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IdentificationPharmacologyInteractionsReferencesTrialsEconomicsPropertiesSpectraTaxonomyBL-1020
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).
- Structure
- 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).
Target Actions Organism UD(2) dopamine receptor Not Available Human U5-hydroxytryptamine receptor 2A Not Available Human - 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
Drug Interaction Drug group 5'-Deoxy-5'-Methylthioadenosine The serum concentration of BL-1020 can be increased when it is combined with 5'-Deoxy-5'-Methylthioadenosine. Experimental Acebutolol BL-1020 may increase the hypotensive activities of Acebutolol. Approved Alaproclate The risk or severity of adverse effects can be increased when BL-1020 is combined with Alaproclate. Experimental Alfentanil BL-1020 may increase the hypotensive activities of Alfentanil. Approved, Illicit Algeldrate Algeldrate can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy. Experimental Almagate Almagate can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy. Experimental Almasilate Almasilate can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy. Experimental Aloglutamol Aloglutamol can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy. Experimental Alphacetylmethadol BL-1020 may increase the hypotensive activities of Alphacetylmethadol. Experimental, Illicit Alphaprodine BL-1020 may increase the hypotensive activities of Alphaprodine. Illicit Alprenolol BL-1020 may increase the hypotensive activities of Alprenolol. Approved, Withdrawn Aluminium Aluminium can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy. Approved Aluminium acetoacetate Aluminium 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 glycinate Aluminium 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 hydroxide Aluminum hydroxide can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy. Approved Amodiaquine The serum concentration of BL-1020 can be increased when it is combined with Amodiaquine. Approved Amoxapine The risk or severity of adverse effects can be increased when BL-1020 is combined with Amoxapine. Approved Arotinolol BL-1020 may increase the hypotensive activities of Arotinolol. Approved Artemether The serum concentration of BL-1020 can be increased when it is combined with Artemether. Approved Artemisinin The serum concentration of BL-1020 can be increased when it is combined with Artemisinin. Investigational Artemotil The serum concentration of BL-1020 can be increased when it is combined with Artemotil. Experimental Artenimol The serum concentration of BL-1020 can be increased when it is combined with Artenimol. Approved Artesunate The serum concentration of BL-1020 can be increased when it is combined with Artesunate. Approved Atenolol BL-1020 may increase the hypotensive activities of Atenolol. Approved Atovaquone The serum concentration of BL-1020 can be increased when it is combined with Atovaquone. Approved Befunolol BL-1020 may increase the hypotensive activities of Befunolol. Experimental Betaxolol BL-1020 may increase the hypotensive activities of Betaxolol. Approved Bevantolol BL-1020 may increase the hypotensive activities of Bevantolol. Approved Bezitramide BL-1020 may increase the hypotensive activities of Bezitramide. Experimental, Illicit, Withdrawn Bismuth Subcitrate Bismuth 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 subnitrate Bismuth subnitrate can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy. Experimental Bisoprolol BL-1020 may increase the hypotensive activities of Bisoprolol. Approved Bopindolol BL-1020 may increase the hypotensive activities of Bopindolol. Approved Bucindolol BL-1020 may increase the hypotensive activities of Bucindolol. Investigational Bufuralol BL-1020 may increase the hypotensive activities of Bufuralol. Experimental, Investigational Bupranolol BL-1020 may increase the hypotensive activities of Bupranolol. Approved Buprenorphine BL-1020 may increase the hypotensive activities of Buprenorphine. Approved, Illicit, Investigational, Vet Approved Butorphanol BL-1020 may increase the hypotensive activities of Butorphanol. Approved, Illicit, Vet Approved Calcium Carbonate Calcium 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 silicate Calcium silicate can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy. Experimental Carfentanil BL-1020 may increase the hypotensive activities of Carfentanil. Illicit, Vet Approved Carteolol BL-1020 may increase the hypotensive activities of Carteolol. Approved Carvedilol BL-1020 may increase the hypotensive activities of Carvedilol. Approved, Investigational Celiprolol BL-1020 may increase the hypotensive activities of Celiprolol. Approved, Investigational Chloroquine The serum concentration of BL-1020 can be increased when it is combined with Chloroquine. Approved, Vet Approved Chlorproguanil The serum concentration of BL-1020 can be increased when it is combined with Chlorproguanil. Investigational Citalopram The risk or severity of adverse effects can be increased when BL-1020 is combined with Citalopram. Approved Clomipramine The risk or severity of adverse effects can be increased when BL-1020 is combined with Clomipramine. Approved, Vet Approved Cloranolol BL-1020 may increase the hypotensive activities of Cloranolol. Experimental Codeine BL-1020 may increase the hypotensive activities of Codeine. Approved, Illicit Cycloguanil embonate The serum concentration of BL-1020 can be increased when it