Page last updated: 2024-11-13

ivosidenib

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

ivosidenib: an inhibitor of isocitrate dehydrogenase 1 (IDH1) for treatment of acute myeloid leukemia (AML) [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ivosidenib : A tertiary carboxamide resulting from the formal condensation of the carboxy group of (2S)-1-(4-cyanopyridin-2-yl)-5-oxopyrrolidine-2-carboxylic acid with the secondary amino group of (2S)-2-(2-chlorophenyl)-N-(3,3-difluorocyclobutyl)-2-[(5-fluoropyridin-3-yl)amino]acetamide. It is approved by the FDA for the treatment of acute myeloid leukemia (AML) in patients with an isocitrate dehydrogenase-1 (IDH1) mutation. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID71657455
CHEMBL ID3989958
CHEBI ID145430
SCHEMBL ID15122512

Synonyms (58)

Synonym
ivosidenibum
1448347-49-6
tibsovo
CHEBI:145430 ,
ag-120 ,
n-{(1s)-1-(2-chlorophenyl)-2-[(3,3-difluorocyclobutyl)amino]-2-oxoethyl}-1-(4-cyanopyridin-2-yl)-n-(5-fluoropyridin-3-yl)-5-oxo-l-prolinamide
(2s)-n-{(1s)-1-(2-chlorophenyl)-2-[(3,3-difluorocyclobutyl)amino]-2-oxoethyl}-1-(4-cyanopyridin-2-yl)-n-(5-fluoropyridin-3-yl)-5-oxopyrrolidine-2-carboxamide
ivosidenib
S8206
HY-18767
CS-5122
SCHEMBL15122512
AC-32624
ag120
gtpl9217
(2s)-n-[(1s)-1-(2-chlorophenyl)-2-[(3,3-difluorocyclobutyl)amino]-2-oxoethyl]-1-(4-cyanopyridin-2-yl)-n-(5-fluoropyridin-3-yl)-5-oxopyrrolidine-2-carboxamide
ivosidenib [orange book]
ivosidenib [who-dd]
ivosidenib [inn]
glycinamide, 1-(4-cyano-2-pyridinyl)-5-oxo-l-prolyl-2-(2-chlorophenyl)-n-(3,3-difluorocyclobutyl)-n2-(5-fluoro-3-pyridinyl)-, (2s)-
Q2PCN8MAM6 ,
ivosidenib [mi]
ivosidenib [usan]
ivosidenib [usan:inn:who-dd]
unii-q2pcn8mam6
AKOS028113340
EX-A992
(s)-n-((s)-1-(2-chlorophenyl)-2-(3,3-difluorocyclobutylamino)-2-oxoethyl)-1-(4-cyanopyridin-2-yl)-n-
mfcd29036964
(2s)-1-(4-cyano-2-pyridinyl)-5-oxo-l-prolyl-2-(2-chloroph)-n-(3,3-difluorocyclobutyl)-n2-(5-fluoro-3-pyridinyl)-glycinamide
bdbm363689
us9850277, compound 176
(s)-n-((s)-1-(2-chlorophenyl)-2-((3,3-difluorocyclobutyl)amino)-2-oxoethyl)-1-(4-cyanopyridin-2-yl)-n-(5-fluoropyridin-3-yl)-5-oxopyrrolidine-2-carboxamide
NCGC00476170-06
NCGC00476170-04
rg120
Q27895417
(s)-n-((s)-1-(2-chlorophenyl)-2-(3,3-difluorocyclobutylamino)-2-oxoethyl)-1-(4-cyanopyridin-2-yl)-n-(5-fluoropyridin-3-yl)-5-oxopyrrolidine-2-carboxamide
DB14568
AS-35058
CHEMBL3989958
AMY38924
CCG-270141
nsc-789102
nsc789102
ivosidenib (usan/inn)
tibsovo (tn)
D11090
A900315
(s)-n-((s)-1-(2-chlorophenyl)-2-((3,3-difluorocyclobutyl)amino)-2-oxoethyl)-1-(4-cyanopyridin-2-yl)-n-(5-fluoropyridin-3-yl)-5-oxopyrrolidine-2-carboxamide;ag-120
DTXSID801027928
wijzxsajmhavgx-dhlkqenfsa-n
(2s)-n-((1s)-1-(2-chlorophenyl)-2-((3,3-difluorocyclobutyl)amino)-2-oxoethyl)-1-(4-cyanopyridin-2-yl)-n-(5-fluoropyridin-3-yl)-5-oxopyrrolidine-2-carboxamide
l01xx62
n-((1s)-1-(2-chlorophenyl)-2-((3,3-difluorocyclobutyl)amino)-2-oxoethyl)-1-(4-cyanopyridin-2-yl)-n-(5-fluoropyridin-3-yl)-5-oxo-l-prolinamide
n-((1s)-1-(2-chlorophenyl)-2-((3,3-difluorocyclobutyl)amino)-2-oxoethyl)-1-(4-cyano-2-pyridinyl)-n-(5-fluoro-3-pyridinyl)-5-oxo-l-prolinamide
(2s)-2-(2-chlorophenyl)-2-{1-[(2s)-1-(4-cyanopyridin-2-yl)-5-oxopyrrolidin-2-yl]-n-(5-fluoropyridin-3-yl)formamido}-n-(3,3-difluorocyclobutyl)acetamide
EN300-21623926

