Compounds > rg7388
Page last updated: 2024-08-03 17:52:18

rg7388

Description

RG7388: structure in first source [MeSH]

Cross-References

ID SourceID
PubMed CID53358942
CHEMBL ID2402737
SCHEMBL ID442856
MeSH IDM0592199

Synonyms (53)

Synonym
4-{[(2r,3s,4r,5s)-3-(3-chloro-2-fluoro-phenyl)-4-(4-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-3-methoxy-benzoic acid
TVTXCJFHQKSQQM-LJQIRTBHSA-N
4-((2r,3s,4r,5s)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-neopentylpyrrolidine-2-carboxamido)-3-methoxybenzoic acid
S7205
idasanutlin [usan]
idasanutlin [who-dd]
idasanutlin [inn]
1229705-06-9
idasanutlin
idasanutlin [usan:inn]
rg7388
ro-5503781
rg-7388
qsq883v35u ,
benzoic acid, 4-((((2r,3s,4r,5s)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-(2,2-dimethylpropyl)-2-pyrrolidinyl)carbonyl)amino)-3-methoxy-
ro5503781
unii-qsq883v35u
bdbm50437206
chembl2402737 ,
HY-15676
CS-1473
SCHEMBL442856
benzoic acid, 4-[[[(2r,3s,4r,5s)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-(2,2-dimethylpropyl)-2-pyrrolidinyl]carbonyl]amino]-3-methoxy-
AC-32968
AKOS026674115
5-[9-isopropyl-8-methyl-2-(4-morpholinyl)-9h-purin-6-yl]-2-pyrimidinamine
J-690081
EX-A831
rg-7388;idasanutlin
ro 5503781
4-[[(2r,3s,4r,5s)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-(2,2-dimethylpropyl)pyrrolidine-2-carbonyl]amino]-3-methoxybenzoic acid
idasanutlin (rg-7388)
DB12325
NCGC00378976-08
idasanutlin (rg7388)
4-((2r,3s,4r,5s)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-neopentylpyrrolidine-2-carboxamido)-3-methoxybenzoic acid.
mfcd26142931
rg-7388;rg 7388;rg7388; ro5503781; ro-5503781; ro 5503781
BCP11659
idasanutlin (usan/inn)
D11219
AMY1857
4-[[[(2r,3s,4r,5s)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-(2,2-dimethylpropyl)-2-pyrrolidinyl]carbonyl]amino]-3-methoxybenzoic acid
CCG-270248
nsc-779404
nsc779404
Q27287480
A857397
BP-25380
DTXSID001025954
4-((((2r,3s,4r,5s)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-(2,2-dimethylpropyl)-2-pyrrolidinyl)carbonyl)amino)-3-methoxy-benzoic acid
4-[(2r,3s,4r,5s)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-(2,2-dimethylpropyl)pyrrolidine-2-amido]-3-methoxybenzoic acid
EN300-26181975

Protein Targets (9)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
PPM1D proteinHomo sapiens (human)Potency23.3617AID1347411
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency13.4504AID1645841
GVesicular stomatitis virusPotency21.3174AID1645842
Interferon betaHomo sapiens (human)Potency22.8506AID1347411; AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency21.3174AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency21.3174AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency21.3174AID1645842

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
Cellular tumor antigen p53Homo sapiens (human)IC500.0095AID1182106; AID1182107
E3 ubiquitin-protein ligase Mdm2Homo sapiens (human)IC500.0078AID1182106; AID1182107; AID1555896; AID759660

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
E3 ubiquitin-protein ligase Mdm2Homo sapiens (human)Kd0.0050AID1075196; AID1807821

Bioassays (50)

