GARENOXACIN MESYLATE ANHYDROUS

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C23H20F2N2O4.CH4O3S
Molecular Weight	522.518
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure of GARENOXACIN MESYLATE ANHYDROUS

Structure Search

SMILES

CS(O)(=O)=O.C[C@H]1NCC2=C1C=CC(=C2)C3=C(OC(F)F)C4=C(C=C3)C(=O)C(=CN4C5CC5)C(O)=O

InChI

InChIKey=UPHLDCUEQOTSAD-RFVHGSKJSA-N

InChI=1S/C23H20F2N2O4.CH4O3S/c1-11-15-5-2-12(8-13(15)9-26-11)16-6-7-17-19(21(16)31-23(24)25)27(14-3-4-14)10-18(20(17)28)22(29)30;1-5(2,3)4/h2,5-8,10-11,14,23,26H,3-4,9H2,1H3,(H,29,30);1H3,(H,2,3,4)/t11-;/m1./s1

HIDE SMILES / InChI

Molecular Formula	C23H20F2N2O4
Molecular Weight	426.4127
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	1 / 1
E/Z Centers	0
Optical Activity	UNSPECIFIED

Molecular Formula	CH4O3S
Molecular Weight	96.106
Charge	0
Count

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

Description
Sources: http://www.ema.europa.eu/docs/en_GB/document_library/Application_withdrawal_assessment_report/2010/01/WC500067888.pdf
Curator's Comment: description was created based on several sources, including, http://www.shijiebiaopin.com/upload/product/201233119022430.pdf

Garenoxacin is an antibacterial agent active against a range of aerobic Gram-positive and Gram-negative bacteria. It exerts its action by inhibiting bacterial DNA gyrase and topoisomerase IV. The drug was withdrawn from the market in Europe and was never approved in the USA. Garenoxacin is still marketed in Japan under the name Geninax.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Topoisomerase IV 62 Target ID: CHEMBL2363076 Sources: http://www.shijiebiaopin.net/upload/product/201233119022430.pdf	Inhibitor 8504
Bacterial DNA gyrase 66 Target ID: CHEMBL2311224 Sources: http://www.shijiebiaopin.net/upload/product/201233119022430.pdf	Inhibitor 8504

Conditions

Condition	Modality	Highest Phase	Product
Acute bacterial exacerbation of chronic bronchitis 31 Sources: http://www.ema.europa.eu/docs/en_GB/document_library/Application_withdrawal_assessment_report/2010/01/WC500067888.pdf	Curative	Approved 8583	GARENOXACIN MESYLATE Approved Use Acute bacterial exacerbation of chronic bronchitis, Acute bacterial sinusitis, Community-acquired pneumonia, Uncomplicated skin and skin structures infections, Complicated skin and skin structure infections including diabetic foot infections, Complicated intra-abdominal infections, including post-surgical and acute pelvic infections.
Acute bacterial sinusitis 26 Sources: http://www.ema.europa.eu/docs/en_GB/document_library/Application_withdrawal_assessment_report/2010/01/WC500067888.pdf	Curative	Approved 8583	GARENOXACIN MESYLATE Approved Use Laryngopharyngitis, Tonsillitis (including peritonsillitis and peritonsillar abscess), Acute bronchitis, Pneumonia, Secondary infection in chronic respiratory lesion, Otitis media, Sinusitis
Community-acquired pneumonia 47 Sources: http://www.ema.europa.eu/docs/en_GB/document_library/Application_withdrawal_assessment_report/2010/01/WC500067888.pdf	Curative	Approved 8583	GARENOXACIN MESYLATE Approved Use Acute bacterial exacerbation of chronic bronchitis, Acute bacterial sinusitis, Community-acquired pneumonia, Uncomplicated skin and skin structures infections, Complicated skin and skin structure infections including diabetic foot infections, Complicated intra-abdominal infections, including post-surgical and acute pelvic infections.
Skin and skin structure infections 81 Sources: http://www.ema.europa.eu/docs/en_GB/document_library/Application_withdrawal_assessment_report/2010/01/WC500067888.pdf	Curative	Approved 8583	GARENOXACIN MESYLATE Approved Use Acute bacterial exacerbation of chronic bronchitis, Acute bacterial sinusitis, Community-acquired pneumonia, Uncomplicated skin and skin structures infections, Complicated skin and skin structure infections including diabetic foot infections, Complicated intra-abdominal infections, including post-surgical and acute pelvic infections.
Complicated intra-abdominal infections 20 Sources: http://www.ema.europa.eu/docs/en_GB/document_library/Application_withdrawal_assessment_report/2010/01/WC500067888.pdf	Curative	Approved 8583	GARENOXACIN MESYLATE Approved Use Acute bacterial exacerbation of chronic bronchitis, Acute bacterial sinusitis, Community-acquired pneumonia, Uncomplicated skin and skin structures infections, Complicated skin and skin structure infections including diabetic foot infections, Complicated intra-abdominal infections, including post-surgical and acute pelvic infections.
Otitis media 42 Sources: http://www.shijiebiaopin.net/upload/product/201233119022430.pdf	Curative	Approved 8583	GENINAX Approved Use Laryngopharyngitis, Tonsillitis (including peritonsillitis and peritonsillar abscess), Acute bronchitis, Pneumonia, Secondary infection in chronic respiratory lesion, Otitis media, Sinusitis Launch Date 2006
Tonsillitis 36 Sources: http://www.shijiebiaopin.net/upload/product/201233119022430.pdf	Curative	Approved 8583	GENINAX Approved Use Laryngopharyngitis, Tonsillitis (including peritonsillitis and peritonsillar abscess), Acute bronchitis, Pneumonia, Secondary infection in chronic respiratory lesion, Otitis media, Sinusitis Launch Date 2006
Laryngopharyngitis 3 Sources: http://www.shijiebiaopin.net/upload/product/201233119022430.pdf	Curative	Approved 8583	GENINAX Approved Use Laryngopharyngitis, Tonsillitis (including peritonsillitis and peritonsillar abscess), Acute bronchitis, Pneumonia, Secondary infection in chronic respiratory lesion, Otitis media, Sinusitis Launch Date 2006