Research Excerpts

Overview

Ivosidenib (AG-120) is an oral, targeted agent that suppresses production of the oncometabolite 2-hydroxyglutarate via inhibition of the mutant isocitrate dehydrogenase 1 (IDH1) enzyme. The drug is approved in the United States for specific cases of acute myeloid leukemia.

ExcerptReferenceRelevance
"Ivosidenib is an IDH1 inhibitor, approved for use in patients with IDH1-mutated AML."( Multicenter Phase I Trial of Ivosidenib as Maintenance Treatment Following Allogeneic Hematopoietic Cell Transplantation for IDH1-Mutated Acute Myeloid Leukemia.
Amrein, PC; Bottoms, AS; Breton, E; Brock, J; Brunner, AM; Chen, YB; DeFilipp, Z; El-Jawahri, A; Fathi, AT; Ho, VT; Kelley, D; Kim, AS; Kim, HT; Knight, LW; Levis, MJ; Li, S; Marchione, DM; McAfee, SL; Mims, AS; Perry, LH; Soiffer, RJ; Wahl, JL, 2023
)
1.92
"Ivosidenib (AG-120) is an oral, targeted agent that suppresses production of the oncometabolite 2-hydroxyglutarate via inhibition of the mutant isocitrate dehydrogenase 1 (IDH1; mIDH1) enzyme. "( Ivosidenib induces deep durable remissions in patients with newly diagnosed IDH1-mutant acute myeloid leukemia.
Agresta, SV; Altman, JK; Arellano, ML; Attar, EC; Choe, S; Dai, D; de Botton, S; DiNardo, CD; Donnellan, W; Erba, HP; Fan, B; Fathi, AT; Hickman, D; Kantarjian, HM; Kapsalis, SM; Liu, H; Mannis, GN; Mims, AS; Pollyea, DA; Prince, GT; Roboz, GJ; Stein, AS; Stein, EM; Stone, RM; Tallman, MS; Uy, GL; Wang, H; Watts, JM; Wu, B; Yen, KE; Zhang, V, 2020
)
3.44
"Ivosidenib (AG-120) is a selective inhibitor of mutant IDH1 approved in the United States for specific cases of acute myeloid leukemia."( Phase I Study of the Mutant IDH1 Inhibitor Ivosidenib: Safety and Clinical Activity in Patients With Advanced Chondrosarcoma.
Agresta, S; Beeram, M; Burris, H; Choe, S; Cote, GM; Fan, B; Gliser, C; Janku, F; Jiang, L; Mir, O; Pandya, SS; Tap, WD; Trent, JC; Villalobos, VM; Wagner, AJ; Wu, B; Yen, K, 2020
)
1.54
"Ivosidenib (AG-120) is a targeted, potent, oral inhibitor of the mutant IDH1 protein."( Clinical pharmacokinetics and pharmacodynamics of ivosidenib in patients with advanced hematologic malignancies with an IDH1 mutation.
Agresta, SV; Attar, EC; Dai, D; de Botton, S; DiNardo, CD; Fan, B; Lemieux, I; Liu, G; Liu, H; Stein, E; Yang, H, 2020
)
1.53
"Ivosidenib is a selective, potent inhibitor of the IDH1 mutant protein."( Evaluating ivosidenib for the treatment of acute myeloid leukemia.
Donker, ML; Ossenkoppele, GJ, 2020
)
1.67
"Ivosidenib is a promising, most probably practice changing, new drug for the treatment of IDH1-mutated AML. "( Evaluating ivosidenib for the treatment of acute myeloid leukemia.
Donker, ML; Ossenkoppele, GJ, 2020
)
2.39
"Ivosidenib is an oral inhibitor of the mutant isocitrate dehydrogenase 1 (IDH1) enzyme, approved for treatment of "( Mutant Isocitrate Dehydrogenase 1 Inhibitor Ivosidenib in Combination With Azacitidine for Newly Diagnosed Acute Myeloid Leukemia.
