m6A-centered Crosstalk Information

Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
Crosstalk ID
M6ACROT05249
 [1], [2]
Non-coding RNA hsa_Circ_0072309 miR-607  lncRNA       miRNA   circRNA Indirect Enhancement m6A modification USP7 USP7 FTO Demethylation : m6A sites
m6A Modification:
m6A Regulator Fat mass and obesity-associated protein (FTO) ERASER
 Regulator Info 
m6A Target Ubiquitin carboxyl-terminal hydrolase 7 (USP7)
 Targert Gene 
Epigenetic Regulation that have Cross-talk with This m6A Modification:
Epigenetic Regulation Type Non-coding RNA (ncRNA)
Epigenetic Regulator hsa_circ_0072309 (Circ_LIFR) circRNA View Details
Regulated Target hsa-miR-607 View Details
Crosstalk Relationship ncRNA  →  m6A Enhancement
Crosstalk Mechanism ncRNAs indirectly impacts m6A modification through downstream signaling pathways
Crosstalk Summary Circ_LIFR interacted with hsa-miR-607 via its miRNA response element to upregulate the expression of FTO, an m6A demethylase and downstream target of miR-607, thus promoting tumorigenesis of NSCLC.The m6A demethylase FTO promotes the growth of Non-small cell lung cancer cells by increasing the expression of USP7.Genetic knockdown or pharmacological inhibition (P5091 or P22027) of Ubiquitin carboxyl-terminal hydrolase 7 (USP7) reduced the proliferation rate of lung cancer cells and decreased the capacity of colony formation of lung cancer cells in vitro, whereas lung cancer cells growth inhibition by FTO knockdown is restored by overexertion of USP7.
Responsed Disease Non-small cell lung cancer ICD-11: 2C25.Y
 Disease Info 
Responsed Drug P5091
 Drug Info 
Cell Process Ubiquitination degradation
In-vitro Model
 A-549 Lung adenocarcinoma Homo sapiens CVCL_0023
RERF-LC-A1 Lung squamous cell carcinoma Homo sapiens CVCL_4402
NCI-H1882 Lung small cell carcinoma Homo sapiens CVCL_1504
NCI-H522 Lung adenocarcinoma Homo sapiens CVCL_1567
HSAEC (Human small airway epithelial cells)
In-vivo Model Equal numbers of A549 cells expressing either control or shFTO were injected subcutaneously, within 30 min of harvesting, over the right and left flanks in male nu/nu mice between 4 and 6 weeks of age.
Full List of Potential Compound(s) Related to This m6A-centered Crosstalk
Ubiquitin carboxyl-terminal hydrolase 7 (USP7) 7 Compound(s) Regulating the Target Click to Show/Hide the Full List
 Compound Name PMID26077642-Compound-Vif2 Patented [3]
MOA Inhibitor
External Link
TTD: D03EML
 Compound Name PMID26077642-Compound-Vif1 Patented [3]
MOA Inhibitor
External Link
TTD: D0PT1W
 Compound Name ADC-03 Preclinical [4]
MOA Inhibitor
External Link
TTD: D0AN9V
 Compound Name P22077 Preclinical [5]
Synonyms
1247819-59-5; P 22077; 1-[5-(2,4-Difluoro-phenylsulfanyl)-4-nitro-thiophen-2-yl]-ethanone; CHEMBL2159498; 1-[5-(2,4-difluorophenyl)sulfanyl-4-nitrothiophen-2-yl]ethanone; 1-[5-[(2,4-Difluorophenyl)thio]-4-nitro-2-thienyl]-ethanone; 1-(5-(2,4-difluorophenylthio)-4-nitrothiophen-2-yl)ethanone; P-22077; 1-(5-((2,4-Difluorophenyl)thio)-4-nitrothiophen-2-yl)ethanone; 1-{5-[(2,4-Difluorophenyl)sulfanyl]-4-nitrothiophen-2-yl}ethan-1-one; C12H7F2NO3S2; SCHEMBL2680945; DTXSID40677376; HMS3653G09; BCP07858; EX-A1445; 1-(5-((2,4-difluorophenyl)thio)-4-nitrothiophen-2-yl)ethan-1-one; 2624AH; BDBM50393440; MFCD22580421; s7133; ZINC91696068; AKOS024458186; CCG-267643; CS-1860; QC-8199; AC-32695; AK313221; AS-55923; DA-46729; HY-13865; AB0003913; FT-0707469; SW219709-1; EC-000.2542; J3.502.624J; Z1646327284; 1-[5-(2,4-difluorophenyl)sulfanyl-4-nitro-2-thienyl]ethanone; 1-[5-[(2,4-Difluorophenyl)thio]-4-nitro-2-thienyl]ethanon; 1-(5-((2,4-difluorophenyl)thio)-4-nitrothiophen-2-yl) ethanone
