Ozenoxacin

D06A - Antibiotics for dermatological use ATC D06AX14 Small molecule approved 2017 Topical Natural product

JFDA label: Ozanex 10mg/g

Mechanism of Action

Inhibitor of DNA gyrase — DNA gyrase inhibitor; Inhibitor of Topoisomerase IV — Topoisomerase IV inhibitor; Inhibitor of DNA topoisomerase IV — DNA topoisomerase IV inhibitor

Target	Action	Gene / class
DNA gyrase efficacy	INHIBITOR
DNA topoisomerase IV efficacy	INHIBITOR
Topoisomerase IV efficacy	INHIBITOR

Indications

Approved

Impetigo

Contraindications

Source: Lexicomp

There are no contraindications listed in the manufacturer's labeling Absolute

Dosing

Source: Lexicomp

Impetigo: Topical: Apply a thin layer to affected area (up to 100 cm2) twice daily for 5 days.

Impetigo: Infants ≥2 months of age, Children, and Adolescents: Topical: Apply a thin layer to the affected area twice daily for 5 days. Note: Affected area may be up to 2% of the total BSA (not exceeding 100 cm2) for patients 2 for patients ≥12 years.

Refer to adult dosing.

Warnings & Precautions

Source: Lexicomp

Superinfection

Prolonged use may result in fungal or bacterial superinfection; discontinue use if superinfection occurs. Other warnings/precautions:

Appropriate use

For topical use only; not for oral, ophthalmic, intranasal, or intravaginal use.

Pregnancy & Lactation

Pregnancy

Systemic absorption following topical application is negligible; exposure to the fetus is not expected.

Lactation

It is not known if ozenoxacin is present in breast milk. However, systemic absorption following topical application is negligible and exposure to the breastfeeding infant is not expected. According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and benefits of treatment to the mother.

Chemistry & Properties

Formula	C21H21N3O3
Molecular weight	363.42 g/mol
IUPAC name	1-cyclopropyl-8-methyl-7-[5-methyl-6-(methylamino)-3-pyridinyl]-4-oxoquinoline-3-carboxylic acid
CAS	245765-41-7
PubChem CID	9863827
InChIKey	`XPIJWUTXQAGSLK-UHFFFAOYSA-N`
logP	3.76 (XLogP 4.1)
Polar surface area	84.22 Å²
H-bond acceptors / donors	5 / 2
Drug-likeness (QED)	0.74
Lipinski violations	0

SMILES

CNc1ncc(-c2ccc3c(=O)c(C(=O)O)cn(C4CC4)c3c2C)cc1C

Biology & Pharmacokinetics

Pharmacokinetics predicted

Bioavailability	10.0%
Half-life	1.592 h
Volume of distribution	0.917 L/kg
Protein binding	87.1%
BBB penetrant	No

Enzyme interactions

Enzyme	Role	Detail
CYP2C8	Inhibitor	—
CYP3A4	Substrate	—

Transporters

BCRP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)

Registered Products (1)

Brand	Form / strength	Pack	Agent	Citizen (JOD)
Ozanex 10mg/g	Cream Ozenoxacin 0.01 g/1 g	(10 GM) / TUB	Ibn Rushd Drug Store	14.460