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tolbutamide

Trade name: orinase

Small moleculeapproved

Approved

May 31, 1957

Tolbutamide is an oral antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM). It is structurally similar to acetohexamide, chlorpropamide and tolazamide and belongs to the sulfonylurea class of insulin secretagogues, which act by stimulating β cells of the pancreas to release insulin. Sulfonylureas lower blood glucose in patients with NIDDM by directly stimulating the acute release of insulin from functioning beta cells of pancreatic islet tissue by an unknown process that involves a sulfonylurea receptor (receptor 1) on the beta cell. Sulfonylureas inhibit the ATP-potassium channels on the beta cell membrane and potassium efflux, which results in depolarization and calcium influx, calcium-calmodulin binding, kinase activation, and release of insulin-containing granules by exocytosis, an effect similar to that of glucose. — NCATS

Clinical trial activity

17 trials · 19 clinical orgs · 18 marketing orgs

Phase 1
16
Phase 2
0
Phase 3
0
Phase 4
0

Earliest trial started Jan 1, 2003 (NCT00185003)

Timeline

1950s

  1. May 31, 1957

    Pharmacia & Upjohn — Earliest FDA Approval

  2. May 31, 1957

    Pharmacia & Upjohn — NDA Secondary Org

  3. May 31, 1957

    Pharmacia & Upjohn — NDA Organization

1970s

  1. Jul 10, 1974

    Sandoz — NDA Secondary Org

  2. Jan 30, 1979

    Watson Pharmaceuticals — Marketing Organization

  3. Apr 10, 1979

    Mylan — Marketing Organization

  4. Apr 10, 1979

    PHARMOBEDIENT — Marketing Organization

  5. Aug 3, 1979

    Alta Pharma — Marketing Organization

  6. Nov 20, 1979

    Parke-Davis — Marketing Organization

  7. Nov 20, 1979

    Warner Lambert — Marketing Organization

1980s

  1. Feb 5, 1980

    DAVA Pharmaceuticals — Marketing Organization

  2. Mar 25, 1980

    Ivax — Marketing Organization

  3. Mar 25, 1980

    Ani Pharmaceuticals — Marketing Organization

  4. Jun 4, 1980

    Fosun — Marketing Organization

  5. Jun 4, 1980

    Chartwell Pharmaceuticals — Marketing Organization

  6. Feb 20, 1981

    Barr Laboratories — Marketing Organization

  7. Oct 5, 1983

    Ascot Pharmaceuticals — Marketing Organization

  8. Nov 19, 1984

    Superpharm — Marketing Organization

  9. Mar 19, 1985

    Vanguard — Marketing Organization

2000s

  1. Jan 1, 2003

    Earliest Phase 1 Sponsor(trial)

Indications

Approved for

Studied for

Mechanism of action

Approval history

  • approvedPriority reviewMay 31, 1957

Chemistry & pharmacology

Loading structure…

SMILES

CCCCNC(=O)NS(=O)(=O)c1ccc(C)cc1
Mol. weight
270.35 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Achiral Molecule
Inorganic
No
Polymer
No
Delivery
Oral, Parenteral
Availability
Discontinued

Oral

Yes

Parenteral

Yes

Topical

No

Sources

Also known as

  • 1-butyl-3-(p-methylphenylsulfonyl)urea
  • 1-butyl-3-(p-methylphenylsulfonyl)urea
  • 1-butyl-3-(p-tolylsulfonyl)urea
  • 1-butyl-3-(p-tolylsulfonyl)urea
  • 1-butyl-3-tosylurea
  • 1-butyl-3-tosylurea
  • 1-p-toluenesulfonyl-3-butylurea
  • 1-p-toluenesulfonyl-3-butylurea
  • 3-(p-tolyl-4-sulfonyl)-1-butylurea
  • 3-(p-tolyl-4-sulfonyl)-1-butylurea
  • aglicid
  • arkozal
  • glyconon
  • glyconon
  • n-(4-methylbenzenesulfonyl)-n'-butylurea
  • n-(4-methylbenzenesulfonyl)-n'-butylurea
  • n-(4-methylphenylsulfonyl)-n'-butylurea
  • n-(4-methylphenylsulfonyl)-n'-butylurea
  • n-butyl-n'-(4-methylphenylsulfonyl)urea
  • n-butyl-n'-(4-methylphenylsulfonyl)urea
  • n-butyl-n'-p-toluenesulfonylurea
  • n-butyl-n'-p-toluenesulfonylurea
  • n-butyl-n'-(p-tolylsulfonyl)urea
  • n-butyl-n'-(p-tolylsulfonyl)urea
  • n-n-butyl-n'-tosylurea
  • n-n-butyl-n'-tosylurea
  • n-(p-methylbenzenesulfonyl)-n'-butylurea
  • n-(p-methylbenzenesulfonyl)-n'-butylurea
  • n-(sulfonyl-p-methylbenzene)-n'-n-butylurea
  • n-(sulfonyl-p-methylbenzene)-n'-n-butylurea
  • orinase
  • orinase
  • orinase
  • orinase diagnostic
  • orinase diagnostic
  • orinase (tn)
  • orinase (tn)
  • pramidex
  • pramidex
  • rastinon
  • rastinon
  • tolbutamid
  • tolbutamida
  • tolbutamida
  • tolbutamida
  • tolbutamide
  • tolbutamide
  • tolbutamide
  • tolbutamide
  • tolbutamide
  • tolbutamide
  • tolbutamide
  • tolbutamide
  • tolbutamide
  • tolbutamide
  • tolbutamide
  • tolbutamide sodium
  • tolbutamide sodium
  • tolbutamide sodium
  • tolbutamide sodium
  • tolbutamide sodium, sterile
  • tolbutamide sodium, sterile
  • tolbutamide sodium, sterile
  • tolbutamidum
  • tolbutamidum
  • tolumid
  • tolumide
  • tolylsulfonylbutylurea
  • tolylsulfonylbutylurea