Assay IDTitleYearJournalArticle
AID1483357Inhibition of p53-MDM2 interaction in human U2OS cells assessed as p53 accumulation at 1 uM after 7 hrs by Western blot analysis2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
ISSN: 1520-4804		1,4,5-Trisubstituted Imidazole-Based p53-MDM2/MDMX Antagonists with Aliphatic Linkers for Conjugation with Biological Carriers.
AID1182123Oral bioavailability in C57 mouse at 50 mg/kg2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
ISSN: 1464-3391		Discovery of potent and selective spiroindolinone MDM2 inhibitor, RO8994, for cancer therapy.
AID759673Cell cycle arrest in human SJSA1 cells assessed as accumulation at G2/M phase after 24 hrs2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
ISSN: 1520-4804		Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development.
AID1182120Cmax in C57 mouse at 50 mg/kg, po2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
ISSN: 1464-3391		Discovery of potent and selective spiroindolinone MDM2 inhibitor, RO8994, for cancer therapy.
AID1075195Antiproliferative activity against human SJSA1 cells assessed as inhibition of EdU incorporation after 1 hr by Click-iT EdU HCS assay in presence of 10% human serum2014Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4
ISSN: 1520-4804		Discovery of AMG 232, a potent, selective, and orally bioavailable MDM2-p53 inhibitor in clinical development.
AID759675Cell cycle arrest in human SJSA1 cells assessed as accumulation at G1 phase after 24 hrs2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
ISSN: 1520-4804		Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development.
AID1483352Inhibition of p53-MDM2 interaction in human HCT116 cells assessed as p53 activation by measuring increase in MDM2 expression at 1 uM after 7 hrs by Western blot analysis2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
ISSN: 1520-4804		1,4,5-Trisubstituted Imidazole-Based p53-MDM2/MDMX Antagonists with Aliphatic Linkers for Conjugation with Biological Carriers.
AID1483334Inhibition of p53-MDM2 interaction in human U2OS cells assessed as p53 activation by measuring increase in MDM2 expression at 1 uM after 7 hrs by Western blot analysis2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
ISSN: 1520-4804		1,4,5-Trisubstituted Imidazole-Based p53-MDM2/MDMX Antagonists with Aliphatic Linkers for Conjugation with Biological Carriers.
AID1807821Binding affinity to HDM2 (unknown origin)2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
ISSN: 1520-4804		Discovery of
AID759670Antitumor activity against human SJSA1 cells xenografted in nude mouse assessed as tumor growth inhibition at 25 mg/kg, po after 2 weeks relative to control2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
ISSN: 1520-4804		Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development.
AID1483347Cell cycle arrest in wild type p53 expressing human U2OS cells assessed as increase in accumulation at G1 phase at 1 uM after 24 hrs by propidium iodide-based FACS analysis2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
ISSN: 1520-4804		1,4,5-Trisubstituted Imidazole-Based p53-MDM2/MDMX Antagonists with Aliphatic Linkers for Conjugation with Biological Carriers.
AID1483335Inhibition of p53-MDM2 interaction in human U2OS cells assessed as p53 activation by measuring increase in p21 expression at 1 uM after 24 hrs by Western blot analysis2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
ISSN: 1520-4804		1,4,5-Trisubstituted Imidazole-Based p53-MDM2/MDMX Antagonists with Aliphatic Linkers for Conjugation with Biological Carriers.
AID759643Oral bioavailability in C57 mouse at 50 mg/kg2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
ISSN: 1520-4804		Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development.
AID1182119AUC in C57 mouse at 50 mg/kg, po2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
ISSN: 1464-3391		Discovery of potent and selective spiroindolinone MDM2 inhibitor, RO8994, for cancer therapy.
AID1483359Induction of human N-terminal MDM2 (1 to 125 residues) dimerization expressed in Escherichia coli BL21 (DE3) by 1H NMR spectroscopic method2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
ISSN: 1520-4804		1,4,5-Trisubstituted Imidazole-Based p53-MDM2/MDMX Antagonists with Aliphatic Linkers for Conjugation with Biological Carriers.
