Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C21H21FO5S |
| Molecular Weight | 404.452 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 5 / 5 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
OC[C@H]1O[C@H]([C@H](O)[C@@H](O)[C@@H]1O)C2=CC(CC3=CC4=C(S3)C=CC=C4)=C(F)C=C2
InChI
InChIKey=AHFWIQIYAXSLBA-RQXATKFSSA-N
InChI=1S/C21H21FO5S/c22-15-6-5-12(21-20(26)19(25)18(24)16(10-23)27-21)7-13(15)9-14-8-11-3-1-2-4-17(11)28-14/h1-8,16,18-21,23-26H,9-10H2/t16-,18-,19+,20-,21+/m1/s1
| Molecular Formula | C21H21FO5S |
| Molecular Weight | 404.452 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 5 / 5 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
Ipragliflozin L-proline is a sodium-glucose cotransporter 2 (SGLT2) inhibitor. It was developed and marketed as Suglat® by Astellas cooperating with Kotobuki Pharmaceutical and Merck Sharp & Dohme, and approved by Pharmaceuticals and Medical Devices Agency of Japan (PMDA) on Jan 17, 2014. It is indicated for the treatment of type 2 diabetes.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL3884 Sources: https://www.ncbi.nlm.nih.gov/pubmed/22507206 |
7.38 nM [IC50] | ||
Target ID: CHEMBL3884 Sources: https://www.ncbi.nlm.nih.gov/pubmed/22507206 |
7.38 nM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | SUGLAT Approved UseIpragliflozin L-proline is indicated for the treatment of type 2 diabetes. Launch Date2014 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
17.89 ng/mL |
1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
53.72 ng/mL |
3 mg single, oral dose: 3 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
174.34 ng/mL |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
523.63 ng/mL |
30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
1392.39 ng/mL |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
3421.41 ng/mL |
300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
398.05 ng/mL |
20 mg 1 times / day steady-state, oral dose: 20 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
975.53 ng/mL |
50 mg 1 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
1731.61 ng/mL |
100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
1174.67 ng/mL |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
1464.17 ng/mL |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
976.32 ng/mL |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
1260.674 ng/mL |
100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
1690.752 ng/mL |
100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED |
|
1491.293 ng/mL |
100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
1975.718 ng/mL |
100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED |
|
1592.925 ng/mL |
100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
1676.536 ng/mL |
100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED |
|
1584.996 ng/mL |
100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
2124.083 ng/mL |
100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED |
|
1044.74 mg/mL |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
1088.77 mg/mL |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
1160.97 mg/mL |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
1277.19 ng/mL |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
1456.05 ng/mL |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
1625.63 ng/mL |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
1448.14 ng/mL |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
1576.08 ng/mL |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
1397.58 ng/mL |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
1761.06 ng/mL |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
58.94 ng × h/mL |
1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
244.64 ng × h/mL |
3 mg single, oral dose: 3 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
855.06 ng × h/mL |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
2895.83 ng × h/mL |
30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
9696.47 ng × h/mL |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
27298.54 ng × h/mL |
300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
1894.04 ng × h/mL |
20 mg 1 times / day steady-state, oral dose: 20 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
4693.11 ng × h/mL |
50 mg 1 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
9113.99 ng × h/mL |
100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
5238.53 ng × h/mL |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
5490.74 ng × h/mL |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
5291.35 ng × h/mL |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
8519.799 ng × h/mL |
100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
9844.079 ng × h/mL |
100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED |
|
10325.042 ng × h/mL |
100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
13772.018 ng × h/mL |
100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED |
|
8231.224 ng × h/mL |
100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
9582.693 ng × h/mL |
100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED |
|
10050.118 ng × h/mL |
100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
14027.041 ng × h/mL |
100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED |
|
4821.35 ng × h/mL |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
4482.28 ng × h/mL |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
5947.6 ng × h/mL |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
