TOLVAPTAN

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

Structure Search

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)

HIDE SMILES / InChI

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	( + / - )

Description
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.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Vasopressin V2 receptor 15 Target ID: CHEMBL1790 Sources: https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=5526617c-c7b9-4556-886d-729bbabbc566&type=display	Antagonist 2760		0.43 nM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Hypervolemic and euvolemic hyponatremia 1 Sources: https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=5526617c-c7b9-4556-886d-729bbabbc566&type=display	Primary		Approved 8360	Samsca Approved Use Samsca® 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 Date 1.24260477E12

C_max

Value	Dose	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	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

T_1/2

Value	Dose	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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204441lbl.pdf https://pubmed.ncbi.nlm.nih.gov/17925589	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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204441lbl.pdf https://pubmed.ncbi.nlm.nih.gov/17925589	Other AEs: Thirst, Urinary frequency... Other AEs: Thirst (6 patients) Urinary frequency (6 patients) Dry mouth (2 patients) Headache NOS (2 patients) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204441lbl.pdf https://pubmed.ncbi.nlm.nih.gov/17925589
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204441lbl.pdf	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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204441lbl.pdf	Disc. AE: Pollakiuria, Polyuria... AEs leading to discontinuation/dose reduction: Pollakiuria (6.6%) Polyuria (6.6%) Nocturia (6.6%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204441lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204441lbl.pdf	healthy, adult Health Status: healthy Age Group: adult Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204441lbl.pdf	Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204441lbl.pdf
1 mg single, intravenous Dose: 1 mg Route: intravenous Route: single Dose: 1 mg Sources: https://pubmed.ncbi.nlm.nih.gov/22257581	healthy, adult n = 14 Health Status: healthy Age Group: adult Population Size: 14 Sources: https://pubmed.ncbi.nlm.nih.gov/22257581	Sources: https://pubmed.ncbi.nlm.nih.gov/22257581
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204441lbl.pdf	unhealthy Health Status: unhealthy Condition: autosomal dominant polycystic kidney disease Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204441lbl.pdf	Other AEs: Liver injury... Other AEs: Liver injury (serious) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204441lbl.pdf

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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204441lbl.pdf https://pubmed.ncbi.nlm.nih.gov/17925589	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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204441lbl.pdf https://pubmed.ncbi.nlm.nih.gov/17925589
Headache NOS	2 patients	480 mg single, oral Highest studied dose Dose: 480 mg Route: oral Route: single Dose: 480 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204441lbl.pdf https://pubmed.ncbi.nlm.nih.gov/17925589	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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204441lbl.pdf https://pubmed.ncbi.nlm.nih.gov/17925589
Thirst	6 patients	480 mg single, oral Highest studied dose Dose: 480 mg Route: oral Route: single Dose: 480 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204441lbl.pdf https://pubmed.ncbi.nlm.nih.gov/17925589	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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204441lbl.pdf https://pubmed.ncbi.nlm.nih.gov/17925589
Urinary frequency	6 patients	480 mg single, oral Highest studied dose Dose: 480 mg Route: oral Route: single Dose: 480 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204441lbl.pdf https://pubmed.ncbi.nlm.nih.gov/17925589	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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204441lbl.pdf https://pubmed.ncbi.nlm.nih.gov/17925589
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204441lbl.pdf	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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204441lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204441lbl.pdf	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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204441lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204441lbl.pdf	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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204441lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204441lbl.pdf	unhealthy Health Status: unhealthy Condition: autosomal dominant polycystic kidney disease Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204441lbl.pdf

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1709			inhibitor 1599

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
BCRP 691 NTCP 34 BSEP 401 MATE1 304 MATE2 261 MRP2 367 MRP3 157 MRP4 203 OAT1 595 OAT3 636 OATP1B1 781 OATP1B3 700 OCT1 506 OCT2 638 P-gp 1437	P-gp 1527

