New-Generation Glucokinase Activators: Potential Game-Changers in Type 2 Diabetes Treatment
Achieving glycemic control and sustaining functional pancreatic β-cell activity remains an unmet medical need in the treatment of type 2 diabetes mellitus (T2DM). Glucokinase activators (GKAs) constitute a class of anti-diabetic drugs designed to regulate blood sugar levels and enhance β-cell functi...
| Main Authors: | , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2024-01-01
|
| Series: | International Journal of Molecular Sciences |
| Subjects: | |
| Online Access: | https://www.mdpi.com/1422-0067/25/1/571 |
| _version_ | 1797358666372874240 |
|---|---|
| author | Dania Haddad Vanessa Sybil Dsouza Fahd Al-Mulla Ashraf Al Madhoun |
| author_facet | Dania Haddad Vanessa Sybil Dsouza Fahd Al-Mulla Ashraf Al Madhoun |
| author_sort | Dania Haddad |
| collection | DOAJ |
| description | Achieving glycemic control and sustaining functional pancreatic β-cell activity remains an unmet medical need in the treatment of type 2 diabetes mellitus (T2DM). Glucokinase activators (GKAs) constitute a class of anti-diabetic drugs designed to regulate blood sugar levels and enhance β-cell function in patients with diabetes. A significant progression in GKA development is underway to address the limitations of earlier generations. Dorzagliatin, a dual-acting GKA, targets both the liver and pancreas and has successfully completed two phase III trials, demonstrating favorable results in diabetes treatment. The hepato-selective GKA, TTP399, emerges as a strong contender, displaying clinically noteworthy outcomes with minimal adverse effects. This paper seeks to review the current literature, delve into the mechanisms of action of these new-generation GKAs, and assess their efficacy and safety in treating T2DM based on published preclinical studies and recent clinical trials. |
| first_indexed | 2024-03-08T15:04:40Z |
| format | Article |
| id | doaj.art-72ee2883bf614deaa9fce5eb1246a85c |
| institution | Directory Open Access Journal |
| issn | 1661-6596 1422-0067 |
| language | English |
| last_indexed | 2024-03-08T15:04:40Z |
| publishDate | 2024-01-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | International Journal of Molecular Sciences |
| spelling | doaj.art-72ee2883bf614deaa9fce5eb1246a85c2024-01-10T15:00:03ZengMDPI AGInternational Journal of Molecular Sciences1661-65961422-00672024-01-0125157110.3390/ijms25010571New-Generation Glucokinase Activators: Potential Game-Changers in Type 2 Diabetes TreatmentDania Haddad0Vanessa Sybil Dsouza1Fahd Al-Mulla2Ashraf Al Madhoun3Genetics and Bioinformatics Department, Dasman Diabetes Institute, Dasman 15462, KuwaitGenetics and Bioinformatics Department, Dasman Diabetes Institute, Dasman 15462, KuwaitGenetics and Bioinformatics Department, Dasman Diabetes Institute, Dasman 15462, KuwaitGenetics and Bioinformatics Department, Dasman Diabetes Institute, Dasman 15462, KuwaitAchieving glycemic control and sustaining functional pancreatic β-cell activity remains an unmet medical need in the treatment of type 2 diabetes mellitus (T2DM). Glucokinase activators (GKAs) constitute a class of anti-diabetic drugs designed to regulate blood sugar levels and enhance β-cell function in patients with diabetes. A significant progression in GKA development is underway to address the limitations of earlier generations. Dorzagliatin, a dual-acting GKA, targets both the liver and pancreas and has successfully completed two phase III trials, demonstrating favorable results in diabetes treatment. The hepato-selective GKA, TTP399, emerges as a strong contender, displaying clinically noteworthy outcomes with minimal adverse effects. This paper seeks to review the current literature, delve into the mechanisms of action of these new-generation GKAs, and assess their efficacy and safety in treating T2DM based on published preclinical studies and recent clinical trials.https://www.mdpi.com/1422-0067/25/1/571dorzagliatinTTP399glucokinase activatortype 2 diabetesclinical trialssafety |
| spellingShingle | Dania Haddad Vanessa Sybil Dsouza Fahd Al-Mulla Ashraf Al Madhoun New-Generation Glucokinase Activators: Potential Game-Changers in Type 2 Diabetes Treatment International Journal of Molecular Sciences dorzagliatin TTP399 glucokinase activator type 2 diabetes clinical trials safety |
| title | New-Generation Glucokinase Activators: Potential Game-Changers in Type 2 Diabetes Treatment |
| title_full | New-Generation Glucokinase Activators: Potential Game-Changers in Type 2 Diabetes Treatment |
| title_fullStr | New-Generation Glucokinase Activators: Potential Game-Changers in Type 2 Diabetes Treatment |
| title_full_unstemmed | New-Generation Glucokinase Activators: Potential Game-Changers in Type 2 Diabetes Treatment |
| title_short | New-Generation Glucokinase Activators: Potential Game-Changers in Type 2 Diabetes Treatment |
| title_sort | new generation glucokinase activators potential game changers in type 2 diabetes treatment |
| topic | dorzagliatin TTP399 glucokinase activator type 2 diabetes clinical trials safety |
| url | https://www.mdpi.com/1422-0067/25/1/571 |
| work_keys_str_mv | AT daniahaddad newgenerationglucokinaseactivatorspotentialgamechangersintype2diabetestreatment AT vanessasybildsouza newgenerationglucokinaseactivatorspotentialgamechangersintype2diabetestreatment AT fahdalmulla newgenerationglucokinaseactivatorspotentialgamechangersintype2diabetestreatment AT ashrafalmadhoun newgenerationglucokinaseactivatorspotentialgamechangersintype2diabetestreatment |