TOFOGLIFLOZIN

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C22H26O6.H2O
Molecular Weight	404.4535
Optical Activity	UNSPECIFIED
Defined Stereocenters	5 / 5
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

O.CCC1=CC=C(CC2=CC3=C(CO[C@]34O[C@H](CO)[C@@H](O)[C@H](O)[C@H]4O)C=C2)C=C1

InChI

InChIKey=ZXOCGDDVNPDRIW-NHFZGCSJSA-N

InChI=1S/C22H26O6.H2O/c1-2-13-3-5-14(6-4-13)9-15-7-8-16-12-27-22(17(16)10-15)21(26)20(25)19(24)18(11-23)28-22;/h3-8,10,18-21,23-26H,2,9,11-12H2,1H3;1H2/t18-,19-,20+,21-,22+;/m1./s1

HIDE SMILES / InChI

Molecular Formula	C22H26O6
Molecular Weight	386.4382
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	5 / 5
E/Z Centers	0
Optical Activity	UNSPECIFIED

Molecular Formula	H2O
Molecular Weight	18.0153
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/24848755 | http://www.kowa-souyaku.co.jp/upload/item/66/93/7-wse_167.doc

Tofogliflozin is a SGLT2 selective inhibitor which was developed by Chugai Pharmaceutical for the treatment of Type 2 Diabetes Mellitus. The drug was approved in Japan in 2013 and it is being marketed under the names Apleway and Debereza.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Sodium/glucose cotransporter 2 25 Target ID: CHEMBL3884 Sources: https://www.ncbi.nlm.nih.gov/pubmed/22889351	Inhibitor 8504		2.9 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Type 2 diabetes mellitus 262 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24848755	Primary		Approved 8583	DEBERZA Approved Use The treatment of type 2 diabetes mellitus. Launch Date 2012

C_max

Value	Dose	Analyte	Population
509 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=20 \| https://www.info.pmda.go.jp/go/interview/2/270072_3969021F1024_2_002_1F.pdf#page=49	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
344 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=20 \| https://www.info.pmda.go.jp/go/interview/2/270072_3969021F1024_2_002_1F.pdf#page=49	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT
444 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=20 \| https://www.info.pmda.go.jp/go/interview/2/270072_3969021F1024_2_002_1F.pdf#page=49	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1020 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=20 \| https://www.info.pmda.go.jp/go/interview/2/270072_3969021F1024_2_002_1F.pdf#page=49	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
742 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=20 \| https://www.info.pmda.go.jp/go/interview/2/270072_3969021F1024_2_002_1F.pdf#page=49	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
1050 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=20 \| https://www.info.pmda.go.jp/go/interview/2/270072_3969021F1024_2_002_1F.pdf#page=49	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
310 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=33 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=44	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
220 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=33 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=44	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
506 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=33 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=44	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
394 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=33 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=44	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1210 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=33 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=44	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1930 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=33 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=44	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1570 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=33 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=44	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
3710 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=33 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=44	160 mg single, oral dose: 160 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
6740 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=33 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=44	320 mg single, oral dose: 320 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
11900 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=33 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=44	640 mg single, oral dose: 640 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
69.3 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=35 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=72	2.5 mg 1 times / day multiple, oral dose: 2.5 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
59.9 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=35 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=72	2.5 mg 1 times / day multiple, oral dose: 2.5 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
484 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=35 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=72	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
391 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=35 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=72	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1810 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=35 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=72	80 mg 1 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1660 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=35 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=72	80 mg 1 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
35.6 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=37 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=415	2.5 mg 1 times / day multiple, oral dose: 2.5 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
36.7 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=37 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=415	2.5 mg 1 times / day multiple, oral dose: 2.5 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
89.4 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=37 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=415	5 mg 1 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
77 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=37 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=415	5 mg 1 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
355 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=38 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=415	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
340 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=38 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=415	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
939 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=38 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=415	60 mg 1 times / day multiple, oral dose: 60 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1000 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=38 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=415	60 mg 1 times / day multiple, oral dose: 60 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
2030 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=38 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=415	120 mg 1 times / day multiple, oral dose: 120 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1610 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=38 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=415	120 mg 1 times / day multiple, oral dose: 120 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
410 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=40 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=41 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=420	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
391 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=40 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=41 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=420	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
399 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=40 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=41 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=420	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
360 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=40 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=41 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=420	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1230 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=42 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=89	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
846 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=42 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=89	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
2140 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=20 \| https://www.info.pmda.go.jp/go/interview/2/270072_3969021F1024_2_002_1F.pdf#page=49	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1990 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=20 \| https://www.info.pmda.go.jp/go/interview/2/270072_3969021F1024_2_002_1F.pdf#page=49	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT
1890 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=20 \| https://www.info.pmda.go.jp/go/interview/2/270072_3969021F1024_2_002_1F.pdf#page=49	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
4190 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=20 \| https://www.info.pmda.go.jp/go/interview/2/270072_3969021F1024_2_002_1F.pdf#page=49	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
3690 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=20 \| https://www.info.pmda.go.jp/go/interview/2/270072_3969021F1024_2_002_1F.pdf#page=49	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
3730 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=20 \| https://www.info.pmda.go.jp/go/interview/2/270072_3969021F1024_2_002_1F.pdf#page=49	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1330 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=33 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=44	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1040 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=33 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=44	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1900 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=33 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=44	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1820 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=33 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=44	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
5640 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=33 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=44	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
8830 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=33 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=44	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
7090 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=33 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=44	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
21800 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=33 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=44	160 mg single, oral dose: 160 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
38100 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=33 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=44	320 mg single, oral dose: 320 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
99100 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=33 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=44	640 mg single, oral dose: 640 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
204 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=35 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=72	2.5 mg 1 times / day multiple, oral dose: 2.5 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
192 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=35 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=72	2.5 mg 1 times / day multiple, oral dose: 2.5 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1680 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=35 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=72	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1550 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=35 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=72	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
7240 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=35 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=72	80 mg 1 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
6740 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=35 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=72	80 mg 1 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
184 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=37 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=415	2.5 mg 1 times / day multiple, oral dose: 2.5 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
179 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=37 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=415	2.5 mg 1 times / day multiple, oral dose: 2.5 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
380 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=37 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=415	5 mg 1 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
387 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=37 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=415	5 mg 1 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1500 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=38 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=415	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1380 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=38 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=415	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
4620 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=38 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=415	60 mg 1 times / day multiple, oral dose: 60 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
4740 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=38 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=415	60 mg 1 times / day multiple, oral dose: 60 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
10900 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=38 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=415	120 mg 1 times / day multiple, oral dose: 120 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
9690 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=38 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=415	120 mg 1 times / day multiple, oral dose: 120 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1740 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=40 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=41 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=420	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2070 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=40 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=41 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=420	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2040 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=40 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=41 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=420	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1970 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=40 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=41 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=420	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
6720 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=42 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=89	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3830 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=42 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=89	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN

T_1/2

Value	Dose	Analyte	Population
5.4 h OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=20 \| https://www.info.pmda.go.jp/go/interview/2/270072_3969021F1024_2_002_1F.pdf#page=49	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
5.82 h OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=20 \| https://www.info.pmda.go.jp/go/interview/2/270072_3969021F1024_2_002_1F.pdf#page=49	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT
5.65 h OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=20 \| https://www.info.pmda.go.jp/go/interview/2/270072_3969021F1024_2_002_1F.pdf#page=49	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
5.39 h OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=20 \| https://www.info.pmda.go.jp/go/interview/2/270072_3969021F1024_2_002_1F.pdf#page=49	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
5.48 h OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=20 \| https://www.info.pmda.go.jp/go/interview/2/270072_3969021F1024_2_002_1F.pdf#page=49	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
5.65 h OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=20 \| https://www.info.pmda.go.jp/go/interview/2/270072_3969021F1024_2_002_1F.pdf#page=49	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
5.71 h OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=33 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=44	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
6.09 h OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=33 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=44	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
5.29 h OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=33 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=44	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
5.7 h OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=33 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=44	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
5.77 h OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=33 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=44	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
5.73 h OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=33 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=44	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
5.36 h OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=33 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=44	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
5.63 h OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=33 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=44	160 mg single, oral dose: 160 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
5.53 h OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=33 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=44	320 mg single, oral dose: 320 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
6.06 h OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=33 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=44	640 mg single, oral dose: 640 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
4.37 h OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=35 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=72	2.5 mg 1 times / day multiple, oral dose: 2.5 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
4.35 h OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=35 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=72	2.5 mg 1 times / day multiple, oral dose: 2.5 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
4.14 h OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=35 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=72	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
7.64 h OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=35 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=72	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
4.07 h OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=35 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=72	80 mg 1 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
17 h OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=35 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=72	80 mg 1 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
4.71 h OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=37 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=415	2.5 mg 1 times / day multiple, oral dose: 2.5 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
5.08 h OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=37 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=415	2.5 mg 1 times / day multiple, oral dose: 2.5 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
5.19 h OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=37 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=415	5 mg 1 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
4.8 h OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=37 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=415	5 mg 1 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
4.75 h OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=38 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=415	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
4.34 h OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=38 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=415	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
4.74 h OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=38 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=415	60 mg 1 times / day multiple, oral dose: 60 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
4.44 h OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=38 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=415	60 mg 1 times / day multiple, oral dose: 60 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
4.98 h OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=38 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=415	120 mg 1 times / day multiple, oral dose: 120 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
4.75 h OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=38 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=415	120 mg 1 times / day multiple, oral dose: 120 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
6.21 h OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=40 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=41 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=420	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
5.65 h OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=40 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=41 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=420	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
6.06 h OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=40 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=41 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=420	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
6.52 h OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=40 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=41 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=420	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
9.01 h OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=42 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=89	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
11.5 h OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=42 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=89	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN

F_unbound

Value	Dose	Analyte	Population
17.4% OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=30 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_I100_1.pdf#page=64		TOFOGLIFLOZIN plasma	Homo sapiens
16.9% OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=40 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=41 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=420	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
15.1% OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=40 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=41 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=420	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
15.6% OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=40 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=41 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=420	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
19.7% OTHER GOV'T https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=40 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_A100_1.pdf#page=41 \| https://www.pmda.go.jp/drugs/2014/P201400036/780069000_22600AMX00549_K101_1.pdf#page=420	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TOFOGLIFLOZIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

Doses

Dose	Population	Adverse events
640 mg single, oral Highest studied dose Dose: 640 mg Route: oral Route: single Dose: 640 mg Sources: https://pubmed.ncbi.nlm.nih.gov/28427104/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/28427104/	Sources: https://pubmed.ncbi.nlm.nih.gov/28427104/
40 mg 1 times / day multiple, oral Studied dose Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/24678906/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FASTED Sources: https://pubmed.ncbi.nlm.nih.gov/24678906/	Disc. AE: Weight decrease... AEs leading to discontinuation/dose reduction: Weight decrease (grade 2, 1.7%) Sources: https://pubmed.ncbi.nlm.nih.gov/24678906/
80 mg 1 times / day multiple, oral Studied dose Dose: 80 mg, 1 times / day Route: oral Route: multiple Dose: 80 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/28427104/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: FASTED Sources: https://pubmed.ncbi.nlm.nih.gov/28427104/	Sources: https://pubmed.ncbi.nlm.nih.gov/28427104/

AEs

AE	Significance	Dose	Population
Weight decrease	grade 2, 1.7% Disc. AE	40 mg 1 times / day multiple, oral Studied dose Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/24678906/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FASTED Sources: https://pubmed.ncbi.nlm.nih.gov/24678906/

PubMed

Title	Date	PubMed
In vitro-in vivo correlation of the inhibition potency of sodium-glucose cotransporter inhibitors in rat: a pharmacokinetic and pharmacodynamic modeling approach.	2013-04	23386251
Selective SGLT2 inhibition by tofogliflozin reduces renal glucose reabsorption under hyperglycemic but not under hypo- or euglycemic conditions in rats.	2013-02-15	23249697
Discovery of tofogliflozin, a novel C-arylglucoside with an O-spiroketal ring system, as a highly selective sodium glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes.	2012-09-13	22889351
Tofogliflozin, a potent and highly specific sodium/glucose cotransporter 2 inhibitor, improves glycemic control in diabetic rats and mice.	2012-06	22410641

Patents

Sample Use Guides

In Vivo Use Guide

In general, for adults, take 20 mg of tofogliflozin once a day, before or after breakfast.

Route of Administration: Oral

In Vitro Use Guide

Primary cultured proximal tubular epithelial cells from human normal kidney were treated with or without 3 nM or 30 nM tofogliflozin and with or without 22.8 mM glucose. Tofogliflozin dose-dependently suppressed glucose entry into tubular cells.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 19:57:19 GMT 2025` Edited by `admin` on `Mon Mar 31 19:57:19 GMT 2025`
Record UNII	P8DD8KX4O4
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

TOFOGLIFLOZIN

Official Name

English

TOFOGLIFLOZIN HYDRATE

Preferred Name

English

SPIRO(ISOBENZOFURAN-1(3H),2'-(2H)PYRAN)-3',4',5'-TRIOL,6-((4-ETHYLPHENYL)METHYL)-3',4',5',6'-TETRAHYDRO-6'-(HYDROXYMETHYL)-,HYDRATE (1:1),(1S,3'R,4'S,5'S,6'R)-

Common Name

English

TOFOGLIFLOZIN MONOHYDRATE

Common Name

English

TOFOGLIFLOZIN MONOHYDRATE [MI]

Common Name

English

CSG452

Code

English

TOFOGLIFLOZIN [USAN]

Common Name

English

TOFOGLIFLOZIN HYDRATE [JAN]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C98083