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 46931953
TTD: D2K6DU
 Compound Name HBX19818 Preclinical [6]
Synonyms
HBX 19818; 1426944-49-1; CHEMBL2398213; 9-Chloro-5,6,7,8-tetrahydro-N-[3-[methyl(phenylmethyl)amino]propyl]-2-acridinecarboxamide; N-(3-(benzyl(methyl)amino)propyl)-9-chloro-5,6,7,8-tetrahydroacridine-2-carboxamide; N-[3-[benzyl(methyl)amino]propyl]-9-chloro-5,6,7,8-tetrahydroacridine-2-carboxamide; SCHEMBL20007093; BDBM50436150; HBX-19818; NCGC00378705-01; HY-17540; J3.502.626F
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 73349008
TTD: DA0OZ2
 Compound Name ADC-01 Preclinical [4]
MOA Inhibitor
External Link
TTD: DRJU35
 Compound Name P5091 Preclinical [7]
Synonyms
882257-11-6; P005091; 1-(5-(2,3-dichlorophenylthio)-4-nitrothiophen-2-yl)ethanone; P-5091; 1-[5-(2,3-Dichloro-phenylsulfanyl)-4-nitro-thiophen-2-yl]-ethanone; CHEMBL2159495; P5091 (P005091); 1-[5-(2,3-dichlorophenyl)sulfanyl-4-nitrothiophen-2-yl]ethanone; 1-(5-((2,3-Dichlorophenyl)thio)-4-nitrothiophen-2-yl)ethanone; Cyto5D7; C12H7Cl2NO3S2; SCHEMBL2681288; DTXSID90384841; 1-[5-[(2,3-Dichlorophenyl)thio]-4-nitro-2-thienyl]ethanone; HMS3653E09; HMS3743M19; ZINC125366; BCP07750; EX-A2120; BDBM50393437; MFCD00123202; s7132; AKOS024458314; CCG-240421; CS-1445; MCULE-6661883192; QC-8200; SB19505; AC-32692; AK270202; BS-17872; DA-40897; HY-15667; FT-0714931; SW219710-1; Y1893; J3.502.625H; P 5091; P-05091; P005091(P5091); P 005091; P-005091; 1-[5-(2,3-dichlorophenyl)sulfanyl-4-nitro-2-thienyl]ethanone; 1-[5-(2,3-dichlorophenylsulfanyl)-4-nitro-2-thienyl]ethanone; 1-[5-[(2,3-Dichlorophenyl)thio]-4-n?itro-2-thienyl]ethanone; 1-{5-[(2,3-Dichlorophenyl)sulfanyl]-4-nitrothiophen-2-yl}ethan-1-one
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 2819993
TTD: DV3KC5
2C25: Lung cancer 52 Compound(s) Regulating the Disease Click to Show/Hide the Full List
 Compound Name Adagrasib Approved [8]
Synonyms
2326521-71-3; MRTX-849; UNII-8EOO6HQF8Y; 8EOO6HQF8Y; 2-((S)-4-(7-(8-Chloronaphthalen-1-yl)-2-(((S)-1-methylpyrrolidin-2-yl)methoxy)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)-1-(2-fluoroacryloyl)piperazin-2-yl)acetonitrile; CHEMBL4594350; SCHEMBL20974691; GTPL10888; Kras G12C inhibitor MRTX849; BCP31538; EX-A3258; MRTX 849; MFCD32263433; s8884; compound 20 [PMID: 32250617]; BS-16211; HY-130149; CS-0105265; 2-Piperazineacetonitrile, 4-(7-(8-chloro-1-naphthalenyl)-5,6,7,8-tetrahydro-2-(((2S)-1-methyl-2-pyrrolidinyl)methoxy)pyrido(3,4-d)pyrimidin-4-yl)-1-(2-fluoro-1-oxo-2-propen-1-yl)-, (2S)-
    Click to Show/Hide
External Link
CID: 138611145
TTD: DUQV41
 Compound Name Amivantamab Approved [9]
External Link
TTD: DQ5X1Z
 Compound Name Mobocertinib Approved [10]
Synonyms
1847461-43-1; TAK-788; TAK788; AP32788; UNII-39HBQ4A67L; 39HBQ4A67L; propan-2-yl 2-[4-{[2-(dimethylamino)ethyl](methyl)amino}-2-methoxy-5-(prop-2-enamido)anilino]-4-(1-methyl-1H-indol-3-yl)pyrimidine-5-carboxylate; Mobocertinib [INN]; Mobocertinib [USAN]; AP-32788; Mobocertinib (TAK788); Mobocertinib(TAK-788); SCHEMBL17373133; GTPL10468; BDBM368374; BCP31045; EX-A3392; US10227342, Example 10; MFCD32669806; NSC825519; s6813; TAK-788;AP32788; WHO 11183; NSC-825519; example 94 [WO2015195228A1]; HY-135815; CS-0114256; TAK-788;TAK 788; AP 32788; 5-Pyrimidinecarboxylic acid, 2-((4-((2-(dimethylamino)ethyl)methylamino)-2-methoxy-5-((1-oxo-2-propen-1-yl)amino)phenyl)amino)-4-(1-methyl-1H-indol-3-yl)-, 1-methylethyl ester; C(C=C)(=O)NC=1C(=CC(=C(C=1)NC1=NC=C(C(=N1)C1=CN(C2=CC=CC=C12)C)C(=O)OC(C)C)OC)N(C)CCN(C)C; Isopropyl 