Choe, S; Daigle, S; de Botton, S; DiNardo, CD; Döhner, H; Fan, B; Fathi, AT; Frankfurt, O; Franovic, A; Frattini, MG; Gianolio, DA; Goldwasser, M; Gong, J; Kantarjian, HM; Lersch, F; Martinelli, G; Patel, PA; Raffoux, E; Schuh, AC; Stein, AS; Stein, EM; Stone, RM; Tan, P; Vyas, P; Winkler, T; Wu, B; Zeidan, AM; Zhang, V, 2021
)
2.33
"Ivosidenib is a once daily (q.d.), orally available, potent mutant isocitrate dehydrogenase 1 (mIDH1) inhibitor approved for treatment of patients with relapsed or refractory (R/R) acute myeloid leukemia (AML) and intensive chemotherapy ineligible AML with a susceptible IDH1 mutation. "( Population pharmacokinetic and exposure-response analyses of ivosidenib in patients with IDH1-mutant advanced hematologic malignancies.
Fan, B; Jiang, X; Kapsalis, S; Kleijn, HJ; Le, K; Liu, G; Liu, H; Poland, B; Wada, R; Yang, H, 2021
)
2.31
"Ivosidenib (AG-120) is an oral, targeted, small-molecule inhibitor of mutant IDH1."( Durable Remissions with Ivosidenib in IDH1-Mutated Relapsed or Refractory AML.
Agresta, S; Altman, JK; Arellano, ML; Attar, EC; Choe, S; Collins, RH; Dai, D; de Botton, S; DiNardo, CD; Donnellan, W; Erba, HP; Fan, B; Fathi, AT; Foran, JM; Goldwasser, M; Kantarjian, HM; Kapsalis, SM; Liu, H; Mannis, GN; Mims, AS; Pigneux, A; Pollyea, DA; Prince, GT; Roboz, GJ; Sekeres, MA; Slack, JL; Stein, AS; Stein, EM; Stone, RM; Stuart, RK; Swords, R; Tallman, MS; Traer, E; Uy, GL; Wang, H; Willekens, C; Wu, B; Yang, H; Yen, KE; Zhang, V, 2018
)
1.51
"Ivosidenib (AG-120) is a targeted mutant IDH1 inhibitor under evaluation in a phase 1 dose escalation and expansion study of IDH1-mutant advanced solid tumors including cholangiocarcinoma, chondrosarcoma, and glioma."( Clinical pharmacokinetics and pharmacodynamics of ivosidenib, an oral, targeted inhibitor of mutant IDH1, in patients with advanced solid tumors.
Agresta, S; Dai, D; Fan, B; Gliser, C; Goyal, L; Jiang, L; Liu, G; Lowery, MA; Manyak, E; Mellinghoff, IK; Nimkar, T; Pandya, SS; Prahl Judge, M; Tap, WD; Wen, PY; Yang, H, 2020
)
1.53
"Ivosidenib is an oral, targeted inhibitor of mutant IDH1 (mIDH1) approved in the USA for the treatment of mIDH1 acute myeloid leukaemia in newly diagnosed patients ineligible for intensive chemotherapy and patients with relapsed or refractory disease."( Safety and activity of ivosidenib in patients with IDH1-mutant advanced cholangiocarcinoma: a phase 1 study.
Abou-Alfa, GK; Agresta, SV; Aguado-Fraile, E; Azad, NS; Beeram, M; Burris, HA; Choe, S; Cleary, JM; Fan, B; Gliser, C; Gore, L; Goyal, L; Hollebecque, A; Janku, F; Jiang, L; Lowery, MA; Maher, EA; Pandya, SS; Shroff, RT; Trent, JC; Wu, B; Zhu, AX, 2019
)
1.55
"Ivosidenib is a novel oral inhibitor of mutated isocitrate dehydrogenase 1 approved for the treatment of refractory or relapsed acute myeloid leukemia in patients with isocitrate dehydrogenase 1 mutations or as first-line agent in patients unable to tolerate chemotherapy. "( Ivosidenib induction therapy complicated by myopericarditis and cardiogenic shock: A case report and literature review.
Chen, A; Hernandez Burgos, P; Patel, J, 2020
)
3.44

