Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C19H26F3N3O3 |
Molecular Weight | 401.4232 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)(C)OC[C@H]1N(CCNC1=O)C(=O)C[C@H](N)CC2=C(F)C=C(F)C(F)=C2
InChI
InChIKey=LCDDAGSJHKEABN-MLGOLLRUSA-N
InChI=1S/C19H26F3N3O3/c1-19(2,3)28-10-16-18(27)24-4-5-25(16)17(26)8-12(23)6-11-7-14(21)15(22)9-13(11)20/h7,9,12,16H,4-6,8,10,23H2,1-3H3,(H,24,27)/t12-,16-/m1/s1
Evogliptin (Suganon) is an orally bioavailable, selective dipeptidyl peptidase-4 (DPP-4; CD26 antigen) inhibitor being developed by Dong-A ST for the treatment of type 2 diabetes mellitus. Evogliptin was approved in South Korea on 2 October 2015 for blood
glucose lowering in patients with type 2 diabetes mellitus
inadequately controlled by diet and exercise alone or by
metformin plus diet and exercise. In July 2015, Dong-A ST signed a licensing out agreement
for evogliptin with Geropharm for Russia, Ukraine and
Kazakhstan markets. In April 2015, Dong-A ST
signed a licensing agreement with Eurofarma Laboratorios of
Brazil for 17 Latin America countries including Mexico. Evogliptin is a potent DPP-4 inhibitor with a 50 %
inhibitory concentration (IC50) against soluble human
DPP-4 of 0.98 nmol/L and an IC50 of 1.26 nmol/L against
membrane-bound human DPP-4. It displayed
6000-fold higher potency for human DPP-4 than for human
DPP-8 and DPP-9, and 20,000-fold greater potency
for DPP-4 than for DPP-1, DPP-2 and other closely-related
enzymes. Evogliptin is effective in improving glycosylated hemoglobin (HbA1c) and fasting plasma glucose without inducing hypoglycemia events, which potentially can improve adherence and prevent complications. It is also found that evogliptin has benefits on insulin secretory and β-cell functions. Based on the current clinical data, evogliptin has a neutral effect on body weight. These attributes contribute to the clinical practice in monotherapy or in combination with other antidiabetic agents. Evogliptin was generally well tolerated in clinical trials.
Originator
Approval Year
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/26541763
The recommended dosage of oral evogliptin is 5 mg
once daily without regard to food. Dosage adjustment
is not required in patients with renal impairment and the
drug has a low potential for interaction with other concurrently administered drugs
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/26541763
Evogliptin is a potent DPP-4 inhibitor with a 50 %
inhibitory concentration (IC50) against soluble human
DPP-4 of 0.98 nmol/L and an IC50 of 1.26 nmol/L against
membrane-bound human DPP-4. It displayed
6000-fold higher potency for human DPP-4 than for human
DPP-8 and DPP-9, and 20,000-fold greater potency
for DPP-4 than for DPP-1, DPP-2 and other closely-related
enzymes.
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A10BH07
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A10BD22
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C171769
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DTXSID00153545
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Evogliptin
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1222102-29-5
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DB12625
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ACTIVE MOIETY