Details
Stereochemistry | ACHIRAL |
Molecular Formula | C10H8F2N4O |
Molecular Weight | 238.1939 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
c1cc(c(Cn2cc(C(=N)O)nn2)c(c1)F)F
InChI
InChIKey=POGQSBRIGCQNEG-UHFFFAOYSA-N
InChI=1S/C10H8F2N4O/c11-7-2-1-3-8(12)6(7)4-16-5-9(10(13)17)14-15-16/h1-3,5H,4H2,(H2,13,17)
Molecular Formula | C10H8F2N4O |
Molecular Weight | 238.1939 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionCurator's Comment:: description was created based on several sources, including:
http://www.rxlist.com/banzel-drug.htm
https://www.drugs.com/mtm/rufinamide.html
Curator's Comment:: description was created based on several sources, including:
http://www.rxlist.com/banzel-drug.htm
https://www.drugs.com/mtm/rufinamide.html
Rufinamide is an anti-epileptic drug that is FDA approved for the treatment of lennox-gastaut syndrome (LGS). The principal mechanism of action of rufinamide is modulation of the activity of sodium channels and, in particular, prolongation of the inactive state of the channel. Hormonal contraceptives may be less effective with rufinamide. Patients on valproate should begin at a rufinamide dose lower than 10 mg/kg per day (pediatric patients) or 400 mg per day (adults). Common adverse reactions include headache, dizziness, fatigue, somnolence, and nausea.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL4296 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23221868 |
3.8 µM [EC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Palliative | BANZEL Approved UseI NDICATIONS AND USAGE BANZEL is indicated for adjunctive treatment of seizures associated with Lennox-Gastaut Syndrome in pediatric patients 1 year of age and older and in adults. BANZEL is indicated for adjunctive treatment of seizures associated with Lennox-Gastaut Syndrome (LGS) in pediatric patients 1 year of age and older, and in adults (1) Launch Date1.2266208E12 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
3.8 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/18503564/ |
800 mg single, oral dose: 800 mg route of administration: Oral experiment type: SINGLE co-administered: |
RUFINAMIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
70.3 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/18503564/ |
800 mg single, oral dose: 800 mg route of administration: Oral experiment type: SINGLE co-administered: |
RUFINAMIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
7.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/18503564/ |
800 mg single, oral dose: 800 mg route of administration: Oral experiment type: SINGLE co-administered: |
RUFINAMIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
10 h |
200 mg 2 times / day unknown, oral dose: 200 mg route of administration: Oral experiment type: UNKNOWN co-administered: |
RUFINAMIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
66% |
200 mg 2 times / day unknown, oral dose: 200 mg route of administration: Oral experiment type: UNKNOWN co-administered: |
RUFINAMIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
3600 mg 2 times / day multiple, oral MTD Dose: 3600 mg, 2 times / day Route: oral Route: multiple Dose: 3600 mg, 2 times / day Sources: Page: p.1125, p.1139 |
healthy n = 15 Health Status: healthy Population Size: 15 Sources: Page: p.1125, p.1139 |
|
22.5 mg/kg 2 times / day multiple, oral Studied dose Dose: 22.5 mg/kg, 2 times / day Route: oral Route: multiple Dose: 22.5 mg/kg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Lennox-Gastaut Syndrome Sources: Page: p.1 |
Other AEs: Depression worsened, Suicidal behavior... Other AEs: Depression worsened Sources: Page: p.1Suicidal behavior (serious) Leukopenia (serious) Mood change Central nervous system disorder NOS Hypersensitivity reaction |
22.5 mg/kg 2 times / day multiple, oral Studied dose Dose: 22.5 mg/kg, 2 times / day Route: oral Route: multiple Dose: 22.5 mg/kg, 2 times / day Sources: Page: p.4 |
unhealthy Health Status: unhealthy Condition: Lennox-Gastaut Syndrome Sources: Page: p.4 |
Disc. AE: Fatigue... Other AEs: QT shortened... AEs leading to discontinuation/dose reduction: Fatigue (1-2) Other AEs:QT shortened (serious) Sources: Page: p.4 |
22.5 mg/kg 2 times / day multiple, oral Studied dose Dose: 22.5 mg/kg, 2 times / day Route: oral Route: multiple Dose: 22.5 mg/kg, 2 times / day Sources: Page: p.7 |
unhealthy Health Status: unhealthy Condition: Lennox-Gastaut Syndrome Sources: Page: p.7 |
Disc. AE: Convulsion, Rash... AEs leading to discontinuation/dose reduction: Convulsion (2%) Sources: Page: p.7Rash (2%) |