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
OCT1 523	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/204441Orig1s000ClinPharmR.pdf#page=5 Page: 6.0	yes [IC50 0.837 uM]
P-gp 1626	inhibitor 3240 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
OCT2 639	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/204441Orig1s000ClinPharmR.pdf#page=6 Page: 6.0	yes [IC50 27.2 uM]
OATP1B3 709	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/204441Orig1s000ClinPharmR.pdf#page=5 Page: 6.0	yes [IC50 4.14 uM]
NTCP 35	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/204441Orig1s000ClinPharmR.pdf#page=16 Page: 16.0	yes [IC50 41.5 uM]
OAT3 638	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/204441Orig1s000ClinPharmR.pdf#page=5 Page: 6.0	yes [IC50 5.47 uM]
MRP2 459	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/204441Orig1s000ClinPharmR.pdf#page=5 Page: 6.0	yes [IC50 50 uM]
MRP3 208	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/204441Orig1s000ClinPharmR.pdf#page=5 Page: 6.0	yes [IC50 50 uM]
MRP4 237	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/204441Orig1s000ClinPharmR.pdf#page=5 Page: 6.0	yes [IC50 50 uM]
OATP1B1 796	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/204441Orig1s000ClinPharmR.pdf#page=5 Page: 6.0	yes [IC50 6.15 uM]
MATE1 306	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/204441Orig1s000ClinPharmR.pdf#page=5 Page: 6.0	yes [IC50 7.965 uM]
BCRP 765	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/204441Orig1s000ClinPharmR.pdf#page=6 Page: 6,11	yes [IC50 8.32 uM]
MATE2 261	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/204441Orig1s000ClinPharmR.pdf#page=5 Page: 6.0	yes [IC50 >10 uM]
OAT1 599	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/204441Orig1s000ClinPharmR.pdf#page=5 Page: 6.0	yes [IC50 >30 uM]
BSEP 402	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/204441Orig1s000ClinPharmR.pdf#page=5 Page: 6.0	yes [Ki 34 uM]

Drug as victim

Target	Modality	Activity	Metabolite	Clinical evidence
P-gp 1527	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/204441Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	yes
CYP3A4 1709	substrate 3326 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
hERG 1632	inhibitor 1613 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022275s000_PharmR_P1.pdf#page=31 Page: 31.0

