Identification

Name
APD791
Accession Number
DB05227
Type
Small Molecule
Groups
Investigational
Description

APD791 is an oral anti-thrombotic drug candidate being evaluated in a Phase 1 clinical trial by Arena. APD791 is intended to lower the risk of arterial thrombosis by reducing the amplification of platelet aggregation, arterial constriction and intimal hyperplasia mediated by serotonin.

Synonyms
Not Available
Categories
UNII
Not Available
CAS number
Not Available
Weight
Not Available
Chemical Formula
Not Available
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

Pharmacology

Indication

For the treatment and prophylaxis of arterial thrombosis.

Pharmacodynamics

APD791 is intended to lower the risk of arterial thrombosis by reducing the amplification of platelet aggregation, arterial constriction and intimal hyperplasia mediated by serotonin. Preclinical testing suggests that APD791 could have a unique risk-benefit profile because its anti-thrombotic activity may be less likely to cause the increased bleeding seen with anti-thrombotic agents that are members of other classes of drugs.

Mechanism of action

APD791 targets the 5-HT2A serotonin receptor, blocking the signal of serotonin, which facilitates thrombosis.

TargetActionsOrganism
U5-hydroxytryptamine receptor 2ANot AvailableHuman
Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half life
Not Available
Clearance
Not Available
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(R)-warfarinThe risk or severity of adverse effects can be increased when APD791 is combined with (R)-warfarin.
(S)-WarfarinThe risk or severity of adverse effects can be increased when APD791 is combined with (S)-Warfarin.
2,5-Dimethoxy-4-ethylthioamphetamineThe risk or severity of adverse effects can be increased when APD791 is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
3,4-MethylenedioxyamphetamineThe risk or severity of adverse effects can be increased when 3,4-Methylenedioxyamphetamine is combined with APD791.
4-Bromo-2,5-dimethoxyamphetamineThe risk or severity of adverse effects can be increased when 4-Bromo-2,5-dimethoxyamphetamine is combined with APD791.
4-hydroxycoumarinThe risk or severity of adverse effects can be increased when APD791 is combined with 4-hydroxycoumarin.
4-MethoxyamphetamineThe risk or severity of adverse effects can be increased when 4-Methoxyamphetamine is combined with APD791.
5-methoxy-N,N-dimethyltryptamineThe risk or severity of adverse effects can be increased when APD791 is combined with 5-methoxy-N,N-dimethyltryptamine.
7-NitroindazoleThe risk or severity of adverse effects can be increased when 7-Nitroindazole is combined with APD791.
AcenocoumarolThe risk or severity of adverse effects can be increased when APD791 is combined with Acenocoumarol.
Food Interactions
Not Available

References

General References
Not Available
External Links
PubChem Substance
347910037

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedNot AvailableHealthy Volunteers2
1CompletedScreeningAcute Coronary Syndromes (ACS)1
1TerminatedScreeningAcute Coronary Syndromes (ACS)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
Not Available
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Taxonomy

Classification
Not classified

Targets

Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Virus receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodop...
Gene Name
HTR2A
Uniprot ID
P28223
Uniprot Name
5-hydroxytryptamine receptor 2A
Molecular Weight
52602.58 Da

Drug created on October 21, 2007 16:24 / Updated on November 02, 2018 06:09