2-((5-acrylamido-4-((2-(dimethylamino)ethyl)(methyl)amino)-2-methoxyphenyl)amino)-4-(1-methyl-1H-indol-3-yl)pyrimidine-5-carboxylate; Isopropyl 2-(5-acrylamido-4-((2-(dimethylamino)ethyl)(methyl)amino)-2-methoxyphenylamino)-4-(1-methyl-1H-indol-3-yl)pyrimidine-5-carboxylate; Propan-2-yl 2-(5-(acryloylamino)-4-((2-(dimethylamino)ethyl)(methyl)amino)-2-methoxyanilino)-4-(1-methyl-1H-indol-3-yl)pyrimidine-5-carboxylate; propan-2-yl 2-[4-[2-(dimethylamino)ethyl-methylamino]-2-methoxy-5-(prop-2-enoylamino)anilino]-4-(1-methylindol-3-yl)pyrimidine-5-carboxylate
    Click to Show/Hide
External Link
CID: 118607832
TTD: DI4HA7
 Compound Name Sugemalimab Approved in China [11]
External Link
TTD: DDZ48Y
 Compound Name Sacituzumab govitecan Approved [12]
Synonyms
1491917-83-9; 1535963-91-7; 1796566-95-4; CYSTEINYL CL2A-SN-38; DA64T2C2IO; DTXSID401335985; EX-A4354; F82944; GOVITECAN CYSTEINYL CONJUGATE; hRS 7SN38; hRS7-SN38; IMMU 132; IMMU-132; M9BYU8XDQ6; Sacituzumab govitecan; Sacituzumab govitecan [USAN]; sacituzumab-govitecan; Satralizumab linker; SN-38 CYSTEINYL CONJUGATE; UNII-M9BYU8XDQ6
    Click to Show/Hide
External Link
CID: 91668186
TTD: D8LAE2
 Compound Name Atezolizumab Approved [13]
External Link
TTD: D0YM2K
 Compound Name Tepotinib Approved [14]
Synonyms
1100598-32-0; EMD 1214063; UNII-1IJV77EI07; Tepotinib (EMD 1214063); EMD1214063; 1IJV77EI07; MSC-2156119J; Benzonitrile, 3-[1,6-dihydro-1-[[3-[5-[(1-methyl-4-piperidinyl)methoxy]-2-pyrimidinyl]phenyl]methyl]-6-oxo-3-pyridazinyl]-; C29H28N6O2; Tepotinib [INN]; Benzonitrile, 3-[1,6-Dihydro-1-[[3-[5-[(1-Methyl-4-Piperidinyl)Methoxy]-2-PyriMidinyl]Phenyl]Methyl]-6-Oxo-3-Pyridazinyl]; Benzonitrile, 3-(1,6-dihydro-1-((3-(5-((1-methyl-4-piperidinyl)methoxy)-2-pyrimidinyl)phenyl)methyl)-6-oxo
    Click to Show/Hide
External Link
CID: 25171648
TTD: D0R8QG
DrugBank: DB15133
 Compound Name Sotorasib Approved [15]
Synonyms
AMG-510; AMG510; AMG-510 racemate; 2252403-56-6; AMG 510; Kras G12C inhibitor 9; 2296729-00-3; UNII-2B2VM6UC8G; 2B2VM6UC8G; CHEMBL4535757; 2296729-00-3 (racemate); 4-((S)-4-Acryloyl-2-methylpiperazin-1-yl)-6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(2-isopropyl-4-methylpyridin-3-yl)pyrido[2,3-d]pyrimidin-2(1H)-one; 6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-propan-2-ylpyridin-3-yl)-4-[(2S)-2-methyl-4-prop-2-enoylpiperazin-1-yl]pyrido[2,3-d]pyrimidin-2-one; Sotorasib [INN]; 6-Fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-propan-2-ylpyridin-3-yl)-4-((2S)-2-methyl-4-prop-2-enoylpiperazin-1-yl)pyrido(2,3-d)pyrimidin-2-one; AMG510 racemate; Sotorasib [USAN]; AMG-510(racemate); Kras mutant-targeting AMG 510; SCHEMBL20560375; GTPL10678; AMG 510 pound>>AMG-510; AMY16918; BCP30452; BCP33368; EX-A3538; BDBM50514402; NSC818433; s8830; WHO 11370; DB15569; NSC-818433; BS-16684; HY-114277; CS-0081316; compound (R)-38 [PMID: 31820981]; (1m)-6-Fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-(propan-2-yl)pyridin-3-yl)-4-((2S)-2-methyl-4-(prop-2-enoyl)piperazin-1-yl)pyrido(2,3-d)pyrimidin-2(1H)-one; (1S)-4-((S)-4-Acryloyl-2-methylpiperazin-1-yl)-6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(2-isopropyl-4-methylpyridin-3-yl)pyrido[2,3-d]pyrimidin-2(1H)-one; 2296729-66-1; Pyrido(2,3-d)pyrimidin-2(1H)-one, 6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-(1-methylethyl)-3-pyridinyl)-4-((2S)-2-methyl-4-(1-oxo-2-propen-1-yl)-1-piperazinyl)-
    Click to Show/Hide
External Link
CID: 137278711
TTD: D0R7LD
DrugBank: DB15569
 Compound Name Entrectinib Approved [16]
Synonyms
