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
DrugInteractionDrug group
AmikacinThe risk or severity of adverse effects can be increased when Amikacin is combined with APD791.Approved, Investigational, Vet Approved
BenzphetamineThe risk or severity of adverse effects can be increased when Benzphetamine is combined with APD791.Approved, Illicit
Benzyl alcoholThe risk or severity of adverse effects can be increased when Benzyl alcohol is combined with APD791.Approved
BupropionThe risk or severity of adverse effects can be increased when Bupropion is combined with APD791.Approved
CetirizineThe risk or severity of adverse effects can be increased when Cetirizine is combined with APD791.Approved
ClemastineThe risk or severity of adverse effects can be increased when Clemastine is combined with APD791.Approved, Investigational
ClindamycinThe risk or severity of adverse effects can be increased when Clindamycin is combined with APD791.Approved, Vet Approved
CodeineThe risk or severity of adverse effects can be increased when Codeine is combined with APD791.Approved, Illicit
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with APD791.Approved
DexbrompheniramineThe risk or severity of adverse effects can be increased when Dexbrompheniramine is combined with APD791.Approved
DimenhydrinateThe risk or severity of adverse effects can be increased when Dimenhydrinate is combined with APD791.Approved
DotarizineThe risk or severity of adverse effects can be increased when APD791 is combined with Dotarizine.Investigational
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of APD791.Approved, Vet Approved
EperisoneThe risk or severity of adverse effects can be increased when Eperisone is combined with APD791.Approved, Investigational
EthanolAPD791 may increase the central nervous system depressant (CNS depressant) activities of Ethanol.Approved
EthosuximideThe risk or severity of adverse effects can be increased when Ethosuximide is combined with APD791.Approved
EtomidateThe risk or severity of adverse effects can be increased when Etomidate is combined with APD791.Approved
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with APD791.Approved, Illicit, Investigational, Vet Approved
FlunarizineThe risk or severity of adverse effects can be increased when Flunarizine is combined with APD791.Approved
FluspirileneThe risk or severity of adverse effects can be increased when Fluspirilene is combined with APD791.Approved, Investigational
Fluticasone propionateThe risk or severity of adverse effects can be increased when Fluticasone propionate is combined with APD791.Approved
FluvoxamineThe risk or severity of adverse effects can be increased when APD791 is combined with Fluvoxamine.Approved, Investigational
GabapentinThe risk or severity of adverse effects can be increased when Gabapentin is combined with APD791.Approved, Investigational
GuanfacineThe risk or severity of adverse effects can be increased when Guanfacine is combined with APD791.Approved, Investigational
HydrocodoneAPD791 may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.Approved, Illicit
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of APD791.Approved
LamotrigineThe risk or severity of adverse effects can be increased when Lamotrigine is combined with APD791.Approved, Investigational
LevetiracetamThe risk or severity of adverse effects can be increased when Levetiracetam is combined with APD791.Approved, Investigational
LoratadineThe risk or severity of adverse effects can be increased when Loratadine is combined with APD791.Approved, Investigational
Magnesium carbonateThe risk or severity of adverse effects can be increased when Magnesium carbonate is combined with APD791.Approved, Investigational
Magnesium citrateThe risk or severity of adverse effects can be increased when Magnesium citrate is combined with APD791.Approved
Magnesium sulfateThe therapeutic efficacy of APD791 can be increased when used in combination with Magnesium sulfate.Approved, Investigational, Vet Approved
Magnesium TrisilicateThe risk or severity of adverse effects can be increased when Magnesium Trisilicate is combined with APD791.Approved
MeclizineThe risk or severity of adverse effects can be increased when Meclizine is combined with APD791.Approved
MethsuximideThe risk or severity of adverse effects can be increased when Methsuximide is combined with APD791.Approved
OndansetronThe risk or severity of adverse effects can be increased when Ondansetron is combined with APD791.Approved
OxycodoneThe risk or severity of adverse effects can be increased when Oxycodone is combined with APD791.Approved, Illicit, Investigational
OxymorphoneThe risk or severity of adverse effects can be increased when Oxymorphone is combined with APD791.Approved, Investigational, Vet Approved
ParomomycinThe risk or severity of adverse effects can be increased when Paromomycin is combined with APD791.Approved, Investigational
ParoxetineThe risk or severity of adverse effects can be increased when APD791 is combined with Paroxetine.Approved, Investigational
PenfluridolThe risk or severity of adverse effects can be increased when Penfluridol is combined with APD791.Experimental
PhenobarbitalThe risk or severity of adverse effects can be increased when Phenobarbital is combined with APD791.Approved, Investigational
PramipexoleAPD791 may increase the sedative activities of Pramipexole.Approved, Investigational
PregabalinThe therapeutic efficacy of APD791 can be increased when used in combination with Pregabalin.Approved, Illicit, Investigational
ProchlorperazineThe risk or severity of adverse effects can be increased when Prochlorperazine is combined with APD791.Approved, Vet Approved
PromethazineThe risk or severity of adverse effects can be increased when Promethazine is combined with APD791.Approved, Investigational
PseudoephedrineThe risk or severity of adverse effects can be increased when APD791 is combined with Pseudoephedrine.Approved
PyrantelThe risk or severity of adverse effects can be increased when Pyrantel is combined with APD791.Approved, Vet Approved
QuetiapineThe risk or severity of adverse effects can be increased when Quetiapine is combined with APD791.Approved
RizatriptanThe risk or severity of adverse effects can be increased when Rizatriptan is combined with APD791.Approved
ScopolamineThe risk or severity of adverse effects can be increased when Scopolamine is combined with APD791.Approved, Investigational
SumatriptanThe risk or severity of adverse effects can be increased when Sumatriptan is combined with APD791.Approved, Investigational
TetracyclineThe risk or severity of adverse effects can be increased when Tetracycline is combined with APD791.Approved, Vet Approved
TetrahydropalmatineThe risk or severity of adverse effects can be increased when Tetrahydropalmatine is combined with APD791.Investigational
TopiramateThe risk or severity of adverse effects can be increased when Topiramate is combined with APD791.Approved
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with APD791.Approved, Investigational
TrimethadioneThe risk or severity of adverse effects can be increased when Trimethadione is combined with APD791.Approved
VancomycinThe risk or severity of adverse effects can be increased when Vancomycin is combined with APD791.Approved
VecuroniumThe risk or severity of adverse effects can be increased when Vecuronium is combined with APD791.Approved
VinpocetineThe risk or severity of adverse effects can be increased when Vinpocetine is combined with APD791.Investigational
ZiconotideThe risk or severity of adverse effects can be increased when Ziconotide is combined with APD791.Approved
ZolmitriptanThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with APD791.Approved, Investigational
ZonisamideThe risk or severity of adverse effects can be increased when Zonisamide is combined with APD791.Approved, Investigational
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 August 02, 2018 05:29