Vorasidenib

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C14H13ClF6N6
Molecular Weight	414.737
Optical Activity	UNSPECIFIED
Defined Stereocenters	2 / 2
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

C[C@@H](NC1=NC(=NC(N[C@H](C)C(F)(F)F)=N1)C2=CC=CC(Cl)=N2)C(F)(F)F

InChI

InChIKey=QCZAWDGAVJMPTA-RNFRBKRXSA-N

InChI=1S/C14H13ClF6N6/c1-6(13(16,17)18)22-11-25-10(8-4-3-5-9(15)24-8)26-12(27-11)23-7(2)14(19,20)21/h3-7H,1-2H3,(H2,22,23,25,26,27)/t6-,7-/m1/s1

HIDE SMILES / InChI

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/27355333 | https://clinicaltrials.gov/ct2/show/NCT02492737 | https://clinicaltrials.gov/ct2/show/NCT02481154

Vorasidenib (also known as AG 881) was developed as an isocitrate dehydrogenase (IDH) type 1 in the cytoplasm and type 2 in the mitochondria, with potential antineoplastic activity. It is known that IDH is an essential enzyme for cellular respiration in the tricarboxylic acid (TCA) cycle. Isocitrate dehydrogenases 1 and 2 (IDH1/2) are homodimeric enzymes that catalyze the conversion of isocitrate to α-ketoglutarate (α-KG) in the tricarboxylic acid cycle. Vorasidenib participated in phase I clinical trials in patients with advanced hematologic malignancies and in gliomas.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Isocitrate dehydrogenase [NADP], mitochondrial 6 Target ID: P48735 Gene ID: 3418.0 Gene Symbol: IDH2 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/27355333	Inhibitor 8504
Isocitrate dehydrogenase [NADP] cytoplasmic 5 Target ID: O75874 Gene ID: 3417.0 Gene Symbol: IDH1 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/27355333	Inhibitor 8504

Conditions

Condition	Modality	Highest Phase	Product
Acute myeloid leukemia 141 Sources: https://clinicaltrials.gov/ct2/show/record/NCT02492737	Primary	Phase I 438	Unknown Approved Use Unknown
Myelodysplastic syndromes 61 Sources: https://clinicaltrials.gov/ct2/show/NCT02492737	Primary	Phase I 438	Unknown Approved Use Unknown
Glioma 25 Sources: https://clinicaltrials.gov/ct2/show/record/NCT02481154	Primary	Phase I 438	Unknown Approved Use Unknown

