TEBIPENEM PIVOXIL

China [CN]

​Mechanism of Action and Antimicrobial Spectrum

Mechanism of Action: After oral administration, it is hydrolyzed by esterases into tebipenem, which binds to bacterial penicillin-binding proteins (PBPs), inhibiting cell wall synthesis. It is stable against renal dehydropeptidase I and does not require co-administration with enzyme inhibitors.

Antimicrobial Spectrum: Effective against Gram-positive bacteria (MSSA, Streptococcus pneumoniae, including penicillin/macrolide-resistant strains), Gram-negative bacteria (Haemophilus influenzae, Moraxella catarrhalis, including ESBL-producing strains), and some anaerobic bacteria. It has weak activity against MRSA.

Clinical Applications

Indications: Approved in Japan for use in children (0.5-16 years old) with otitis media, sinusitis, and bacterial pneumonia; Tebipenem Pivoxil HBr is currently undergoing Phase III clinical trials for complex urinary tract infections (cUTI) and acute pyelonephritis in adults.

Dosage and Administration:  The usual dose for children is 4 mg/kg/dose, twice daily, taken orally after meals; for severe cases, the dose can be increased to 6 mg/kg/dose, with a treatment course generally ≤7 days.

Dosage Form: 10% granules (containing strawberry flavoring, can be mixed with condensed milk, etc., to improve compliance in children).

Pharmacokinetics

It is well absorbed orally, and after hydrolysis, tebipenem reaches peak plasma concentrations quickly and is widely distributed. It has low plasma protein binding and is mainly excreted by the kidneys, with a cumulative urinary excretion rate of approximately 74.4%. Dosage adjustment is required in patients with renal impairment.

In children, weight-normalized creatinine clearance and age are the main factors affecting tebipenem clearance and distribution.​