7325.78 ng × h/mL |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
8240.8 ng × h/mL |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
10506.14 ng × h/mL |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
12103.73 ng × h/mL |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
12687.14 ng × h/mL |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
9103.55 ng × h/mL |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
11814.32 ng × h/mL |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
4.35 h |
1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
10.01 h |
3 mg single, oral dose: 3 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
13.34 h |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
12.43 h |
30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
11.71 h |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
10.34 h |
300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
13.93 h |
20 mg 1 times / day steady-state, oral dose: 20 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
11.24 h |
50 mg 1 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
15.36 h |
100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
13.67 h |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
16.9 h |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
17 h |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
15.046 h |
100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
17.93 h |
100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED |
|
15.234 h |
100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
15.568 h |
100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED |
|
16.717 h |
100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
23.654 h |
100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED |
|
16.798 h |
100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
20.292 h |
100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED |
|
14.97 h |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
15.37 h |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
17.08 h |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
15.18 h |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
19.16 h |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
20.56 h |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
20.76 h |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
21.22 h |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
16.18 h |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
15.78 h |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
IPRAGLIFLOZIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
3.5% |
IPRAGLIFLOZIN plasma | Homo sapiens |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Efficacy, safety, and tolerability of ipragliflozin in Asian patients with type 2 diabetes mellitus and inadequate glycemic control with metformin: Results of a phase 3 randomized, placebo-controlled, double-blind, multicenter trial. | 2016-05 |
|
| Efficacy and safety of ipragliflozin in patients with type 2 diabetes inadequately controlled on metformin: a dose-finding study. | 2013-05 |
|
| Inhibition of the sodium glucose co-transporter-2: its beneficial action and potential combination therapy for type 2 diabetes mellitus. | 2013-05 |
|
| No pharmacokinetic interaction between ipragliflozin and sitagliptin, pioglitazone, or glimepiride in healthy subjects. | 2012-10 |
|
| Active- and placebo-controlled dose-finding study to assess the efficacy, safety, and tolerability of multiple doses of ipragliflozin in patients with type 2 diabetes mellitus. | 2012-08-14 |
|
| Combination treatment with ipragliflozin and metformin: a randomized, double-blind, placebo-controlled study in patients with type 2 diabetes mellitus. | 2012-08 |
|
| Discovery of Ipragliflozin (ASP1941): a novel C-glucoside with benzothiophene structure as a potent and selective sodium glucose co-transporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes mellitus. | 2012-05-15 |
|
| Pharmacological profile of ipragliflozin (ASP1941), a novel selective SGLT2 inhibitor, in vitro and in vivo. | 2012-04 |
|
| Antidiabetic effects of SGLT2-selective inhibitor ipragliflozin in streptozotocin-nicotinamide-induced mildly diabetic mice. | 2012 |
|
| Effect of Ipragliflozin (ASP1941), a novel selective sodium-dependent glucose co-transporter 2 inhibitor, on urinary glucose excretion in healthy subjects. | 2011-12-01 |
|
| Safety, pharmacokinetic, and pharmacodynamic profiles of ipragliflozin (ASP1941), a novel and selective inhibitor of sodium-dependent glucose co-transporter 2, in patients with type 2 diabetes mellitus. | 2011-12 |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.pmda.go.jp/files/000206796.pdf
The usual adult dosage is 50 mg of ipragliflozin orally administered once daily before or after breakfast. The dose may be increased up to 100 mg once daily with careful monitoring of the patient’s clinical course in the case of inadequate efficacy.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.pmda.go.jp/files/000206796.pdf
The inhibitory effect of ipragliflozin on SGLT2 and SGLT1 as measured by sodiumdependent 14C-methyl-α-D-glucopyranoside (14C-AMG) uptake was evaluated in human SGLT2- or SGLT1-expressing CHO cells. As a result, IC50 values were 7.38 and 1880 nmol/L, respectively.
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Chemical
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