Details
Stereochemistry | ACHIRAL |
Molecular Formula | C8H8N2O3S |
Molecular Weight | 212.226 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
NS(=O)(=O)CC1=NOC2=C1C=CC=C2
InChI
InChIKey=UBQNRHZMVUUOMG-UHFFFAOYSA-N
InChI=1S/C8H8N2O3S/c9-14(11,12)5-7-6-3-1-2-4-8(6)13-10-7/h1-4H,5H2,(H2,9,11,12)
Molecular Formula | C8H8N2O3S |
Molecular Weight | 212.226 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Zonisamide is an antiseizure drug chemically classified as a sulfonamide and unrelated to other antiseizure agents. The precise mechanism by which zonisamide exerts its antiseizure effect is unknown, although it is believed that the drug blocks sodium and calcium channels, which leads to the suppression of neuronal hypersynchronization (i.e. convulsions). Sonisamide has also been found to potentiate dopaminergic and serotonergic neurotransmission but does not appear to potentiate syanptic activity by GABA (gamma amino butyric acid). Zonisamide binds to sodium channels and voltage sensitive calcium channels, which suppresses neuronal depolarization and hypersynchronization. Zonisamide also inhibits carbonic anhydrase to a weaker extent, but such an effect is not thought to contribute substantially to the drug's anticonvulsant activity. Zonisamide is approved in the United States, United Kingdom, and Australia for adjunctive treatment of partial seizures in adults and in Japan for both adjunctive and monotherapy for partial seizures (simple, complex, secondarily generalized), generalized (tonic, tonic-clonic (grand mal), and atypical absence) and combined seizures.
CNS Activity
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL205 Sources: https://www.ncbi.nlm.nih.gov/pubmed/25882523 |
35.0 nM [Ki] | ||
Target ID: CHEMBL261 Sources: https://www.ncbi.nlm.nih.gov/pubmed/25882523 |
56.0 nM [Ki] | ||
Target ID: CHEMBL2039 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19948168 |
25.0 µM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | ZONEGRAN Approved UseZONEGRAN is indicated as adjunctive therapy in the treatment of partial seizures in adults
with epilepsy. Launch Date2000 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
18.4 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15496640 |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
ZONISAMIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
197.4 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15496640 |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
ZONISAMIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
63 h |
unknown, oral |
ZONISAMIDE plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
60% |
unknown, oral |
ZONISAMIDE plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
7.5 g single, oral Overdose |
unhealthy, 15 years n = 1 Health Status: unhealthy Age Group: 15 years Sex: F Population Size: 1 Sources: |
Other AEs: Coma... |
8.7 g single, oral Overdose |
unhealthy, 20 years n = 1 Health Status: unhealthy Age Group: 20 years Sex: F Population Size: 1 Sources: |
Other AEs: Emesis... |
12.6 g single, oral Overdose |
unhealthy, 25 years n = 1 Health Status: unhealthy Age Group: 25 years Sex: F Population Size: 1 Sources: |
Other AEs: Vomiting, Somnolence... |
300 mg 2 times / day steady, oral Highest studied dose Dose: 300 mg, 2 times / day Route: oral Route: steady Dose: 300 mg, 2 times / day Sources: |
unhealthy, 35 years (range: 17.9-64.1 years) n = 51 Health Status: unhealthy Condition: refractory partial epilepsy Age Group: 35 years (range: 17.9-64.1 years) Sex: M+F Population Size: 51 Sources: |
|
100 mg 1 times / day multiple, oral (starting) Recommended Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
unhealthy, adult n = 1336 Health Status: unhealthy Condition: epilepsy Age Group: adult Population Size: 1336 Sources: |
Disc. AE: Somnolence, Fatigue... AEs leading to discontinuation/dose reduction: Somnolence (6%) Sources: Fatigue (6%) Ataxia (6%) Anorexia (3%) Attention concentration difficulty (2%) Memory impairment (2%) Mental retardation (2%) Nausea (2%) Vomiting (2%) Weight loss (1%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Coma | 1% | 7.5 g single, oral Overdose |
unhealthy, 15 years n = 1 Health Status: unhealthy Age Group: 15 years Sex: F Population Size: 1 Sources: |
Emesis | 1% | 8.7 g single, oral Overdose |
unhealthy, 20 years n = 1 Health Status: unhealthy Age Group: 20 years Sex: F Population Size: 1 Sources: |
Somnolence | 1% | 12.6 g single, oral Overdose |
unhealthy, 25 years n = 1 Health Status: unhealthy Age Group: 25 years Sex: F Population Size: 1 Sources: |
Vomiting | 1% | 12.6 g single, oral Overdose |
