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
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. |
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
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FDA ORPHAN DRUG |
697019
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admin on Sat Dec 16 14:31:29 GMT 2023 , Edited by admin on Sat Dec 16 14:31:29 GMT 2023
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C164146
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39IS23Q1EW
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39IS23Q1EW
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ACTIVE MOIETY