Toxicity

ExcerptReferenceRelevance
" Common (≥20%) adverse events, regardless of cause, were fatigue (31 [42%]; two [3%] grade ≥3), nausea (25 [34%]; one [1%] grade ≥3), diarrhoea (23 [32%]), abdominal pain (20 [27%]; two [3%] grade ≥3), decreased appetite (20 [27%]; one [1%] grade ≥3), and vomiting (17 [23%])."( Safety and activity of ivosidenib in patients with IDH1-mutant advanced cholangiocarcinoma: a phase 1 study.
Abou-Alfa, GK; Agresta, SV; Aguado-Fraile, E; Azad, NS; Beeram, M; Burris, HA; Choe, S; Cleary, JM; Fan, B; Gliser, C; Gore, L; Goyal, L; Hollebecque, A; Janku, F; Jiang, L; Lowery, MA; Maher, EA; Pandya, SS; Shroff, RT; Trent, JC; Wu, B; Zhu, AX, 2019
)
0.82
" The objective of our study is to determine the incidence, grade, clinical, and histopathologic features of dermatologic adverse events (DAEs) secondary to IDHi."( Dermatologic adverse events associated with IDH inhibitors ivosidenib and enasidenib for the treatment of acute myeloid leukemia.
Cowen, EA; Dusza, S; Markova, A; Parisi, R; Pulitzer, MP; Stein, EM; Stoll, JR; Zhu, H, 2022
)
0.96

Pharmacokinetics

Ivosidenib 500-mg QD has favorable pharmacokinetic and pharmacodynamic profiles in patients with advanced hematologic malignancies with an IDH1 mutation.

ExcerptReferenceRelevance
" We explored the pharmacokinetic (PK) and pharmacodynamic (PD) profiles of ivosidenib in these populations."( Clinical pharmacokinetics and pharmacodynamics of ivosidenib, an oral, targeted inhibitor of mutant IDH1, in patients with advanced solid tumors.
Agresta, S; Dai, D; Fan, B; Gliser, C; Goyal, L; Jiang, L; Liu, G; Lowery, MA; Manyak, E; Mellinghoff, IK; Nimkar, T; Pandya, SS; Prahl Judge, M; Tap, WD; Wen, PY; Yang, H, 2020
)
1.04
"Ivosidenib 500-mg QD has favorable pharmacokinetic and pharmacodynamic profiles in patients with advanced hematologic malignancies with an IDH1 mutation."( Clinical pharmacokinetics and pharmacodynamics of ivosidenib in patients with advanced hematologic malignancies with an IDH1 mutation.
Agresta, SV; Attar, EC; Dai, D; de Botton, S; DiNardo, CD; Fan, B; Lemieux, I; Liu, G; Liu, H; Stein, E; Yang, H, 2020
)
2.25
"Develop a physiologically based pharmacokinetic (PBPK) model of ivosidenib using in vitro and clinical PK data from healthy participants (HPs), refine it with clinical data on ivosidenib co-administered with itraconazole, and develop a model for patients with acute myeloid leukemia (AML) and apply it to predict ivosidenib drug-drug interactions (DDI)."( Physiologically based pharmacokinetic modeling and simulation to predict drug-drug interactions of ivosidenib with CYP3A perpetrators in patients with acute myeloid leukemia.
Fan, B; Ke, A; Le, K; Prakash, C; Yang, H, 2020
)
1.01

Compound-Compound Interactions

The study evaluated the safety and efficacy of ivosidenib or enasidenib combined with intensive chemotherapy in patients with newly diagnosed mIDH1/2 acute myeloid leukemia.