1108743-60-7; RXDX-101; UNII-L5ORF0AN1I; Entrectinib (RXDX-101); L5ORF0AN1I; Benzamide, N-[5-[(3,5-difluorophenyl)methyl]-1H-indazol-3-yl]-4-(4-methyl-1-piperazinyl)-2-[(tetrahydro-2H-pyran-4-yl)amino]-; Benzamide, N-(5-((3,5-difluorophenyl)methyl)-1H-indazol-3-yl)-4-(4-methyl-1-piperazinyl)-2-((tetrahydro-2H-pyran-4-yl)amino)-; Entrectinib [USAN:INN]; YMX; Kinome_2659; Entrectinib(rxdx-101); Entrectinib (USAN/INN); SCHEMBL3512601; GTPL8290; CHEMBL1983268; KS-00000TSK
    Click to Show/Hide
External Link
CID: 25141092
TTD: D0O0LS
DrugBank: DB11986
 Compound Name Repotrectinib Approved [17]
Synonyms
FIKPXCOQUIZNHB-RRKGBCIJSA-N; SCHEMBL20438940; TPX 0005; BCP19778
    Click to Show/Hide
External Link
CID: 135565923
TTD: D05NFR
 Compound Name MYL-1402O Phase 3 [18]
Synonyms
bevacizumab biosimilar
    Click to Show/Hide
External Link
TTD: DYH3Q6
 Compound Name AB154 Phase 3 [19]
Synonyms
Domvanalimab
    Click to Show/Hide
External Link
TTD: DT1FS0
 Compound Name Datopotamab deruxtecan Phase 3 [20]
External Link
TTD: DP41HV
 Compound Name CS1001 Phase 3 [21]
External Link
TTD: D3MP1S
 Compound Name JDQ443 Phase 3 [22]
Synonyms
(S)-JDQ-443; 1-(6-((4S)-4-(5-Chloro-6-methyl-1H-indazol-4-yl)-5-methyl-3-(1-methyl-1H-indazol-5-yl)-1H-pyrazol-1-yl)-2-azaspiro[3.3]heptan-2-yl)prop-2-en-1-one; 1-[6-[(4R)-4-(5-chloro-6-methyl-1H-indazol-4-yl)-5-methyl-3-(1-methyl-1H-inda zol-5-yl)-1H-pyrazol-1-yl]-2-azaspiro[3.3]hept-2-yl]- 2-Propen-1-one; 1-[6-[(4R)-4-(5-Chloro-6-methyl-1H-indazol-4-yl)-5-methyl-3-(1-methyl-1H-indazol-5-yl)-1H-pyrazol-1-yl]-2-azaspiro[3.3]hept-2-yl]-2-propen-1-one; 1-[6-[4-(5-chloro-6-methyl-1H-indazol-4-yl)-5-methyl-3-(1-methylindazol-5-yl)pyrazol-1-yl]-2-azaspiro[3.3]heptan-2-yl]prop-2-en-1-one; 1-{6-[(4M)-4-(5-chloro-6-methyl-1H-indazol-4-yl)-5- methyl-3-(1-methyl-1H-indazol-5-yl)-1H-pyrazol-1-yl]-2- azaspiro[3.3]heptan-2-yl}prop-2-en-1-one; 1-{6-[(4M)-4-(5-Chloro-6-methyl-1H-indazol-4-yl)-5-methyl-3-(1-methyl-1H-indazol-5-yl)-1H-pyrazol-1-yl]-2-azaspiro[3.3]heptan-2-yl}prop-2-en-1-one; 2653994-08-0; 2653994-10-4; 2-Propen-1-one, 1-[6-[(4R)-4-(5-chloro-6-methyl-1H-indazol-4-yl)-5-methyl-3-(1-methyl-1H-indazol-5-yl)-1H-pyrazol-1-yl]-2-azaspiro[3.3]hept-2-yl]-; AKOS040757949; AT36708; BDBM50579985; CHEMBL5077861; compound 5 [PMID: 35404998]; CS-0226220; CS-0311034; EX-A5693; example 1a [WO2021120890A1]; GLXC-25533; GTPL11715; HY-139612A; JDQ 443; JDQ 443 [WHO-DD]; JDQ443; JDQ-443; MS-29737; NSC846146; NSC-846146; NVP-JDQ443; NVP-JDQ-443; Opnurasib; opnurasib [INN]; -PROPEN-1-ONE, 1-(6-((4R)-4-(5-CHLORO-6-METHYL-1H-INDAZOL-4-YL)-5-METHYL-3-(1-METHYL-1H-INDAZOL-5-YL)-1H-PYRAZOL-1-YL)-2-AZASPIRO(3.3)HEPT-2-YL)-; Q3W0H3V1LQ; SCHEMBL23533580
    Click to Show/Hide
External Link
CID: 156501355
TTD: D37IQM
 Compound Name TRS003 Phase 3 [23]
External Link
TTD: D2KVG4
 Compound Name Tusamitamab ravtansine Phase 3 [24]
Synonyms
SAR408701
    Click to Show/Hide
External Link
TTD: D2D6NJ
 Compound Name RG6058 Phase 3 [25]
Synonyms
Tiragolumab
    Click to Show/Hide
External Link
TTD: D0L4VD
 Compound Name GSK4069889 Phase 2 [26]
Synonyms
TSR-022
    Click to Show/Hide
External Link
TTD: DZW53X
 Compound Name APL-101 Phase 2 [27]
Synonyms
Bozitinib; PLB-1001; 1440964-89-5; Vebreltinib; Vebreltinib [USAN]; UNII-2WZP8A9VFN; 2WZP8A9VFN; Bozitinib (PLB-1001); SCHEMBL15594471; BDBM107096; CBI-3103; s6762; WHO 11677; HY-125017; CS-0088607; US9695175, 44; 1,2,4-Triazolo(4,3-b)pyridazine, 6-(1-cyclopropyl-1H-pyrazol-4-yl)-3-(difluoro(6- fluoro-2-methyl-2H-indazol-5-yl)methyl)-; 6-(1-Cyclopropyl-1H-pyrazol-4-yl)-3-(difluoro(6-fluoro-2-methyl-2H-indazol-5- yl)methyl)-1,2,4-triazolo(4,3-b)pyridazine
    Click to Show/Hide
