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

General Information of Drug (ID: DMT4QHD)

• Drug Name: GDC-0032 Drug Info
• Synonyms: Taselisib; 1282512-48-4; GDC 0032; UNII-L08J2O299M; 2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)-1H-pyrazol-1-yl)-2-methylpropanamide; CHEMBL2387080; GDC0032; L08J2O299M; Taselisib [INN]; 2-Methyl-2-(4-{2-[3-Methyl-1-(Propan-2-Yl)-1h-1,2,4-Triazol-5-Yl]-5,6-Dihydroimidazo[1,2-D][1,4]benzoxazepin-9-Yl}-1h-Pyrazol-1-Yl)propanamide; Taselisib [USAN:INN]; GTPL7794; SCHEMBL1485247; SYN1202; DTXSID00155842; BEUQXVWXFDOSAQ-UHFFFAOYSA-N

Indication

Disease Entry	ICD 11	Status	REF
Breast cancer	2C60-2C65	Phase 3	[1]
Solid tumour/cancer	2A00-2F9Z	Phase 2/3	[2]

• Cross-matching ID:
  PubChem CID: 51001932
  CAS Number: CAS 1282512-48-4
  TTD Drug ID: DMT4QHD

Molecule-Related Drug Atlas

Drug(s) Targeting PI3-kinase alpha (PIK3CA)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BAY 80-6946	DMLOS5R	Follicular lymphoma	2A80	Approved	[4]
Alpelisib	DMEXMYK	Breast cancer	2C60-2C65	Approved	[5]
Buparlisib	DM1WEHC	Breast cancer	2C60-2C65	Phase 3	[6]
LY3023414	DMD9KYF	Prostate cancer	2C82.0	Phase 2	[7]
PA-799	DMLSYJQ	Colorectal cancer	2B91.Z	Phase 1/2	[8]
MLN1117	DMCVBQD	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[9]
PWT-33597	DMJY15D	Solid tumour/cancer	2A00-2F9Z	Phase 1	[10]
BLY719	DMYHNV3	Solid tumour/cancer	2A00-2F9Z	Phase 1	[11]
HHCYH33	DMRQ4L6	Breast cancer	2C60-2C65	Phase 1	[12]
LY3849524	DM8I68X	Breast cancer	2C60-2C65	Phase 1	[13]

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	[14]
IPI-145	DMWA24P	Follicular lymphoma	2A80	Approved	[15]
Buparlisib	DM1WEHC	Breast cancer	2C60-2C65	Phase 3	[6]
Enzastaurin	DM5H0R9	Diffuse large B-cell lymphoma	2A81	Phase 3	[1]
Rigosertib	DMOSTXF	Myelodysplastic syndrome	2A37	Phase 3	[16]
PQR309	DMMCYZ8	Squamous head and neck cell carcinom	2D60.0	Phase 2	[17]
SAR245409	DMQM7IL	Solid tumour/cancer	2A00-2F9Z	Phase 2	[18]
XL147	DMML7BE	Solid tumour/cancer	2A00-2F9Z	Phase 2	[18]
SF1126	DML10K3	Head and neck cancer	2D42	Phase 2	[19]
PF-05212384	DMBL3VD	Solid tumour/cancer	2A00-2F9Z	Phase 2	[20]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
PI3-kinase alpha (PIK3CA)	TTEUNMR	PK3CA_HUMAN	Modulator	[3]
PI3-kinase gamma (PIK3CG)	TTHBTOP	PK3CG_HUMAN	Inhibitor	[1]

References

• [1] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [2] 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: 7794).
• [3] Company report (BioOncology)
• [4] 2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85.
• [5] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [6] Targeting the phosphoinositide 3-kinase pathway in cancer. Nat Rev Drug Discov. 2009 Aug;8(8):627-44.
• [7] Company report (Lilly)
• [8] The selective class I PI3K inhibitor CH5132799 targets human cancers harboring oncogenic PIK3CA mutations. Clin Cancer Res. 2011 May 15;17(10):3272-81.
• [9] National Cancer Institute Drug Dictionary (drug id 714372).
• [10] Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
• [11] In vitro anticancer activity of PI3K alpha selective inhibitor BYL719 in head and neck cancer. Anticancer Res. 2015 Jan;35(1):175-82.
• [12] Adaptive resistance to PI3Kalpha-selective inhibitor CYH33 is mediated by genomic and transcriptomic alterations in ESCC cells. Cell Death Dis. 2021 Jan 14;12(1):85.
• [13] ClinicalTrials.gov (NCT05307705) A Study of LOXO-783 Administered as Monotherapy and in Combination With Anticancer Therapies for Patients With Advanced Breast Cancer and Other Solid Tumors With a PIK3CA H1047R Mutation. U.S.National Institutes of Health.
• [14] 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.
• [15] 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.
• [16] 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.
• [17] 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).
• [18] 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).
• [19] 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.
• [20] First-in-Human Study of PF-05212384 (PKI-587), a Small-Molecule, Intravenous, Dual Inhibitor of PI3K and mTOR in Patients with Advanced Cancer. Clin Cancer Res. 2015 Apr 15;21(8):1888-95.