ExcerptReferenceRelevance
"Develop a physiologically based pharmacokinetic (PBPK) model of ivosidenib using in vitro and clinical PK data from healthy participants (HPs), refine it with clinical data on ivosidenib co-administered with itraconazole, and develop a model for patients with acute myeloid leukemia (AML) and apply it to predict ivosidenib drug-drug interactions (DDI)."( Physiologically based pharmacokinetic modeling and simulation to predict drug-drug interactions of ivosidenib with CYP3A perpetrators in patients with acute myeloid leukemia.
Fan, B; Ke, A; Le, K; Prakash, C; Yang, H, 2020
)
1.01
" Given their effectiveness as single agents in mIDH1/2 relapsed or refractory acute myeloid leukemia (AML), this phase 1 study evaluated the safety and efficacy of ivosidenib or enasidenib combined with intensive chemotherapy in patients with newly diagnosed mIDH1/2 AML."( Ivosidenib or enasidenib combined with intensive chemotherapy in patients with newly diagnosed AML: a phase 1 study.
Almon, C; Choe, S; Cooper, M; DiNardo, CD; Döhner, H; Fan, B; Fathi, AT; Franovic, A; Frattini, MG; Hua, L; Kantarjian, HM; Lersch, F; Löwenberg, B; McCloskey, JK; Mims, AS; Nabhan, S; Odenike, O; Ossenkoppele, GJ; Patel, PA; Pollyea, DA; Pratz, KW; Roshal, M; Savona, MR; Seet, CS; Stein, AS; Stein, EM; Stone, RM; Tallman, MS; Wang, H; Winer, ES; Wu, B, 2021
)
2.26
" An open-label phase 1 study is evaluating the safety and efficacy of ivosidenib or enasidenib combined with intensive induction and consolidation chemotherapy in adult patients with newly diagnosed mIDH1/2 acute myeloid leukemia (AML; NCT02632708)."( Pharmacokinetic/Pharmacodynamic Evaluation of Ivosidenib or Enasidenib Combined With Intensive Induction and Consolidation Chemotherapy in Patients With Newly Diagnosed IDH1/2-Mutant Acute Myeloid Leukemia.
Almon, C; Chen, Y; Cooper, M; Fan, B; Hossain, M; Hua, L; Nabhan, S; Yang, H; Yin, F, 2022
)
1.21

Bioavailability

ExcerptReferenceRelevance
" Herein, we report the discovery and optimization of a series of quinolinones to provide potent and orally bioavailable mIDH1 inhibitors with selectivity over wild-type IDH1."( Discovery and Optimization of Quinolinone Derivatives as Potent, Selective, and Orally Bioavailable Mutant Isocitrate Dehydrogenase 1 (mIDH1) Inhibitors.
Ashwell, S; Bair, KW; Barr, KJ; Campbell, AM; Caravella, JA; Castro, J; Clarke, A; Diebold, RB; Diep, H; Dinsmore, C; Ericsson, A; Fritzen, E; Gotur, D; Gustafson, GR; Hubbs, SE; Josephine, HR; Katz, M; Kauffman, G; Kershaw, M; Lancia, DR; Lin, J; Lu, W; Luke, GP; Shelekhin, T; Toms, AV; Walker, D; Wang, L; Wang, Z; Yao, L, 2019
)
0.51
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
" These findings support the dosing of ivosidenib or enasidenib in combination with intensive chemotherapy for the treatment of patients with newly diagnosed mIDH1/2 AML."( Pharmacokinetic/Pharmacodynamic Evaluation of Ivosidenib or Enasidenib Combined With Intensive Induction and Consolidation Chemotherapy in Patients With Newly Diagnosed IDH1/2-Mutant Acute Myeloid Leukemia.
Almon, C; Chen, Y; Cooper, M; Fan, B; Hossain, M; Hua, L; Nabhan, S; Yang, H; Yin, F, 2022
)
1.25
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
antineoplastic agentA substance that inhibits or prevents the proliferation of neoplasms.
EC 1.1.1.42 (isocitrate dehydrogenase) inhibitorAn EC 1.1.1.* (oxidoreductase acting on donor CH-OH group, NAD(+) or NADP(+) acceptor) inhibitor that interferes with the action of any isocitrate dehydrogenase (EC 1.1.1.42).
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (6)

ClassDescription
monochlorobenzenesAny member of the class of chlorobenzenes containing a mono- or poly-substituted benzene ring in which only one substituent is chlorine.
cyanopyridineAny pyridine carrying at least one cyano substituent.
pyrrolidin-2-onesA pyrrolidinone in which the oxo group is at position 2 of the pyrrolidine ring.
organofluorine compoundAn organofluorine compound is a compound containing at least one carbon-fluorine bond.
tertiary carboxamideA carboxamide resulting from the formal condensation of a carboxylic acid with a secondary amine; formula RC(=O)NHR(1)R(2).
secondary carboxamideA carboxamide resulting from the formal condensation of a carboxylic acid with a primary amine; formula RC(=O)NHR(1).
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Isocitrate dehydrogenase [NADP] cytoplasmicHomo sapiens (human)IC50 (µMol)0.02950.00350.52745.1760AID1366792; AID1366793; AID1610103; AID1610104; AID1610105; AID1753737; AID1753739
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Isocitrate dehydrogenase [NADP] cytoplasmicHomo sapiens (human)EC50 (µMol)0.01990.01250.62492.4000AID1753746; AID1753747
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (11)

