Identification

Name
BL-1020
Accession Number
DB05687
Type
Small Molecule
Groups
Investigational
Description

BL-1020 is a first in class novel compound for the treatment of schizophrenia. It is being developed by BioLineRx (BioLine).

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

Investigated for use/treatment in schizophrenia and schizoaffective disorders.

Structured Indications
Not Available
Pharmacodynamics

Extensive preclinical testing of BL-1020 has shown it to have a positive safety and pharmacokinetic profile. BL-1020 reduces dopamine activity while avoiding the side affects associated with unmitigated dopamine blockade. In animal models of schizophrenia, BL-1020 reduces behaviors characteristic of psychosis and causes minimal or no impairment of movement, the most severe side effect of classic antipsychotic drugs. Biochemical testing confirms that BL-1020 works via the mechanism previously established for classic antipsychotics. BL-1020 is structurally and mechanistically distinct from the atypical antipsychotics and is not anticipated to trigger diabetes or elevated cholesterol. Preliminary studies do not reveal toxicity.

Mechanism of action

In radioligand binding studies, BL-1020 displayed strong interaction with dopamine receptors especially D2L and D2S (Ki of 0.27 nM and 0.17 nM respectively), the serotonin receptor 5-HY2a (Ki 0.25 nM) as well as moderate interaction with the GABAA receptor (Ki 3.29 microK).

TargetActionsOrganism
UD(2) dopamine receptorNot AvailableHuman
U5-hydroxytryptamine receptor 2ANot AvailableHuman
Absorption

Orally available.

Volume of distribution
Not Available
Protein binding
Not Available
Metabolism

BL-1020, after oral administration, crosses the blood brain barrier intact and is metabolized to GABA and perphenazine.

