Details
Stereochemistry | RACEMIC |
Molecular Formula | C26H25ClN2O3 |
Molecular Weight | 448.941 |
Optical Activity | ( + / - ) |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=CC=CC=C1C(=O)NC2=CC(C)=C(C=C2)C(=O)N3CCCC(O)C4=C3C=CC(Cl)=C4
InChI
InChIKey=GYHCTFXIZSNGJT-UHFFFAOYSA-N
InChI=1S/C26H25ClN2O3/c1-16-6-3-4-7-20(16)25(31)28-19-10-11-21(17(2)14-19)26(32)29-13-5-8-24(30)22-15-18(27)9-12-23(22)29/h3-4,6-7,9-12,14-15,24,30H,5,8,13H2,1-2H3,(H,28,31)
Molecular Formula | C26H25ClN2O3 |
Molecular Weight | 448.941 |
Charge | 0 |
Count |
|
Stereochemistry | RACEMIC |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Optical Activity | ( + / - ) |
DescriptionSources: http://www.drugbank.ca/drugs/DB06212Curator's Comment: Description was created based on several sources, including
https://www.drugs.com/samsca.html
Sources: http://www.drugbank.ca/drugs/DB06212
Curator's Comment: Description was created based on several sources, including
https://www.drugs.com/samsca.html
Tolvaptan is a selective and competitive arginine vasopressin receptor 2 antagonist. Vasopressin acts on the V2 receptors found in the walls of the vasculature and luminal membranes of renal collecting ducts. By blocking V2 receptors in the renal collecting ducts, aquaporins do not insert themselves into the walls thus preventing water absorption. This action ultimately results in an increase in urine volume, decrease urine osmolality, and increase electrolyte-free water clearance to reduce intravascular volume and an increase serum sodium levels. Tolvaptan is especially useful for heart failure patients as they have higher serum levels of vasopressin. Tolvaptan is used to treat low blood sodium levels (hyponatremia) associated with various conditions like congestive heart failure, cirrhosis, and syndrome of inappropriate antidiuretic hormones (SIADH). FDA approved on May 19, 2009. Tolvaptan is sold under the trade names Samsca and Jinarc.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL1790 |
0.43 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Samsca Approved UseSamsca® is indicated for the treatment of clinically significant hypervolemic and euvolemic hyponatremia (serum sodium <125 mEq/L or less marked hyponatremia that is symptomatic and has resisted correction with fluid restriction), including patients with heart failure and Syndrome of Inappropriate Antidiuretic Hormone (SIADH). Launch Date2009 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
198 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/22120090 |
30 mg 1 times / day multiple, oral dose: 30 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
TOLVAPTAN blood | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
125 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/22120090 |
15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered: |
TOLVAPTAN blood | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
154 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/22120090 |
15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered: |
TOLVAPTAN blood | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1193 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/22120090 |
30 mg 1 times / day multiple, oral dose: 30 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
TOLVAPTAN blood | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
683 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/22120090 |
15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered: |
TOLVAPTAN blood | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
719 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/22120090 |
15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered: |
TOLVAPTAN blood | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
3.3 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/22120090 |
30 mg 1 times / day multiple, oral dose: 30 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
