Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C19H18F6N4O3 |
| Molecular Weight | 464.3616 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
COC(=O)C1=C2CN(CCN2C(=N1)C(F)(F)F)C(=O)C[C@H](N)CC3=C(F)C=C(F)C(F)=C3
InChI
InChIKey=WIIAMRXFUJLYEF-SNVBAGLBSA-N
InChI=1S/C19H18F6N4O3/c1-32-17(31)16-14-8-28(2-3-29(14)18(27-16)19(23,24)25)15(30)6-10(26)4-9-5-12(21)13(22)7-11(9)20/h5,7,10H,2-4,6,8,26H2,1H3/t10-/m1/s1
| Molecular Formula | C19H18F6N4O3 |
| Molecular Weight | 464.3616 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
SP-2086 H3PO4 (Retagliptin Phosphate), tetrahydro-imidazo[1,5-a] pyrazine
derivative, is a competitive DPP-4 inhibitor innovated in China under development by Jiangsu Hengrui Medicine for the treatment of Type 2 diabetes. In completed phase II trials, retagliptin monotherapy or in combination with metformin significantly decreased the HbA1c level in type 2 diabetic patients. Two phase III trials for retagliptin monotherapy aCnd in combination with metformin, respectively, were ongoing in China. Jiangsu Hengrui Medicine withdrew its application from the Chinese
FDA in April 2016 but is expected to refile the application.
Originator
Approval Year
Sample Use Guides
The dosage of phosphate retagliptin tablet is recommended at 100 mg/d for patients with normal renal function and those with mild renal dysfunction,at 50 mg/d for patients with moderate renal dysfunction,and at 25 mg/d for patients with severe renal dysfunction.
Route of Administration:
Oral
| Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 16:07:32 GMT 2023
by
admin
on
Fri Dec 15 16:07:32 GMT 2023
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| Record UNII |
328C4R3P9L
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| Record Status |
Validated (UNII)
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| Record Version |
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ACTIVE MOIETY |
Official Title: the Pharmacokinetics,Pharmacodynamics,Safety and Tolerability Study Following Single and Multiple Dose of SP2086 in Type 2 Diabetes Patients
Purpose: SP2086 is a novel inhibitor of Dipeptide base peptidase 4, allows an insulin-independent approach to improve type 2 diabetes hyperglycemia. In this single-dose and multiple-dose study the investigators evaluated the safety, tolerability and PK/PD profiles of SP2086 in Type 2 Diabetes Patients.
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