External Link
CID: 72202701
TTD: DV3Y7F
 Compound Name SGN-LIV1A Phase 2 [28]
Synonyms
Ladiratuzumab Vedotin
    Click to Show/Hide
External Link
TTD: DS6B1L
 Compound Name BNT116 Phase 2 [29]
External Link
TTD: DR39GZ
 Compound Name AZD7789 Phase 2 [30]
External Link
TTD: DNI7E3
 Compound Name L-DOS47 Phase 1/2 [31]
External Link
TTD: DN3Z5D
 Compound Name NC318 Phase 2 [32]
External Link
TTD: D9UZ5Q
 Compound Name Vorolanib Phase 2 [33]
Synonyms
UNII-YP8G3I74EL; YP8G3I74EL; 1013920-15-4; (S,Z)-N-(1-(Dimethylcarbamoyl)pyrrolidin-3-yl)-5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide; Vorolanib [INN]; SCHEMBL2439528; CHEMBL4297587; N-((3S)-1-(dimethylcarbamoyl)pyrrolidin-3-yl)-5-((Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide; s6843; DB15247; HY-109019; CS-0030517; Q27294638; 1H-Pyrrole-3-carboxamide, N-((3S)-1-((dimethylamino)carbonyl)-3-pyrrolidinyl)-5-((Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl)-2,4-dimethyl-
    Click to Show/Hide
External Link
CID: 59215954
TTD: D8AG3S
DrugBank: DB15247
 Compound Name Xofigo Phase 2 [34]
External Link
TTD: D6B7FP
 Compound Name Bintrafusp alfa Phase 2 [35]
External Link
TTD: D5J3BL
 Compound Name Voyager-V1 Phase 2 [36]
Synonyms
VSV-IFNBeta-NIS
    Click to Show/Hide
External Link
TTD: D4AGB6
 Compound Name AB-106 Phase 2 [37]
Synonyms
DS6051b; GTPL11198; AB106
    Click to Show/Hide
External Link
CID: 154699459
TTD: D2KV8B
 Compound Name RO-5126766 Phase 2 [38]
Synonyms
VS-6766; CH-5126766; Dual Raf/MEK protein kinase inhibitor (cancer), Roche
    Click to Show/Hide
External Link
CID: 16719221
TTD: D0M6BD
DrugBank: DB15254
 Compound Name TC-210 Phase 1/2 [39]
External Link
TTD: DX6O9V
 Compound Name EMB-01 Phase 1/2 [40]
External Link
TTD: DWQ6J1
 Compound Name NM21-1480 Phase 1/2 [41]
External Link
TTD: DUVH60
 Compound Name MRx0518 Phase 1/2 [42]
External Link
TTD: DP4J2K
 Compound Name DZD9008 Phase 1/2 [43]
External Link
TTD: DM8Y2N
 Compound Name BGB-A425 Phase 1/2 [44]
External Link
TTD: D7UIZ1
 Compound Name Rilvegostomig Phase 1/2 [45]
Synonyms
AZD2936
    Click to Show/Hide
External Link
TTD: D4RMC9
 Compound Name IK-007 Phase 1/2 [46]
Synonyms
grapiprant
    Click to Show/Hide
External Link
TTD: D1KES8
 Compound Name IBI318 Phase 1 [47]
External Link
TTD: DX30BA
 Compound Name GEN-011 Phase 1 [48]
External Link
TTD: DR1YQ7
 Compound Name ENV-105 Phase 1 [49]
Synonyms
Carotuximab
    Click to Show/Hide
External Link
TTD: DQ8K3R
 Compound Name AMG 160 Phase 1 [50]
External Link
TTD: DOY4E6
 Compound Name ADP-A2M10 Phase 1 [51]
External Link
TTD: DM38KC
 Compound Name MEDI5752 Phase 1 [52]
External Link
TTD: D7L1MP
 Compound Name PF-07104091 Phase 1 [53]
External Link
TTD: D5TH2B
 Compound Name PF-06936308 Phase 1 [54]
External Link
TTD: D2LUK7
 Compound Name GEM3PSCA Phase 1 [55]
External Link
TTD: D1L7DE
 Compound Name PF-07257876 Phase 1 [56]
External Link
TTD: D1A7OP
 Compound Name Cosibelimab Phase 1 [57]
Synonyms
CK-301/TG-1501
    Click to Show/Hide
External Link
TTD: D17URP
 Compound Name Gemcitabine Approved [58]
External Link
CID: 60750
TTD: D0AJ3K
DrugBank: DB00441
 Compound Name SMI-4a Investigative [59]
Synonyms
