Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C17H20F2N4O3S |
| Molecular Weight | 398.428 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 3 / 3 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CS(=O)(=O)N1C=C2CN(CC2=N1)[C@H]3CO[C@@H]([C@@H](N)C3)C4=C(F)C=CC(F)=C4
InChI
InChIKey=MKMPWKUAHLTIBJ-ISTRZQFTSA-N
InChI=1S/C17H20F2N4O3S/c1-27(24,25)23-7-10-6-22(8-16(10)21-23)12-5-15(20)17(26-9-12)13-4-11(18)2-3-14(13)19/h2-4,7,12,15,17H,5-6,8-9,20H2,1H3/t12-,15+,17-/m1/s1
Omarigliptin is a new once-weekly dipeptidyl peptidase-4 (DPP-4) inhibitor developed for the treatment of type 2 diabetes. It potently but reversibly inhibits DPP-4 enzyme, which prolongs the circulating half-life of glucagon-like peptide-1 that increases insulin secretion in a glucose-dependent manner. Benefiting from glucose-dependent insulin secretion, omarigliptin is associated with low risk of hypoglycemia. Marizev (omarigliptin) 25 mg and 12.5 mg tablets were approved by Japan's Pharmaceuticals and Medical Devices Agency (PMDA) on 28th Sept 2015. Japan was the first country to have approved omarigliptin.
Originator
Approval Year
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
549 nM |
25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
523 nM |
25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: HIGH-FAT |
|
141.51 nM |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
749.54 nM |
25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
2709.59 nM |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
297.84 nM |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
1712.32 nM |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
223.03 nM |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
15.66 nM |
1 mg 1 times / week multiple, oral dose: 1 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
21.25 nM |
1 mg 1 times / week multiple, oral dose: 1 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
236.65 nM |
10 mg 1 times / week multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
278.21 nM |
10 mg 1 times / week multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
802.6 nM |
25 mg 1 times / week multiple, oral dose: 25 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
700.63 nM |
25 mg 1 times / week multiple, oral dose: 25 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
1083.59 nM |
50 mg 1 times / week multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
1305.97 nM |
50 mg 1 times / week multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
6.45 nM |
0.5 mg single, oral dose: 0.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
20.7 nM |
1.5 mg single, oral dose: 1.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
88.2 nM |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
219 nM |
12.5 mg single, oral dose: 12.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
484 nM |
25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
904 nM |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
2210 nM |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
3850 nM |
200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
9290 nM |
400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
206 nM |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
195 nM |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
184 nM |
10 mg 1 times / week multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
195 nM |
10 mg 1 times / week multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
610 nM |
25 mg 1 times / week multiple, oral dose: 25 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
565 nM |
25 mg 1 times / week multiple, oral dose: 25 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
988 nM |
50 mg 1 times / week multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
1080 nM |
50 mg 1 times / week multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
2320 nM |
100 mg 1 times / week multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
2400 nM |
100 mg 1 times / week multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
60.4 nM |
3 mg single, oral dose: 3 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
61.4 nM |
3 mg single, oral dose: 3 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
48.7 nM |
3 mg single, oral dose: 3 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
41.4 nM |
3 mg single, oral dose: 3 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
41 nM |
3 mg single, oral dose: 3 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
56.1 nM |
3 mg single, oral dose: 3 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
572 nM |
25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
554 nM |
25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
22.7 μM × h |
25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
23 μM × h |
25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: HIGH-FAT |
|
5.34 μM × h |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
23.81 μM × h |
25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
94.63 μM × h |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
9.07 μM × h |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
48.66 μM × h |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
8.75 μM × h |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
1.03 μM × h |
1 mg 1 times / week multiple, oral dose: 1 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
1.4 μM × h |
1 mg 1 times / week multiple, oral dose: 1 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
8.92 μM × h |
10 mg 1 times / week multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
9.75 μM × h |
10 mg 1 times / week multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
21.19 μM × h |
25 mg 1 times / week multiple, oral dose: 25 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
22.31 μM × h |
25 mg 1 times / week multiple, oral dose: 25 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
40.32 μM × h |
50 mg 1 times / week multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
