General Information of Drug (ID: DMXRPT6)

Drug Name
GSK1070916 Drug Info
Synonyms GSK-1070916
Indication
Disease Entry ICD 11 Status REF
Advanced solid tumour 2A00-2F9Z Phase 1 [1]
Cross-matching ID
PubChem CID
46885626
ChEBI ID
CHEBI:91362
CAS Number
CAS 942918-07-2
TTD Drug ID
DMXRPT6

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Clinical Trial Drug(s)
Discontinued Drug(s)
Investigative Drug(s)
Drug(s) Targeting Aurora kinase B (AURKB)
Drug Name Drug ID Indication ICD 11 Highest Status REF
AT9283 DMQ94CT Solid tumour/cancer 2A00-2F9Z Phase 3 [3]
PHA-739358 DMGYBZI Prostate cancer 2C82.0 Phase 2 [4]
VX-680 DM93YKJ Solid tumour/cancer 2A00-2F9Z Phase 2 [5]
ABT-348 DMMZOYN Haematological malignancy 2B33.Y Phase 2 [6]
HPP-607 DM5VSZR Solid tumour/cancer 2A00-2F9Z Phase 1 [7]
CYC116 DMUMHXT Solid tumour/cancer 2A00-2F9Z Phase 1 [8]
AMG 900 DMASGXJ Solid tumour/cancer 2A00-2F9Z Phase 1 [9]
SNS-314 DMAC5F2 Solid tumour/cancer 2A00-2F9Z Phase 1 [10]
BI-847325 DMY4B6J Solid tumour/cancer 2A00-2F9Z Phase 1 [11]
R763 DME0CJ9 Haematological malignancy 2B33.Y Phase 1 [12]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting Aurora kinase C (AURKC)
Drug Name Drug ID Indication ICD 11 Highest Status REF
PHA-739358 DMGYBZI Prostate cancer 2C82.0 Phase 2 [13]
ABT-348 DMMZOYN Haematological malignancy 2B33.Y Phase 2 [6]
HPP-607 DM5VSZR Solid tumour/cancer 2A00-2F9Z Phase 1 [7]
AMG 900 DMASGXJ Solid tumour/cancer 2A00-2F9Z Phase 1 [9]
SNS-314 DMAC5F2 Solid tumour/cancer 2A00-2F9Z Phase 1 [10]
GSK1070916A DMCJUI9 Solid tumour/cancer 2A00-2F9Z Phase 1 [2]
MK-6592 DMB5NOI Solid tumour/cancer 2A00-2F9Z Discontinued in Phase 1 [14]
Indirubin-3'-monoxime DMLRQH0 Discovery agent N.A. Investigative [15]
SU 6656 DMF1P6W Discovery agent N.A. Investigative [16]
6-bromoindirubin-3-oxime DM12WYV Discovery agent N.A. Investigative [15]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Aurora kinase B (AURKB) TT5LS6T AURKB_HUMAN Modulator [2]
Aurora kinase C (AURKC) TTLYXIT AURKC_HUMAN Modulator [2]

References

1 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. (Ligand id: 8358).
2 Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase. J Med Chem. 2010 May 27;53(10):3973-4001.
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 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 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.
7 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).
8 Clinical pipeline report, company report or official report of Cyclacel.
9 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.
10 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.
11 doi: 10.1158/1535-7163.TARG-13-B281
12 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.
13 Potent and selective Aurora inhibitors identified by the expansion of a novel scaffold for protein kinase inhibition. J Med Chem. 2005 Apr 21;48(8):3080-4.
14 Clinical experience with aurora kinase inhibitors: a review. Oncologist. 2009 Aug;14(8):780-93.
15 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.
16 The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315.