C_max

Value	Dose	Analyte	Population
8.86 μg/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241017F1022_2_007_1F.pdf#page=41	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
8.36 μg/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241017F1022_2_007_1F.pdf#page=43	400 mg 1 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
11.06 μg/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241017F1022_2_007_1F.pdf#page=43	400 mg 1 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
10.9 μg/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241017F1022_2_007_1F.pdf#page=43	400 mg 1 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
2.09 μg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=25	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
4.89 μg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=25	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
7.43 μg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=25	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
12.34 μg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=25	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
0.6 μg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=27	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1.16 μg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=27	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
2.81 μg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=27	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
6.15 μg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=27	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
6.95 μg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=27	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
10.67 μg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=27	800 mg single, oral dose: 800 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
5.76 μg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=27	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
4.69 μg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=27	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: HIGH-FAT
9.8 μg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=28	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
8.3 μg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=28	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
7 μg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=28	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
11 μg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=28	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
12.6 μg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=28	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
10.1 μg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=28	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
6 μg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=28	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
9.2 μg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=28	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
7.1 μg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=28	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
118.1 μg × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241017F1022_2_007_1F.pdf#page=41	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
75.3 μg × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241017F1022_2_007_1F.pdf#page=43	400 mg 1 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
110.9 μg × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241017F1022_2_007_1F.pdf#page=43	400 mg 1 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
114.9 μg × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241017F1022_2_007_1F.pdf#page=43	400 mg 1 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
21.5 μg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=25	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
48.9 μg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=25	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
100.7 μg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=25	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
165.5 μg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=25	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
6.9 μg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=27	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
14.3 μg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=27	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
38.6 μg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=27	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
83.5 μg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=27	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
102.8 μg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=27	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
149.1 μg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=27	800 mg single, oral dose: 800 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
71.7 μg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=27	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
63.8 μg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=27	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: HIGH-FAT
113.9 μg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=28	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
108.6 μg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=28	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
113.9 μg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=28	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
113 μg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=28	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
136.4 μg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=28	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
205.4 μg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=28	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
138 μg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=28	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
156.5 μg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=28	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
165 μg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=28	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Analyte	Population
12.4 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241017F1022_2_007_1F.pdf#page=41	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
11.66 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241017F1022_2_007_1F.pdf#page=43	400 mg 1 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
9.76 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241017F1022_2_007_1F.pdf#page=43	400 mg 1 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
10.67 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241017F1022_2_007_1F.pdf#page=43	400 mg 1 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
14.46 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=25	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
12.65 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=25	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
12.36 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=25	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
12.39 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=25	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
10.5 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=27	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
11.7 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=27	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
15.4 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=27	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
12.6 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=27	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
13.4 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=27	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
13.2 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=27	800 mg single, oral dose: 800 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
14.1 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=27	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
14.9 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=27	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: HIGH-FAT
16.7 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=28	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
20.2 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=28	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
16.3 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=28	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
11.8 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=28	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
14.4 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=28	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
26.5 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=28	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
32.7 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=28	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
24.5 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=28	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
28.5 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700040/480297000_21900AMX01088000_A100_1.pdf#page=28	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	GARENOXACIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
20% OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241017F1022_2_007_1F.pdf#page=49	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:		GARENOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