AID759652Cmax in C57 mouse at 50 mg/kg, po2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
ISSN: 1520-4804		Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development.
AID759653AUC in C57 mouse at 50 mg/kg, po2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
ISSN: 1520-4804		Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development.
AID1483358Induction of human N-terminal MDM2 (1 to 118 residues) dimerization expressed in Escherichia coli BL21 (DE3) by 1H NMR spectroscopic method2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
ISSN: 1520-4804		1,4,5-Trisubstituted Imidazole-Based p53-MDM2/MDMX Antagonists with Aliphatic Linkers for Conjugation with Biological Carriers.
AID759667AUC in nude mouse xenografted with human SJSA1 cells at 25 mg/kg, po2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
ISSN: 1520-4804		Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development.
AID759666AUC in nude mouse xenografted with human SJSA1 cells at 12.5 mg/kg, po2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
ISSN: 1520-4804		Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development.
AID759661Cytotoxicity against human SJSA1 cells expressing wild type p53 assessed as growth inhibition by MTT assay2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
ISSN: 1520-4804		Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development.
AID759647Apparent terminal half-life in C57 mouse at 5 mg/kg, iv2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
ISSN: 1520-4804		Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development.
AID759658Cytotoxicity against human MDA-MB-435 cells expressing p53 mutant assessed as growth inhibition by MTT assay2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
ISSN: 1520-4804		Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development.
AID1483348Inhibition of p53-MDM2 interaction in human U2OS cells assessed as p53 activation by measuring p21 accumulation at 1 uM after 7 hrs by Western blot analysis2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
ISSN: 1520-4804		1,4,5-Trisubstituted Imidazole-Based p53-MDM2/MDMX Antagonists with Aliphatic Linkers for Conjugation with Biological Carriers.
AID1483360Induction of human N-terminal MDM2 (18 to 125 residues) dimerization expressed in Escherichia coli BL21 (DE3) by 1H NMR spectroscopic method2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
ISSN: 1520-4804		1,4,5-Trisubstituted Imidazole-Based p53-MDM2/MDMX Antagonists with Aliphatic Linkers for Conjugation with Biological Carriers.
AID1182113Clearance in human liver microsomes at 1 mM preincubated for 5 mins in presence of NADPH by LC-MS/MS method2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
ISSN: 1464-3391		Discovery of potent and selective spiroindolinone MDM2 inhibitor, RO8994, for cancer therapy.
AID759672Induction of apoptosis in human SJSA1 cells after 48 hrs by annexin V staining assay2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
ISSN: 1520-4804		Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development.
AID759660Binding affinity to GST-tagged MDM2 (unknown origin) assessed as inhibition of interaction with p53 after 1 hr by HTRF assay2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
ISSN: 1520-4804		Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development.
AID759662Cytotoxicity against human RKO cells expressing wild type p53 assessed as growth inhibition by MTT assay2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
ISSN: 1520-4804		Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development.
AID1075196Binding affinity to human MDM2 by by Surface Plasmon Resonace (SPR) spectroscopy binding assay2014Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4
ISSN: 1520-4804		Discovery of AMG 232, a potent, selective, and orally bioavailable MDM2-p53 inhibitor in clinical development.
AID1182117Apparent terminal half life in C57 mouse at 5 mg/kg, iv2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
ISSN: 1464-3391		Discovery of potent and selective spiroindolinone MDM2 inhibitor, RO8994, for cancer therapy.
AID759663Cytotoxicity against human HCT116 cells expressing wild type p53 assessed as growth inhibition by MTT assay2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