438190-29-5; SMI 4a; TCS PIM-1 4a; (Z)-SMI-4a; (Z)-5-(3-(trifluoromethyl)benzylidene)thiazolidine-2,4-dione; (5Z)-5-[3-(trifluoromethyl)benzylidene]-1,3-thiazolidine-2,4-dione; CHEMBL183906; (5Z)-5-[[3-(TRIFLUOROMETHYL)PHENYL]METHYLENE]-2,4-THIAZOLIDINEDIONE; (5Z)-5-[[3-(trifluoromethyl)phenyl]methylidene]-1,3-thiazolidine-2,4-dione; 327033-36-3; C11H6F3NO2S; (Z)-5-(3-(Trifluoromethyl)benzylidene)-thiazolidine-2,4-dione; (5Z)-5-{[3-(trifluoromethyl)phenyl]methylidene}-1,3-thiazolidine-2,4-dione; Pim inhibitor 4a; 3vc4; SMI-4q; TCS PIM-1-4a; 5-(3-(Trifluoromethyl)benzylidene)thiazolidine-2,4-dione; 5-[3-(Trifluoromethyl)benzylidene]thiazolidine-2,4-dione; cc-717; thiazolidine-2,4-dione, 4a; SCHEMBL2541382; SCHEMBL2541388; BDBM26626; AOB6260; EX-A111; SYN1113; BDBM138364; HMS3229J21; 2720AH; HY-16576A; MFCD01152003; s8005; ZINC12576047; AKOS001314163; SMI-4a, >=98% (HPLC); CCG-265027; NCGC00345836-02; NCGC00345836-14; AC-32861; HY-15474; AB0165836; EC-000.2291; J3.561.866J; A11945; W-5256; US8877795, 12; Q27451064; 5-[[3-(trifluoromethyl)phenyl]methylene]-2,4-thiazolidinedione
    Click to Show/Hide
External Link
CID: 1361334
TTD: DAJ3D2
References
Ref 1 Circular RNA hsa_circ_0072309 promotes tumorigenesis and invasion by regulating the miR-607/FTO axis in non-small cell lung carcinoma. Aging (Albany NY). 2021 Apr 20;13(8):11629-11645. doi: 10.18632/aging.202856. Epub 2021 Apr 20.
Ref 2 The m6A demethylase FTO promotes the growth of lung cancer cells by regulating the m6A level of USP7 mRNA. Biochem Biophys Res Commun. 2019 May 7;512(3):479-485. doi: 10.1016/j.bbrc.2019.03.093. Epub 2019 Mar 21.
Ref 3 Deubiquitinases (DUBs) and DUB inhibitors: a patent review. Expert Opin Ther Pat. 2015;25(10):1191-1208. doi: 10.1517/13543776.2015.1056737. Epub 2015 Jun 16.
Ref 4 Advances in Deubiquitinating Enzyme Inhibition and Applications in Cancer Therapeutics. Cancers (Basel). 2020 Jun 15;12(6):1579. doi: 10.3390/cancers12061579.
Ref 5 P22077 inhibits LPS-induced inflammatory response by promoting K48-linked ubiquitination and degradation of TRAF6. Aging (Albany NY). 2020 Jun 9;12(11):10969-10982. doi: 10.18632/aging.103309. Epub 2020 Jun 9.
Ref 6 Small-molecule inhibitor of USP7/HAUSP ubiquitin protease stabilizes and activates p53 in cells. Mol Cancer Ther. 2009 Aug;8(8):2286-95. doi: 10.1158/1535-7163.MCT-09-0097. Epub 2009 Aug 11.
Ref 7 USP7 inhibitor P5091 inhibits Wnt signaling and colorectal tumor growth. Biochem Pharmacol. 2017 May 1;131:29-39. doi: 10.1016/j.bcp.2017.02.011. Epub 2017 Feb 16.
Ref 8 FDA Approved Drug Products from FDA Official Website. 2022. Application Number: 216340.
Ref 9 FDA Approved Drug Products from FDA Official Website. 2022. Application Number: 761210.
Ref 10 ClinicalTrials.gov (NCT04129502) TAK-788 as First-line Treatment Versus Platinum-Based Chemotherapy for Non-Small Cell Lung Cancer (NSCLC) With EGFR Exon 20 Insertion Mutations. U.S. National Institutes of Health.
Ref 11 Sugemalimab: First Approval. Drugs. 2022 Apr;82(5):593-599.
Ref 12 ClinicalTrials.gov (NCT05089734) Open-Label, Global, Multicenter, Randomized, Phase 3 Study of Sacituzumab Govitecan Versus Docetaxel in Patients With Advanced or Metastatic Non-Small Cell Lung Cancer (NSCLC) With Progression on or After Platinum-Based Chemotherapy and Anti-PD-1/PD-L1 Immunotherapy. U.S.National Institutes of Health.
Ref 13 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
Ref 14 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2021
Ref 15 FDA Approved Drug Products from FDA Official Website. 2023. Application Number: 214665.
Ref 16 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
Ref 17 FDA Approved Drug Products from FDA Official Website. 2023. Application Number: 218213
Ref 18 ClinicalTrials.gov (NCT04633564) Multicenter, Double-Blind, Randomized, Parallel-Group Study to Assess the Efficacy and Safety of MYL-1402O Compared With Avastin?, in the First-line Treatment of Patients With Stage IV Non-Squamous Non-Small Cell Lung Cancer. U.S.National Institutes of Health.
