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

General Information of Drug (ID: DMI6KQM)

• Drug Name: GSK1059615 Drug Info
• Synonyms: KS-00001CUQ; CTK8F0346; HMS3654N17; BCP02498; AKOS026750445; NCGC00346509-01; FT-0669060

Indication

Disease Entry	ICD 11	Status	REF
Breast cancer	2C60-2C65	Discontinued in Phase 1	[1]
Endometrial cancer	2C76	Discontinued in Phase 1	[1]
Lymphoma	2A80-2A86	Discontinued in Phase 1	[1]

• Cross-matching ID:
  PubChem CID: 23582824
  ChEBI ID: CHEBI:71955
  CAS Number: CAS 958852-01-2
  TTD Drug ID: DMI6KQM

Molecule-Related Drug Atlas

Drug(s) Targeting PI3-kinase gamma (PIK3CG)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BAY 80-6946	DMLOS5R	Follicular lymphoma	2A80	Approved	[3]
IPI-145	DMWA24P	Follicular lymphoma	2A80	Approved	[4]
Buparlisib	DM1WEHC	Breast cancer	2C60-2C65	Phase 3	[2]
Enzastaurin	DM5H0R9	Diffuse large B-cell lymphoma	2A81	Phase 3	[5]
Rigosertib	DMOSTXF	Myelodysplastic syndrome	2A37	Phase 3	[6]
GDC-0032	DMT4QHD	Breast cancer	2C60-2C65	Phase 3	[5]
PQR309	DMMCYZ8	Squamous head and neck cell carcinom	2D60.0	Phase 2	[7]
SAR245409	DMQM7IL	Solid tumour/cancer	2A00-2F9Z	Phase 2	[8]
XL147	DMML7BE	Solid tumour/cancer	2A00-2F9Z	Phase 2	[8]
SF1126	DML10K3	Head and neck cancer	2D42	Phase 2	[9]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
PI3-kinase gamma (PIK3CG)	TTHBTOP	PK3CG_HUMAN	Inhibitor	[2]

References

• [1] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028447)
• [2] Targeting the phosphoinositide 3-kinase pathway in cancer. Nat Rev Drug Discov. 2009 Aug;8(8):627-44.
• [3] BAY 80-6946 is a highly selective intravenous PI3K inhibitor with potent p110 and p110 activities in tumor cell lines and xenograft models.Mol Cancer Ther.2013 Nov;12(11):2319-30.
• [4] PI3K-delta and PI3K-gamma inhibition by IPI-145 abrogates immune responses and suppresses activity in autoimmune and inflammatory disease models. Chem Biol. 2013 Nov 21;20(11):1364-74.
• [5] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [6] Phase I study of oral rigosertib (ON 01910.Na), a dual inhibitor of the PI3K and Plk1 pathways, in adult patients with advanced solid malignancies. Clin Cancer Res. 2014 Mar 15;20(6):1656-65.
• [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: 2155).
• [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: 2156).
• [9] An integrin-targeted, pan-isoform, phosphoinositide-3 kinase inhibitor, SF1126, has activity against multiple myeloma in vivo.Cancer Chemother Pharmacol.2013 Apr;71(4):867-81.