ISSN: 1520-4804		Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development.
AID1182116Total plasma clearance in C57 mouse at 5 mg/kg, iv2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
ISSN: 1464-3391		Discovery of potent and selective spiroindolinone MDM2 inhibitor, RO8994, for cancer therapy.
AID1483346Cell cycle arrest in wild type p53 expressing human U2OS cells assessed as decrease in accumulation at S phase at 1 uM after 24 hrs by propidium iodide-based FACS analysis2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
ISSN: 1520-4804		1,4,5-Trisubstituted Imidazole-Based p53-MDM2/MDMX Antagonists with Aliphatic Linkers for Conjugation with Biological Carriers.
AID759656Clearance in human liver microsomes at 1 mM by LC-MS/MS analysis2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
ISSN: 1520-4804		Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development.
AID1182107Inhibition of p53-MDM2 (unknown origin) interaction using 0.02% BSA buffer after 1 hr by HTRF assay2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
ISSN: 1464-3391		Discovery of potent and selective spiroindolinone MDM2 inhibitor, RO8994, for cancer therapy.
AID1555896Inhibition of MDM2 (unknown origin)2019European journal of medicinal chemistry, Aug-15, Volume: 176ISSN: 1768-3254Development of selective small molecule MDM2 degraders based on nutlin.
AID1182106Inhibition of p53-MDM2 (unknown origin) interaction using 0.2% BSA buffer after 1 hr by HTRF assay2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
ISSN: 1464-3391		Discovery of potent and selective spiroindolinone MDM2 inhibitor, RO8994, for cancer therapy.
AID1129365Cytotoxicity against human SJSA1 cells assessed as growth inhibition after 16 hrs by EdU incorporation assay in presence of 10% human serum2014Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7
ISSN: 1520-4804		Novel inhibitors of the MDM2-p53 interaction featuring hydrogen bond acceptors as carboxylic acid isosteres.
AID759649Total plasma clearance in C57 mouse at 5 mg/kg, iv2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
ISSN: 1520-4804		Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development.
AID759674Inhibition of MDM2 in human SJSA1 cells assessed as induction of p53 stabilization after 20 hrs by Western blot analysis2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
ISSN: 1520-4804		Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development.
AID759671Antitumor activity against human SJSA1 cells xenografted in nude mouse assessed as tumor growth inhibition at 12.5 mg/kg, po after 2 weeks relative to control2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
ISSN: 1520-4804		Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development.
AID1483353Inhibition of p53-MDM2 interaction in human HCT116 cells assessed as p53 activation by measuring increase in p21 expression at 1 uM after 24 hrs by Western blot analysis2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
ISSN: 1520-4804		1,4,5-Trisubstituted Imidazole-Based p53-MDM2/MDMX Antagonists with Aliphatic Linkers for Conjugation with Biological Carriers.
AID759659Cytotoxicity against human SW480 cells expressing p53 mutant assessed as growth inhibition by MTT assay2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
ISSN: 1520-4804		Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development.
AID1347172Secondary qRT-PCR qHTS assay for selected Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
ISSN: 1091-6490		Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347170Vero cells viability counterscreen for qRT-PCR qHTS assay of selected Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
ISSN: 1091-6490		Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347412qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation2020ACS chemical biology, 07-17, Volume: 15, Issue:7
ISSN: 1554-8937		High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
ISSN: 1554-8937		High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347163384 well plate NINDS AMC confirmatory qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
ISSN: 1091-6490		Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347164384 well plate NINDS Rhodamine confirmatory qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
ISSN: 1091-6490		Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.