is combined with Cycloguanil embonate. Experimental Dapoxetine The risk or severity of adverse effects can be increased when BL-1020 is combined with Dapoxetine. Investigational Dapsone The serum concentration of BL-1020 can be increased when it is combined with Dapsone. Approved, Investigational Dextromoramide BL-1020 may increase the hypotensive activities of Dextromoramide. Experimental, Illicit Dextropropoxyphene BL-1020 may increase the hypotensive activities of Dextropropoxyphene. Approved, Illicit, Withdrawn Dezocine BL-1020 may increase the hypotensive activities of Dezocine. Approved Dihydrocodeine BL-1020 may increase the hypotensive activities of Dihydrocodeine. Approved, Illicit Dihydroetorphine BL-1020 may increase the hypotensive activities of Dihydroetorphine. Experimental, Illicit Dihydromorphine BL-1020 may increase the hypotensive activities of Dihydromorphine. Experimental, Illicit Diphenoxylate BL-1020 may increase the hypotensive activities of Diphenoxylate. Approved, Illicit Doxycycline The serum concentration of BL-1020 can be increased when it is combined with Doxycycline. Approved, Investigational, Vet Approved DPDPE BL-1020 may increase the hypotensive activities of DPDPE. Investigational Epanolol BL-1020 may increase the hypotensive activities of Epanolol. Experimental Escitalopram The risk or severity of adverse effects can be increased when BL-1020 is combined with Escitalopram. Approved, Investigational Esmolol BL-1020 may increase the hypotensive activities of Esmolol. Approved Ethylmorphine BL-1020 may increase the hypotensive activities of Ethylmorphine. Approved, Illicit Etorphine BL-1020 may increase the hypotensive activities of Etorphine. Illicit, Vet Approved Fenfluramine The risk or severity of adverse effects can be increased when BL-1020 is combined with Fenfluramine. Illicit, Withdrawn Fentanyl BL-1020 may increase the hypotensive activities of Fentanyl. Approved, Illicit, Investigational, Vet Approved Fluoxetine The risk or severity of adverse effects can be increased when BL-1020 is combined with Fluoxetine. Approved, Vet Approved Fluvoxamine The risk or severity of adverse effects can be increased when BL-1020 is combined with Fluvoxamine. Approved, Investigational Halofantrine The serum concentration of BL-1020 can be increased when it is combined with Halofantrine. Approved Heroin BL-1020 may increase the hypotensive activities of Heroin. Approved, Illicit Hydrocodone BL-1020 may increase the hypotensive activities of Hydrocodone. Approved, Illicit Hydromorphone BL-1020 may increase the hypotensive activities of Hydromorphone. Approved, Illicit Hydrotalcite Hydrotalcite can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy. Experimental Hydroxychloroquine The serum concentration of BL-1020 can be increased when it is combined with Hydroxychloroquine. Approved Indalpine The risk or severity of adverse effects can be increased when BL-1020 is combined with Indalpine. Investigational, Withdrawn Indenolol BL-1020 may increase the hypotensive activities of Indenolol. Withdrawn Ketobemidone BL-1020 may increase the hypotensive activities of Ketobemidone. Approved Labetalol BL-1020 may increase the hypotensive activities of Labetalol. Approved Landiolol BL-1020 may increase the hypotensive activities of Landiolol. Investigational Levobunolol BL-1020 may increase the hypotensive activities of Levobunolol. Approved Levomethadyl Acetate BL-1020 may increase the hypotensive activities of Levomethadyl Acetate. Approved Levomilnacipran The risk or severity of adverse effects can be increased when BL-1020 is combined with Levomilnacipran. Approved Levorphanol BL-1020 may increase the hypotensive activities of Levorphanol. Approved Lofentanil BL-1020 may increase the hypotensive activities of Lofentanil. Illicit Lumefantrine The serum concentration of BL-1020 can be increased when it is combined with Lumefantrine. Approved Magaldrate Magaldrate can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy. Withdrawn Magnesium Hydroxide Magnesium 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 oxide Magnesium 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 peroxide Magnesium 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 silicate Magnesium silicate can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy. Experimental Magnesium Trisilicate Magnesium Trisilicate can cause a decrease in the absorption of BL-1020 resulting in a reduced serum concentration and potentially a decrease in efficacy. Approved Mefloquine The serum concentration of BL-1020 can be increased when it is combined with Mefloquine. Approved Mepindolol BL-1020 may increase the hypotensive activities of Mepindolol. Experimental Meptazinol BL-1020 may increase the hypotensive activities of Meptazinol. Experimental Methadone BL-1020 may increase the hypotensive activities of Methadone. Approved Methadyl Acetate BL-1020 may increase the hypotensive activities of Methadyl Acetate. Approved, Illicit Metipranolol BL-1020 may increase the hypotensive activities of Metipranolol. Approved Metoprolol BL-1020 may increase the hypotensive activities of Metoprolol. Approved, Investigational Milnacipran The risk or severity of adverse effects can be increased when BL-1020 is combined with Milnacipran. Approved Mizoribine The serum concentration of BL-1020 can be increased when it is combined with Mizoribine. Investigational Morphine BL-1020 may increase the hypotensive activities of Morphine. Approved, Investigational Nadolol