TOLVAPTAN blood | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
3.5 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/22120090 |
15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered: |
TOLVAPTAN blood | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
3.2 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/22120090 |
15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered: |
TOLVAPTAN blood | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
Doses
Dose | Population | Adverse events |
---|---|---|
480 mg single, oral Highest studied dose Dose: 480 mg Route: oral Route: single Dose: 480 mg Sources: |
healthy, 32 years (range: 20-51 years) n = 6 Health Status: healthy Age Group: 32 years (range: 20-51 years) Sex: M+F Population Size: 6 Sources: |
Other AEs: Thirst, Urinary frequency... Other AEs: Thirst (6 patients) Sources: Urinary frequency (6 patients) Dry mouth (2 patients) Headache NOS (2 patients) |
96 mg 1 times / day steady, oral (mean) Dose: 96 mg, 1 times / day Route: oral Route: steady Dose: 96 mg, 1 times / day Sources: |
unhealthy, 39 years n = 961 Health Status: unhealthy Condition: autosomal dominant polycystic kidney disease Age Group: 39 years Sex: M+F Population Size: 961 Sources: |
Disc. AE: Pollakiuria, Polyuria... AEs leading to discontinuation/dose reduction: Pollakiuria (6.6%) Sources: Polyuria (6.6%) Nocturia (6.6%) |
300 mg 1 times / day multiple, oral Highest studied dose Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
healthy, adult Health Status: healthy Age Group: adult Sources: |
|
1 mg single, intravenous Dose: 1 mg Route: intravenous Route: single Dose: 1 mg Sources: |
healthy, adult n = 14 Health Status: healthy Age Group: adult Population Size: 14 Sources: |
|
60 mg 1 times / day steady, oral (total) Recommended Dose: 60 mg, 1 times / day Route: oral Route: steady Dose: 60 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Condition: autosomal dominant polycystic kidney disease Sources: |
Other AEs: Liver injury... Other AEs: Liver injury (serious) Sources: |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Dry mouth | 2 patients | 480 mg single, oral Highest studied dose Dose: 480 mg Route: oral Route: single Dose: 480 mg Sources: |
healthy, 32 years (range: 20-51 years) n = 6 Health Status: healthy Age Group: 32 years (range: 20-51 years) Sex: M+F Population Size: 6 Sources: |
Headache NOS | 2 patients | 480 mg single, oral Highest studied dose Dose: 480 mg Route: oral Route: single Dose: 480 mg Sources: |
healthy, 32 years (range: 20-51 years) n = 6 Health Status: healthy Age Group: 32 years (range: 20-51 years) Sex: M+F Population Size: 6 Sources: |
Thirst | 6 patients | 480 mg single, oral Highest studied dose Dose: 480 mg Route: oral Route: single Dose: 480 mg Sources: |
healthy, 32 years (range: 20-51 years) n = 6 Health Status: healthy Age Group: 32 years (range: 20-51 years) Sex: M+F Population Size: 6 Sources: |
Urinary frequency | 6 patients | 480 mg single, oral Highest studied dose Dose: 480 mg Route: oral Route: single Dose: 480 mg Sources: |
healthy, 32 years (range: 20-51 years) n = 6 Health Status: healthy Age Group: 32 years (range: 20-51 years) Sex: M+F Population Size: 6 Sources: |
Nocturia | 6.6% Disc. AE |
96 mg 1 times / day steady, oral (mean) Dose: 96 mg, 1 times / day Route: oral Route: steady Dose: 96 mg, 1 times / day Sources: |
unhealthy, 39 years n = 961 Health Status: unhealthy Condition: autosomal dominant polycystic kidney disease Age Group: 39 years Sex: M+F Population Size: 961 Sources: |
Pollakiuria | 6.6% Disc. AE |
96 mg 1 times / day steady, oral (mean) Dose: 96 mg, 1 times / day Route: oral Route: steady Dose: 96 mg, 1 times / day Sources: |
unhealthy, 39 years n = 961 Health Status: unhealthy Condition: autosomal dominant polycystic kidney disease Age Group: 39 years Sex: M+F Population Size: 961 Sources: |
Polyuria | 6.6% Disc. AE |
