Trelagliptin
Trelagliptin (SYR-472) is a selective inhibitor of DPP-4 and is developed for the treatment of type 2 diabetes mellitus (T2DM) [1].
Dipeptidyl peptidase (DPP)-4 also known as adenosine deaminase complexing protein 2 or CD26 is an antigenic enzyme that expressed on the surface of most cell types and plays an important role in regulating immune system, signal transduction and apoptosis [2, 3].
Trelagliptin (SYR-472) is a potent DPP-4 inhibitor and can be administered once weekly which unlike its other class approved agents that be taken once daily [1]. In Japan, clinical trials had been conducted to detect the effectiveness of Trelagliptin by comparing with the approved medicine—alogliptin and it was shown that Trelagliptin once-weekly exhibited similar efficacy and safety to alogliptin once daily, which indicated that Trelagliptin could be a useful new antidiabetes drug that needs to be given once a week [2].
Trelagliptin (SYR-472) has been used in phase 2 and phase 3 clinical trials for the treatment of patients with T2DM showed similar efficacy and safety to alogliptin once daily and produced clinically and statistically significant improvements in glycaemic control with well tolerated in Japan [2, 3].
References:
[1]. McKeage, K., Trelagliptin: First Global Approval. Drugs, 2015. 75(10): p. 1161-4.
[2]. Inagaki, N., et al., Once-weekly trelagliptin versus daily alogliptin in Japanese patients with type 2 diabetes: a randomised, double-blind, phase 3, non-inferiority study. Lancet Diabetes Endocrinol, 2015. 3(3): p. 191-7.
[3]. Inagaki, N., et al., SYR-472, a novel once-weekly dipeptidyl peptidase-4 (DPP-4) inhibitor, in type 2 diabetes mellitus: a phase 2, randomised, double-blind, placebo-controlled trial. Lancet Diabetes Endocrinol, 2014. 2(2): p. 125-32.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 357.38 |
Cas No. | 865759-25-7 |
Formula | C18H20FN5O2 |
Synonyms | SYR-472,SYR472,SYR 472,Trelagliptin |
Solubility | ≥11.6 mg/mL in DMSO; ≥3.68 mg/mL in EtOH with gentle warming and ultrasonic; ≥93.8 mg/mL in H2O |
Chemical Name | 2-[[6-[(3R)-3-aminopiperidin-1-yl]-3-methyl-2,4-dioxopyrimidin-1-yl]methyl]-4-fluorobenzonitrile |
SDF | Download SDF |
Canonical SMILES | CN1C(=O)C=C(N(C1=O)CC2=C(C=CC(=C2)F)C#N)N3CCCC(C3)N |
Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Description | Trelagliptin is a long acting inhibitor of dipeptidyl peptidase-4 (DPP-4). | |||||
Targets | DPP-4 | |||||
IC50 |
Quality Control & MSDS
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