saccharin
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
Earliest trial started Sep 1, 2013 (NCT01488383)
Timeline
2010s
- Jan 1, 2015
Earliest Phase 3 Sponsor(trial)
Indications
Studied for
Mechanism of action
- Unspecified targetUnclear
unclear
Chemistry & pharmacology
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
- WikipediaSaccharin ↗
- NCATSFST467XS7D ↗
- ChEMBLCHEMBL310671 ↗
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 ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT06330636 | N/A | Sep 11, 2023 | University of Nottingham |
| NCT04578431 | N/A | Nov 1, 2020 | Aarhus University |
| NCT03954418 | N/A | Jun 1, 2019 | Aarhus University |
| NCT03032640 | N/A | Jan 26, 2017 | Advent Health, Translational Research Institute for Metabolism and Diabetes, Florida |
| NCT02318446 | Phase 3 | Mar 1, 2015 | Maharashtra University of Health Sciences, SMT KASHIBAI NAVALE MEDICAL COLLEGE |
| NCT01488383 | N/A | Sep 1, 2013 | Government of Spain |
Organizations
Research & Development (7)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Aarhus University | Academic/Hospital | 2 | 2 | 1 | 2019 |
| Advent Health | Academic/Hospital | 1 | 1 | 1 | 2017 |
| Government of Spain | Government | 1 | 1 | 1 | 2013 |
| Maharashtra University of Health Sciences | Academic/Hospital | 1 | 1 | 1 | 2015 |
| SMT KASHIBAI NAVALE MEDICAL COLLEGE | Academic/Hospital | 1 | 0 | 1 | 2015 |
| Translational Research Institute for Metabolism and Diabetes, Florida | Academic/Hospital | 1 | 0 | 1 | 2017 |
| University of Nottingham | Academic/Hospital | 1 | 1 | 1 | 2023 |