96 mg 1 times / day steady, oral (mean) Dose: 96 mg, 1 times / day Route: oral Route: steady Dose: 96 mg, 1 times / day Sources: |
unhealthy, 39 years n = 961 Health Status: unhealthy Condition: autosomal dominant polycystic kidney disease Age Group: 39 years Sex: M+F Population Size: 961 Sources: |
Liver injury | serious | 60 mg 1 times / day steady, oral (total) Recommended Dose: 60 mg, 1 times / day Route: oral Route: steady Dose: 60 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Condition: autosomal dominant polycystic kidney disease Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
yes [IC50 0.837 uM] | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/204441Orig1s000ClinPharmR.pdf#page=6 Page: 6,11 |
yes [IC50 15.9 uM] | weak (co-administration study) Comment: administration with digoxin increased Digoxin Cmax and AUC by 30% and 20%, respectively Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/204441Orig1s000ClinPharmR.pdf#page=6 Page: 6,11 |
||
yes [IC50 27.2 uM] | ||||
yes [IC50 4.14 uM] | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/204441Orig1s000ClinPharmR.pdf#page=16 Page: 16.0 |
yes [IC50 41.5 uM] | |||
yes [IC50 5.47 uM] | ||||
yes [IC50 50 uM] | ||||
yes [IC50 50 uM] | ||||
yes [IC50 50 uM] | ||||
yes [IC50 6.15 uM] | ||||
yes [IC50 7.965 uM] | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/204441Orig1s000ClinPharmR.pdf#page=6 Page: 6,11 |
yes [IC50 8.32 uM] | |||
yes [IC50 >10 uM] | ||||
yes [IC50 >30 uM] | ||||
yes [Ki 34 uM] |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/204441Orig1s000ClinPharmR.pdf#page=11 Page: 11.0 |
yes | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/204441Orig1s000ClinPharmR.pdf#page=96 Page: 96.0 |
yes | yes (co-administration study) Comment: administration with ketoconazole caused a 3.5-fold and 5-fold increase in tolvaptan Cmax and AUC, respectively; administration with rifmapin reduced Cmax and AUC of tolvaptan to 10 and 20%, respectively; Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/204441Orig1s000ClinPharmR.pdf#page=96 Page: 96.0 |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022275s000_PharmR_P1.pdf#page=31 Page: 31.0 |
PubMed
Title | Date | PubMed |
---|---|---|
Trial finds tolvaptan may help manage congestion in people with heart failure, but did not reduce death or hospitalisation. | 2004 Dec |
|
Pharmacology of new agents for acute heart failure syndromes. | 2005 Sep 19 |
|
Overview of randomized clinical trials in acute heart failure syndromes. | 2005 Sep 19 |
|
Vasopressin antagonists. | 2006 Aug |
|
Comparison of 60-day mortality in hospitalized heart failure patients with versus without hypothermia. | 2006 Dec 1 |
|
Vasopressin-2-receptor antagonism augments water excretion without changes in renal hemodynamics or sodium and potassium excretion in human heart failure. | 2006 Feb |
|
Hyponatremia and heart failure--treatment considerations. | 2006 Jan-Feb |
|
Vasopressin antagonists as aquaretic agents for the treatment of hyponatremia. | 2006 Jul |
|
Vasopressin receptor antagonists. | 2006 Jun |
|
[Diuretics]. | 2006 May |
|
Tolvaptan: a selective vasopressin type 2 receptor antagonist in congestive heart failure. | 2006 May |
|
Vasopressin excess and hyponatremia. | 2006 May |
|
Vasopressin antagonists--progress and promise. | 2006 Nov 16 |
|
AVP receptor antagonists as aquaretics: review and assessment of clinical data. | 2006 Sep |
|
Improvement in hyponatremia during hospitalization for worsening heart failure is associated with improved outcomes: insights from the Acute and Chronic Therapeutic Impact of a Vasopressin Antagonist in Chronic Heart Failure (ACTIV in CHF) trial. | 2007 |
|
Aquaretic agents: what's beyond the treatment of hyponatremia? | 2007 |
|
Therapeutic potential of vasopressin receptor antagonists. | 2007 |
|
Cerebral correlates of hyponatremia. | 2007 |
|
[Vasopressin antagonists in treatment of hyponatremia]. | 2007 Aug |