Doses

Dose	Population	Adverse events
1200 mg 1 times / day multiple, oral Highest studied dose Dose: 1200 mg, 1 times / day Route: oral Route: multiple Dose: 1200 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/12821477/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: FASTED Sources: https://pubmed.ncbi.nlm.nih.gov/12821477/	Other AEs: Headache, Pharyngitis... Other AEs: Headache (grade 1-2) Pharyngitis (grade 1-2) Dizziness (grade 1-2) Sources: https://pubmed.ncbi.nlm.nih.gov/12821477/
800 mg 1 times / day multiple, intravenous Highest studied dose Dose: 800 mg, 1 times / day Route: intravenous Route: multiple Dose: 800 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/17692724/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/17692724/	Sources: https://pubmed.ncbi.nlm.nih.gov/17692724/
800 mg single, oral Highest studied dose Dose: 800 mg Route: oral Route: single Dose: 800 mg Sources: https://pubmed.ncbi.nlm.nih.gov/17692724/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/17692724/	Sources: https://pubmed.ncbi.nlm.nih.gov/17692724/
400 mg 2 times / day multiple, oral Studied dose Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/17919545/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/17919545/	Disc. AE: Facial swelling, Dizziness... AEs leading to discontinuation/dose reduction: Facial swelling (0.7%) Dizziness (grade 1-2, 0.4%) Nausea (1.1%) Chest pain (0.4%) ALT increased (0.4%) Flatulence (0.4%) Dyspnea (0.4%) Tachycardia (0.4%) Vomiting (0.4%) Abdominal pain (0.4%) Sources: https://pubmed.ncbi.nlm.nih.gov/17919545/

AEs

AE	Significance	Dose	Population
Dizziness	grade 1-2	1200 mg 1 times / day multiple, oral Highest studied dose Dose: 1200 mg, 1 times / day Route: oral Route: multiple Dose: 1200 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/12821477/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: FASTED Sources: https://pubmed.ncbi.nlm.nih.gov/12821477/
Headache	grade 1-2	1200 mg 1 times / day multiple, oral Highest studied dose Dose: 1200 mg, 1 times / day Route: oral Route: multiple Dose: 1200 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/12821477/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: FASTED Sources: https://pubmed.ncbi.nlm.nih.gov/12821477/
Pharyngitis	grade 1-2	1200 mg 1 times / day multiple, oral Highest studied dose Dose: 1200 mg, 1 times / day Route: oral Route: multiple Dose: 1200 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/12821477/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: FASTED Sources: https://pubmed.ncbi.nlm.nih.gov/12821477/
ALT increased	0.4% Disc. AE	400 mg 2 times / day multiple, oral Studied dose Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/17919545/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/17919545/
Abdominal pain	0.4% Disc. AE	400 mg 2 times / day multiple, oral Studied dose Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/17919545/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/17919545/
Chest pain	0.4% Disc. AE	400 mg 2 times / day multiple, oral Studied dose Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/17919545/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/17919545/
Dyspnea	0.4% Disc. AE	400 mg 2 times / day multiple, oral Studied dose Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/17919545/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/17919545/
Flatulence	0.4% Disc. AE	400 mg 2 times / day multiple, oral Studied dose Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/17919545/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/17919545/
Tachycardia	0.4% Disc. AE	400 mg 2 times / day multiple, oral Studied dose Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/17919545/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/17919545/
Vomiting	0.4% Disc. AE	400 mg 2 times / day multiple, oral Studied dose Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/17919545/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/17919545/
Facial swelling	0.7% Disc. AE	400 mg 2 times / day multiple, oral Studied dose Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/17919545/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/17919545/
Nausea	1.1% Disc. AE	400 mg 2 times / day multiple, oral Studied dose Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/17919545/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/17919545/
Dizziness	grade 1-2, 0.4% Disc. AE	400 mg 2 times / day multiple, oral Studied dose Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/17919545/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/17919545/