unhealthy, 25 years n = 1 Health Status: unhealthy Age Group: 25 years Sex: F Population Size: 1 Sources: |
Weight loss | 1% Disc. AE |
100 mg 1 times / day multiple, oral (starting) Recommended Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
unhealthy, adult n = 1336 Health Status: unhealthy Condition: epilepsy Age Group: adult Population Size: 1336 Sources: |
Attention concentration difficulty | 2% Disc. AE |
100 mg 1 times / day multiple, oral (starting) Recommended Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
unhealthy, adult n = 1336 Health Status: unhealthy Condition: epilepsy Age Group: adult Population Size: 1336 Sources: |
Memory impairment | 2% Disc. AE |
100 mg 1 times / day multiple, oral (starting) Recommended Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
unhealthy, adult n = 1336 Health Status: unhealthy Condition: epilepsy Age Group: adult Population Size: 1336 Sources: |
Mental retardation | 2% Disc. AE |
100 mg 1 times / day multiple, oral (starting) Recommended Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
unhealthy, adult n = 1336 Health Status: unhealthy Condition: epilepsy Age Group: adult Population Size: 1336 Sources: |
Nausea | 2% Disc. AE |
100 mg 1 times / day multiple, oral (starting) Recommended Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
unhealthy, adult n = 1336 Health Status: unhealthy Condition: epilepsy Age Group: adult Population Size: 1336 Sources: |
Vomiting | 2% Disc. AE |
100 mg 1 times / day multiple, oral (starting) Recommended Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
unhealthy, adult n = 1336 Health Status: unhealthy Condition: epilepsy Age Group: adult Population Size: 1336 Sources: |
Anorexia | 3% Disc. AE |
100 mg 1 times / day multiple, oral (starting) Recommended Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
unhealthy, adult n = 1336 Health Status: unhealthy Condition: epilepsy Age Group: adult Population Size: 1336 Sources: |
Ataxia | 6% Disc. AE |
100 mg 1 times / day multiple, oral (starting) Recommended Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
unhealthy, adult n = 1336 Health Status: unhealthy Condition: epilepsy Age Group: adult Population Size: 1336 Sources: |
Fatigue | 6% Disc. AE |
100 mg 1 times / day multiple, oral (starting) Recommended Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
unhealthy, adult n = 1336 Health Status: unhealthy Condition: epilepsy Age Group: adult Population Size: 1336 Sources: |
Somnolence | 6% Disc. AE |
100 mg 1 times / day multiple, oral (starting) Recommended Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
unhealthy, adult n = 1336 Health Status: unhealthy Condition: epilepsy Age Group: adult Population Size: 1336 Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no [IC50 >133 uM] | ||||
no [IC50 >133 uM] | ||||
no [IC50 >133 uM] | ||||
no [IC50 >133 uM] | ||||
no | ||||
no | ||||
no | ||||
Page: (Label) 4 |
weak [IC50 267 uM] | |||
Page: (Label) 3, (PMDA_I100) 20 |
weak [Ki 1076 uM] | |||
Page: (Label) 3 |
weak | |||
Page: (Label) 3 |
weak | |||
Page: (Label) 3 |
weak | |||
Page: (Label) 3 |
weak | |||
Page: (Label) 3 |
weak | |||
Page: (Label) 3 |
weak | |||
Page: (Label) 3 |
weak | |||
Page: (Label) 3 |
weak | yes (co-administration study) Comment: <25% inhibition at levels approximately two-fold or greater than clinically relevant unbound serum concentrations. ; Coadministration of multiple dosing of zonisamide did not significantly affect the pharmacokinetic parameters of desipramine (CYP2D6 substrate). Page: (Label) 3 |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: (Label) 2, (PMDA_I100) 20 |
major [Km 312 uM] | yes (co-administration study) Comment: The half-life of zonisamide following a 400 mg dose in patients concurrently on enzyme-inducing AEDs such as phenytoin, carbamazepine, or phenobarbital was between 27-38 hours (46 hr on the non-enzyme inducing AED, valproate). Page: (Label) 2, (PMDA_I100) 20 |
||
minor [Km 179 uM] | ||||
minor [Km 188 uM] | ||||
yes | ||||
yes | ||||
yes |
PubMed
Title | Date | PubMed |
---|---|---|
Cognitive deterioration associated with focal cortical dysplasia. | 1999 Jan |
|
Anticonvulsant-induced suppression of IFN-gamma production by lymphocytes obtained from cervical lymph nodes in glioma-bearing mice. | 2000 Apr |
|
Effects of combined administration of zonisamide and valproic acid or phenytoin to nitric oxide production, monoamines and zonisamide concentrations in the brain of seizure-susceptible EL mice. | 2000 Sep 15 |
|
A solvent used for antiepileptic drugs increases serum and brain zonisamide concentrations in seizure-susceptible el mice. | 2001 Aug |
|
[Clinical features and treatment of refractory epilepsy in children]. | 2001 Dec |