|
Pharmacokinetic and pharmacodynamic interaction between tolvaptan, a non-peptide AVP antagonist, and furosemide or hydrochlorothiazide. | 2007 Aug |
|
Effects of tolvaptan, an oral vasopressin V2 receptor antagonist, in hyponatremia. | 2007 Aug |
|
Tolvaptan, an oral vasopressin V2 receptor antagonist for heart failure? | 2007 Dec |
|
Clinical trials update from the European Society of Cardiology Congress in Vienna, 2007: PROSPECT, EVEREST, ARISE, ALOFT, FINESSE, Prague-8, CARESS in MI and ACUITY. | 2007 Dec |
|
Pharmacokinetics, pharmacodynamics, and safety of tolvaptan, a nonpeptide AVP antagonist, during ascending single-dose studies in healthy subjects. | 2007 Dec |
|
Diagnosis and management of hyponatremia in cancer patients. | 2007 Dec |
|
Aminocarbonylation route to tolvaptan. | 2007 Dec 1 |
|
Recognition and treatment of hyponatremia in acutely ill hospitalized patients. | 2007 Feb |
|
New agents for managing hyponatremia in hospitalized patients. | 2007 Feb 1 |
|
[Arginine vasopressin antagonism--new treatment option in chronic heart failure]. | 2007 Jan 18 |
|
Gateways to clinical trials. | 2007 Jan-Feb |
|
Gateways to clinical trials. | 2007 Jul-Aug |
|
[Recent progress in vasopressin research on cardiovascular diseases]. | 2007 Jun |
|
Vaptans: a promising therapy in the management of advanced cirrhosis. | 2007 Jun |
|
Arginine vasopressin receptor antagonists for heart failure: a winter climbing to the Everest's tip? | 2007 Jun 5 |
|
Multicenter, randomized, double-blind, placebo-controlled study on the effect of oral tolvaptan on left ventricular dilation and function in patients with heart failure and systolic dysfunction. | 2007 Jun 5 |
|
Clinical trials update from the American College of Cardiology 2007: ALPHA, EVEREST, FUSION II, VALIDD, PARR-2, REMODEL, SPICE, COURAGE, COACH, REMADHE, pro-BNP for the evaluation of dyspnoea and THIS-diet. | 2007 Jun-Jul |
|
Gateways to clinical trials. | 2007 Mar |
|
Climbing the mountain of acute decompensated heart failure: the EVEREST Trials. | 2007 Mar 28 |
|
Short-term clinical effects of tolvaptan, an oral vasopressin antagonist, in patients hospitalized for heart failure: the EVEREST Clinical Status Trials. | 2007 Mar 28 |
|
Effects of oral tolvaptan in patients hospitalized for worsening heart failure: the EVEREST Outcome Trial. | 2007 Mar 28 |
|
What new drugs can nephrologists look forward to in the next year or two? | 2007 May |
|
Hyponatremia: current treatment strategies and the role of vasopressin antagonists. | 2007 May |
|
[Vasopressin V2-receptor antagonist, tolvaptan, for treatment of heart failure]. | 2007 May 28 |
|
Current issues for nurse practitioners: Hyponatremia. | 2007 Nov |
|
Hyponatremia and vasopressin antagonism in congestive heart failure. | 2007 Nov |
|
Effects of nonpeptide vasopressin V2 antagonist tolvaptan in rats with heart failure. | 2007 Nov 15 |
|
Water in health and disease: new aspects of disturbances in water metabolism. | 2007 Oct |
|
V2 receptor antagonism with tolvaptan in heart failure. | 2007 Oct |
|
Tolvaptan, an orally active vasopressin V(2)-receptor antagonist - pharmacology and clinical trials. | 2007 Spring |
|
Polycystic kidney diseases: from molecular discoveries to targeted therapeutic strategies. | 2008 Feb |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.drugs.com/pro/samsca.html
The usual starting dose for Samsca (Tolvaptan) is 15 mg administered once daily without regard to meals. Increase the dose to 30 mg once daily, after at least 24 hours, to a maximum of 60 mg once daily, as needed to achieve the desired level of serum sodium. Do not administer Samsca for more than 30 days to minimize the risk of liver injury
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/21816754
Curator's Comment: Tolvaptan inhibits ERK-dependent cell proliferation, Cl⁻ secretion, and in vitro cyst growth of human ADPKD cells stimulated by vasopressin.