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT05097716Phase 1Nov 2, 2021Pfizer
NCT03948243Phase 1Apr 1, 2019Oregon State University, University of Illinois at Chicago
NCT03723395Phase 1Sep 17, 2018Seattle Genetics
NCT03457597Phase 1Mar 6, 2018Corcept Therapeutics
NCT03291288Phase 1Feb 26, 2018Daiichi Sankyo
NCT03716427Phase 1Nov 10, 2016Cognition Therapeutics
NCT02515526N/AJun 1, 2015Umm Al-Qura University, University of Cologne
NCT02473627Phase 1May 1, 2015Daiichi Sankyo
NCT02211079Phase 1Sep 1, 2014Johnson and Johnson
NCT01525628Phase 1Apr 1, 2012Boehringer Ingelheim
NCT01218620Phase 1Sep 1, 2010National Cancer Institute (NCI), University of Wisconsin
NCT01185548Phase 1Jul 1, 2010Eli Lilly
NCT01147887Phase 1Jun 1, 2010Johnson and Johnson
NCT02182401Phase 1Jul 1, 2009Boehringer Ingelheim
NCT00930306Phase 1Jun 1, 2009AstraZeneca, ICON
NCT00369304Phase 1Jul 1, 2006Pfizer, Wyeth
NCT00185003Phase 1Jan 1, 2003Radboud University, ZonMw: The Netherlands Organisation for Health Research and Development
Showing 17 of 17 trials
Page 1 / 1

Organizations

Research & Development (19)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
Boehringer IngelheimFor profit2212009
Daiichi SankyoFor profit2212015
Johnson and JohnsonFor profit2212010
PfizerFor profit2212006
AstraZenecaFor profit1112009
Cognition TherapeuticsFor profit1112016
Corcept TherapeuticsFor profit1112018
Eli LillyFor profit1112010
ICONFor profit1012009
National Cancer Institute (NCI)Government1112010
Oregon State UniversityAcademic/Hospital1012019
Radboud UniversityAcademic/Hospital1112003
Seattle GeneticsFor profit1112018
Umm Al-Qura UniversityAcademic/Hospital1012015
University of CologneAcademic/Hospital1112015
University of Illinois at ChicagoAcademic/Hospital1112019
University of WisconsinAcademic/Hospital1012010
WyethFor profit1012006
ZonMw: The Netherlands Organisation for Health Research and DevelopmentAcademic/Hospital1012003
19 organizations
Page 1 / 1

Marketing (20)

OrganizationOrg typeRelationshipDate
Alta PharmaFor profitMKTGAug 3, 1979
Ani PharmaceuticalsFor profitSYNMar 25, 1980
Ani PharmaceuticalsFor profitMKTGMar 25, 1980
Ascot PharmaceuticalsFor profitMKTGOct 5, 1983
Barr LaboratoriesFor profitMKTGFeb 20, 1981
Chartwell PharmaceuticalsFor profitMKTGJun 4, 1980
DAVA PharmaceuticalsFor profitMKTGFeb 5, 1980
FosunFor profitMKTGJun 4, 1980
IvaxFor profitMKTGMar 25, 1980
MylanFor profitMKTGApr 10, 1979
PHARMOBEDIENTFor profitMKTGApr 10, 1979
Parke-DavisFor profitMKTGNov 20, 1979
Pharmacia & UpjohnFor profitNDA2May 31, 1957
Pharmacia & UpjohnFor profitNDAMay 31, 1957
Puracap PharmaceuticalFor profitMKTG—
SandozFor profitNDA2Jul 10, 1974
SuperpharmFor profitMKTGNov 19, 1984
VanguardFor profitMKTGMar 19, 1985
Warner LambertFor profitMKTGNov 20, 1979
Watson PharmaceuticalsFor profitMKTGJan 30, 1979