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
5'-Deoxy-5'-MethylthioadenosineThe serum concentration of BL-1020 can be increased when it is combined with 5'-Deoxy-5'-Methylthioadenosine.Experimental
AcebutololBL-1020 may increase the hypotensive activities of Acebutolol.Approved
AlaproclateThe risk or severity of adverse effects can be increased when BL-1020 is combined with Alaproclate.Experimental
AlfentanilBL-1020 may increase the hypotensive activities of Alfentanil.Approved, Illicit
AlmasilateAlmasilate can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved, Experimental
AloglutamolAloglutamol can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
AlphacetylmethadolBL-1020 may increase the hypotensive activities of Alphacetylmethadol.Experimental, Illicit
AlphaprodineBL-1020 may increase the hypotensive activities of Alphaprodine.Illicit
AlprenololBL-1020 may increase the hypotensive activities of Alprenolol.Approved, Withdrawn
AluminiumAluminium can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Aluminium acetoacetateAluminium acetoacetate can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
Aluminium glycinateAluminium glycinate can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
Aluminum hydroxideAluminum hydroxide can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
AmodiaquineThe serum concentration of BL-1020 can be increased when it is combined with Amodiaquine.Approved, Investigational
AmoxapineThe risk or severity of adverse effects can be increased when BL-1020 is combined with Amoxapine.Approved
ArotinololBL-1020 may increase the hypotensive activities of Arotinolol.Approved, Investigational
ArtemetherThe serum concentration of BL-1020 can be increased when it is combined with Artemether.Approved
ArtemisininThe serum concentration of BL-1020 can be increased when it is combined with Artemisinin.Investigational
ArtemotilThe serum concentration of BL-1020 can be increased when it is combined with Artemotil.Experimental
ArtenimolThe serum concentration of BL-1020 can be increased when it is combined with Artenimol.Approved, Investigational
ArtesunateThe serum concentration of BL-1020 can be increased when it is combined with Artesunate.Approved, Investigational
AtenololBL-1020 may increase the hypotensive activities of Atenolol.Approved
AtovaquoneThe serum concentration of BL-1020 can be increased when it is combined with Atovaquone.Approved
BefunololBL-1020 may increase the hypotensive activities of Befunolol.Experimental
BetaxololBL-1020 may increase the hypotensive activities of Betaxolol.Approved
BevantololBL-1020 may increase the hypotensive activities of Bevantolol.Approved
BezitramideBL-1020 may increase the hypotensive activities of Bezitramide.Experimental, Illicit, Withdrawn
Bismuth SubcitrateBismuth Subcitrate can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Bismuth subnitrateBismuth subnitrate can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
BisoprololBL-1020 may increase the hypotensive activities of Bisoprolol.Approved
BopindololBL-1020 may increase the hypotensive activities of Bopindolol.Approved
BucindololBL-1020 may increase the hypotensive activities of Bucindolol.Investigational
BufuralolBL-1020 may increase the hypotensive activities of Bufuralol.Experimental, Investigational
BupranololBL-1020 may increase the hypotensive activities of Bupranolol.Approved
BuprenorphineBL-1020 may increase the hypotensive activities of Buprenorphine.Approved, Illicit, Investigational, Vet Approved
ButorphanolBL-1020 may increase the hypotensive activities of Butorphanol.Approved, Illicit, Vet Approved
Calcium CarbonateCalcium Carbonate can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Calcium silicateCalcium silicate can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
CarfentanilBL-1020 may increase the hypotensive activities of Carfentanil.Illicit, Investigational, Vet Approved
CarteololBL-1020 may increase the hypotensive activities of Carteolol.Approved
CarvedilolBL-1020 may increase the hypotensive activities of Carvedilol.Approved, Investigational
CeliprololBL-1020 may increase the hypotensive activities of Celiprolol.Approved, Investigational
ChloroquineThe serum concentration of BL-1020 can be increased when it is combined with Chloroquine.Approved, Vet Approved
ChlorproguanilThe serum concentration of BL-1020 can be increased when it is combined with Chlorproguanil.Investigational
CitalopramThe risk or severity of adverse effects can be increased when BL-1020 is combined with Citalopram.Approved
ClomipramineThe risk or severity of adverse effects can be increased when BL-1020 is combined with Clomipramine.Approved, Vet Approved
CloranololBL-1020 may increase the hypotensive activities of Cloranolol.Experimental
CodeineBL-1020 may increase the hypotensive activities of Codeine.Approved, Illicit
Cycloguanil embonateThe serum concentration of BL-1020 can be increased when it is combined with Cycloguanil embonate.Experimental
DapoxetineThe risk or severity of adverse effects can be increased when BL-1020 is combined with Dapoxetine.Investigational
DapsoneThe serum concentration of BL-1020 can be increased when it is combined with Dapsone.Approved, Investigational
DextromoramideBL-1020 may increase the hypotensive activities of Dextromoramide.Experimental, Illicit
DextropropoxypheneBL-1020 may increase the hypotensive activities of Dextropropoxyphene.Approved, Illicit, Investigational, Withdrawn
