CEDAZURIDINE

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 Search

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

Description
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212576s000lbl.pdf| https://www.cancer.gov/publications/dictionaries/cancer-drug/def/cedazuridine

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

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Cytidine deaminase 5 Target ID: P32320 Gene ID: 978.0 Gene Symbol: CDA Target Organism: Homo sapiens (Human) Sources: https://pubmed.ncbi.nlm.nih.gov/24520856\|https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212576s000lbl.pdf	Inhibitor 8297		0.4 µM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
myelodysplastic syndromes 1 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212576s000lbl.pdf	Palliative		Approved 8429	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.

Sample Use Guides

In Vivo Use Guide

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 `Sat Dec 16 14:31:29 UTC 2023` Edited by `admin` on `Sat Dec 16 14:31:29 UTC 2023`
Record UNII	39IS23Q1EW
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

CEDAZURIDINE

Official 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

CEDAZURIDINE COMPONENT OF INQOVI

Brand Name

English

E-7727

Code

English

INQOVI COMPONENT CEDAZURIDINE

Brand Name

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