General Information of Drug (ID: DMM0LRE)

Drug Name
TGX-221 Drug Info
Synonyms TGX 221
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
9907093
ChEBI ID
CHEBI:91428
CAS Number
CAS 663619-89-4
TTD Drug ID
DMM0LRE

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Clinical Trial Drug(s)
Discontinued Drug(s)
Investigative Drug(s)
Approved Drug(s)
Drug(s) Targeting PI3-kinase beta (PIK3CB)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Buparlisib DM1WEHC Breast cancer 2C60-2C65 Phase 3 [4]
PQR309 DMMCYZ8 Squamous head and neck cell carcinom 2D60.0 Phase 2 [5]
PA-799 DMLSYJQ Colorectal cancer 2B91.Z Phase 1/2 [6]
AZD8186 DMWYF1H Solid tumour/cancer 2A00-2F9Z Phase 1 [7]
GSK2636771 DMCBGLW Prostate cancer 2C82.0 Phase 1 [8]
BAY 1082439 DMLRGX1 Solid tumour/cancer 2A00-2F9Z Phase 1 [9]
AZD6482 DMVP4E5 Thrombosis DB61-GB90 Terminated [10]
PP121 DMU8KTO Discovery agent N.A. Investigative [11]
PIK-75 DM9BQTX Discovery agent N.A. Investigative [12]
KU-0060648 DMQWS6U Discovery agent N.A. Investigative [13]
⏷ Show the Full List of 10 Drug(s)
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 [4]
Enzastaurin DM5H0R9 Diffuse large B-cell lymphoma 2A81 Phase 3 [16]
Rigosertib DMOSTXF Myelodysplastic syndrome 2A37 Phase 3 [17]
GDC-0032 DMT4QHD Breast cancer 2C60-2C65 Phase 3 [16]
PQR309 DMMCYZ8 Squamous head and neck cell carcinom 2D60.0 Phase 2 [18]
SAR245409 DMQM7IL Solid tumour/cancer 2A00-2F9Z Phase 2 [19]
XL147 DMML7BE Solid tumour/cancer 2A00-2F9Z Phase 2 [19]
SF1126 DML10K3 Head and neck cancer 2D42 Phase 2 [20]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [21]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [22]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [23]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [24]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [25]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [26]
Cupric Sulfate DMP0NFQ Fungal infection 1F29-1F2F Approved [27]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [28]
Nicotine DMWX5CO Lung cancer 2C25.0 Approved [29]
Tamibarotene DM3G74J T-cell leukaemia 2A90 Phase 3 [23]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [2]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [30]
Quercetin DM3NC4M Obesity 5B81 Approved [31]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [32]
Remdesivir DMBFZ6L Coronavirus Disease 2019 (COVID-19) 1D6Y Approved [33]
Acetic Acid, Glacial DM4SJ5Y infection in the ear canal AA0Y Approved [34]
Nefazodone DM4ZS8M Major depressive disorder 6A70.3 Approved [35]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [36]
Leflunomide DMR8ONJ Arthritis FA20 Approved [37]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [38]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Capivasertib DM9SKW8 Breast cancer 2C60-2C65 Approved [39]
Nicotine DMWX5CO Lung cancer 2C25.0 Approved [40]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [41]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [42]
Gefitinib DM15F0X Colon adenocarcinoma Approved [43]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [44]
Imiquimod DM1TMA3 Alopecia areata ED70.2 Approved [45]
Selenium DM25CGV N. A. N. A. Approved [46]
Methimazole DM25FL8 Hyperthyroidism 5A02 Approved [47]
Ribavirin DMEYLH9 Hepatitis C virus infection 1E51.1 Approved [48]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [41]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [22]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [49]
Methotrexate DM2TEOL Anterior urethra cancer Approved [50]
Cladribine DM3JDRP Hairy cell leukaemia 2A82.2 Approved [51]
Quercetin DM3NC4M Obesity 5B81 Approved [31]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [52]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [53]
Thalidomide DM70BU5 Adult T-cell leukemia/lymphoma Approved [54]
Testosterone DM7HUNW Hot flushes GA30 Approved [55]
⏷ 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
PI3-kinase beta (PIK3CB) TTTHBCA PK3CB_HUMAN Inhibitor [1]
PI3-kinase gamma (PIK3CG) TTHBTOP PK3CG_HUMAN Inhibitor [1]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Forkhead box protein O3 (FOXO3) OTHXQG4P FOXO3_HUMAN Protein Interaction/Cellular Processes [2]
Phosphatidylinositol 3,4,5-trisphosphate 3-phosphatase and dual-specificity protein phosphatase PTEN (PTEN) OTOWDUNT PTEN_HUMAN Drug Response [3]
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform (PIK3CB) OTO8JQJA PK3CB_HUMAN Drug Response [3]
RAC-alpha serine/threonine-protein kinase (AKT1) OT8H2YY7 AKT1_HUMAN Post-Translational Modifications [3]

References

1 PI 3-kinase p110beta: a new target for antithrombotic therapy. Nat Med. 2005 May;11(5):507-14.
2 Estrogen-mediated inactivation of FOXO3a by the G protein-coupled estrogen receptor GPER. BMC Cancer. 2015 Oct 15;15:702. doi: 10.1186/s12885-015-1699-6.
