Chemical Property of SYR-472
Chemical Property:
- Appearance/Colour:White to off-white solid
- PSA：171.65000
- LogP:1.23468
- Storage Temp.:-20°C
- Purity/Quality:
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99%min *data from raw suppliers
Trelagliptinsuccinate >98% *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
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SDS file from LookChem
Useful:
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Description
Similar to omarigliptin,
trelagliptin succinate (XIX) is a highly selective, orally
delivered inhibitor of DPP-4 developed by Takeda Pharmaceuticals
and approved in Japan in March 2015 for the
treatment of type 2 DM. Interestingly, trelagliptin is
structurally similar to alogliptin, a DPP-4 inhibitor also
marketed by Takeda and described in our 2010 review,
differing only in the presence of a fluorine in the 5-position of
the cyanobenzyl moiety. Both trelagliptin and alogliptin are
potent inhibitors of DPP-4, with IC50s of 1.3 and 5.3 nM,
respectively. Notably, while similar drugs are dosed once
daily, trelagliptin is the first DPP-4 inhibitor approved for onceweekly
dosing. Kinetic analysis has revealed that trelagliptin is a
substrate-competitive, reversible, slow-binding inhibitor (t1/2 for
dissociation = ca. 30 min) of DPP-4, although the dissociation
time is insufficient to explain its long-acting effects. In a phase
III trial, once-weekly trelagliptin (100 mg) showed similar
efficacy and safety to once-daily alogliptin (25 mg) in patients
with type 2 DM inadequately controlled by diet and exercise.
The medicinal chemistry discovery of trelagliptin and
alogliptin as well as reviews of this class of compounds
have been published.
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Uses
Trelagliptin succinate (SYR-472) is a selective, long acting dipeptidyl peptidase-4 (DPP-4) inhibitor. An antidiabetic agent.
Orally active DPP-4 inhibitor that produces clinically and statistically significant improvements in glycaemic control in patients with type 2 diabetes. SYR472 has a long duration of action and is well tolerated in clinical studies.
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Clinical Use
Trelagliptin (SYR-472), a novel dipeptidyl peptidase-4 inhibitor used for the treatment of type 2 diabetes mellitus. Trelagliptin (as the salt Trelagliptin succinate) was approved for use in Japan in March 2015. Takeda, the company that developed Trelagliptin, chose to not get approval for the drug in the USA and EU.
