saccharin

Small moleculeexperimental

Saccharin is the most established of the artificial sweeteners on the market, this mixture of dextrose and saccharin has been in use for over a century and is found in diet versions of soft drinks. It is 300-500 times sweeter than sugar and contains zero calories. In 1977, the FDA tried to ban its use after evidence showed it caused cancer in rats. Extensive lobbying by the diet food industry allowed products to stay on the shelves as long as they carried warnings about the cancer risks in animals. This warning was removed in 2001 when the Calorie Control Council insisted the link between animal and human cancers could not automatically be made. Consumption of saccharin-sweetened products can benefit diabetics as the substance goes directly through the human digestive system without being digested. While saccharin has no food energy, it can trigger the release of insulin in humans due to its sweet taste. The T1R2/R3 sweet taste receptor exist on the surface of pancreatic beta cells. Saccharin is a unique in that it inhibits glucose-stimulated insulin secretion (GSIS) at submaximal and maximal glucose concentrations, with the other sweeteners having no effect. Investigation of saccharin’s dose-response characteristics showed that concentrations of 0.1 and 0.5 mM stimulated insulin secretion, while concentrations of 1 and 2.5 mM inhibited insulin secretion. Saccharin’s effect on insulin secretion was shown to be reversible in INS-1 832/13 clonal pancreatic beta cells after chronic exposure to 1 mM saccharin. Artificial sweeteners may affect insulin secretion via interaction with the sweet taste receptor, also saccharin may affect other cellular processes linked to insulin secretion, and that these effects are both time- and concentration-dependent — NCATS

Clinical trial activity

6 trials · 7 clinical orgs · 0 marketing orgs

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

Earliest trial started Sep 1, 2013 (NCT01488383)

Timeline

2010s

  1. Jan 1, 2015

    Earliest Phase 3 Sponsor(trial)

Indications

Mechanism of action

  • Unspecified targetUnclear

    unclear

Chemistry & pharmacology

Loading structure…

SMILES

O=C1NS(=O)(=O)C2=CC=CC=C12
Mol. weight
183.185 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Achiral Molecule
Inorganic
No
Polymer
No

Oral

No

Parenteral

No

Topical

No

Sources

Also known as

  • benzosulfinide
  • benzosulfinide
  • benzosulphinide
  • benzosulphinide
  • e954
  • e954
  • gluside
  • gluside
  • saccharin
  • saccharin
  • saccharin
  • saccharin
  • saccharin
  • saccharin sodium
  • saccharin sodium dihydrate
  • saccharin sodium salt hydrate
  • sodium saccharin
  • sodium saccharin
  • sweeta
  • sweeta

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT06330636N/ASep 11, 2023University of Nottingham
NCT04578431N/ANov 1, 2020Aarhus University
NCT03954418N/AJun 1, 2019Aarhus University
NCT03032640N/AJan 26, 2017Advent Health, Translational Research Institute for Metabolism and Diabetes, Florida
NCT02318446Phase 3Mar 1, 2015Maharashtra University of Health Sciences, SMT KASHIBAI NAVALE MEDICAL COLLEGE
NCT01488383N/ASep 1, 2013Government of Spain
Showing 6 of 6 trials
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Organizations

Research & Development (7)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
Aarhus UniversityAcademic/Hospital2212019
Advent HealthAcademic/Hospital1112017
Government of SpainGovernment1112013
Maharashtra University of Health SciencesAcademic/Hospital1112015
SMT KASHIBAI NAVALE MEDICAL COLLEGEAcademic/Hospital1012015
Translational Research Institute for Metabolism and Diabetes, FloridaAcademic/Hospital1012017
University of NottinghamAcademic/Hospital1112023
7 organizations
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