Rx00034 - Azacitidine


Interactive 3D Model

Interactive Drug Target Network

Interactive Bipartite Drug Repurposing Graph

Rx00034
Primary Indication
Secondary Indication

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Disease prevalence from Electronic Health Records

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Disease A Disease B A∩B A∩¬B B∩¬A Odds-Ratio P-Value Adjusted P-Value
refractory anemia with excess blasts, refractory anemia with excess blasts in transformation myelodysplastic syndrome 169 254 1504 1785.009 0 0.0
French-American-British myelodysplastic syndrome myelodysplastic syndrome 225 941 1504 641.476 0 0.0
refractory anemia with ringed sideroblasts myelodysplastic syndrome 214 323 1504 1777.456 0 0.0
refractory anemia myelodysplastic syndrome 866 68895 1504 33.722 0 0.0
acute myelogenous leukemia with multilineage dysplasia acute myeloid leukemia 941 941 941 4287.911 0 0.0
chronic myelomonocytic leukemia myelodysplastic syndrome 48 433 1504 297.4 1.91E-98 6.12e-95

Chemical, Pharmacological and Biological Annotations


ATC Code:
No ATC code annotated in DrugBank
Brands:
Ladakamycin; Mylosar
Categories:
Enzyme Inhibitors; Antimetabolites, Antineoplastic
ChEBI ID:
2038
PubChem ID:
9444
KEGG Drug ID:
D03021
SMILE:
NC1=NC(=O)N(C=N1)[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O
InChI:
1S/C8H12N4O5/c9-7-10-2-12(8(16)11-7)6-5(15)4(14)3(1-13)17-6/h2-6,13-15H,1H2,(H2,9,11,16)/t3-,4-,5-,6-/m1/s1
Classification:
Kingdom:
Organic Compounds
Superclass:
Organooxygen Compounds
Class:
Carbohydrates and Carbohydrate Conjugates
Subclass:
Glycosyl Compounds
Indication:
For treatment of patients with the following French-American-British myelodysplastic syndrome subtypes: refractory anemia or refractory anemia with ringed sideroblasts (if accompanied by neutropenia or thrombocytopenia or requiring transfus...
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Pharmacodynamics:
Azacitidine is believed to exert its antineoplastic effects by causing hypomethylation of DNA and direct cytotoxicity on abnormal hematopoietic cells in the bone marrow. The concentration of azacitidine required for maximum inhibition of DN...
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Description:
A pyrimidine nucleoside analogue that inhibits DNA methyltransferase, impairing DNA methylation. It is also an antimetabolite of cytidine, incorporated primarily into RNA. Azacytidine has been used as an antineoplastic agent. [PubChem]
Mechanism:
Azacitidine (5-azacytidine) is a chemical analogue of the cytosine nucleoside used in DNA and RNA. Azacitidine is thought to induce antineoplastic activity via two mechanisms; inhibition of DNA methyltransferase at low doses, causing hypome...
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Adsorption, Distribution, Metabolism, Excretion and Toxicity


Human Intestinal Absorption:
+
Blood Brain Barrier:
+
Caco-2 permeable:
-
P-glycoprotein substrate:
Non-substrate
P-glycoprotein inhibitor I:
Non-inhibitor
P-glycoprotein inhibitor II:
Non-inhibitor
Renal organic cation transporter:
Non-inhibitor
CYP450 2C9 substrate:
Non-inhibitor
CYP450 2D6 substrate:
Non-inhibitor
CYP450 2C19 substrate:
Non-inhibitor
CYP450 inhibitory promiscuity:
Low CYP Inhibitory Promiscuity
Ames test:
AMES toxic
Carcinogenicity:
Non-carcinogens
Biodegradation:
Not ready biodegradable
Rat acute toxicity:
1.7991 LD50, mol/kg
hERG inhibition (predictor I):
Weak inhibitor
hERG inhibition (predictor II):
Non-inhibitor

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Dudley Laboratory
Department of Genetics and Genomic Sciences
Icahn Institute for Genomics and Multiscale Biology
Icahn School of Medicine at Mount Sinai
One Gustave L. Levy Place, Box 1498
Manhattan, New York City, NY
repurposedb@dudleylab.org