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Details

Stereochemistry ABSOLUTE
Molecular Formula C9H14F2N2O5
Molecular Weight 268.2147
Optical Activity UNSPECIFIED
Defined Stereocenters 4 / 4
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of CEDAZURIDINE

SMILES

OC[C@H]1O[C@@H](N2CC[C@@H](O)NC2=O)C(F)(F)[C@@H]1O

InChI

InChIKey=VUDZSIYXZUYWSC-DBRKOABJSA-N
InChI=1S/C9H14F2N2O5/c10-9(11)6(16)4(3-14)18-7(9)13-2-1-5(15)12-8(13)17/h4-7,14-16H,1-3H2,(H,12,17)/t4-,5-,6-,7-/m1/s1

HIDE SMILES / InChI

Molecular Formula C9H14F2N2O5
Molecular Weight 268.2147
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 4 / 4
E/Z Centers 0
Optical Activity UNSPECIFIED

Cedazuridine is a specific cytidine deaminase (CDA) inhibitor that was approved in combination with decitabine for the treatment of variable forms of myelodysplastic syndrome (MDS). It is known that decitabine is rapidly metabolized by CDA prior to reaching systemic circulation when administered orally. Thus, cedazuridine by inhibition of CDA increases systemic exposure of decitabine.

CNS Activity

Curator's Comment: Neither cedazuridine nor its metabolites cross the blood-brain barrier.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Target ID: P32320
Gene ID: 978.0
Gene Symbol: CDA
Target Organism: Homo sapiens (Human)
0.4 µM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Palliative
INQOVI

Approved Use

INQOVI is indicated for treatment of adult patients with myelodysplastic syndromes (MDS), including previously treated and untreated, de novo and secondary MDS with the following French-AmericanBritish subtypes (refractory anemia, refractory anemia with ringed sideroblasts, refractory anemia with excess blasts, and chronic myelomonocytic leukemia [CMML]) and intermediate-1, intermediate-2, and high-risk International Prognostic Scoring System groups.
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
371 ng/mL
100 mg 1 times / day steady-state, oral
dose: 100 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered: DECITABINE
CEDAZURIDINE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: UNKNOWN
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
2950 ng × h/mL
100 mg 1 times / day steady-state, oral
dose: 100 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered: DECITABINE
CEDAZURIDINE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: UNKNOWN
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
6.7 h
100 mg 1 times / day steady-state, oral
dose: 100 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered: DECITABINE
CEDAZURIDINE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: UNKNOWN
food status: FASTED
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
20%
100 mg 1 times / day steady-state, oral
dose: 100 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered: DECITABINE
CEDAZURIDINE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: UNKNOWN
food status: FASTED

Sample Use Guides

The recommended dosage of INQOVI is 1 tablet (containing 35 mg decitabine and 100 mg cedazuridine) orally once daily on Days 1 through 5 of each 28-day cycle for a minimum of 4 cycles until disease progression or unacceptable toxicity. A complete or partial response may take longer than 4 cycles.
Route of Administration: Oral
Substance Class Chemical
Created
by admin
on Wed Apr 02 00:03:12 GMT 2025
Edited
by admin
on Wed Apr 02 00:03:12 GMT 2025
Record UNII
39IS23Q1EW
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
CEDAZURIDINE
USAN   INN  
Official Name English
INQOVI COMPONENT CEDAZURIDINE
Preferred Name English
CEDAZURIDINE [USAN]
Common Name English
(4R)-2'-DEOXY-2',2'-DIFLUORO-3,4,5,6-TETRAHYDROURIDINE
Systematic Name English
URIDINE, 2'-DEOXY-2',2'-DIFLUORO-3,4,5,6-TETRAHYDRO-, (4R)-
Systematic Name English
Cedazuridine [WHO-DD]
Common Name English
CEDAZURIDINE [ORANGE BOOK]
Common Name English
E-7727
Code English
ASTX-727 COMPONENT CEDAZURIDINE
Code English
E7727
Code English
ASTX727 COMPONENT CEDAZURIDINE
Code English
cedazuridine [INN]
Common Name English
Classification Tree Code System Code
FDA ORPHAN DRUG 697019
Created by admin on Wed Apr 02 00:03:12 GMT 2025 , Edited by admin on Wed Apr 02 00:03:12 GMT 2025
Code System Code Type Description
USAN
GH-142
Created by admin on Wed Apr 02 00:03:12 GMT 2025 , Edited by admin on Wed Apr 02 00:03:12 GMT 2025
PRIMARY
PUBCHEM
25267009
Created by admin on Wed Apr 02 00:03:12 GMT 2025 , Edited by admin on Wed Apr 02 00:03:12 GMT 2025
PRIMARY
INN
10741
Created by admin on Wed Apr 02 00:03:12 GMT 2025 , Edited by admin on Wed Apr 02 00:03:12 GMT 2025
PRIMARY
CAS
1141397-80-9
Created by admin on Wed Apr 02 00:03:12 GMT 2025 , Edited by admin on Wed Apr 02 00:03:12 GMT 2025
PRIMARY
SMS_ID
100000181098
Created by admin on Wed Apr 02 00:03:12 GMT 2025 , Edited by admin on Wed Apr 02 00:03:12 GMT 2025
PRIMARY
NCI_THESAURUS
C164146
Created by admin on Wed Apr 02 00:03:12 GMT 2025 , Edited by admin on Wed Apr 02 00:03:12 GMT 2025
PRIMARY
FDA UNII
39IS23Q1EW
Created by admin on Wed Apr 02 00:03:12 GMT 2025 , Edited by admin on Wed Apr 02 00:03:12 GMT 2025
PRIMARY
RXCUI
2384449
Created by admin on Wed Apr 02 00:03:12 GMT 2025 , Edited by admin on Wed Apr 02 00:03:12 GMT 2025
PRIMARY
DAILYMED
39IS23Q1EW
Created by admin on Wed Apr 02 00:03:12 GMT 2025 , Edited by admin on Wed Apr 02 00:03:12 GMT 2025
PRIMARY
Related Record Type Details
BINDER->LIGAND
BINDING
EXCRETED UNCHANGED
After oral administration of [14C]-cedazuridine, 17.1% (range, 12.0% to 24.1%) of the administered dose was excreted in the urine as unchanged cedazuridine within 75 hours.
URINE
TARGET -> INHIBITOR
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Volume of Distribution PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC ONCE DAILY

AT STEADY-STATE

ORAL ADMINISTRATION

Tmax PHARMACOKINETIC ONCE DAILY

ORAL ADMINISTRATION

ORAL BIOAVAILABILITY PHARMACOKINETIC