C_max

Value	Dose	Analyte	Population
26.7 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
21.8 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
70.2 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
104 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
178 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
302 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
45.7 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
66.5 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	25 mg 1 times / day steady-state, oral dose: 25 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
195 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	50 mg 1 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
223 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
412 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	200 mg 1 times / day steady-state, oral dose: 200 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
493 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	300 mg 1 times / day steady-state, oral dose: 300 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
47 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	VORASIDENIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
81.4 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	VORASIDENIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
91.9 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VORASIDENIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
226 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	VORASIDENIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
226 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	200 mg 2 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	VORASIDENIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
449 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:	VORASIDENIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
452 ng × h/mL EXPERIMENT https://pdfs.semanticscholar.org/956e/e4837b17d4c1f34bb06e9b54ae88a70a5176.pdf	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
940 ng × h/mL EXPERIMENT https://pdfs.semanticscholar.org/956e/e4837b17d4c1f34bb06e9b54ae88a70a5176.pdf	25 mg 1 times / day steady-state, oral dose: 25 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2282 ng × h/mL EXPERIMENT https://pdfs.semanticscholar.org/956e/e4837b17d4c1f34bb06e9b54ae88a70a5176.pdf	50 mg 1 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2476 ng × h/mL EXPERIMENT https://pdfs.semanticscholar.org/956e/e4837b17d4c1f34bb06e9b54ae88a70a5176.pdf	100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
7020 ng × h/mL EXPERIMENT https://pdfs.semanticscholar.org/956e/e4837b17d4c1f34bb06e9b54ae88a70a5176.pdf	200 mg 1 times / day steady-state, oral dose: 200 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
7020 ng × h/mL EXPERIMENT https://pdfs.semanticscholar.org/956e/e4837b17d4c1f34bb06e9b54ae88a70a5176.pdf	300 mg 1 times / day steady-state, oral dose: 300 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
84.4 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
103 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
265 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
496 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
814 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1540 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
284 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
507 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	25 mg 1 times / day steady-state, oral dose: 25 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1310 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	50 mg 1 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1500 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3160 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	200 mg 1 times / day steady-state, oral dose: 200 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
4010 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	300 mg 1 times / day steady-state, oral dose: 300 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
260 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	VORASIDENIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
409 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	VORASIDENIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
378 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VORASIDENIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
990 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	VORASIDENIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
990 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	200 mg 2 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	VORASIDENIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1860 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:	VORASIDENIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Analyte	Population
67.2 h EXPERIMENT https://pdfs.semanticscholar.org/956e/e4837b17d4c1f34bb06e9b54ae88a70a5176.pdf	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
67.2 h EXPERIMENT https://pdfs.semanticscholar.org/956e/e4837b17d4c1f34bb06e9b54ae88a70a5176.pdf	25 mg 1 times / day steady-state, oral dose: 25 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
67.2 h EXPERIMENT https://pdfs.semanticscholar.org/956e/e4837b17d4c1f34bb06e9b54ae88a70a5176.pdf	50 mg 1 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
67.2 h EXPERIMENT https://pdfs.semanticscholar.org/956e/e4837b17d4c1f34bb06e9b54ae88a70a5176.pdf	100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
67.2 h EXPERIMENT https://pdfs.semanticscholar.org/956e/e4837b17d4c1f34bb06e9b54ae88a70a5176.pdf	200 mg 1 times / day steady-state, oral dose: 200 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
67.2 h EXPERIMENT https://pdfs.semanticscholar.org/956e/e4837b17d4c1f34bb06e9b54ae88a70a5176.pdf	300 mg 1 times / day steady-state, oral dose: 300 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
68.7 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
87.3 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
46.9 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
64.7 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
55.1 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
47.4 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
68.7 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
87.3 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	25 mg 1 times / day steady-state, oral dose: 25 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
46.9 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	50 mg 1 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
64.7 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
55.1 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	200 mg 1 times / day steady-state, oral dose: 200 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
47.4 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	300 mg 1 times / day steady-state, oral dose: 300 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
176 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	VORASIDENIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
54.1 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	VORASIDENIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
45.5 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VORASIDENIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
51 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	VORASIDENIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
51 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	200 mg 2 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	VORASIDENIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
78.8 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:	VORASIDENIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
6% EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364866			VORASIDENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

PubMed

Title	Date	PubMed
Inhibitors of Mutant Isocitrate Dehydrogenases 1 and 2 (mIDH1/2): An Update and Perspective.	2018-10-25	29847930
Crystal structures of pan-IDH inhibitor AG-881 in complex with mutant human IDH1 and IDH2.	2018-09-18	30131249
Targeting isocitrate dehydrogenase (IDH) in cancer.	2016-05	27355333
The Evolving Landscape in the Development of Isocitrate Dehydrogenase Mutant Inhibitors.	2016	27292784

Sample Use Guides

In Vivo Use Guide

oral doses of AG-881 to determine maximum tolerated dose (MTD) and/or the recommended Phase II dose

Route of Administration: Oral

Name

Type

Language

Vorasidenib

Official Name

English

1,3,5-Triazine-2,4-diamine, 6-(6-chloro-2-pyridinyl)-N2,N4-bis[(1R)-2,2,2-trifluoro-1-methylethyl]-

Preferred Name

English

vorasidenib [INN]

Common Name

English

AG-881

Code

English

Vorasidenib [WHO-DD]

Common Name

English

VORASIDENIB [USAN]

Common Name

English

6-(6-Chloro-2-pyridinyl)-N2,N4-bis[(1R)-2,2,2-trifluoro-1-methylethyl]-1,3,5-triazine-2,4-diamine

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C137826