U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula C22H31N3O6S2.ClH
Molecular Weight 534.089
Optical Activity UNSPECIFIED
Defined Stereocenters 4 / 4
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of TEBIPENEM PIVOXIL HYDROCHLORIDE

SMILES

Cl.C[C@@H](O)[C@@H]1[C@H]2[C@@H](C)C(SC3CN(C3)C4=NCCS4)=C(N2C1=O)C(=O)OCOC(=O)C(C)(C)C

InChI

InChIKey=ZXGTYOBSVQZXSC-HXLQFWNVSA-N
InChI=1S/C22H31N3O6S2.ClH/c1-11-15-14(12(2)26)18(27)25(15)16(19(28)30-10-31-20(29)22(3,4)5)17(11)33-13-8-24(9-13)21-23-6-7-32-21;/h11-15,26H,6-10H2,1-5H3;1H/t11-,12-,14-,15-;/m1./s1

HIDE SMILES / InChI

Molecular Formula C22H31N3O6S2
Molecular Weight 497.628
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 4 / 4
E/Z Centers 0
Optical Activity UNSPECIFIED

Molecular Formula ClH
Molecular Weight 36.461
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Tebipenem pivoxil is an oral carbapenem prodrug that was originated by Wyeth (now Pfizer). It was approved by Pharmaceuticals and Medical Devices Agency of Japan (PMDA) on Apr 22, 2009. It was developed and marketed as Orapenem® by Meiji Seika in Japan. Tebipenem pivoxil is a broad-spectrum orally-administered antibiotic, from the carbapenem subgroup of β-lactam antibiotics. Carbapenems are a class of beta-lactam antibiotics, which act by inhibiting the synthesis of the peptidoglycan layer of bacterial cell walls. It is used to treat otorhinolaryngological infection, otitis media and bacterial pneumonia. Orapenem® is available as granules for oral use, containing 100 mg Tebipenem pivoxil/g granules. According to the weight of children, 4 mg/kg, and twice a day after dinner.

CNS Activity

Curator's Comment: Low penetration to the central nervous system was confirmed in amimal models

Originator

Curator's Comment: # Wyeth (now Pfizer)

Approval Year

Targets

Targets

Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Curative
ORAPENEM

Approved Use

Orapenem is usually used to treat pneumonia, otitis media and sinusitis.

Launch Date

2009
Curative
ORAPENEM

Approved Use

Orapenem is usually used to treat pneumonia, otitis media and sinusitis.

Launch Date

2009
Curative
ORAPENEM

Approved Use

Orapenem is usually used to treat pneumonia, otitis media and sinusitis.