Research

Studies (69)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's44 (63.77)24.3611
2020's25 (36.23)2.80

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials10 (14.49%)5.53%
Reviews5 (7.25%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other54 (78.26%)84.16%
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
nutlin-3b
1
Nutlin;
piperazinone		anticoronaviral agent201720177.0low000010
sar405838
4
201420217.0medium000031
rg7112
4
201320218.5medium000031
amg 232
3
201420198.3high000030
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
imidazole
1
imidazole201520159.0low000010
verapamil
1
aromatic ether;
nitrile;
polyether;
tertiary amino compound		2014201410.0low000010
hydroxyurea
2
one-carbon compound;
ureas		antimetabolite;
antimitotic;
antineoplastic agent;
DNA synthesis inhibitor;
EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor;
genotoxin;
immunomodulator;
radical scavenger;
teratogenic agent		201820224.0low100011
letrozole
1
nitrile;
triazoles		antineoplastic agent;
EC 1.14.14.14 (aromatase) inhibitor		201820186.0low000010
metformin
1
guanidinesenvironmental contaminant;
geroprotector;
hypoglycemic agent;
xenobiotic		202020204.0low000010
4-aminobenzoic acid
55
aminobenzoate;
aromatic amino-acid anion		Escherichia coli metabolite;
plant metabolite;
Saccharomyces cerevisiae metabolite		201320226.0high90004510
vorinostat
2
dicarboxylic acid diamide;
hydroxamic acid		antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor		201820195.5low000020
temozolomide
2
imidazotetrazine;
monocarboxylic acid amide;
triazene derivative		alkylating agent;
antineoplastic agent;
prodrug		201920214.0low000011
cytarabine
2
beta-D-arabinoside;
monosaccharide derivative;
pyrimidine nucleoside		antimetabolite;
antineoplastic agent;
antiviral agent;
immunosuppressive agent		202120222.5low200002
quinuclidines
1
quinuclidines;
saturated organic heterobicyclic parent		202220222.0low000001
pyrazines
1
diazine;
pyrazines		Daphnia magna metabolite201920195.0low000010
hydrazine
1
azane;
hydrazines		EC 4.3.1.10 (serine-sulfate ammonia-lyase) inhibitor201920195.0low000010
azacitidine
1
N-glycosyl-1,3,5-triazine;
nucleoside analogue		antineoplastic agent201920195.0low000010
alpha-aminopyridine
4
201620235.0low000031
triazoles
2
1,2,3-triazole201820195.5low000020
bendamustine hydrochloride
1
202120213.0low000001
lenalidomide
1
aromatic amine;
dicarboximide;
isoindoles;
piperidones		angiogenesis inhibitor;
antineoplastic agent;
immunomodulator		201920195.0low000010
2-oxindole
1
gamma-lactam;
indolinone		201520159.0low000010
decitabine
1
2'-deoxyribonucleoside201920195.0low000010
posaconazole
1
aromatic ether;
conazole antifungal drug;
N-arylpiperazine;
organofluorine compound;
oxolanes;
triazole antifungal drug;
triazoles		trypanocidal drug201820186.0low000010
sirolimus
1
antibiotic antifungal drug;
cyclic acetal;
cyclic ketone;
ether;
macrolide lactam;
organic heterotricyclic compound;
secondary alcohol		antibacterial drug;
anticoronaviral agent;
antineoplastic agent;
bacterial metabolite;
geroprotector;
immunosuppressive agent;
mTOR inhibitor		201720177.0low000010
palbociclib
1
aminopyridine;
aromatic ketone;
cyclopentanes;
piperidines;
pyridopyrimidine;
secondary amino compound;
tertiary amino compound		antineoplastic agent;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor		201720177.0low000010
nutlin-3a
6
stilbenoid201420187.5low000060
trametinib
1
acetamides;
aromatic amine;
cyclopropanes;
organofluorine compound;
organoiodine compound;
pyridopyrimidine;
ring assembly		anticoronaviral agent;
antineoplastic agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
geroprotector		201920195.0low000010
mln 8237
1
benzazepine201720177.0low000010
navitoclax
1
aryl sulfide;
monochlorobenzenes;
morpholines;
N-sulfonylcarboxamide;
organofluorine compound;
piperazines;
secondary amino compound;
sulfone;
tertiary amino compound		antineoplastic agent;
apoptosis inducer;
B-cell lymphoma 2 inhibitor		202320231.0low000001
4,4-difluoro-4-bora-3a,4a-diaza-s-indacene
1
BODIPY compound201820186.0low000010
incb-018424
1
nitrile;
pyrazoles;
pyrrolopyrimidine		antineoplastic agent;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor		201820186.0low000010
gilteritinib
1
aromatic amine;
monomethoxybenzene;
N-methylpiperazine;
oxanes;
piperidines;
primary carboxamide;
pyrazines;
secondary amino compound		antineoplastic agent;
apoptosis inducer;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor		201920195.0low000010
abt-199
7
aromatic ether;
C-nitro compound;