Processvia Protein(s)Taxonomy
glyoxylate cycleIsocitrate dehydrogenase [NADP] cytoplasmicHomo sapiens (human)
tricarboxylic acid cycleIsocitrate dehydrogenase [NADP] cytoplasmicHomo sapiens (human)
isocitrate metabolic processIsocitrate dehydrogenase [NADP] cytoplasmicHomo sapiens (human)
2-oxoglutarate metabolic processIsocitrate dehydrogenase [NADP] cytoplasmicHomo sapiens (human)
glutathione metabolic processIsocitrate dehydrogenase [NADP] cytoplasmicHomo sapiens (human)
response to oxidative stressIsocitrate dehydrogenase [NADP] cytoplasmicHomo sapiens (human)
female gonad developmentIsocitrate dehydrogenase [NADP] cytoplasmicHomo sapiens (human)
response to steroid hormoneIsocitrate dehydrogenase [NADP] cytoplasmicHomo sapiens (human)
regulation of phospholipid catabolic processIsocitrate dehydrogenase [NADP] cytoplasmicHomo sapiens (human)
regulation of phospholipid biosynthetic processIsocitrate dehydrogenase [NADP] cytoplasmicHomo sapiens (human)
NADP metabolic processIsocitrate dehydrogenase [NADP] cytoplasmicHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (8)

Processvia Protein(s)Taxonomy
magnesium ion bindingIsocitrate dehydrogenase [NADP] cytoplasmicHomo sapiens (human)
isocitrate dehydrogenase (NADP+) activityIsocitrate dehydrogenase [NADP] cytoplasmicHomo sapiens (human)
protein bindingIsocitrate dehydrogenase [NADP] cytoplasmicHomo sapiens (human)
identical protein bindingIsocitrate dehydrogenase [NADP] cytoplasmicHomo sapiens (human)
protein homodimerization activityIsocitrate dehydrogenase [NADP] cytoplasmicHomo sapiens (human)
cadherin bindingIsocitrate dehydrogenase [NADP] cytoplasmicHomo sapiens (human)
NADP bindingIsocitrate dehydrogenase [NADP] cytoplasmicHomo sapiens (human)
NAD bindingIsocitrate dehydrogenase [NADP] cytoplasmicHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (10)