BL-1020 may increase the hypotensive activities of Nadolol. Approved Nalbuphine BL-1020 may increase the hypotensive activities of Nalbuphine. Approved Nicomorphine BL-1020 may increase the hypotensive activities of Nicomorphine. Experimental Normethadone BL-1020 may increase the hypotensive activities of Normethadone. Approved, Illicit Olanzapine The risk or severity of adverse effects can be increased when BL-1020 is combined with Olanzapine. Approved, Investigational Opium BL-1020 may increase the hypotensive activities of Opium. Approved, Illicit Oxprenolol BL-1020 may increase the hypotensive activities of Oxprenolol. Approved Oxycodone BL-1020 may increase the hypotensive activities of Oxycodone. Approved, Illicit, Investigational Oxymorphone BL-1020 may increase the hypotensive activities of Oxymorphone. Approved, Investigational, Vet Approved Paroxetine The risk or severity of adverse effects can be increased when BL-1020 is combined with Paroxetine. Approved, Investigational Penbutolol BL-1020 may increase the hypotensive activities of Penbutolol. Approved, Investigational Pentazocine BL-1020 may increase the hypotensive activities of Pentazocine. Approved, Vet Approved Pethidine BL-1020 may increase the hypotensive activities of Pethidine. Approved Phenazocine BL-1020 may increase the hypotensive activities of Phenazocine. Experimental Phenoperidine BL-1020 may increase the hypotensive activities of Phenoperidine. Experimental Pindolol BL-1020 may increase the hypotensive activities of Pindolol. Approved Piritramide BL-1020 may increase the hypotensive activities of Piritramide. Investigational Practolol BL-1020 may increase the hypotensive activities of Practolol. Approved Primaquine The serum concentration of BL-1020 can be increased when it is combined with Primaquine. Approved Proguanil The serum concentration of BL-1020 can be increased when it is combined with Proguanil. Approved Propranolol BL-1020 may increase the hypotensive activities of Propranolol. Approved, Investigational Pyrimethamine The serum concentration of BL-1020 can be increased when it is combined with Pyrimethamine. Approved, Vet Approved Pyronaridine The serum concentration of BL-1020 can be increased when it is combined with Pyronaridine. Investigational Quinacrine The serum concentration of BL-1020 can be increased when it is combined with Quinacrine. Approved Quinidine The serum concentration of BL-1020 can be increased when it is combined with Quinidine. Approved Quinine The serum concentration of BL-1020 can be increased when it is combined with Quinine. Approved Radicicol The serum concentration of BL-1020 can be increased when it is combined with Radicicol. Experimental Remifentanil BL-1020 may increase the hypotensive activities of Remifentanil. Approved Sertraline The risk or severity of adverse effects can be increased when BL-1020 is combined with Sertraline. Approved Sinefungin The serum concentration of BL-1020 can be increased when it is combined with Sinefungin. Experimental Sotalol BL-1020 may increase the hypotensive activities of Sotalol. Approved Sufentanil BL-1020 may increase the hypotensive activities of Sufentanil. Approved, Investigational Sulfadoxine The serum concentration of BL-1020 can be increased when it is combined with Sulfadoxine. Approved Sulfametopyrazine The serum concentration of BL-1020 can be increased when it is combined with Sulfametopyrazine. Approved, Withdrawn tafenoquine The serum concentration of BL-1020 can be increased when it is combined with tafenoquine. Investigational Talinolol BL-1020 may increase the hypotensive activities of Talinolol. Investigational Tapentadol BL-1020 may increase the hypotensive activities of Tapentadol. Approved Tertatolol BL-1020 may increase the hypotensive activities of Tertatolol. Experimental Thiopental The risk or severity of adverse effects can be increased when BL-1020 is combined with Thiopental. Approved, Vet Approved Tilidine BL-1020 may increase the hypotensive activities of Tilidine. Experimental Timolol BL-1020 may increase the hypotensive activities of Timolol. Approved Tramadol BL-1020 may increase the hypotensive activities of Tramadol. Approved, Investigational Trazodone The risk or severity of adverse effects can be increased when BL-1020 is combined with Trazodone. Approved, Investigational Trimethoprim The serum concentration of BL-1020 can be increased when it is combined with Trimethoprim. Approved, Vet Approved Vilazodone The risk or severity of adverse effects can be increased when BL-1020 is combined with Vilazodone. Approved Vortioxetine The risk or severity of adverse effects can be increased when BL-1020 is combined with Vortioxetine. Approved Zimelidine The risk or severity of adverse effects can be increased when BL-1020 is combined with Zimelidine. Withdrawn - Food Interactions
- Not Available
References
- Synthesis Reference
- Not Available
- General References
- Not Available
- External Links
- Not Available
- ATC Codes
- Not Available
- AHFS Codes
- Not Available
- PDB Entries
- Not Available
- FDA label
- Not Available
- MSDS
- Not Available
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 2 Completed Treatment Schizoaffective Disorders / Schizophrenic Disorders 1 2 Completed Treatment Schizophrenic Disorders 1 2, 3 Terminated Treatment Cognitive Effect on Schizophrenic Patients / Schizophrenic Disorders 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
- 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 August 17, 2016 12:24