monochlorobenzenes;
N-alkylpiperazine;
N-arylpiperazine;
N-sulfonylcarboxamide;
oxanes;
pyrrolopyridine		antineoplastic agent;
apoptosis inducer;
B-cell lymphoma 2 inhibitor		201620234.6low100043
apr-246
1
202220222.0low000001
sar405838
1
201720177.0low000010
warfarin
1
benzenes;
hydroxycoumarin;
methyl ketone		201820186.0low000010
rg7112
3
201420179.0medium000030
gsk2830371
2
201620187.0medium000020
selinexor
1
201920195.0low000010
pf-06463922
1
aminopyridine;
aromatic ether;
azamacrocycle;
benzamides;
cyclic ether;
monofluorobenzenes;
nitrile;
organic heterotetracyclic compound;
pyrazoles		antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor		202320231.0low000001
enasidenib
1
1,3,5-triazines;
aminopyridine;
aromatic amine;
organofluorine compound;
secondary amino compound;
tertiary alcohol		antineoplastic agent;
EC 1.1.1.42 (isocitrate dehydrogenase) inhibitor		201920195.0low000010
pp242
1
aromatic amine;
biaryl;
hydroxyindoles;
phenols;
primary amino compound;
pyrazolopyrimidine		antineoplastic agent;
mTOR inhibitor		202320231.0low000001
pyrimidinones
1
201920195.0low000010
ConditionIndicatedStudiesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
Acute Disease0
1
201820186.0low100010
Acute Myelogenous Leukemia0
10
201620234.4low500064
Adenocarcinoma, Clear Cell0
1
202320231.0low000001
Angiogenesis, Pathologic0
1
201520159.0low000010
Astrocytoma, Grade IV0
2
201920214.0low000011
Atypical Lipomatous Tumor0
1
201720177.0low000010
B-Cell Chronic Lymphocytic Leukemia0
2
202320231.0low000002
B-Cell Lymphoma0
1
201620168.0low000010
Benign Neoplasms0
12
201420225.8low4000102
Benign Neoplasms, Brain0
2
201520216.0low000011
Blast Crisis0
1
201620168.0low100010
Blast Phase0
1
201620168.0low100010
Body Weight0
1
201920195.0low000010
Bone Cancer0
2
2014201410.0low000020
Bone Neoplasms0
2
2014201410.0low000020
Brain Neoplasms0
2
201520216.0low000011
Brain Stem Neoplasms0
1
202120213.0low000001
Brain Stem Neoplasms, Primary0
1
202120213.0low000001
Breast Cancer0
2
201820195.5low000020
Breast Neoplasms1
2
201820195.5low000020
Cancer of Lung0
2
201520235.0low000011
Cancer of Ovary0
3
201620234.3low000021
Cancer of Prostate0
1
201920195.0low000010
Cancer of Skin0
1
201820186.0low000010
Carcinoma, Non-Small Cell Lung0
1
201520159.0low000010
Carcinoma, Non-Small-Cell Lung0
1
201520159.0low000010
Carcinoma, Ovarian Epithelial0
1
202320231.0low000001
Congenital Zika Syndrome0
1
202020204.0low000010
Diffuse Intrinsic Pontine Glioma0
1
202120213.0low000001
Diffuse Mixed Small and Large Cell Lymphoma0
1
201820186.0low000010
DIPG Brain Tumors0
1
202120213.0low000001
Disease Models, Animal0
5
201620215.4low000041
Dysplastic Nevus Syndrome, Hereditary0
1
201820186.0low000010
Electrocardiogram QT Prolonged0
1
201820186.0low100010
Emesis0
1
202220222.0low100001
Enlarged Spleen0
1
202220222.0low100001
Epithelial Ovarian Cancer0
1
202320231.0low000001
Erythremia0
4
201820224.2low100031
Glioblastoma1
2
201920214.0low000011
Granulocytic Leukemia0
1
201820186.0low100010
Hematologic Malignancies0
1
201720177.0low000010
Hematologic Neoplasms0
1
201720177.0low000010
Invasiveness, Neoplasm0
1
201920195.0low000010
Leukemia, Lymphoblastic, Acute, T Cell0
1
202320231.0low000001
Leukemia, Lymphocytic, Chronic, B-Cell0
2
202320231.0low000002
Leukemia, Lymphocytic, Chronic, T Cell0
1
202120213.0low000001
Leukemia, Myeloid0
1
201820186.0low100010
Leukemia, Myeloid, Acute1
10
201620234.4low500064
Leukemia, Prolymphocytic, T-Cell0
1
202120213.0low000001
Liposarcoma0
1
201720177.0low000010
Local Neoplasm Recurrence0
1
201520159.0low000010
Long QT Syndrome0
1
201820186.0low100010
Lung Neoplasms0
2
201520235.0low000011
Lymphoma, B-Cell0
1
201620168.0low000010
Lymphoma, Non-Hodgkin1
1
201820186.0low000010
Malignant Melanoma0
2
201720186.5low000020
Melanoma0
2
201720186.5low000020
Minimal Disease, Residual0
1
201920195.0low000010
Nausea0
1
202220222.0low100001
Neoplasms1
12
201420225.8low4000102
Neuroblastoma0
8
201420236.2low000062
Osteogenic Sarcoma0
2
2014201410.0low000020
Osteosarcoma0
2
2014201410.0low000020
Ovarian Neoplasms0
3
201620234.3low000021
Polycythemia Vera1
4
201820224.2low100031
Precursor T-Cell Lymphoblastic Leukemia-Lymphoma0
1
202320231.0low000001
Prostatic Neoplasms0
1
201920195.0low000010
Recrudescence0
1
202020204.0low000010
Rhabdomyosarcoma0
1
201520159.0low000010
Sarcoma0
1
201520159.0low000010
Sarcoma, Epithelioid0
1
201520159.0low000010
Skin Neoplasms0
1
201820186.0low000010
Vomiting0
1
202220222.0low100001
Zika Virus Infection0
1
202020204.0low000010