41.56 μM × h |
50 mg 1 times / week multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
0.147 μM × h |
0.5 mg single, oral dose: 0.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
1.2 μM × h |
1.5 mg single, oral dose: 1.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
4.13 μM × h |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
10.6 μM × h |
12.5 mg single, oral dose: 12.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
20.9 μM × h |
25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
39.4 μM × h |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
82.5 μM × h |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
155 μM × h |
200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
323 μM × h |
400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
9.59 μM × h |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
9.99 μM × h |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
7.37 μM × h |
10 mg 1 times / week multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
8.76 μM × h |
10 mg 1 times / week multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
22 μM × h |
25 mg 1 times / week multiple, oral dose: 25 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
22 μM × h |
25 mg 1 times / week multiple, oral dose: 25 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
40.7 μM × h |
50 mg 1 times / week multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
47.8 μM × h |
50 mg 1 times / week multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
82.3 μM × h |
100 mg 1 times / week multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
87.8 μM × h |
100 mg 1 times / week multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
3055 nM × h |
3 mg single, oral dose: 3 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
3675 nM × h |
3 mg single, oral dose: 3 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
3580 nM × h |
3 mg single, oral dose: 3 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
3352 nM × h |
3 mg single, oral dose: 3 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
3151 nM × h |
3 mg single, oral dose: 3 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
2432 nM × h |
3 mg single, oral dose: 3 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
22.4 μM × h |
25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
23.8 μM × h |
25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
46.8 h |
25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
46 h |
25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: HIGH-FAT |
|
66.65 h |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
38.89 h |
25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
43.41 h |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
49.91 h |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
33.43 h |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
89.45 h |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
144.88 h |
1 mg 1 times / week multiple, oral dose: 1 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
143.52 h |
10 mg 1 times / week multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
82.48 h |
25 mg 1 times / week multiple, oral dose: 25 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
73.73 h |
50 mg 1 times / week multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
93.3 h |
1.5 mg single, oral dose: 1.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
115.94 h |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
68.88 h |
12.5 mg single, oral dose: 12.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
49.52 h |
25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
47.65 h |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
42.62 h |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
45.19 h |
200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
42.45 h |
400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
119.59 h |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
98.22 h |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
83.18 h |
10 mg 1 times / week multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
66.74 h |
25 mg 1 times / week multiple, oral dose: 25 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
48.3 h |
50 mg 1 times / week multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
41.74 h |
100 mg 1 times / week multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
148 h |
3 mg single, oral dose: 3 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
156 h |
3 mg single, oral dose: 3 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
160 h |
3 mg single, oral dose: 3 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
215 h |
3 mg single, oral dose: 3 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
264 h |
3 mg single, oral dose: 3 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
163 h |
3 mg single, oral dose: 3 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
34.6 h |
25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
34.5 h |
25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered: |
OMARIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
24% |
OMARIGLIPTIN plasma | Homo sapiens |
Doses
AEs
Sample Use Guides
For adults, take 2 tablets (25 mg of the active ingredient) at a time, once a week. If you are a patient with severe or end stage renal dysfunction, take 1 tablet (12.5 mg) at a time, once a week.
Route of Administration:
Oral
Omarigliptin is a competitive, reversible inhibitor of DPP-4
(IC50 = 1.6 nM, Ki = 0.8 nM) and is more potent than
sitagliptin (IC50 = 18 nM). It is highly selective over all
proteases tested (IC50 > 67 uM), including QPP, FAP, PEP,
DPP8, and DPP9. The compound has weak ion channel activity
(IC50 > 30 uM at IKr, Cav1.2, and Nav1.5). An expansive
selectivity counterscreen (168 radioligand binding or enzymatic
assays) was carried out at MDS Pharma. An IC50 > 10 uM was
obtained in all assays.
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ACTIVE MOIETY