|
Zonisamide has beneficial effects on Parkinson's disease patients. | 2001 Dec |
|
Effect of immobilization stress on anticonvulsant actions and pharmacokinetics of zonisamide in mice. | 2001 Jan |
|
Contribution of sodium valproate to the syndrome of inappropriate secretion of antidiuretic hormone. | 2001 Jan |
|
Progress report on new antiepileptic drugs: a summary of the Fifth Eilat Conference (EILAT V). | 2001 Jan |
|
Extremely high drug-reductase activity based on aldehyde oxidase in monkey liver. | 2001 Jul |
|
New anticonvulsants for use in pediatric patients (part I). | 2001 Mar-Apr |
|
Contrasting effects of zonisamide and acetazolamide on amygdaloid kindling in rats. | 2001 Nov |
|
Regional accumulation of 14C-zonisamide in rat brain during kainic acid-induced limbic seizures. | 2001 Nov |
|
Zonisamide in West syndrome. | 2001 Nov |
|
Review of treatment options for refractory epilepsy: new medications and vagal nerve stimulation. | 2001 Nov |
|
Determination of effects of antiepileptic drugs on SNAREs-mediated hippocampal monoamine release using in vivo microdialysis. | 2001 Oct |
|
Influence of oral adsorbent AST-120 on anticonvulsive effect of zonisamide in rats. | 2001 Oct-Nov |
|
[Efficacy of anticonvulsants on acute encephalitis with refractory, repetitive partial seizures (AERRPS)]. | 2001 Sep |
|
Long-term observations of two siblings with Lafora disease treated with zonisamide. | 2001 Sep |
|
Levetiracetam, oxcarbazepine, remacemide and zonisamide for drug resistant localization-related epilepsy: a systematic review. | 2001 Sep |
|
New and emerging prophylactic agents for migraine. | 2002 |
|
Treatment of epilepsy in women of reproductive age: pharmacokinetic considerations. | 2002 |
|
Third generation anticonvulsants in bipolar disorder: a review of efficacy and summary of clinical recommendations. | 2002 Apr |
|
New antiepileptic drugs: review on drug interactions. | 2002 Feb |
|
Marketed new antiepileptic drugs: are they better than old-generation agents? | 2002 Feb |
|
Randomized controlled trial of zonisamide for the treatment of partial-onset seizures. | 2002 Jun 11 |
|
New antiepileptic drugs. | 2002 Mar |
|
Effects of endogenous steroids on CYP3A4-mediated drug metabolism by human liver microsomes. | 2002 May |
|
Long-term response to zonisamide in patients with West syndrome. | 2002 May 28 |
|
Zonisamide treatment of bipolar disorder: a case report. | 2002 Nov |
|
Antipsychotic, antidepressant, anxiolytic, and anticonvulsant drugs induce type II nitric oxide synthase mRNA in rat brain. | 2002 Nov 29 |
|
Newer GABAergic agents for pharmacotherapy of infantile spasms. | 2002 Oct |
|
Selective mutism and obsessive compulsive disorders associated with zonisamide. | 2002 Oct |
|
[Urolithiasis induced by combined ACTH and zonisamide treatment in a patient with startle induced epilepsy]. | 2002 Sep |
|
Use of anticonvulsants for treatment of neuropathic pain. | 2002 Sep 10 |
|
Antiepileptic drug use during the first 12 months of vagus nerve stimulation therapy: a registry study. | 2002 Sep 24 |
|
Clinical care of pregnant women with epilepsy: neural tube defects and folic acid supplementation. | 2003 |
|
Selection criteria for the clinical use of the newer antiepileptic drugs. | 2003 |
|
Zonisamide for weight loss in obese adults: a randomized controlled trial. | 2003 Apr 9 |
|
Effects of concomitant antiepileptic drugs on serum carbamazepine concentration in epileptic patients: quantitative analysis based on extracellular water volume as a transforming factor. | 2003 Jan |
|
Visual hallucinations associated with zonisamide. | 2003 Jan |
|
Zonisamide-induced restless legs syndrome. | 2003 Jan 14 |
|
Acute zonisamide overdose: a death revisited. | 2003 Jun |
|
Therapeutic drug monitoring of the newer antiepileptic drugs. | 2003 Jun |
|
The effect of systemic zonisamide (Zonegran) on thermal hyperalgesia and mechanical allodynia in rats with an experimental mononeuropathy. | 2003 Jun |
|
Effects of valproate, phenytoin, and zonisamide on clonic and tonic seizures induced by acute and repeated exposure of mice to flurothyl. | 2003 Mar |
|
Treating bipolar depression. | 2003 Mar |
|
Review of the newer antiepileptic drugs. | 2003 Mar |
Patents
Sample Use Guides
ZONEGRAN (zonisamide) is recommended as adjunctive therapy for the treatment of partial
seizures in adults. Safety and efficacy in pediatric patients below the age of 16 have not been
established. ZONEGRAN should be administered once or twice daily, using 25 mg or 100
mg capsules. ZONEGRAN is given orally and can be taken with or without food. Capsules
should be swallowed whole.