Safety/Toxicity (1)

ArticleYear
Cell Cycle Arrest and Cytotoxic Effects of SAHA and RG7388 Mediated through p21
Medicina (Kaunas, Lithuania), , Jan-29, Volume: 55, Issue:2		2019

Long-term Use (1)

ArticleYear
Preclinical optimization of MDM2 antagonist scheduling for cancer treatment by using a model-based approach.
Clinical cancer research : an official journal of the American Association for Cancer Research, , Jul-15, Volume: 20, Issue:14		2014

Pharmacokinetics (4)

ArticleYear
Accelerating Clinical Development of Idasanutlin through a Physiologically Based Pharmacokinetic Modeling Risk Assessment for CYP450 Isoenzyme-Related Drug-Drug Interactions.
Drug metabolism and disposition: the biological fate of chemicals, , Volume: 50, Issue:3		2022
A single-center, open-label study investigating the excretion balance, pharmacokinetics, metabolism, and absolute bioavailability of a single oral dose of [
Cancer chemotherapy and pharmacology, , Volume: 84, Issue:1		2019
Lack of UGT polymorphism association with idasanutlin pharmacokinetics in solid tumor patients.
Cancer chemotherapy and pharmacology, , Volume: 83, Issue:1		2019
Effects of posaconazole (a strong CYP3A4 inhibitor), two new tablet formulations, and food on the pharmacokinetics of idasanutlin, an MDM2 antagonist, in patients with advanced solid tumors.
Cancer chemotherapy and pharmacology, , Volume: 81, Issue:3		2018