DezocineBL-1020 may increase the hypotensive activities of Dezocine.Approved, Investigational
DihydrocodeineBL-1020 may increase the hypotensive activities of Dihydrocodeine.Approved, Illicit
DihydroetorphineBL-1020 may increase the hypotensive activities of Dihydroetorphine.Experimental, Illicit
DihydromorphineBL-1020 may increase the hypotensive activities of Dihydromorphine.Experimental, Illicit
DiphenoxylateBL-1020 may increase the hypotensive activities of Diphenoxylate.Approved, Illicit
DoxycyclineThe serum concentration of BL-1020 can be increased when it is combined with Doxycycline.Approved, Investigational, Vet Approved
DPDPEBL-1020 may increase the hypotensive activities of DPDPE.Experimental
EpanololBL-1020 may increase the hypotensive activities of Epanolol.Experimental
EscitalopramThe risk or severity of adverse effects can be increased when BL-1020 is combined with Escitalopram.Approved, Investigational
EsmololBL-1020 may increase the hypotensive activities of Esmolol.Approved
EthylmorphineBL-1020 may increase the hypotensive activities of Ethylmorphine.Approved, Illicit
EtorphineBL-1020 may increase the hypotensive activities of Etorphine.Illicit, Vet Approved
FenfluramineThe risk or severity of adverse effects can be increased when BL-1020 is combined with Fenfluramine.Illicit, Investigational, Withdrawn
FentanylBL-1020 may increase the hypotensive activities of Fentanyl.Approved, Illicit, Investigational, Vet Approved
FluoxetineThe risk or severity of adverse effects can be increased when BL-1020 is combined with Fluoxetine.Approved, Vet Approved
FluvoxamineThe risk or severity of adverse effects can be increased when BL-1020 is combined with Fluvoxamine.Approved, Investigational
HalofantrineThe serum concentration of BL-1020 can be increased when it is combined with Halofantrine.Approved
HeroinBL-1020 may increase the hypotensive activities of Heroin.Approved, Illicit, Investigational
HydrocodoneBL-1020 may increase the hypotensive activities of Hydrocodone.Approved, Illicit
HydromorphoneBL-1020 may increase the hypotensive activities of Hydromorphone.Approved, Illicit
HydrotalciteHydrotalcite can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental, Investigational
HydroxychloroquineThe serum concentration of BL-1020 can be increased when it is combined with Hydroxychloroquine.Approved
IndalpineThe risk or severity of adverse effects can be increased when BL-1020 is combined with Indalpine.Investigational, Withdrawn
IndenololBL-1020 may increase the hypotensive activities of Indenolol.Withdrawn
KetobemidoneBL-1020 may increase the hypotensive activities of Ketobemidone.Approved, Investigational
LabetalolBL-1020 may increase the hypotensive activities of Labetalol.Approved
LandiololBL-1020 may increase the hypotensive activities of Landiolol.Investigational
LevobunololBL-1020 may increase the hypotensive activities of Levobunolol.Approved
Levomethadyl AcetateBL-1020 may increase the hypotensive activities of Levomethadyl Acetate.Approved, Investigational
LevomilnacipranThe risk or severity of adverse effects can be increased when BL-1020 is combined with Levomilnacipran.Approved
LevorphanolBL-1020 may increase the hypotensive activities of Levorphanol.Approved
LofentanilBL-1020 may increase the hypotensive activities of Lofentanil.Illicit
LumefantrineThe serum concentration of BL-1020 can be increased when it is combined with Lumefantrine.Approved
MagaldrateMagaldrate can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved, Withdrawn
Magnesium HydroxideMagnesium Hydroxide can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Magnesium oxideMagnesium oxide can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Magnesium peroxideMagnesium peroxide can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
Magnesium silicateMagnesium silicate can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved, Experimental
Magnesium TrisilicateMagnesium Trisilicate can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
MefloquineThe serum concentration of BL-1020 can be increased when it is combined with Mefloquine.Approved
MepindololBL-1020 may increase the hypotensive activities of Mepindolol.Experimental
MeptazinolBL-1020 may increase the hypotensive activities of Meptazinol.Experimental
MethadoneBL-1020 may increase the hypotensive activities of Methadone.Approved
Methadyl AcetateBL-1020 may increase the hypotensive activities of Methadyl Acetate.Approved, Illicit
MetipranololBL-1020 may increase the hypotensive activities of Metipranolol.Approved
MetoprololBL-1020 may increase the hypotensive activities of Metoprolol.Approved, Investigational
MilnacipranThe risk or severity of adverse effects can be increased when BL-1020 is combined with Milnacipran.Approved
MizoribineThe serum concentration of BL-1020 can be increased when it is combined with Mizoribine.Investigational
MorphineBL-1020 may increase the hypotensive activities of Morphine.Approved, Investigational
NadololBL-1020 may increase the hypotensive activities of Nadolol.Approved
NalbuphineBL-1020 may increase the hypotensive activities of Nalbuphine.Approved
NebivololBL-1020 may increase the hypotensive activities of Nebivolol.Approved, Investigational
NefazodoneThe risk or severity of adverse effects can be increased when BL-1020 is combined with Nefazodone.Approved, Withdrawn
NicomorphineBL-1020 may increase the hypotensive activities of Nicomorphine.Experimental
NormethadoneBL-1020 may increase the hypotensive activities of Normethadone.Approved, Illicit