22.5 mg/kg 2 times / day multiple, oral Studied dose Dose: 22.5 mg/kg, 2 times / day Route: oral Route: multiple Dose: 22.5 mg/kg, 2 times / day Sources: Page: p.8 |
unhealthy Health Status: unhealthy Condition: Lennox-Gastaut Syndrome Sources: Page: p.8 |
Disc. AE: Vomiting, Dizziness... AEs leading to discontinuation/dose reduction: Vomiting (1%) Sources: Page: p.8Dizziness (3%) Headache (2%) Nausea (1%) Ataxia (1%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Central nervous system disorder NOS | 22.5 mg/kg 2 times / day multiple, oral Studied dose Dose: 22.5 mg/kg, 2 times / day Route: oral Route: multiple Dose: 22.5 mg/kg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Lennox-Gastaut Syndrome Sources: Page: p.1 |
|
Depression worsened | 22.5 mg/kg 2 times / day multiple, oral Studied dose Dose: 22.5 mg/kg, 2 times / day Route: oral Route: multiple Dose: 22.5 mg/kg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Lennox-Gastaut Syndrome Sources: Page: p.1 |
|
Hypersensitivity reaction | 22.5 mg/kg 2 times / day multiple, oral Studied dose Dose: 22.5 mg/kg, 2 times / day Route: oral Route: multiple Dose: 22.5 mg/kg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Lennox-Gastaut Syndrome Sources: Page: p.1 |
|
Mood change | 22.5 mg/kg 2 times / day multiple, oral Studied dose Dose: 22.5 mg/kg, 2 times / day Route: oral Route: multiple Dose: 22.5 mg/kg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Lennox-Gastaut Syndrome Sources: Page: p.1 |
|
Leukopenia | serious | 22.5 mg/kg 2 times / day multiple, oral Studied dose Dose: 22.5 mg/kg, 2 times / day Route: oral Route: multiple Dose: 22.5 mg/kg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Lennox-Gastaut Syndrome Sources: Page: p.1 |
Suicidal behavior | serious | 22.5 mg/kg 2 times / day multiple, oral Studied dose Dose: 22.5 mg/kg, 2 times / day Route: oral Route: multiple Dose: 22.5 mg/kg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Lennox-Gastaut Syndrome Sources: Page: p.1 |
Fatigue | 1-2 Disc. AE |
22.5 mg/kg 2 times / day multiple, oral Studied dose Dose: 22.5 mg/kg, 2 times / day Route: oral Route: multiple Dose: 22.5 mg/kg, 2 times / day Sources: Page: p.4 |
unhealthy Health Status: unhealthy Condition: Lennox-Gastaut Syndrome Sources: Page: p.4 |
QT shortened | serious | 22.5 mg/kg 2 times / day multiple, oral Studied dose Dose: 22.5 mg/kg, 2 times / day Route: oral Route: multiple Dose: 22.5 mg/kg, 2 times / day Sources: Page: p.4 |
unhealthy Health Status: unhealthy Condition: Lennox-Gastaut Syndrome Sources: Page: p.4 |
Convulsion | 2% Disc. AE |
22.5 mg/kg 2 times / day multiple, oral Studied dose Dose: 22.5 mg/kg, 2 times / day Route: oral Route: multiple Dose: 22.5 mg/kg, 2 times / day Sources: Page: p.7 |
unhealthy Health Status: unhealthy Condition: Lennox-Gastaut Syndrome Sources: Page: p.7 |
Rash | 2% Disc. AE |
22.5 mg/kg 2 times / day multiple, oral Studied dose Dose: 22.5 mg/kg, 2 times / day Route: oral Route: multiple Dose: 22.5 mg/kg, 2 times / day Sources: Page: p.7 |
unhealthy Health Status: unhealthy Condition: Lennox-Gastaut Syndrome Sources: Page: p.7 |
Ataxia | 1% Disc. AE |
22.5 mg/kg 2 times / day multiple, oral Studied dose Dose: 22.5 mg/kg, 2 times / day Route: oral Route: multiple Dose: 22.5 mg/kg, 2 times / day Sources: Page: p.8 |
unhealthy Health Status: unhealthy Condition: Lennox-Gastaut Syndrome Sources: Page: p.8 |
Nausea | 1% Disc. AE |
22.5 mg/kg 2 times / day multiple, oral Studied dose Dose: 22.5 mg/kg, 2 times / day Route: oral Route: multiple Dose: 22.5 mg/kg, 2 times / day Sources: Page: p.8 |
unhealthy Health Status: unhealthy Condition: Lennox-Gastaut Syndrome Sources: Page: p.8 |
Vomiting | 1% Disc. AE |
22.5 mg/kg 2 times / day multiple, oral Studied dose Dose: 22.5 mg/kg, 2 times / day Route: oral Route: multiple Dose: 22.5 mg/kg, 2 times / day Sources: Page: p.8 |
unhealthy Health Status: unhealthy Condition: Lennox-Gastaut Syndrome Sources: Page: p.8 |
Headache | 2% Disc. AE |
22.5 mg/kg 2 times / day multiple, oral Studied dose Dose: 22.5 mg/kg, 2 times / day Route: oral Route: multiple Dose: 22.5 mg/kg, 2 times / day Sources: Page: p.8 |
unhealthy Health Status: unhealthy Condition: Lennox-Gastaut Syndrome Sources: Page: p.8 |
Dizziness | 3% Disc. AE |
22.5 mg/kg 2 times / day multiple, oral Studied dose Dose: 22.5 mg/kg, 2 times / day Route: oral Route: multiple Dose: 22.5 mg/kg, 2 times / day Sources: Page: p.8 |