Sourcing

Vendor/Aggregator	ID	URL
001 Chemical	DY526018	https://www.001chemical.com/chem/150683-30-0
AEchem Scientific Corp., USA	AE1-013459	http://www.aechemsc.com/info_products/AE1-013459.php
AK Scientific, Inc. (AKSCI)	66720	http://www.aksci.com/item_detail.php?cat=66720
Achemtek	0102-014531	http://www.achemtek.com/150683-30-0
Acorn PharmaTech	ACN-040195	http://www.acornpharmatech.com/
Alsachim	2932	http://www.alsachim.com/product-C4002-glo.bal-view.html
Ambinter	Amb17620728	http://www.ambinter.com/reference/17620728
Anward	ANW-59865	http://www.anward.com/pro_result/46316
Ark Pharm	AK-33401	http://www.arkpharminc.com/products/150683-30-0.html
AstaTech, Inc.	40033	http://www.astatechinc.com/CPSResult.php?CRNO=39143
Aurora Fine Chemicals LLC	A13.108.065	http://online.aurorafinechemicals.com/info?ID=A13.108.065
AvaChem Scientific	2634	http://www.avachem.com/productSearch.asp?2634
Axon MedChem	1591	https://www.axonmedchem.com/product/1591
BOC Sciences	1246818-18-7	https://www.bocsci.com/tolvaptan-d7-cas-1246818-18-7-item-484313.html
Boerchem	BC650606	http://www.boerchem.com/?product_38814.html
Chem Scene	CS-0572	http://www.chemscene.com/150683-30-0.html
ChemMol	30115910	http://www.chemmol.com/chemmol/30115910.html
ChemMol	44012557	http://www.chemmol.com/chemmol/44012557.html
ChemMol	49400063	http://www.chemmol.com/chemmol/49400063.html
ChemWise	AR60127	http://www.chemwisellc.com/product/tolvaptan-2/
ChemWise	AR60125	http://www.chemwisellc.com/product/tolvaptan/
Chemspace	CSSB00016987605	https://chem-space.com/CSSB00016987605
Clearsynth	CS-O-02900	https://www.clearsynth.com/en/CSO02900.html
Clearsynth	CS-O-31027	https://www.clearsynth.com/en/CSO31027.html
Clearsynth	CS-T-44605	https://www.clearsynth.com/en/CST44605.html
DC Chemicals	DC9148	http://www.dcchemicals.com/product_show-Tolvaptan.html
Finetech	FT-0675288	http://www.finetechnology-ind.com/prod/detail/pub/331947-44-5.html
Finetech	FT-0675287	http://www.finetechnology-ind.com/prod/detail/pub/331947-66-1.html
Hairui	HR120724	http://www.hairuichem.com/en/product/150683-30-0.html
Hefei Hirisun Pharmatech Co., Ltd	HR130551	http://www.hirisunpharm.com/150683-30-0.html
Hello Bio	HB2651	http://www.hellobio.com/4-methylhistamine-dihydrochloride.html
LGC Standards	MM3561.00	https://www.lgcstandards.com/US/en/p/MM3561.00
Lab Network	LN00196860	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN00196860
Matrix Scientific	94534	https://www.matrixscientific.com/094534.html
MedChem Express	HY-17000	https://www.medchemexpress.com/Tolvaptan.html
MolPort	MolPort-008-155-996	https://www.molport.com/shop/molecule-link/MolPort-008-155-996
Molcore	MC526018	https://www.molcore.com/product/150683-30-0
OChem	24490	http://www.ocheminc.com/index.php?act=psearch&pid=683T300
Oakwood	361970	http://www.oakwoodchemical.com/ProductsList.aspx?CategoryID=-2&txtSearch=150823&ExtHyperLink=1
Shanghai Send Pharmaceutical Technology Co., Ltd	send21416	http://shsendpharm.com/
Sigma-Aldrich	T7455_SIGMA	https://www.sigmaaldrich.com/catalog/product/sigma/t7455?utm_source=pubchem&utm_campaign=pubchem_2017&utm_medium=referral
Sun-shine Chemical	Tolvaptan	http://www.sun-shinechem.com/Details/Tolvaptan/2010/150683-30-0.html
Tocris	5181	https://www.tocris.com/products/tolvaptan_5181
TripleBond	CT0200	http://www.triplebond-canada.com/prod/1632/
Yuhao Chemical	RT9638	http://www.chemyuhao.com/150683-30-0.html
abcr GmbH	AB358162	http://www.abcr.com/shop/en/AB358162
eNovation Chemicals	D142062	https://www.enovationchem.com/ProductDetails.asp?ProductID=D142062
iChemical	EBD30732	http://www.ichemical.com/products/150683-30-0.html?utm_source=PubChem&utm_medium=website&utm_campaign=product%20catalogs