Processvia Protein(s)Taxonomy
extracellular regionIsocitrate dehydrogenase [NADP] cytoplasmicHomo sapiens (human)
cytoplasmIsocitrate dehydrogenase [NADP] cytoplasmicHomo sapiens (human)
peroxisomeIsocitrate dehydrogenase [NADP] cytoplasmicHomo sapiens (human)
peroxisomal matrixIsocitrate dehydrogenase [NADP] cytoplasmicHomo sapiens (human)
cytosolIsocitrate dehydrogenase [NADP] cytoplasmicHomo sapiens (human)
secretory granule lumenIsocitrate dehydrogenase [NADP] cytoplasmicHomo sapiens (human)
extracellular exosomeIsocitrate dehydrogenase [NADP] cytoplasmicHomo sapiens (human)
tertiary granule lumenIsocitrate dehydrogenase [NADP] cytoplasmicHomo sapiens (human)
ficolin-1-rich granule lumenIsocitrate dehydrogenase [NADP] cytoplasmicHomo sapiens (human)
cytosolIsocitrate dehydrogenase [NADP] cytoplasmicHomo sapiens (human)
mitochondrionIsocitrate dehydrogenase [NADP] cytoplasmicHomo sapiens (human)
peroxisomeIsocitrate dehydrogenase [NADP] cytoplasmicHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (34)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1366793Inhibition of IDH1 R132C mutant in human HT1080 cells assessed as reduction in 2-hydroxyglutarate production2017Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
Discovery and structure-activity-relationship study of novel conformationally restricted indane analogues for mutant isocitric dehydrogenase 1 (IDH1) inhibitors.
AID1610112Half life in ICR mouse at 5 mg/kg, po measured upto 24 hrs by LCMS analysis2019European journal of medicinal chemistry, Dec-01, Volume: 183Discovery of new small molecule inhibitors targeting isocitrate dehydrogenase 1 (IDH1) with blood-brain barrier penetration.
AID1610111Cmax in ICR mouse at 5 mg/kg, po measured upto 24 hrs by LCMS analysis2019European journal of medicinal chemistry, Dec-01, Volume: 183Discovery of new small molecule inhibitors targeting isocitrate dehydrogenase 1 (IDH1) with blood-brain barrier penetration.
AID1753737Inhibition of IDH1 R132H mutant (unknown origin) assessed as reduction in NADPH consumption using alpha-KG as substrate incubated for 5 mins by diaphorase/resazurin-coupled system
AID1513038Toxicity in patient with IDH1 mutated cholangio carcinoma assessed as fatigue at 100 to 1200 mg administered once daily for 28 days relative to control2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Inhibitors of Mutant Isocitrate Dehydrogenases 1 and 2 (mIDH1/2): An Update and Perspective.
AID1610105Inhibition of IDH1 R132C mutant in human HT1080 cells assessed as reduction in 2-HG production incubated with compound for 48 hrs by D2HG assay kit based fluorescence assay2019European journal of medicinal chemistry, Dec-01, Volume: 183Discovery of new small molecule inhibitors targeting isocitrate dehydrogenase 1 (IDH1) with blood-brain barrier penetration.
AID1513043Toxicity in patient with IDH1 mutated cholangio carcinoma assessed as pneumonia at 100 to 1200 mg administered once daily for 28 days relative to control2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Inhibitors of Mutant Isocitrate Dehydrogenases 1 and 2 (mIDH1/2): An Update and Perspective.
AID1513041Toxicity in patient with IDH1 mutated cholangio carcinoma assessed as vomiting at 100 to 1200 mg administered once daily for 28 days relative to control2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Inhibitors of Mutant Isocitrate Dehydrogenases 1 and 2 (mIDH1/2): An Update and Perspective.
AID1513040Toxicity in patient with IDH1 mutated cholangio carcinoma assessed as nausea at 100 to 1200 mg administered once daily for 28 days relative to control2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Inhibitors of Mutant Isocitrate Dehydrogenases 1 and 2 (mIDH1/2): An Update and Perspective.
AID1610108Volume of distribution at steady state in ICR mouse at 1 mg/kg, iv measured upto 24 hrs by LCMS analysis2019European journal of medicinal chemistry, Dec-01, Volume: 183Discovery of new small molecule inhibitors targeting isocitrate dehydrogenase 1 (IDH1) with blood-brain barrier penetration.
AID1610107Clearance in ICR mouse at 1 mg/kg, iv measured upto 24 hrs by LCMS analysis2019European journal of medicinal chemistry, Dec-01, Volume: 183Discovery of new small molecule inhibitors targeting isocitrate dehydrogenase 1 (IDH1) with blood-brain barrier penetration.
AID1610110AUC in ICR mouse at 1 mg/kg, iv measured upto 24 hrs by LCMS analysis2019European journal of medicinal chemistry, Dec-01, Volume: 183Discovery of new small molecule inhibitors targeting isocitrate dehydrogenase 1 (IDH1) with blood-brain barrier penetration.
AID1610102Inhibition of wild type recombinant human C-terminal His8-tagged IDH1 expressed in Escherichia coli BL21 assessed as reduction in NADP consumption using DL-isocitrate as substrate preincubated for 60 mins followed by substrate addition and measured for 602019European journal of medicinal chemistry, Dec-01, Volume: 183Discovery of new small molecule inhibitors targeting isocitrate dehydrogenase 1 (IDH1) with blood-brain barrier penetration.
AID1513039Toxicity in patient with IDH1 mutated cholangio carcinoma assessed as diarrhea at 100 to 1200 mg administered once daily for 28 days relative to control2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Inhibitors of Mutant Isocitrate Dehydrogenases 1 and 2 (mIDH1/2): An Update and Perspective.