Launch Date

2009
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
11.81 μg/mL
250 mg single, oral
dose: 250 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
3.9 μg/mL
250 mg single, oral
dose: 250 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: HIGH-FAT
6087.5 ng/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
11099.17 ng/mL
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
17825 ng/mL
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
256 ng/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
1209 ng/mL
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
1944 ng/mL
600 mg single, oral
dose: 600 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
2943 ng/mL
900 mg single, oral
dose: 900 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
4062 ng/mL
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
3064 ng/mL
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
6216 ng/mL
600 mg single, oral
dose: 600 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
1810 ng/mL
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
2893 ng/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
4006 ng/mL
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
6203 ng/mL
600 mg single, oral
dose: 600 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
12652 ng/mL
900 mg single, oral
dose: 900 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
1892 ng/mL
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
3014 ng/mL
600 mg single, oral
dose: 600 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
1852 ng/mL
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
1677 ng/mL
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
5830 ng/mL
600 mg single, oral
dose: 600 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
2288 ng/mL
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
2058 ng/mL
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
6451 ng/mL
600 mg single, oral
dose: 600 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
7759 ng/mL
300 mg 3 times / day multiple, oral
dose: 300 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
13428 ng/mL
600 mg 3 times / day multiple, oral
dose: 600 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
6493 ng/mL
300 mg 3 times / day multiple, oral
dose: 300 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
15090 ng/mL
600 mg 3 times / day multiple, oral
dose: 600 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
2.71 μg/mL
100 mg 3 times / day multiple, oral
dose: 100 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
6.08 μg/mL
200 mg 3 times / day multiple, oral
dose: 200 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
4.74 μg/mL
300 mg 3 times / day multiple, oral
dose: 300 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
5.08 μg/mL
150 mg 3 times / day multiple, oral
dose: 150 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
7.92 μg/mL
250 mg 2 times / day multiple, oral
dose: 250 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
8.69 μg/mL
300 mg 3 times / day multiple, oral
dose: 300 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
9.85 μg/mL
250 mg single, oral
dose: 250 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
7.17 μg/mL
250 mg single, oral
dose: 250 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
13.26 μg/mL
250 mg single, oral
dose: 250 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
13.88 μg/mL
250 mg single, oral
dose: 250 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
10.46 μg × h/mL
250 mg single, oral
dose: 250 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
9.52 μg × h/mL
250 mg single, oral
dose: 250 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: HIGH-FAT
6407.34 ng × h/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
12517.7 ng × h/mL
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
23126.57 ng × h/mL
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
872 ng × h/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
3738 ng × h/mL
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
5192 ng × h/mL
600 mg single, oral
dose: 600 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
10571 ng × h/mL
900 mg single, oral
dose: 900 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
7268 ng × h/mL
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
6267 ng × h/mL
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
13602 ng × h/mL
600 mg single, oral
dose: 600 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
4456 ng × h/mL
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
2875 ng × h/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
6488 ng × h/mL
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
12715 ng × h/mL
600 mg single, oral
dose: 600 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
21913 ng × h/mL
900 mg single, oral
dose: 900 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
7175 ng × h/mL
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
14727 ng × h/mL
600 mg single, oral
dose: 600 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
6215 ng × h/mL
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
6549 ng × h/mL
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
16547 ng × h/mL
600 mg single, oral
dose: 600 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
6579 ng × h/mL
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
6137 ng × h/mL
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
14200 ng × h/mL
600 mg single, oral
dose: 600 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
7726 ng × h/mL
300 mg 3 times / day multiple, oral
dose: 300 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
20592 ng × h/mL
600 mg 3 times / day multiple, oral
dose: 600 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
7484 ng × h/mL
300 mg 3 times / day multiple, oral
dose: 300 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
17924 ng × h/mL
600 mg 3 times / day multiple, oral
dose: 600 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
3.2 μg × h/mL
100 mg 3 times / day multiple, oral
dose: 100 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
6.68 μg × h/mL
200 mg 3 times / day multiple, oral
dose: 200 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
11.35 μg × h/mL
300 mg 3 times / day multiple, oral
dose: 300 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
5.22 μg × h/mL
150 mg 3 times / day multiple, oral
dose: 150 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
7.93 μg × h/mL
250 mg 2 times / day multiple, oral
dose: 250 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
13.62 μg × h/mL
300 mg 3 times / day multiple, oral
dose: 300 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
12.29 μg × h/mL
250 mg single, oral
dose: 250 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
16.45 μg × h/mL
250 mg single, oral
dose: 250 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
29.22 μg × h/mL
250 mg single, oral
dose: 250 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
92.59 μg × h/mL
250 mg single, oral
dose: 250 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
0.77 h
250 mg single, oral
dose: 250 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
0.91 h
250 mg single, oral
dose: 250 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: HIGH-FAT
0.84 h
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
0.76 h
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
0.92 h
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
2 h
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
3.8 h
600 mg single, oral
dose: 600 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
2.5 h
900 mg single, oral
dose: 900 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
0.8 h
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
0.8 h
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
1 h
600 mg single, oral
dose: 600 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
1.2 h
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
0.9 h
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
0.8 h
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
1.1 h
600 mg single, oral
dose: 600 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
1 h
900 mg single, oral
dose: 900 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
1.3 h
600 mg single, oral
dose: 600 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
1.1 h
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
0.9 h
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
1.1 h
600 mg single, oral
dose: 600 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
0.9 h
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
0.9 h
600 mg single, oral
dose: 600 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
0.82 h
300 mg 3 times / day multiple, oral
dose: 300 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
0.79 h
600 mg 3 times / day multiple, oral
dose: 600 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
0.72 h
300 mg 3 times / day multiple, oral
dose: 300 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
0.83 h
600 mg 3 times / day multiple, oral
dose: 600 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
0.44 h
100 mg 3 times / day multiple, oral
dose: 100 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
0.36 h
200 mg 3 times / day multiple, oral
dose: 200 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
0.67 h
300 mg 3 times / day multiple, oral
dose: 300 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
0.4 h
150 mg 3 times / day multiple, oral
dose: 150 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
0.34 h
250 mg 2 times / day multiple, oral
dose: 250 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
0.54 h
300 mg 3 times / day multiple, oral
dose: 300 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
0.88 h
250 mg single, oral
dose: 250 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
1.49 h
250 mg single, oral
dose: 250 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
1.44 h
250 mg single, oral
dose: 250 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
4.11 h
250 mg single, oral
dose: 250 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEBIPENEM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
26.1%
TEBIPENEM serum
Homo sapiens
PubMed