unhealthy Health Status: unhealthy Condition: Lennox-Gastaut Syndrome Sources: Page: p.8 |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/021911Orig1s000ClinPharmR_P1.pdf Page: 21, 56 |
inconclusive | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/021911Orig1s000ClinPharmR_P1.pdf Page: 56.0 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/021911Orig1s000ClinPharmR_P1.pdf Page: 21.0 |
weak | yes (co-administration study) Comment: coadministration with triazolam resulted in a 37% decrease in AUC and 23% decrease in Cmax of triazolam Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/021911Orig1s000ClinPharmR_P1.pdf Page: 21.0 |
||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/021911Orig1s000ClinPharmR_P1.pdf Page: 21, 56 |
yes [Ki 450 uM] |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/021911Orig1s000ClinPharmR_P1.pdf Page: 20.0 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/021911Orig1s000ClinPharmR_P1.pdf Page: 40, 56 |
no |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: 39.0 |
PubMed
Title | Date | PubMed |
---|---|---|
Effects of antiepileptic drugs on cognition. | 2001 |
|
Rufinamide: a double-blind, placebo-controlled proof of principle trial in patients with epilepsy. | 2001 Feb |
|
New antiepileptic drugs that are second generation to existing antiepileptic drugs. | 2006 Jun |
|
Rufinamide: Pharmacology, clinical trials, and role in clinical practice. | 2006 Nov |
|
Gateways to clinical trials. | 2006 Oct |
|
Gateways to clinical trials. | 2006 Sep |
|
Rufinamide. | 2007 Jan |
|
Progress report on new antiepileptic drugs: a summary of the Eigth Eilat Conference (EILAT VIII). | 2007 Jan |
|
Rufinamide. | 2007 Jul |
|
[Rufinamide. An orphan drug for treatment of Lennox-Gastaut syndrome]. | 2007 Oct |
|
Pharmacological management of epilepsy: recent advances and future prospects. | 2008 |
|
Use of second-generation antiepileptic drugs in the pediatric population. | 2008 |
|
Pregabalin for the management of partial epilepsy. | 2008 Dec |
|
Rufinamide: clinical pharmacokinetics and concentration-response relationships in patients with epilepsy. | 2008 Jul |
|
The anticonvulsant profile of rufinamide (CGP 33101) in rodent seizure models. | 2008 Jul |
|
Rufinamide for generalized seizures associated with Lennox-Gastaut syndrome. | 2008 May 20 |
|
American Epilepsy Society--62nd Annual Meeting. 5-9 December 2008, Seattle, USA. | 2009 Feb |
|
Minimizing AED adverse effects: improving quality of life in the interictal state in epilepsy care. | 2009 Jun |
|
Truly "rational" polytherapy: maximizing efficacy and minimizing drug interactions, drug load, and adverse effects. | 2009 Jun |
|
Transitional polytherapy: tricks of the trade for monotherapy to monotherapy AED conversions. | 2009 Jun |
|
Effectiveness and tolerability of rufinamide in children and adults with refractory epilepsy: first European experience. | 2009 Mar |
|
Rufinamide (Banzel) for epilepsy. | 2009 Mar 9 |
|
Third-generation antiepileptic drugs: mechanisms of action, pharmacokinetics and interactions. | 2009 Mar-Apr |
|
Adopting an orphan drug: rufinamide for Lennox-Gastaut syndrome. | 2009 May-Jun |
|
Gateways to clinical trials. | 2009 Nov |
|
Gateways to clinical trials. | 2010 Apr |
|
"Epileptic encephalopathy" of infancy and childhood: electro-clinical pictures and recent understandings. | 2010 Dec |
|
Ethyl 1-(2,6-difluoro-benz-yl)-1H-1,2,3-triazole-4-carboxyl-ate. | 2010 Dec 15 |
|
Supporting the recommended paediatric dosing regimen for rufinamide in Lennox-Gastaut syndrome using clinical trial simulation. | 2010 Feb |
|
New Drugs2010, PART 1. | 2010 Feb |
|
Rufinamide: a novel broad-spectrum antiepileptic drug. | 2010 Jan |
|
Drug-induced QT interval shortening: potential harbinger of proarrhythmia and regulatory perspectives. | 2010 Jan |
|
New antiepileptic drugs: lacosamide, rufinamide, and vigabatrin. | 2010 Jul |
|
Severe constipation associated with the use of rufinamide (Banzel) in an adolescent. | 2010 May |
|
[Antiepileptic drugs in North America]. | 2010 May |
|
Experience with rufinamide in a pediatric population: a single center's experience. | 2010 Sep |
Patents
Sample Use Guides
Starting daily dose: 400-800 mg per day in two equally divided doses. Increase by 400-800 mg every other day until a maximum dose of 3200 mg per day, in two divided doses, is reached.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/18503564