Ref 19 ClinicalTrials.gov (NCT04736173) Study to Evaluate Monotherapy Compared to Combination Immunotherapies in Participants With PD-L1 Positive Non-small Cell Lung Cancer. U.S. National Institutes of Health.
Ref 20 ClinicalTrials.gov (NCT05555732) A Randomized Phase 3 Study of Datopotamab Deruxtecan (Dato-DXd) and Pembrolizumab With or Without Platinum Chemotherapy in Subjects With No Prior Therapy for Advanced or Metastatic PD-L1 TPS <50% Non-squamous Non-small Cell Lung Cancer Without Actionable Genomic Alterations (TROPION-Lung07). U.S.National Institutes of Health.
Ref 21 ClinicalTrials.gov (NCT03728556) A Study of CS1001 in Subjects With Stage III Non-Small Cell Lung Cancer. U.S. National Institutes of Health.
Ref 22 ClinicalTrials.gov (NCT05132075) A Randomized, Controlled, Open Label, Phase III Study Evaluating the Efficacy and Safety of JDQ443 Versus Docetaxel in Previously Treated Subjects With Locally Advanced or Metastatic KRAS G12C Mutant Non-small Cell Lung Cancer. U.S.National Institutes of Health.
Ref 23 ClinicalTrials.gov (NCT04416035) A Phase 3, Multicenter, Randomized and Double-Blind Study to Assess the Similarity in Efficacy and Safety Between TRS003 and China-approved Bevacizumab in Subjects With Advanced Nonsquamous NSCLC. U.S.National Institutes of Health.
Ref 24 ClinicalTrials.gov (NCT05245071) Open-label, Phase 2 Study, Evaluating the Efficacy and Safety of Tusamitamab Ravtansine in Non-squamous Non-small-cell Lung Cancer (NSQ NSCLC) Participants With Negative or Moderate CEACAM5 Expression Tumors and High Circulating CEA. U.S.National Institutes of Health.
Ref 25 ClinicalTrials.gov (NCT04294810) A Study of Tiragolumab in Combination With Atezolizumab Compared With Placebo in Combination With Atezolizumab in Patients With Previously Untreated Locally Advanced Unresectable or Metastatic PD-L1-Selected Non-Small Cell Lung Cancer (SKYSCRAPER-01). U.S. National Institutes of Health.
Ref 26 ClinicalTrials.gov (NCT04655976) Study of Cobolimab in Combination With Dostarlimab and Docetaxel in Advanced NSCLC Participants (COSTAR Lung). U.S. National Institutes of Health.
Ref 27 ClinicalTrials.gov (NCT04258033) A Study of PLB1001 in Non-small Cell Lung Cancer With c-Met Dysregulation. U.S. National Institutes of Health.
Ref 28 ClinicalTrials.gov (NCT04032704) A Study of Ladiratuzumab Vedotin in Advanced Solid Tumors. U.S. National Institutes of Health.
Ref 29 ClinicalTrials.gov (NCT05557591) A Phase 2 Study of Cemiplimab (Anti-PD-1 Antibody) in Combination With BNT116 (FixVac Lung) Versus Cemiplimab Monotherapy in First-Line Treatment of Patients With Advanced Non-Small Cell Lung Cancer (NSCLC) With Tumors Expressing PD-L1 >=50%. U.S.National Institutes of Health.
Ref 30 ClinicalTrials.gov (NCT04931654) A Phase I/IIa Open-label Dose Escalation and Expansion Study to Evaluate the Safety, Pharmacokinetics, Pharmacodynamics, and Efficacy of AZD7789, an Anti-PD-1 and Anti-TIM-3 Bispecific Antibody, in Participants With Advanced or Metastatic Solid Tumors. U.S.National Institutes of Health.
Ref 31 ClinicalTrials.gov (NCT02340208) A Phase I/II Open-Label, Non-Randomized Dose Escalation Study of Immunoconjugate L-DOS47. U.S. National Institutes of Health.
Ref 32 ClinicalTrials.gov (NCT04699123) The Study of NC318 Alone or in Combination With Pembrolizumab in Patients With Advanced Non-small Cell Lung Cancer. U.S. National Institutes of Health.
Ref 33 ClinicalTrials.gov (NCT03848611) CM082 and JS001 in Patients With Advanced Non-Small Cell Lung Cancer (NSCLC).. U.S. National Institutes of Health.
Ref 34 ClinicalTrials.gov (NCT02283749) BrUOG L301: Xofigo Following Frontline-Line Chemotherapy For Patients With Non-Small Cell Lung Cancer and Bone Metastases. U.S.National Institutes of Health.
Ref 35 ClinicalTrials.gov (NCT04560686) Bintrafusp Alfa Before Surgery for the Treatment of Untreated Resectable Non-small Cell Lung Cancer. U.S. National Institutes of Health.
Ref 36 ClinicalTrials.gov (NCT04291105) Phase 2 Trial of Voyager V1 in Combination With Cemiplimab in Cancer Patients. U.S. National Institutes of Health.
Ref 37 ClinicalTrials.gov (NCT04395677) A Study of AB-106 in Subjects With Advanced NSCLC Harboring ROS1 Fusion Gene. U.S. National Institutes of Health.
