U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C29H44N8O3
Molecular Weight 552.7126
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of GILTERITINIB

SMILES

CCc1c(NC2CCOCC2)[nH]c(=Nc3ccc(c(c3)OC)N4CCC(CC4)N5CCN(C)CC5)c(C(=O)N)n1

InChI

InChIKey=GYQYAJJFPNQOOW-UHFFFAOYSA-N
InChI=1S/C29H44N8O3/c1-4-23-28(31-20-9-17-40-18-10-20)34-29(26(33-23)27(30)38)32-21-5-6-24(25(19-21)39-3)37-11-7-22(8-12-37)36-15-13-35(2)14-16-36/h5-6,19-20,22H,4,7-18H2,1-3H3,(H2,30,38)(H2,31,32,34)

HIDE SMILES / InChI

Molecular Formula C29H44N8O3
Molecular Weight 552.7126
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment:: https://ash.confex.com/ash/2016/webprogram/Paper92543.html | http://www.activebiochem.com/Product/Gilteritinib.html | https://www.ncbi.nlm.nih.gov/pubmed/26279055 | https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211349Orig1s000MultidisciplineR.pdf

Gilteritinib, also known as ASP2215, is a potent FLT3/AXL inhibitor, which showed potent antileukemic activity against AML with either or both FLT3-ITD and FLT3-D835 mutations. In in vitro, among the 78 tyrosine kinases tested, Gilteritinib inhibited FLT3, LTK, ALK, and AXL kinases by over 50% at 1 nM with an IC50 value of 0.29 nM for FLT3, approximately 800-fold more potent than for c-KIT, the inhibition of which is linked to a potential risk of myelosuppression. Gilteritinib inhibited the growth of MV4-11 cells, which harbor FLT3-ITD, with an IC50 value of 0.92 nM, accompanied with inhibition of pFLT3, pAKT, pSTAT5, pERK, and pS6. Gilteritinib decreased tumor burden in bone marrow and prolonged the survival of mice intravenously transplanted with MV4-11 cells. In previous preclinical studies, gilteritinib has demonstrated superior antitumor effects when given in combination with AraC and either DNR or IDR compared with combination chemotherapy. In November 2018, the FDA approved gilteritinib for treatment of adult patients with relapsed or refractory acute myeloid leukemia (AML) with a FLT3 mutation as detected by an FDA-approved test.

CNS Activity

Curator's Comment:: Concentrations were highest in the liver, then spleen, kidneys, adrenal glands and lung; and lowest in the plasma, followed by the testes, brain and blood

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
XOSPATA

Approved Use

XOSPATA is a kinase inhibitor indicated for the treatment of adult patients who have relapsed or refractory acute myeloid leukemia (AML) with a FLT3 mutation as detected by an FDA-approved test.