Bioavailability (3)

ArticleYear
A single-center, open-label study investigating the excretion balance, pharmacokinetics, metabolism, and absolute bioavailability of a single oral dose of [
Cancer chemotherapy and pharmacology, , Volume: 84, Issue:1		2019
Effects of posaconazole (a strong CYP3A4 inhibitor), two new tablet formulations, and food on the pharmacokinetics of idasanutlin, an MDM2 antagonist, in patients with advanced solid tumors.
Cancer chemotherapy and pharmacology, , Volume: 81, Issue:3		2018
Discovery of AMG 232, a potent, selective, and orally bioavailable MDM2-p53 inhibitor in clinical development.
Journal of medicinal chemistry, , Feb-27, Volume: 57, Issue:4		2014

Dosage (9)

ArticleYear
Combination Therapies Targeting ALK-aberrant Neuroblastoma in Preclinical Models.
Clinical cancer research : an official journal of the American Association for Cancer Research, , 04-03, Volume: 29, Issue:7		2023
Venetoclax and idasanutlin in relapsed/refractory AML: a nonrandomized, open-label phase 1b trial.
Blood, , 03-16, Volume: 141, Issue:11		2023
The MDM2 antagonist idasanutlin in patients with polycythemia vera: results from a single-arm phase 2 study.
Blood advances, , 02-22, Volume: 6, Issue:4		2022
Phase I study of daily and weekly regimens of the orally administered MDM2 antagonist idasanutlin in patients with advanced tumors.
Investigational new drugs, , Volume: 39, Issue:6		2021
A phase 1 study of the MDM2 antagonist RO6839921, a pegylated prodrug of idasanutlin, in patients with advanced solid tumors.
Investigational new drugs, , Volume: 38, Issue:4		2020
Preclinical evaluation of the first intravenous small molecule MDM2 antagonist alone and in combination with temozolomide in neuroblastoma.
International journal of cancer, , 06-15, Volume: 144, Issue:12		2019
Effects of posaconazole (a strong CYP3A4 inhibitor), two new tablet formulations, and food on the pharmacokinetics of idasanutlin, an MDM2 antagonist, in patients with advanced solid tumors.
Cancer chemotherapy and pharmacology, , Volume: 81, Issue:3		2018
Heterogeneous Mechanisms of Secondary Resistance and Clonal Selection in Sarcoma during Treatment with Nutlin.
PloS one, , Volume: 10, Issue:10		2015
Preclinical optimization of MDM2 antagonist scheduling for cancer treatment by using a model-based approach.
Clinical cancer research : an official journal of the American Association for Cancer Research, , Jul-15, Volume: 20, Issue:14		2014

Interactions (4)

ArticleYear
Accelerating Clinical Development of Idasanutlin through a Physiologically Based Pharmacokinetic Modeling Risk Assessment for CYP450 Isoenzyme-Related Drug-Drug Interactions.
Drug metabolism and disposition: the biological fate of chemicals, , Volume: 50, Issue:3		2022
Preclinical evaluation of the first intravenous small molecule MDM2 antagonist alone and in combination with temozolomide in neuroblastoma.
International journal of cancer, , 06-15, Volume: 144, Issue:12		2019
Antitumour activity of the glycoengineered type II anti-CD20 antibody obinutuzumab (GA101) in combination with the MDM2-selective antagonist idasanutlin (RG7388).
European journal of haematology, , Volume: 97, Issue:5		2016
Pre-clinical evaluation of the MDM2-p53 antagonist RG7388 alone and in combination with chemotherapy in neuroblastoma.
Oncotarget, , Apr-30, Volume: 6, Issue:12		2015