3 Functional characterization of an isoform-selective inhibitor of PI3K-p110 as a potential anticancer agent. Cancer Discov. 2012 May;2(5):425-33. doi: 10.1158/2159-8290.CD-12-0003. Epub 2012 Apr 12.
4 Targeting the phosphoinositide 3-kinase pathway in cancer. Nat Rev Drug Discov. 2009 Aug;8(8):627-44.
5 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: 2154).
6 The selective class I PI3K inhibitor CH5132799 targets human cancers harboring oncogenic PIK3CA mutations. Clin Cancer Res. 2011 May 15;17(10):3272-81.
7 National Cancer Institute Drug Dictionary (drug id 751594).
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. (Ligand id: 7967).
9 Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
10 Human target validation of phosphoinositide 3-kinase (PI3K)beta: effects on platelets and insulin sensitivity, using AZD6482 a novel PI3Kbeta inhibitor. J Thromb Haemost. 2012 Oct;10(10):2127-36.
11 Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol. 2008 Nov;4(11):691-9.
12 Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors. Bioorg Med Chem. 2007 Sep 1;15(17):5837-44.
13 1-substituted (Dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-ones endowed with dual DNA-PK/PI3-K inhibitory activity. J Med Chem. 2013 Aug 22;56(16):6386-401.
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 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
17 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.
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: 2155).
19 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).
20 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.
21 Cannabidiol Activates Neuronal Precursor Genes in Human Gingival Mesenchymal Stromal Cells. J Cell Biochem. 2017 Jun;118(6):1531-1546. doi: 10.1002/jcb.25815. Epub 2016 Dec 29.
22 DNA methylome-wide alterations associated with estrogen receptor-dependent effects of bisphenols in breast cancer. Clin Epigenetics. 2019 Oct 10;11(1):138. doi: 10.1186/s13148-019-0725-y.
23 Differential modulation of PI3-kinase/Akt pathway during all-trans retinoic acid- and Am80-induced HL-60 cell differentiation revealed by DNA microarray analysis. Biochem Pharmacol. 2004 Dec 1;68(11):2177-86.
24 Arsenic trioxide reduces the expression of E2F1, cyclin E, and phosphorylation of PI3K signaling molecules in acute leukemia cells. Environ Toxicol. 2021 Sep;36(9):1785-1792. doi: 10.1002/tox.23299. Epub 2021 May 27.
25 Integrating multiple omics to unravel mechanisms of Cyclosporin A induced hepatotoxicity in vitro. Toxicol In Vitro. 2015 Apr;29(3):489-501.
26 Human embryonic stem cell-derived test systems for developmental neurotoxicity: a transcriptomics approach. Arch Toxicol. 2013 Jan;87(1):123-43.
27 Physiological and toxicological transcriptome changes in HepG2 cells exposed to copper. Physiol Genomics. 2009 Aug 7;38(3):386-401.
28 Bringing in vitro analysis closer to in vivo: studying doxorubicin toxicity and associated mechanisms in 3D human microtissues with PBPK-based dose modelling. Toxicol Lett. 2018 Sep 15;294:184-192.
29 ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
30 Differential expression of FOXO1 and FOXO3a confers resistance to oxidative cell death upon endometrial decidualization. Mol Endocrinol. 2006 Oct;20(10):2444-55. doi: 10.1210/me.2006-0118. Epub 2006 May 18.
31 Quercetin and Its Fermented Extract as a Potential Inhibitor of Bisphenol A-Exposed HT-29 Colon Cancer Cells' Viability. Int J Mol Sci. 2023 Mar 15;24(6):5604. doi: 10.3390/ijms24065604.
32 Retinoic acid receptor alpha amplifications and retinoic acid sensitivity in breast cancers. Clin Breast Cancer. 2013 Oct;13(5):401-8.
33 An in vitro study on anti-carcinogenic effect of remdesivir in human ovarian cancer cells via generation of reactive oxygen species. Hum Exp Toxicol. 2022 Jan-Dec;41:9603271221089257. doi: 10.1177/09603271221089257.
34 Motexafin gadolinium and zinc induce oxidative stress responses and apoptosis in B-cell lymphoma lines. Cancer Res. 2005 Dec 15;65(24):11676-88.