Launch Date

1543276800000
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
137 ng/mL
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GILTERITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1257 ng/mL
300 mg 1 times / day multiple, oral
dose: 300 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
GILTERITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
216 ng/mL
450 mg single, oral
dose: 450 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GILTERITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
216.38 ng/mL
120 mg single, oral
dose: 120 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GILTERITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1528 ng/mL
450 mg 1 times / day multiple, oral
dose: 450 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
GILTERITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
374 ng/mL
120 mg 1 times / day steady-state, oral
dose: 120 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
GILTERITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
374 ng/mL
120 mg 1 times / day steady-state, oral
dose: 120 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
GILTERITINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
107.6 ng/mL
40 mg 1 times / day steady, oral
dose: 40 mg
route of administration: oral
experiment type: steady
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
136.7 ng/mL
120 mg single, oral
dose: 120 mg
route of administration: oral
experiment type: single
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
1462 ng/mL
200 mg 1 times / day steady, oral
dose: 200 mg
route of administration: oral
experiment type: steady
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
1525 ng/mL
300 mg 1 times / day steady, oral
dose: 300 mg
route of administration: oral
experiment type: steady
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
1528 ng/mL
450 mg 1 times / day steady, oral
dose: 450 mg
route of administration: oral
experiment type: steady
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
168.2 ng/mL
200 mg single, oral
dose: 200 mg
route of administration: oral
experiment type: single
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
204.3 ng/mL
300 mg single, oral
dose: 300 mg
route of administration: oral
experiment type: single
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
207.6 ng/mL
450 mg single, oral
dose: 450 mg
route of administration: oral
experiment type: single
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
24.9799999999999 ng/mL
40 mg single, oral
dose: 40 mg
route of administration: oral
experiment type: single
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
374.2 ng/mL
120 mg 1 times / day steady, oral
dose: 120 mg
route of administration: oral
experiment type: steady
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
376.4 ng/mL
80 mg 1 times / day steady, oral
dose: 80 mg
route of administration: oral
experiment type: steady
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
75.29 ng/mL
80 mg single, oral
dose: 80 mg
route of administration: oral
experiment type: single
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
2446 ng × h/mL
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GILTERITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
28711 ng × h/mL
300 mg 1 times / day multiple, oral
dose: 300 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
GILTERITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
3324 ng × h/mL
450 mg single, oral
dose: 450 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GILTERITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
3340.23 ng × h/mL
120 mg single, oral
dose: 120 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GILTERITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
37468 ng × h/mL
450 mg 1 times / day multiple, oral
dose: 450 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
GILTERITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
6943 ng × h/mL
120 mg 1 times / day steady-state, oral
dose: 120 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
GILTERITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
6943 ng × h/mL
120 mg 1 times / day steady-state, oral
dose: 120 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
GILTERITINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
1216 ng*h/mL
80 mg single, oral
dose: 80 mg
route of administration: oral
experiment type: single
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
2480 ng*h/mL
120 mg single, oral
dose: 120 mg
route of administration: oral
experiment type: single
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
2482 ng*h/mL
40 mg 1 times / day steady, oral
dose: 40 mg
route of administration: oral
experiment type: steady
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
3022 ng*h/mL
200 mg single, oral
dose: 200 mg
route of administration: oral
experiment type: single
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
31005 ng*h/mL
300 mg 1 times / day steady, oral
dose: 300 mg
route of administration: oral
experiment type: steady
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
31428 ng*h/mL
200 mg 1 times / day steady, oral
dose: 200 mg
route of administration: oral
experiment type: steady
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
3324 ng*h/mL
450 mg single, oral
dose: 450 mg
route of administration: oral
experiment type: single
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
34768 ng*h/mL
450 mg 1 times / day steady, oral
dose: 450 mg
route of administration: oral
experiment type: steady
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
360 ng*h/mL
40 mg single, oral
dose: 40 mg
route of administration: oral
experiment type: single
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
4163 ng*h/mL
300 mg single, oral
dose: 300 mg
route of administration: oral
experiment type: single
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
6943 ng*h/mL
120 mg 1 times / day steady, oral
dose: 120 mg
route of administration: oral
experiment type: steady