PubMed

Title	Date	PubMed
Torsades de Pointes induced by a combination of garenoxacin and disopyramide and other cytochrome P450, family 3, subfamily A polypeptide-4-influencing drugs during hypokalemia due to licorice.	2010-04	19915794
In vitro susceptibility of Mycobacterium tuberculosis clinical isolates to garenoxacin and DA-7867.	2005-10	16189119
Mycobacterium tuberculosis DNA gyrase: interaction with quinolones and correlation with antimycobacterial drug activity.	2004-04	15047530
Garenoxacin (BMS-284756) and moxifloxacin in experimental meningitis caused by vancomycin-tolerant pneumococci.	2003-01	12499193
In vitro antibacterial activities of DQ-113, a potent quinolone, against clinical isolates.	2002-03	11850285
The in vitro activity of BMS-284756, a new des-fluorinated quinolone.	2002-01	11751785
Synthesis, antibacterial activity, and toxicity of 7-(isoindolin-5-yl)-4-oxoquinoline-3-carboxylic acids. Discovery of the novel des-F(6)-quinolone antibacterial agent garenoxacin (T-3811 or BMS-284756).	2002	12572531
Antibacterial spectrum of a novel des-fluoro(6) quinolone, BMS-284756.	2000-12	11083639
In vitro and in vivo antimicrobial activities of T-3811ME, a novel des-F(6)-quinolone.	1999-05	10223917

Patents

Sample Use Guides

In Vivo Use Guide

The usual adult dosage is 400 mg once daily.

Route of Administration: Oral

In Vitro Use Guide

The MICs was 0.025-0.78 ug/ml against aerobic and facultative anaerobic Gram-positive bacteria, 0.00313-12.5 ug/ml against aerobic and facultative anaerobic Gram-negative bacteria, 0.1-3.13 ug/ml against obligate anaerobic Gram-positive bacteria and 0.05-0.78 ug/ml for obligate Gram-negative bacteria. The MICs against C. pneumoniae, C. psittaci, M. pneumoniae and Legionella spp., were 0.008, 0.002, 0.016, 0.0313 and 0.0039-0.0313 ug/ml, respectively.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 20:35:00 GMT 2025` Edited by `admin` on `Mon Mar 31 20:35:00 GMT 2025`
Record UNII	437ZKU48CF
Record Status	`Validated (UNII)`
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Name

Type

Language

GARENOXACIN MESYLATE ANHYDROUS

Common Name

English

GARENOXACIN MESILATE

Preferred Name

English

GARENOXACIN METHANESULFONATE [MI]

Common Name

English

1-CYCLOPROPYL-8-(DIFLUOROMETHOXY)-7-((1R)-1-METHYL-2,3-DIHYDRO-1H-5-ISOINDOLYL)-4-OXO-1,4-DIHYDRO-3-QUINOLINECARBOXYLIC ACID MESYLATE

Systematic Name

English

3-QUINOLINECARBOXYLIC ACID, 1-CYCLOPROPYL-8-(DIFLUOROMETHOXY)-7-((1R)-2,3-DIHYDRO-1-METHYL-1H-ISOINDOL-5-YL)-1,4-DIHYDRO-4-OXO-, METHANESULFONATE (1:1)

Common Name

English

GARENOXACIN MESILATE [MART.]

Common Name

English

GARENOXACIN METHANESULFONATE

Common Name

English

(+)-GARENOXACIN MESYLATE ANHYDROUS

Common Name

English

(R)-1-CYCLOPROPYL-8-(DIFLUOROMETHOXY)-7-(1-METHYL-2,3-DIHYDRO-1H-5-ISOINDOLYL)-4-OXO-1,4-DIHYDRO-3-QUINOLINECARBOXYLIC ACID METHANESULFONATE

Systematic Name

English

T-3811ME

Code

English

3-QUINOLINECARBOXYLIC ACID, 1-CYCLOPROPYL-8-(DIFLUOROMETHOXY)-7-((1R)-2,3-DIHYDRO-1-METHYL-1H-ISOINDOL-5-YL)-1,4-DIHYDRO-4-OXO-, MONOMETHANESULFONATE

Common Name

English

Garenoxacin mesilate [WHO-DD]

Common Name

English

BMS-284756

Code

English

Code System Code Type Description

FDA UNII

437ZKU48CF