Tolvaptan caused a concentration-dependent inhibition of AVP-induced cAMP production with an apparent IC(50) of ∼10(-10) M.
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 15:26:46 GMT 2023
by
admin
on
Fri Dec 15 15:26:46 GMT 2023
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Record UNII |
21G72T1950
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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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LIVERTOX |
NBK548503
Created by
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WHO-ATC |
C03XA01
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EMA ASSESSMENT REPORTS |
SAMSCA (AUTHORIZED: INAPPROPRIATE ADH SYNDROME)
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WHO-VATC |
QC03XA01
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EMA ASSESSMENT REPORTS |
JINARC (AUTHORIZED: POLYCYSTIC KIDNEY, AUTOSOMAL DOMINANT)
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FDA ORPHAN DRUG |
347311
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NDF-RT |
N0000193181
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NCI_THESAURUS |
C2180
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EU-Orphan Drug |
EU/3/13/1175
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LL-16
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SUB22755
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100000091683
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DB06212
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CHEMBL344159
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21G72T1950
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PRIMARY | |||
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Tolvaptan
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4110
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150683-30-0
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DTXSID3048780
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C77082
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m10969
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8196
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7969
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21G72T1950
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PRIMARY | |||
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358257
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PRIMARY | RxNorm | ||
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216237
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2226
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Related Record | Type | Details | ||
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EXCRETED UNCHANGED |
AMOUNT EXCRETED
FECAL
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SALT/SOLVATE -> PARENT |
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ENANTIOMER -> RACEMATE | |||
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METABOLIC ENZYME -> SUBSTRATE |
MAJOR
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ENANTIOMER -> RACEMATE | |||
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TRANSPORTER -> SUBSTRATE | |||
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EXCRETED UNCHANGED |
After oral administration of labeled tolvaptan the fraction of total radioactivity excreted in urine is 40 %. Less than 1% of the dose is excreted as unchanged tolvaptan.
AMOUNT EXCRETED
URINE
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TARGET -> INHIBITOR | |||
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BINDER->LIGAND |
BINDING
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Related Record | Type | Details | ||
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METABOLITE -> PARENT |
FECAL; PLASMA; URINE
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METABOLITE -> PARENT |
FECAL; URINE
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METABOLITE -> PARENT |
MICROSOMAL; PLASMA; URINE
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METABOLITE INACTIVE -> PARENT |
MAJOR
FECAL; MICROSOMAL; PLASMA; URINE
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METABOLITE -> PARENT |
FECAL; PLASMA; URINE
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METABOLITE -> PARENT |
FECAL; MICROSOMAL; PLASMA; URINE
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METABOLITE -> PARENT |
FECAL; MICROSOMAL; PLASMA; URINE
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METABOLITE -> PARENT |
FECAL; MICROSOMAL; PLASMA; URINE
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METABOLITE -> PARENT |
FECAL; PLASMA; URINE
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METABOLITE -> PARENT |
FECAL; MICROSOMAL; PLASMA; URINE
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METABOLITE -> PARENT |
FECAL; MICROSOMAL; PLASMA; URINE
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METABOLITE -> PARENT |
FECAL; URINE
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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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NOAEL | PHARMACOKINETIC |
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Biological Half-life | PHARMACOKINETIC |
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NOAEL | PHARMACOKINETIC |
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Volume of Distribution | PHARMACOKINETIC |
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