35 Involvement of mitochondrial dysfunction in nefazodone-induced hepatotoxicity. Food Chem Toxicol. 2016 Aug;94:148-58. doi: 10.1016/j.fct.2016.06.001. Epub 2016 Jun 8.
36 Chronic occupational exposure to arsenic induces carcinogenic gene signaling networks and neoplastic transformation in human lung epithelial cells. Toxicol Appl Pharmacol. 2012 Jun 1;261(2):204-16.
37 Endoplasmic reticulum stress and MAPK signaling pathway activation underlie leflunomide-induced toxicity in HepG2 Cells. Toxicology. 2017 Dec 1;392:11-21.
38 Comparison of HepG2 and HepaRG by whole-genome gene expression analysis for the purpose of chemical hazard identification. Toxicol Sci. 2010 May;115(1):66-79.
39 Inhibition of cholesterol metabolism underlies synergy between mTOR pathway inhibition and chloroquine in bladder cancer cells. Oncogene. 2016 Aug 25;35(34):4518-28. doi: 10.1038/onc.2015.511. Epub 2016 Feb 8.
40 Nicotine-induced survival signaling in lung cancer cells is dependent on their p53 status while its down-regulation by curcumin is independent. Mol Cancer. 2010 Aug 20;9:220.
41 Role of miRNA in the regulation of cannabidiol-mediated apoptosis in neuroblastoma cells. Oncotarget. 2019 Jan 1;10(1):45-59. doi: 10.18632/oncotarget.26534. eCollection 2019 Jan 1.
42 -Carotene Induces Apoptosis in Human Esophageal Squamous Cell Carcinoma Cell Lines via the Cav-1/AKT/NF-B Signaling Pathway. J Biochem Mol Toxicol. 2016 Mar;30(3):148-57. doi: 10.1002/jbt.21773. Epub 2016 Jan 6.
43 Dihydromyricetin suppresses tumor growth via downregulation of the EGFR/Akt/survivin signaling pathway. J Biochem Mol Toxicol. 2023 Jun;37(6):e23328. doi: 10.1002/jbt.23328. Epub 2023 Feb 19.
44 Oxidative stress induces parallel autophagy and mitochondria dysfunction in human glioma U251 cells. Toxicol Sci. 2009 Aug;110(2):376-88. doi: 10.1093/toxsci/kfp101. Epub 2009 May 18.
45 Effect of toll-like receptor 7 and 9 targeted therapy to prevent the development of hepatocellular carcinoma. Liver Int. 2015 Mar;35(3):1063-76. doi: 10.1111/liv.12626. Epub 2014 Jul 30.
46 Selenium and vitamin E: cell type- and intervention-specific tissue effects in prostate cancer. J Natl Cancer Inst. 2009 Mar 4;101(5):306-20.
47 Low-expressional IGF1 mediated methimazole-induced liver developmental toxicity in fetal mice. Toxicology. 2018 Sep 1;408:70-79. doi: 10.1016/j.tox.2018.07.004. Epub 2018 Jul 7.
48 Ribavirin augments doxorubicin's efficacy in human hepatocellular carcinoma through inhibiting doxorubicin-induced eIF4E activation. J Biochem Mol Toxicol. 2018 Jan;32(1). doi: 10.1002/jbt.22007. Epub 2017 Nov 7.
49 Astaxanthin protects mesenchymal stem cells from oxidative stress by direct scavenging of free radicals and modulation of cell signaling. Chem Biol Interact. 2021 Jan 5;333:109324. doi: 10.1016/j.cbi.2020.109324. Epub 2020 Nov 17.
50 The contribution of methotrexate exposure and host factors on transcriptional variance in human liver. Toxicol Sci. 2007 Jun;97(2):582-94.
51 Comparative effects of retinoic acid, vitamin D and resveratrol alone and in combination with adenosine analogues on methylation and expression of phosphatase and tensin homologue tumour suppressor gene in breast cancer cells. Br J Nutr. 2012 Mar;107(6):781-90. doi: 10.1017/S0007114511003631. Epub 2011 Aug 1.
52 Phenotypic characterization of retinoic acid differentiated SH-SY5Y cells by transcriptional profiling. PLoS One. 2013 May 28;8(5):e63862.
53 Arsenic trioxide inhibits the proliferation of myeloma cell line through notch signaling pathway. Cancer Cell Int. 2013 Mar 13;13(1):25. doi: 10.1186/1475-2867-13-25.
54 Mechanism of thalidomide to enhance cytotoxicity of temozolomide in U251-MG glioma cells in vitro. Chin Med J (Engl). 2009 Jun 5;122(11):1260-6.
55 The exosome-like vesicles derived from androgen exposed-prostate stromal cells promote epithelial cells proliferation and epithelial-mesenchymal transition. Toxicol Appl Pharmacol. 2021 Jan 15;411:115384. doi: 10.1016/j.taap.2020.115384. Epub 2020 Dec 25.