Route of Administration:
Oral
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 17:49:13 GMT 2023
by
admin
on
Sat Dec 16 17:49:13 GMT 2023
|
Record UNII |
459384H98V
|
Record Status |
Validated (UNII)
|
Record Version |
|
-
Download
Name | Type | Language | ||
---|---|---|---|---|
|
Official Name | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Code | English | ||
|
Code | English | ||
|
Systematic Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Brand Name | English |
Classification Tree | Code System | Code | ||
---|---|---|---|---|
|
WHO-ATC |
N03AX15
Created by
admin on Sat Dec 16 17:49:15 GMT 2023 , Edited by admin on Sat Dec 16 17:49:15 GMT 2023
|
||
|
NCI_THESAURUS |
C264
Created by
admin on Sat Dec 16 17:49:16 GMT 2023 , Edited by admin on Sat Dec 16 17:49:16 GMT 2023
|
||
|
NDF-RT |
N0000175753
Created by
admin on Sat Dec 16 17:49:16 GMT 2023 , Edited by admin on Sat Dec 16 17:49:16 GMT 2023
|
||
|
EMA ASSESSMENT REPORTS |
ZONEGRAN (AUTHORIZED: EPILEPSIES, PARTIAL)
Created by
admin on Sat Dec 16 17:49:16 GMT 2023 , Edited by admin on Sat Dec 16 17:49:16 GMT 2023
|
||
|
NDF-RT |
N0000008486
Created by
admin on Sat Dec 16 17:49:16 GMT 2023 , Edited by admin on Sat Dec 16 17:49:16 GMT 2023
|
||
|
WHO-VATC |
QN03AX15
Created by
admin on Sat Dec 16 17:49:16 GMT 2023 , Edited by admin on Sat Dec 16 17:49:16 GMT 2023
|
||
|
LIVERTOX |
NBK548809
Created by
admin on Sat Dec 16 17:49:16 GMT 2023 , Edited by admin on Sat Dec 16 17:49:16 GMT 2023
|
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
459384H98V
Created by
admin on Sat Dec 16 17:49:16 GMT 2023 , Edited by admin on Sat Dec 16 17:49:16 GMT 2023
|
PRIMARY | |||
|
T-111
Created by
admin on Sat Dec 16 17:49:16 GMT 2023 , Edited by admin on Sat Dec 16 17:49:16 GMT 2023
|
PRIMARY | |||
|
1725003
Created by
admin on Sat Dec 16 17:49:16 GMT 2023 , Edited by admin on Sat Dec 16 17:49:16 GMT 2023
|
PRIMARY | |||
|
7047
Created by
admin on Sat Dec 16 17:49:16 GMT 2023 , Edited by admin on Sat Dec 16 17:49:16 GMT 2023
|
PRIMARY | |||
|
100000088020
Created by
admin on Sat Dec 16 17:49:16 GMT 2023 , Edited by admin on Sat Dec 16 17:49:16 GMT 2023
|
PRIMARY | |||
|
N0000185503
Created by
admin on Sat Dec 16 17:49:16 GMT 2023 , Edited by admin on Sat Dec 16 17:49:16 GMT 2023
|
PRIMARY | P-Glycoprotein Inhibitors [MoA] | ||
|
5734
Created by
admin on Sat Dec 16 17:49:16 GMT 2023 , Edited by admin on Sat Dec 16 17:49:16 GMT 2023
|
PRIMARY | |||
|
C022189
Created by
admin on Sat Dec 16 17:49:16 GMT 2023 , Edited by admin on Sat Dec 16 17:49:16 GMT 2023
|
PRIMARY | |||
|
39998
Created by
admin on Sat Dec 16 17:49:16 GMT 2023 , Edited by admin on Sat Dec 16 17:49:16 GMT 2023
|
PRIMARY | RxNorm | ||
|
DTXSID9046023
Created by
admin on Sat Dec 16 17:49:16 GMT 2023 , Edited by admin on Sat Dec 16 17:49:16 GMT 2023
|