In vitro studies with human liver microsomes using con-centrations of rufinamide in the range of 10–300 µmol/L(2.4–72 µg/ml) found no significant inhibition of any ofeight major human CYP isozymes—CYP1A2, CYP2A6,CYP2C9, CYP2C19, CYP2D6, CYP2E1, CYP3A4/5, andCYP4A9/11.
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Jun 26 05:39:43 UTC 2021
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admin
on
Sat Jun 26 05:39:43 UTC 2021
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Record UNII |
WFW942PR79
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Record Status |
Validated (UNII)
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Record Version |
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Classification Tree | Code System | Code | ||
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WHO-ATC |
N03AF03
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NCI_THESAURUS |
C264
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WHO-VATC |
QN03AF03
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LIVERTOX |
865
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EU-Orphan Drug |
EU/3/04/240
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EMA ASSESSMENT REPORTS |
INOVELON (AUTHORIZED: EPILEPSY)
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FDA ORPHAN DRUG |
193504
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Code System | Code | Type | Description | ||
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C079703
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PRIMARY | |||
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7387
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PRIMARY | |||
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RUFINAMIDE
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PRIMARY | |||
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106308-44-5
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WFW942PR79
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PRIMARY | |||
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1606401
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PRIMARY | USP-RS | ||
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129228
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PRIMARY | |||
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7470
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PRIMARY | |||
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SUB10403MIG
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PRIMARY | |||
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CHEMBL1201754
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69036
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PRIMARY | RxNorm | ||
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Rufinamide
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M9696
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PRIMARY | Merck Index | ||
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C75167
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PRIMARY | |||
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DB06201
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106308-44-5
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PRIMARY | |||
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3534
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PRIMARY |
Related Record | Type | Details | ||
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METABOLIC ENZYME -> INHIBITOR |
Ki
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BASIS OF STRENGTH->SUBSTANCE |
ASSAY (HPLC)
USP
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EXCRETED UNCHANGED |
FECAL; URINE
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METABOLIC ENZYME -> INDUCER |
WEAK
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BINDER->LIGAND |
BINDING
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TARGET -> INHIBITOR |
Shifts hNav1.1 opening to more depolarized voltages without further alterations in the gating properties of hNav1.1, hNav1.2, hNav1.3, and hNav1.6;
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Related Record | Type | Details | ||
---|---|---|---|---|
|
METABOLITE -> PARENT |
MAJOR
PLASMA
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Related Record | Type | Details | ||
---|---|---|---|---|
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Tmax | PHARMACOKINETIC |
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Biological Half-life | PHARMACOKINETIC |
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Volume of Distribution | PHARMACOKINETIC |
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