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
6958 ng*h/mL
80 mg 1 times / day steady, oral
dose: 80 mg
route of administration: oral
experiment type: steady
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
1216 ng*h/mL
80 mg single, oral
dose: 80 mg
route of administration: oral
experiment type: single
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
1990 ng*h/mL
40 mg 1 times / day steady, oral
dose: 40 mg
route of administration: oral
experiment type: steady
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
2480 ng*h/mL
120 mg single, oral
dose: 120 mg
route of administration: oral
experiment type: single
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
2544 ng*h/mL
450 mg single, oral
dose: 450 mg
route of administration: oral
experiment type: single
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
3024 ng*h/mL
200 mg single, oral
dose: 200 mg
route of administration: oral
experiment type: single
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
31749 ng*h/mL
300 mg 1 times / day steady, oral
dose: 300 mg
route of administration: oral
experiment type: steady
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
32248 ng*h/mL
200 mg 1 times / day steady, oral
dose: 200 mg
route of administration: oral
experiment type: steady
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
35506 ng*h/mL
450 mg 1 times / day steady, oral
dose: 450 mg
route of administration: oral
experiment type: steady
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
360.4 ng*h/mL
40 mg single, oral
dose: 40 mg
route of administration: oral
experiment type: single
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
4181 ng*h/mL
300 mg single, oral
dose: 300 mg
route of administration: oral
experiment type: single
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
6943 ng*h/mL
120 mg 1 times / day steady, oral
dose: 120 mg
route of administration: oral
experiment type: steady
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
7111 ng*h/mL
80 mg 1 times / day steady, oral
dose: 80 mg
route of administration: oral
experiment type: steady
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
159 h
300 mg 1 times / day multiple, oral
dose: 300 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
GILTERITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
84 h
120 mg single, oral
dose: 120 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GILTERITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
113 h
120 mg 1 times / day steady-state, oral
dose: 120 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
GILTERITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
113 h
120 mg 1 times / day steady-state, oral
dose: 120 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
GILTERITINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
45.8499999999999 h
120 mg 1 times / day steady, oral
dose: 120 mg
route of administration: oral
experiment type: steady
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
141.9 h
200 mg 1 times / day steady, oral
dose: 200 mg
route of administration: oral
experiment type: steady
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
142.2 h
300 mg 1 times / day steady, oral
dose: 300 mg
route of administration: oral
experiment type: steady
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
151.8 h
40 mg 1 times / day steady, oral
dose: 40 mg
route of administration: oral
experiment type: steady
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
86.11 h
80 mg 1 times / day steady, oral
dose: 80 mg
route of administration: oral
experiment type: steady
co-administered:
GILTERITINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
6%
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GILTERITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
6%
300 mg 1 times / day multiple, oral
dose: 300 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
GILTERITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
6%
450 mg single, oral
dose: 450 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GILTERITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
6%
450 mg 1 times / day multiple, oral
dose: 450 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
GILTERITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
6%
120 mg 1 times / day steady-state, oral
dose: 120 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
GILTERITINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
6%
GILTERITINIB plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
300 mg 1 times / day multiple, oral
MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
unhealthy, 62 years (range: 21–90 years)
300 mg single, oral
MTD
unhealthy, 62 years (range: 21–90 years)
450 mg 1 times / day multiple, oral
Dose: 450 mg, 1 times / day
Route: oral
Route: multiple
Dose: 450 mg, 1 times / day
Sources:
unhealthy, 62 years (range: 21–90 years)
Health Status: unhealthy
Age Group: 62 years (range: 21–90 years)
Sex: M+F
Sources:
450 mg single, oral
Dose: 450 mg
Route: oral
Route: single
Dose: 450 mg
Sources:
unhealthy, 62 years (range: 21–90 years)
Health Status: unhealthy
Age Group: 62 years (range: 21–90 years)
Sex: M+F
Sources:
120 mg 1 times / day steady, oral
Recommended
Dose: 120 mg, 1 times / day
Route: oral
Route: steady
Dose: 120 mg, 1 times / day
Sources:
unhealthy
Disc. AE: Pneumonia, Sepsis...
AEs leading to
discontinuation/dose reduction:
Pneumonia (2%)
Sepsis (2%)
Dyspnea (1%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Dyspnea 1%
Disc. AE
120 mg 1 times / day steady, oral
Recommended
Dose: 120 mg, 1 times / day
Route: oral
Route: steady
Dose: 120 mg, 1 times / day
Sources:
unhealthy
Pneumonia 2%
Disc. AE
120 mg 1 times / day steady, oral
Recommended
Dose: 120 mg, 1 times / day
Route: oral
Route: steady
Dose: 120 mg, 1 times / day
Sources:
unhealthy
Sepsis 2%
Disc. AE
120 mg 1 times / day steady, oral
Recommended
Dose: 120 mg, 1 times / day
Route: oral
Route: steady
Dose: 120 mg, 1 times / day
Sources:
unhealthy
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG


OverviewOther

Other InhibitorOther SubstrateOther Inducer








Drug as perpetrator​Drug as victimTox targets

Tox targets

PubMed

PubMed

TitleDatePubMed
Preliminary data on ASP2215: tolerability and efficacy in acute myeloid leukemia patients.
2015 Sep
FLT3 Inhibitors for Treating Acute Myeloid Leukemia.
2016 Oct
Inhibition of FLT3 in AML: a focus on sorafenib.
2017 Mar
Patents

Patents

Sample Use Guides

120 mg orally once-daily
Route of Administration: Oral
Gilteritinib inhibited the growth of MV4-11 cells, which harbor FLT3-ITD, with an IC50 value of 0.92 nM
Substance Class Chemical
Created
by admin
on Sat Jun 26 12:17:10 UTC 2021
Edited
by admin
on Sat Jun 26 12:17:10 UTC 2021
Record UNII
66D92MGC8M
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
GILTERITINIB
INN   USAN   WHO-DD  
USAN   INN  
Official Name English
GILTERITINIB [USAN]
Common Name English
ASP2215
Code English
GILTERITINIB [MI]
Common Name English
GILTERITINIB [INN]
Common Name English
GILTERITINIB [WHO-DD]
Common Name English
2-PYRAZINECARBOXAMIDE, 6-ETHYL-3-((3-METHOXY-4-(4-(4-METHYL-1-PIPERAZINYL)-1-PIPERIDINYL)PHENYL)AMINO)-5-((TETRAHYDRO-2H-PYRAN-4-YL)AMINO)-
Systematic Name English
ASP-2215
Code English
Classification Tree Code System Code
FDA ORPHAN DRUG 587217
Created by admin on Sat Jun 26 12:17:11 UTC 2021 , Edited by admin on Sat Jun 26 12:17:11 UTC 2021
NCI_THESAURUS C1967
Created by admin on Sat Jun 26 12:17:11 UTC 2021 , Edited by admin on Sat Jun 26 12:17:11 UTC 2021
EU-Orphan Drug EU/3/17/1961
Created by admin on Sat Jun 26 12:17:11 UTC 2021 , Edited by admin on Sat Jun 26 12:17:11 UTC 2021
NCI_THESAURUS C129825
Created by admin on Sat Jun 26 12:17:11 UTC 2021 , Edited by admin on Sat Jun 26 12:17:11 UTC 2021
Code System Code Type Description
DRUG BANK
DB12141
Created by admin on Sat Jun 26 12:17:11 UTC 2021 , Edited by admin on Sat Jun 26 12:17:11 UTC 2021
PRIMARY
CAS
1254053-43-4
Created by admin on Sat Jun 26 12:17:11 UTC 2021 , Edited by admin on Sat Jun 26 12:17:11 UTC 2021
PRIMARY
MERCK INDEX
M12137
Created by admin on Sat Jun 26 12:17:11 UTC 2021 , Edited by admin on Sat Jun 26 12:17:11 UTC 2021
PRIMARY
INN
10048
Created by admin on Sat Jun 26 12:17:11 UTC 2021 , Edited by admin on Sat Jun 26 12:17:11 UTC 2021
PRIMARY
NCI_THESAURUS
C116722
Created by admin on Sat Jun 26 12:17:11 UTC 2021 , Edited by admin on Sat Jun 26 12:17:11 UTC 2021
PRIMARY
PUBCHEM
49803313
Created by admin on Sat Jun 26 12:17:11 UTC 2021 , Edited by admin on Sat Jun 26 12:17:11 UTC 2021
PRIMARY
FDA UNII
66D92MGC8M
Created by admin on Sat Jun 26 12:17:11 UTC 2021 , Edited by admin on Sat Jun 26 12:17:11 UTC 2021
PRIMARY
DRUG CENTRAL
5306
Created by admin on Sat Jun 26 12:17:11 UTC 2021 , Edited by admin on Sat Jun 26 12:17:11 UTC 2021
PRIMARY
RXCUI
2105806
Created by admin on Sat Jun 26 12:17:11 UTC 2021 , Edited by admin on Sat Jun 26 12:17:11 UTC 2021
PRIMARY
ChEMBL
CHEMBL3301622
Created by admin on Sat Jun 26 12:17:11 UTC 2021 , Edited by admin on Sat Jun 26 12:17:11 UTC 2021
PRIMARY
LACTMED
Gilteritinib
Created by admin on Sat Jun 26 12:17:11 UTC 2021 , Edited by admin on Sat Jun 26 12:17:11 UTC 2021
PRIMARY
EVMPD
SUB177203
Created by admin on Sat Jun 26 12:17:11 UTC 2021 , Edited by admin on Sat Jun 26 12:17:11 UTC 2021
PRIMARY
Related Record Type Details
SALT/SOLVATE -> PARENT
BINDER->LIGAND
~90% Gilteritinib bound to plasma proteins, mainly albumin
BINDING
EXCRETED UNCHANGED
URINE
METABOLIC ENZYME -> INHIBITOR
Strong CYP3A inhibitor: co-administration of itraconazole, a strong CYP3A and P-gp inhibitor, increased gilteritinib systemic exposure by approximately 2.2- fold. Moderate CYP3A inhibitor: coadministration of fluconazole, a moderate CYP3A inhibitor, increased gilteritinib systemic exposure by approximately 1.4-fold.
IC50
TRANSPORTER -> INHIBITOR
WEAK
TARGET -> INHIBITOR
INHIBITOR
IC50
TRANSPORTER -> SUBSTRATE
TARGET -> INHIBITOR
TRANSPORTER -> INHIBITOR
WEAK
IC50
METABOLIC ENZYME -> INHIBITOR
WEAK
IC50
TARGET -> INHIBITOR
TRANSPORTER -> INHIBITOR
IC50
TRANSPORTER -> INHIBITOR
IC50
TARGET -> INHIBITOR
IC50
METABOLIC ENZYME -> SUBSTRATE
TRANSPORTER -> INHIBITOR
WEAK
IC50
TARGET -> INHIBITOR
INHIBITOR
IC50
TRANSPORTER -> INHIBITOR
IC50
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Blood-to-plasma ratio PHARMACOKINETIC
Tmax PHARMACOKINETIC ORAL

Biological Half-life PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC Vc/F

Vp/F