PRIMARY | |||
|
5575
Created by
admin on Sat Dec 16 17:49:16 GMT 2023 , Edited by admin on Sat Dec 16 17:49:16 GMT 2023
|
PRIMARY | |||
|
68291-97-4
Created by
admin on Sat Dec 16 17:49:15 GMT 2023 , Edited by admin on Sat Dec 16 17:49:15 GMT 2023
|
PRIMARY | |||
|
Zonisamide
Created by
admin on Sat Dec 16 17:49:16 GMT 2023 , Edited by admin on Sat Dec 16 17:49:16 GMT 2023
|
PRIMARY | |||
|
SUB00187MIG
Created by
admin on Sat Dec 16 17:49:15 GMT 2023 , Edited by admin on Sat Dec 16 17:49:15 GMT 2023
|
PRIMARY | |||
|
m11662
Created by
admin on Sat Dec 16 17:49:16 GMT 2023 , Edited by admin on Sat Dec 16 17:49:16 GMT 2023
|
PRIMARY | Merck Index | ||
|
10127
Created by
admin on Sat Dec 16 17:49:15 GMT 2023 , Edited by admin on Sat Dec 16 17:49:15 GMT 2023
|
PRIMARY | |||
|
C47790
Created by
admin on Sat Dec 16 17:49:16 GMT 2023 , Edited by admin on Sat Dec 16 17:49:16 GMT 2023
|
PRIMARY | |||
|
DB00909
Created by
admin on Sat Dec 16 17:49:16 GMT 2023 , Edited by admin on Sat Dec 16 17:49:16 GMT 2023
|
PRIMARY | |||
|
ZONISAMIDE
Created by
admin on Sat Dec 16 17:49:16 GMT 2023 , Edited by admin on Sat Dec 16 17:49:16 GMT 2023
|
PRIMARY | |||
|
CHEMBL750
Created by
admin on Sat Dec 16 17:49:16 GMT 2023 , Edited by admin on Sat Dec 16 17:49:16 GMT 2023
|
PRIMARY | |||
|
7293
Created by
admin on Sat Dec 16 17:49:16 GMT 2023 , Edited by admin on Sat Dec 16 17:49:16 GMT 2023
|
PRIMARY | |||
|
459384H98V
Created by
admin on Sat Dec 16 17:49:16 GMT 2023 , Edited by admin on Sat Dec 16 17:49:16 GMT 2023
|
PRIMARY | |||
|
2872
Created by
admin on Sat Dec 16 17:49:16 GMT 2023 , Edited by admin on Sat Dec 16 17:49:16 GMT 2023
|
PRIMARY |
Related Record | Type | Details | ||
---|---|---|---|---|
|
TARGET -> INHIBITOR |
|
||
|
TARGET -> INHIBITOR | |||
|
TARGET -> INHIBITOR |
|
||
|
BASIS OF STRENGTH->SUBSTANCE |
ASSAY (HPLC)
USP
|
||
|
OFF-TARGET->INHIBITOR |
Following 60 minutes preincubation, non-preincubated sample 4.64 (4.06-5.30) micromolar
Ki
|
||
|
TARGET -> INHIBITOR | |||
|
TARGET -> INHIBITOR | |||
|
BINDER->LIGAND |
BINDING
|
||
|
EXCRETED UNCHANGED |
AMOUNT EXCRETED
URINE
|
||
|
TARGET -> INHIBITOR |
|
||
|
OFF-TARGET->INHIBITOR |
Non preinucabated sample
Ki
|
||
|
METABOLIC ENZYME -> SUBSTRATE | |||
|
TARGET -> INHIBITOR | |||
|
TARGET -> INHIBITOR | |||
|
TARGET -> INHIBITOR |
Related Record | Type | Details | ||
---|---|---|---|---|
|
METABOLITE -> PARENT |
URINE
|
||
|
METABOLITE -> PARENT |
|
||
|
METABOLITE -> PARENT |
MAJOR
URINE
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
ACTIVE MOIETY |
|
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
---|---|---|---|---|---|---|
Volume of Distribution | PHARMACOKINETIC |
|
|
|||
Biological Half-life | PHARMACOKINETIC |
|
|
|||
Tmax | PHARMACOKINETIC |
|
ORAL ADMINISTRATION |
|
||
Tmax | PHARMACOKINETIC |
|
DOSE |
|
||