl}methyl)-2-methylpiperidine-4-carboxylic acid; UNII-1WX8O5XV4R; 1WX8O5XV4R; SCHEMBL17747406; NSC816863; NSC-816863; Aurora A kinase inhibitor LY3295668; HY-114258; CS-0080775; LY3295668 (AK-01); A16869; (2R,4R)-1-[(3-Chloro-2-fluoro-phenyl)methyl]-4-[[3-fluoro-6-[(5-methyl-1H-pyrazol-3-yl)amino]-2-pyridyl]methyl]-2-methyl-piperidine-4-carboxylic acid; 1-((3-Chloro-2-fluorophenyl)methyl)-4-((3-fluoro-6-((5-methyl-1H-pyrazol-3-yl)amino)-2-pyridinyl)methyl)-2-methyl-, (2R,4R)-,4-piperidinecarboxylic acid; 4-Piperidinecarboxylic acid, 1-((3-chloro-2-fluorophenyl)methyl)-4-((3-fluoro-6-((5-methyl-1H-pyrazol-3-yl)amino)-2-pyridinyl)methyl)-2-methyl-, (2R,4R)-; EG7

Indication

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

• Cross-matching ID:
  PubChem CID: 121333423
  CAS Number: CAS 1919888-06-4
  TTD Drug ID: DM8RJTB

Molecule-Related Drug Atlas

Drug(s) Targeting Aurora kinase A (AURKA)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
AT9283	DMQ94CT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[3]
MLN8237	DMO8PT9	Solid tumour/cancer	2A00-2F9Z	Phase 3	[4]
PHA-739358	DMGYBZI	Prostate cancer	2C82.0	Phase 2	[5]
VX-680	DM93YKJ	Solid tumour/cancer	2A00-2F9Z	Phase 2	[6]
ABT-348	DMMZOYN	Haematological malignancy	2B33.Y	Phase 2	[7]
ENMD-2076	DMJZVPB	Acute myeloid leukaemia	2A60	Phase 2	[5]
HPP-607	DM5VSZR	Solid tumour/cancer	2A00-2F9Z	Phase 1	[8]
MLN8054	DMUANF3	Solid tumour/cancer	2A00-2F9Z	Phase 1	[6]
CYC116	DMUMHXT	Solid tumour/cancer	2A00-2F9Z	Phase 1	[9]
AMG 900	DMASGXJ	Solid tumour/cancer	2A00-2F9Z	Phase 1	[10]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Aurora kinase A (AURKA)	TTPS3C0	AURKA_HUMAN	Inhibitor	[2]

References

• [1] ClinicalTrials.gov (NCT03092934) A Study of AK-01 (LY3295668) in Solid Tumors. U.S. National Institutes of Health.
• [2] 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.
• [3] 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.
• [4] 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.
• [5] Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66.
• [6] 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.
• [7] 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.
• [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: 1936).
• [9] Clinical pipeline report, company report or official report of Cyclacel.
• [10] 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.