Rx00019 - Amifostine


Interactive 3D Model

Interactive Drug Target Network

Interactive Bipartite Drug Repurposing Graph

Rx00019
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
ovarian cancer advanced ovarian carcinoma 5625 5625 5625 717.32 0 0.0
moderate xerostomia severe xerostomia 1629 1629 1629 2476.933 0 0.0
head and neck cancer neck cancer 3498 3498 3498 1153.495 0 0.0
severe xerostomia moderate xerostomia 1629 1629 1629 2476.933 0 0.0

Chemical, Pharmacological and Biological Annotations


ATC Code:
V03AF05
Brand:
Ethyol
Category:
Radiation-Protective Agents
ChEBI ID:
2636
PubChem ID:
2141
SMILE:
NCCCNCCSP(O)(O)=O
InChI:
1S/C5H15N2O3PS/c6-2-1-3-7-4-5-12-11(8,9)10/h7H,1-6H2,(H2,8,9,10)
Classification:
Kingdom:
Organic Compounds
Superclass:
Organonitrogen Compounds
Class:
Amines
Subclass:
Polyamines
Indication:
For reduction in the cumulative renal toxicity in patients with ovarian cancer (using cisplatin) and moderate to severe xerostomia in patients undergoing post-operative radiation treatment for head and neck cancer.
Pharmacodynamics:
Amifostine is an organic thiophosphate cytoprotective agent indicated to reduce the cumulative renal toxicity associated with repeated administration of cisplatin in patients with advanced ovarian cancer or non-small cell lung cancer and al...
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Description:
A phosphorothioate proposed as a radiation-protective agent. It causes splenic vasodilation and may block autonomic ganglia. [PubChem]
Mechanism:
The thiol metabolite is responsible for most of the cytoprotective and radioprotective properties of amifostine. It is readily taken up by cells where it binds to and detoxifies reactive metabolites of platinum and alkylating agents as well...
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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:
Non AMES toxic
Carcinogenicity:
Non-carcinogens
Biodegradation:
Ready biodegradable
Rat acute toxicity:
2.3829 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