PubMed

Title	Date	PubMed

Vasopressin receptor antagonists in heart failure.	2003 Dec	14644024
Gateways to clinical trials.	2003 Nov	14685303
[Heart failure. Can vasopressin antagonists improve the prognosis?].	2003 Nov 27	14724989
Gateways to clinical trials.	2003 Sep	14571286
American Heart Association scientific sessions.	2004 Apr	15102593
Vasopressin receptor antagonists: will the "vaptans" fulfill their promise?	2004 Apr 28	15113822
Combination pharmacologic therapies for heart failure: what next after angiotensin-converting enzyme inhibitors and beta-blockers?	2005 Aug	16036056
New drugs for prevention, relief. How you might benefit if 3 medications win FDA approval.	2005 Oct	16294398
Tolvaptan administration does not affect steady state amiodarone concentrations in patients with cardiac arrhythmias.	2005 Sep	16211205
Vasopressin receptor antagonists: pharmacological tools and potential therapeutic agents.	2006 Apr	16553642
Vasopressin v(2) receptor blockade with tolvaptan versus fluid restriction in the treatment of hyponatremia.	2006 Apr 1	16563917
Gateways to clinical trials.	2006 Jan-Feb	16541195
Hyponatremia and heart failure--treatment considerations.	2006 Jan-Feb	16470095
Vasopressin receptor antagonists.	2006 Jun	16672911
[Diuretics].	2006 May	16689377
Tolvaptan: a selective vasopressin type 2 receptor antagonist in congestive heart failure.	2006 May	16634691
Vasopressin excess and hyponatremia.	2006 May	16632011
Gateways to clinical trials.	2006 Sep	17003851
[Vasopressin antagonists in treatment of hyponatremia].	2007 Aug	18018383
Evaluation and management of hyponatremia: an emerging role for vasopressin receptor antagonists.	2007 Feb	17251996
Nephrogenic syndrome of inappropriate antidiuresis in adults: high phenotypic variability in men and women from a large pedigree.	2007 Feb	17229917
New agents for managing hyponatremia in hospitalized patients.	2007 Feb 1	17244874
[Arginine vasopressin antagonism--new treatment option in chronic heart failure].	2007 Jan 18	17237865
Gateways to clinical trials.	2007 Jan-Feb	17344945
Gateways to clinical trials.	2007 Jul-Aug	17922073
[Recent progress in vasopressin research on cardiovascular diseases].	2007 Jun	17657988
Vaptans: a promising therapy in the management of advanced cirrhosis.	2007 Jun	17445935
Arginine vasopressin receptor antagonists for heart failure: a winter climbing to the Everest's tip?	2007 Jun 5	17543635
Tolvaptan for hyponatremia.	2007 Mar 1	17338053
Tolvaptan for hyponatremia.	2007 Mar 1	17338051
Tolvaptan for hyponatremia.	2007 Mar 1	17329708
Climbing the mountain of acute decompensated heart failure: the EVEREST Trials.	2007 Mar 28	17384439
Effects of nonpeptide vasopressin V2 antagonist tolvaptan in rats with heart failure.	2007 Nov 15	17720144

Patents

Sample Use Guides

In Vivo Use Guide

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

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 `Wed Jul 05 22:56:52 UTC 2023` Edited by `admin` on `Wed Jul 05 22:56:52 UTC 2023`
Record UNII	21G72T1950
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

TOLVAPTAN

Official Name

English

TOLVAPTAN [ORANGE BOOK]

Common Name

English

OPC-41061

Code

English

TOLVAPTAN [MART.]

Common Name

English

JINARC

Brand Name

English

SAMSCA

Brand Name

English

JYNARQUE

Brand Name

English

tolvaptan [INN]

Common Name

English

(±)-4'-((7-CHLORO-2,3,4,5-TETRAHYDRO-5-HYDROXY-1H-1-BENZAZEPIN-1-YL) CARBONYL)-O-TOLU-M-TOLUIDIDE

Common Name

English

OPC-41061(TOLVAPTAN)

Code

English

TOLVAPTAN [EMA EPAR]

Common Name

English

BENZAMIDE, N-(4-((7-CHLORO-2,3,4,5-TETRAHYDRO-5-HYDROXY-1H-1-BENZAZEPIN-1-YL)CARBONYL)-3-METHYLPHENYL)-2-METHYL-

Systematic Name

English

TOLVAPTAN [MI]

Common Name

English

TOLVAPTAN [VANDF]

Common Name

English

TOLVAPTAN [JAN]

Common Name

English

Tolvaptan [WHO-DD]

Common Name

English

TOLVAPTAN [USAN]

Common Name

English

Classification Tree Code System Code

LIVERTOX

NBK548503