OlanzapineThe risk or severity of adverse effects can be increased when BL-1020 is combined with Olanzapine.Approved, Investigational
OpiumBL-1020 may increase the hypotensive activities of Opium.Approved, Illicit
OxprenololBL-1020 may increase the hypotensive activities of Oxprenolol.Approved
OxycodoneBL-1020 may increase the hypotensive activities of Oxycodone.Approved, Illicit, Investigational
OxymorphoneBL-1020 may increase the hypotensive activities of Oxymorphone.Approved, Investigational, Vet Approved
ParoxetineThe risk or severity of adverse effects can be increased when BL-1020 is combined with Paroxetine.Approved, Investigational
PenbutololBL-1020 may increase the hypotensive activities of Penbutolol.Approved, Investigational
PentazocineBL-1020 may increase the hypotensive activities of Pentazocine.Approved, Vet Approved
PethidineBL-1020 may increase the hypotensive activities of Pethidine.Approved
PhenazocineBL-1020 may increase the hypotensive activities of Phenazocine.Experimental
PhenoperidineBL-1020 may increase the hypotensive activities of Phenoperidine.Experimental
PindololBL-1020 may increase the hypotensive activities of Pindolol.Approved
PiritramideBL-1020 may increase the hypotensive activities of Piritramide.Investigational
Platelet Activating FactorBL-1020 may increase the hypotensive activities of Platelet Activating Factor.Experimental
PractololBL-1020 may increase the hypotensive activities of Practolol.Approved
PrimaquineThe serum concentration of BL-1020 can be increased when it is combined with Primaquine.Approved
ProguanilThe serum concentration of BL-1020 can be increased when it is combined with Proguanil.Approved
PropranololBL-1020 may increase the hypotensive activities of Propranolol.Approved, Investigational
PyrimethamineThe serum concentration of BL-1020 can be increased when it is combined with Pyrimethamine.Approved, Vet Approved
PyronaridineThe serum concentration of BL-1020 can be increased when it is combined with Pyronaridine.Investigational
QuinacrineThe serum concentration of BL-1020 can be increased when it is combined with Quinacrine.Approved, Investigational
QuinidineThe serum concentration of BL-1020 can be increased when it is combined with Quinidine.Approved
QuinineThe serum concentration of BL-1020 can be increased when it is combined with Quinine.Approved
RadicicolThe serum concentration of BL-1020 can be increased when it is combined with Radicicol.Experimental
RemifentanilBL-1020 may increase the hypotensive activities of Remifentanil.Approved
SertralineThe risk or severity of adverse effects can be increased when BL-1020 is combined with Sertraline.Approved
SinefunginThe serum concentration of BL-1020 can be increased when it is combined with Sinefungin.Experimental
Sodium bicarbonateSodium bicarbonate can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
SotalolBL-1020 may increase the hypotensive activities of Sotalol.Approved
SufentanilBL-1020 may increase the hypotensive activities of Sufentanil.Approved, Investigational
SulfadoxineThe serum concentration of BL-1020 can be increased when it is combined with Sulfadoxine.Approved, Investigational
SulfametopyrazineThe serum concentration of BL-1020 can be increased when it is combined with Sulfametopyrazine.Approved, Withdrawn
tafenoquineThe serum concentration of BL-1020 can be increased when it is combined with tafenoquine.Investigational
TalinololBL-1020 may increase the hypotensive activities of Talinolol.Investigational
TapentadolBL-1020 may increase the hypotensive activities of Tapentadol.Approved
TertatololBL-1020 may increase the hypotensive activities of Tertatolol.Experimental
ThiopentalThe risk or severity of adverse effects can be increased when BL-1020 is combined with Thiopental.Approved, Vet Approved
TilidineBL-1020 may increase the hypotensive activities of Tilidine.Experimental
TimololBL-1020 may increase the hypotensive activities of Timolol.Approved
TramadolBL-1020 may increase the hypotensive activities of Tramadol.Approved, Investigational
TrazodoneThe risk or severity of adverse effects can be increased when BL-1020 is combined with Trazodone.Approved, Investigational
TrimethoprimThe serum concentration of BL-1020 can be increased when it is combined with Trimethoprim.Approved, Vet Approved
TromethamineTromethamine can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
VilazodoneThe risk or severity of adverse effects can be increased when BL-1020 is combined with Vilazodone.Approved
VortioxetineThe risk or severity of adverse effects can be increased when BL-1020 is combined with Vortioxetine.Approved
ZimelidineThe risk or severity of adverse effects can be increased when BL-1020 is combined with Zimelidine.Withdrawn
Food Interactions
Not Available

References

General References
Not Available
External Links
PubChem Substance
347910192

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2CompletedTreatmentSchizoaffective Disorders / Schizophrenic Disorders1
2CompletedTreatmentSchizophrenic Disorders1
2, 3TerminatedTreatmentCognitive Effect on Schizophrenic Patients / Schizophrenic Disorders1

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
Potassium channel regulator activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
Gene Name
DRD2
Uniprot ID
P14416
Uniprot Name
D(2) dopamine receptor
Molecular Weight
50618.91 Da
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 November 18, 2007 11:27 / Updated on November 06, 2017 06:45