BL-1020
Identification
- Generic Name
- BL-1020
- DrugBank Accession Number
- DB05687
- Background
BL-1020 is a first in class novel compound for the treatment of schizophrenia. It is being developed by BioLineRx (BioLine).
- Type
- Small Molecule
- Groups
- Investigational
- Synonyms
- Not Available
Pharmacology
- Indication
Investigated for use/treatment in schizophrenia and schizoaffective disorders.
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- 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 UDopamine D2 receptor Not Available Humans U5-hydroxytryptamine receptor 2A Not Available Humans - 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
- Adverse Effects
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- Toxicity
Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your software1,2-Benzodiazepine The risk or severity of CNS depression can be increased when BL-1020 is combined with 1,2-Benzodiazepine. Acebutolol The serum concentration of Acebutolol can be increased when it is combined with BL-1020. Acetazolamide The risk or severity of CNS depression can be increased when Acetazolamide is combined with BL-1020. Acetohexamide The therapeutic efficacy of Acetohexamide can be decreased when used in combination with BL-1020. Acetophenazine The risk or severity of CNS depression can be increased when Acetophenazine is combined with BL-1020. - Food Interactions
- Not Available
Categories
- Drug Categories
- Classification
- Not classified
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- K1WO7H97QZ
- CAS number
- Not Available
- InChI Key
- Not Available
- InChI
- Not Available
- IUPAC Name
- Not Available
- SMILES
- Not Available
References
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 2 Completed Treatment Schizoaffective Disorders / Schizophrenia 1 2 Completed Treatment Schizophrenia 1 2, 3 Terminated Treatment Cognitive Effect on Schizophrenic Patients / Schizophrenia 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
- Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- 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
- Humans
- 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 at November 18, 2007 18:27 / Updated at June 12, 2020 16:52