Ref 38 ClinicalTrials.gov (NCT04625270) A Study of VS-6766 v. VS-6766 + Defactinib in Recurrent Low-Grade Serous Ovarian Cancer With and Without a KRAS Mutation. U.S. National Institutes of Health.
Ref 39 ClinicalTrials.gov (NCT03907852) Phase 1/2 Trial of Gavo-cel (TC-210) in Patients With Advanced Mesothelin-Expressing Cancer. U.S. National Institutes of Health.
Ref 40 ClinicalTrials.gov (NCT03797391) A Dose Escalation Study of EMB-01 in Participants With Advanced/Metastatic Solid Tumors. U.S. National Institutes of Health.
Ref 41 ClinicalTrials.gov (NCT04442126) A Study of NM21-1480 in Adult Patients With Advanced Solid Tumors. U.S. National Institutes of Health.
Ref 42 ClinicalTrials.gov (NCT03637803) Live Biotherapeutic Product MRx0518 and Pembrolizumab Combination Study in Solid Tumors. U.S. National Institutes of Health.
Ref 43 ClinicalTrials.gov (NCT03974022) Assessing an Oral EGFR Inhibitor, DZD9008 in Patients Who Have Advanced Non-small Cell Lung Cancer With EGFR or HER2 Mutation (WU-KONG1). U.S. National Institutes of Health.
Ref 44 ClinicalTrials.gov (NCT03744468) Study of BGB-A425 in Combination With Tislelizumab in Advanced Solid Tumors. U.S. National Institutes of Health.
Ref 45 ClinicalTrials.gov (NCT04995523) Phase I/II, Open-label, Dose Escalation and Dose Expansion Study to Evaluate Safety, Pharmacokinetics, Pharmacodynamics and Efficacy of AZD2936 Anti-TIGIT/Anti-PD-1 Bispecific Antibody in Participants With Advanced or Metastatic NSCLC. U.S.National Institutes of Health.
Ref 46 ClinicalTrials.gov (NCT03696212) Open Label, Single Arm, Phase 1b/2 Study to Evaluate the Safety and Efficacy of Grapiprant (ARY-007) in Combination With Pembrolizumab in Patients With Advanced or Metastatic Post-PD-1/L1 Non-Small Cell Lung Cancer (NSCLC) Adenocarcinoma. U.S.National Institutes of Health.
Ref 47 ClinicalTrials.gov (NCT04777084) The Efficacy and Safety of the Bispecific Anti-PD-1/PD-L1 Antibody IBI318 Combined With Lenvatinib in NSCLC.. U.S. National Institutes of Health.
Ref 48 ClinicalTrials.gov (NCT04596033) TiTAN-1: Safety, Proliferation and Persistence of GEN-011 Autologous Cell Therapy. U.S. National Institutes of Health.
Ref 49 ClinicalTrials.gov (NCT05401110) IIT2021-12-Reckamp-Osi105: Phase I Study of Osimertinib With Carotuximab in Advanced, EGFR-mutated Non-Small Cell Lung Cancer. U.S.National Institutes of Health.
Ref 50 ClinicalTrials.gov (NCT04822298) Study of AMG 160 in Subjects With Non-Small Cell Lung Cancer. U.S. National Institutes of Health.
Ref 51 Phase I clinical trial evaluating the safety and efficacy of ADP-A2M10 SPEAR T cells in patients with MAGE-A10(+) advanced non-small cell lung cancer. J Immunother Cancer. 2022 Jan;10(1):e003581.
Ref 52 ClinicalTrials.gov (NCT03819465) A Study of Novel Anti-cancer Agents in Patients With Previously Untreated NSCLC (MAGELLAN). U.S. National Institutes of Health.
Ref 53 ClinicalTrials.gov (NCT04553133) PF-07104091 as a Single Agent and in Combination Therapy. U.S. National Institutes of Health.
Ref 54 ClinicalTrials.gov (NCT03674827) Vaccine-Based Immunotherapy Regimen For NSCLC and TNBC. U.S. National Institutes of Health.
Ref 55 ClinicalTrials.gov (NCT03927573) Study With Bispecific Antibody Engaging T-cells, in Patients With Progressive Cancer Diseases With Positive PSCA Marker. U.S. National Institutes of Health.
Ref 56 ClinicalTrials.gov (NCT04881045) A PHASE 1 DOSE ESCALATION AND EXPANSION STUDY EVALUATING THE SAFETY, TOLERABILITY, PHARMACOKINETICS, PHARMACODYNAMICS, AND ANTITUMOR ACTIVITY OF PF-07257876 IN PATIENTS WITH ADVANCED OR METASTATIC TUMORS. U.S.National Institutes of Health.
Ref 57 ClinicalTrials.gov (NCT04786964) Study of Pemetrexed+Platinum Chemotherapy With or Without Cosibelimab (CK-301) in First Line Metastatic Non-squamous Non-Small Cell Lung Cancer (CONTERNO). U.S. National Institutes of Health.
Ref 58 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 59 Pim-1 inhibitor SMI-4a suppresses tumor growth in non-small cell lung cancer via PI3K/AKT/mTOR pathway. Onco Targets Ther. 2019 Apr 23;12:3043-3050.