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
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
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
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212576Orig1s000MultidisciplineR.pdf
Curator's Comment: Neither cedazuridine nor its metabolites cross the blood-brain barrier.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: P32320 Gene ID: 978.0 Gene Symbol: CDA Target Organism: Homo sapiens (Human) |
0.4 µM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Palliative | INQOVI Approved UseINQOVI 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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Edited
Wed Apr 02 00:03:12 GMT 2025
by
admin
on
Wed Apr 02 00:03:12 GMT 2025
|
Record UNII |
39IS23Q1EW
|
Record Status |
Validated (UNII)
|
Record Version |
|
-
Download
Name | Type | Language | ||
---|---|---|---|---|
|
Official Name | English | ||
|
Preferred Name | English | ||
|
Common Name | English | ||
|
Systematic Name | English | ||
|
Systematic Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Code | English | ||
|
Code | English | ||
|
Code | English | ||
|
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 | ||
---|---|---|---|---|---|
|
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 | |||
|
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 | |||
|
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 | |||
|
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 | |||
|
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 | |||
|
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 | |||
|
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 | |||
|
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 | |||
|
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 |
|
||
Tmax | PHARMACOKINETIC |
|
ONCE DAILY |
|
||
ORAL BIOAVAILABILITY | PHARMACOKINETIC |
|
|
|||