AID1610116Drug uptake in brain of athymic BALB/c nude mouse xenografted with human HT1080 cells at 50 mg/kg, po administered as a single dose via gavage measured upto 24 hrs post dosing by LC-MS/MS analysis2019European journal of medicinal chemistry, Dec-01, Volume: 183Discovery of new small molecule inhibitors targeting isocitrate dehydrogenase 1 (IDH1) with blood-brain barrier penetration.
AID1610113AUC in ICR mouse at 5 mg/kg, po measured upto 24 hrs by LCMS analysis2019European journal of medicinal chemistry, Dec-01, Volume: 183Discovery of new small molecule inhibitors targeting isocitrate dehydrogenase 1 (IDH1) with blood-brain barrier penetration.
AID1753746Inhibition of C-terminal NanoLuc 86b-tagged IDH1 R132H (unknown origin) expressed in HEK293T cells assessed as increase in thermal stability by measuring Nano-luciferase activity at 56 degC for 3.5 min by CETSA
AID1753739Inhibition of IDH1 R132C mutant (unknown origin) assessed as reduction in NADPH consumption using alpha-KG as substrate incubated for 5 mins by diaphorase/resazurin-coupled system
AID1366792Inhibition of IDH1 R132H mutant (unknown origin)2017Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
Discovery and structure-activity-relationship study of novel conformationally restricted indane analogues for mutant isocitric dehydrogenase 1 (IDH1) inhibitors.
AID1753747Inhibition of IDH1 R132H mutant (unknown origin) expressed in human U87 cells assessed as R-2-hydroxyglutarate production after 48 hrs by LC-MS analysis
AID1610109Half life in ICR mouse at 1 mg/kg, iv measured upto 24 hrs by LCMS analysis2019European journal of medicinal chemistry, Dec-01, Volume: 183Discovery of new small molecule inhibitors targeting isocitrate dehydrogenase 1 (IDH1) with blood-brain barrier penetration.
AID1610104Inhibition of recombinant human C-terminal His8-tagged IDH1 R132H mutant expressed in Escherichia coli BL21 assessed as reduction in NADPH consumption using alpha-ketoglutarate as substrate preincubated for 60 mins followed by substrate addition measured 2019European journal of medicinal chemistry, Dec-01, Volume: 183Discovery of new small molecule inhibitors targeting isocitrate dehydrogenase 1 (IDH1) with blood-brain barrier penetration.
AID1610115Drug uptake in plasma of athymic BALB/c nude mouse xenografted with human HT1080 cells at 50 mg/kg, po administered as a single dose via gavage measured upto 24 hrs post dosing by LC-MS/MS analysis2019European journal of medicinal chemistry, Dec-01, Volume: 183Discovery of new small molecule inhibitors targeting isocitrate dehydrogenase 1 (IDH1) with blood-brain barrier penetration.
AID1513042Toxicity in patient with IDH1 mutated cholangio carcinoma assessed as febrile neutropenia at 100 to 1200 mg administered once daily for 28 days relative to control2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Inhibitors of Mutant Isocitrate Dehydrogenases 1 and 2 (mIDH1/2): An Update and Perspective.
AID1610114Oral bioavailability in ICR mouse at 5 mg/kg measured upto 24 hrs by LCMS analysis2019European journal of medicinal chemistry, Dec-01, Volume: 183Discovery of new small molecule inhibitors targeting isocitrate dehydrogenase 1 (IDH1) with blood-brain barrier penetration.
AID1610121Drug uptake in tumor of athymic BALB/c nude mouse xenografted with human HT1080 cells at 50 mg/kg, po administered as a single dose via gavage measured upto 24 hrs post dosing by LC-MS/MS analysis2019European journal of medicinal chemistry, Dec-01, Volume: 183Discovery of new small molecule inhibitors targeting isocitrate dehydrogenase 1 (IDH1) with blood-brain barrier penetration.
AID1562422Efflux ratio of apparent permeability from basolateral side to apical side over apical side to basolateral side in MDCK cells harboring MDR1 (unknown origin) at 10 uM incubated for 2 hrs by LC-MS/MS analysis2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Discovery and Optimization of Quinolinone Derivatives as Potent, Selective, and Orally Bioavailable Mutant Isocitrate Dehydrogenase 1 (mIDH1) Inhibitors.
AID1610103Inhibition of recombinant human C-terminal His8-tagged IDH1 R132C mutant expressed in Escherichia coli BL21 assessed as reduction in NADPH consumption using alpha-ketoglutarate as substrate preincubated for 60 mins followed by substrate addition and measu2019European journal of medicinal chemistry, Dec-01, Volume: 183Discovery of new small molecule inhibitors targeting isocitrate dehydrogenase 1 (IDH1) with blood-brain barrier penetration.
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
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (94)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's22 (23.40)24.3611
2020's72 (76.60)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 65.88

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index65.88 (24.57)
Research Supply Index4.76 (2.92)
Research Growth Index4.74 (4.65)
Search Engine Demand Index110.49 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (65.88)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials22 (23.40%)5.53%
Reviews19 (20.21%)6.00%
Case Studies10 (10.64%)4.05%
Observational1 (1.06%)0.25%
Other42 (44.68%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]