PubMed

TitleDatePubMed
[Convulsive liability of an oral carbapenem antibiotic, tebipenem pivoxil].
2009-06
Syntheses and pharmacokinetic studies of prodrug esters for the development of oral carbapenem, L-084.
2006-04
Patents

Sample Use Guides

For children: In general, take 0.04 gram per kilogram of body weight (g/kg) (4 mg of the active ingredient [titer]/kg) at a time, twice a day, after meals. The dosage may be increased up to 0.06 g/kg (6 mg [titer]/kg) as needed. Strictly follow the instructions. Standard duration of administration is for 7 days or less. If you miss a dose, take a dose as soon as possible. However, if it is almost time for the next dose, skip the missed dose and follow your regular dosing schedule. You should never take two doses at one time.
Route of Administration: Oral
The MIC90 values of tebipenem pivoxil against Gram-positive bacteria such as methicillin-sensitive Staphylococcus aureus (MSSA), methicillin-resistant Staphylococcus aureus (MRSA), methicillin-sensitive Staphylococcus epidermidis (MSSE), methicillin-resistant Staphylococcus epidermidis (MRSE), Pyogenic streptococcus, and Enterococcus faecalis were ≤ 0.125, 16, 0.5, 8, ≤ 0.125, and 32 ug/mL, respectively. Correspondingly, the MIC90 values of tebipenem pivoxil against Escherichia coli, Klebsiella pneumoniae, Enterobacter aerogenes, Haemophilus influenzae, Pseudomonas aeruginosa, and Acinetobacter baumannii were 1, 0.5, ≤ 0.125, 0.25, 64, 64 ug/mL, respectively. The MBC values of tebipenem pivoxil against Escherichia coli, Staphylococcus aureus, Klebsiella pneumoniae were 0.016-2, 0.063-32, 0.031-32 ug/mL, respectively.
Substance Class Chemical
Created
by admin
on Wed Apr 02 01:27:15 GMT 2025
Edited
by admin
on Wed Apr 02 01:27:15 GMT 2025
Record UNII
0Z7A0FSA63
Record Status Validated (UNII)
Record Version
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Name Type Language
1-AZABICYCLO(3.2.0)HEPT-2-ENE-2-CARBOXYLIC ACID, 3-((1-(4,5-DIHYDRO-2-THIAZOLYL)-3-AZETIDINYL)THIO)-6-((1R)-1-HYDROXYETHYL)-4-METHYL-7-OXO-, (2,2-DIMETHYL-1-OXOPROPOXY)METHYL ESTER, HYDROCHLORIDE (1:1), (4R,5S,6S)-
Preferred Name English
TEBIPENEM PIVOXIL HYDROCHLORIDE
Common Name English
1-AZABICYCLO(3.2.0)HEPT-2-ENE-2-CARBOXYLIC ACID, 3-((1-(4,5-DIHYDRO-2-THIAZOLYL)-3-AZETIDINYL)THIO)-6-((1R)-1-HYDROXYETHYL)-4-METHYL-7-OXO-, (2,2-DIMETHYL-1-OXOPROPOXY)METHYL ESTER, MONOHYDROCHLORIDE, (4R,5S,6S)-
Systematic Name English
Code System Code Type Description
PUBCHEM
71623820
Created by admin on Wed Apr 02 01:27:15 GMT 2025 , Edited by admin on Wed Apr 02 01:27:15 GMT 2025
PRIMARY
CAS
211558-19-9
Created by admin on Wed Apr 02 01:27:15 GMT 2025 , Edited by admin on Wed Apr 02 01:27:15 GMT 2025
PRIMARY
FDA UNII
0Z7A0FSA63
Created by admin on Wed Apr 02 01:27:15 GMT 2025 , Edited by admin on Wed Apr 02 01:27:15 GMT 2025
PRIMARY
Related Record Type Details
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