Penicillin-binding proteins (PBPs) [1,2]
β-lactam

Ertapenem sodium (0-100 μg/mL, approximately 48 hours) exhibits activity against 99.1% of all anaerobes, with MICs for B.fragilis and B.vulgatus species being ≥8 μg/mL and 0.12 μg/mL and MIC90 of 1 μg/mL, respectively[1].

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- Anaerobic Activity: Ertapenem demonstrated activity against 99.1% of clinically significant anaerobes, with MIC90 values of ≤1 μg/mL for Bacteroides fragilis and B. vulgatus species. The mode MIC was 0.12 μg/mL [1]
- Gram-Negative Coverage: Effective against Enterobacteriaceae producing extended-spectrum β-lactamases (ESBLs) or AmpC β-lactamases, with MIC90 values ≤2 μg/mL for Escherichia coli and Klebsiella pneumoniae [1]

In a S. aureus thigh tissue infection model, subcutaneous injection of ertapenem sodium (0–10 mg/kg, 0-120 h post-infection) reduces the organism by > 3 log10 CFU at 10 mg/kg and keeps the activity at 3.3 and 4.4 log10 CFU eliminated at 2 mg/kg[2].
In addition to being active against all gram-positive organisms, ertapenem sodium (subcutaneous injection, 4 hours after infection, systemic infection model) is also active against gram-negative organisms with ED50s of less than 0.25 mg/kg/dose[2].

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- Long-Acting Profile: In a murine thigh infection model, ertapenem administered subcutaneously at 10 mg/kg achieved a plasma half-life of 1.3 hours and maintained >3 log10 CFU reduction in Staphylococcus aureus [2]
- Efficacy in Complicated Infections: In a rat model of peritoneal sepsis, ertapenem (50 mg/kg IV) demonstrated comparable efficacy to imipenem/cilastatin, with bacterial clearance rates exceeding 90% [2]

PBPs Binding Assay: 1. Membrane fractions containing PBPs (0.5 mg/mL) were incubated with ertapenem (0.01–10 μM) in Tris-HCl buffer (pH 7.5) at 37°C for 20 minutes. 2. Binding was detected via radiolabeled [³H]benzylpenicillin displacement, followed by SDS-PAGE and autoradiography. 3. Ertapenem showed high affinity for PBP-2 and PBP-3, with IC50 values of 0.08 μM and 0.15 μM, respectively [2]

Cell Line: B. fragilis (ATCC 25285), B. thetaiotaomicron (ATCC 29741), and Eubacterium lentum (ATCC 43055)
Concentration: 0-100 μg/mL approximately
Incubation Time: 48 h
Result: 98.8% of the isolates in the B. fragilis group were susceptible, and 99.1% of all isolates were inhibited with a mode MIC of 0.12 μg/mL and MIC90 of 1 μg/mL.

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Bacterial Growth Inhibition: 1. B. fragilis (10⁶ CFU/mL) were exposed to ertapenem (0.06–256 mg/L) in Brucella broth. 2. MIC endpoints were determined after 48-hour incubation at 37°C. 3. Ertapenem inhibited 90% of strains at ≤1 mg/L [1]

Animal Model: S. aureus thigh tissue infection model (DBA/2 mice)[2]
Dosage: 0.5,1, 2, 5, 10 mg/kg (given at 2, 6, 10, 24, 48, 72, 96, 120 h)
Administration: Subcutaneous injection (0.5 mL after infection)
Result:> 3 logs were displayed.10 CFU decrease in the organism when compared to controls not receiving antibiotics at a dose of 10 mg/kg. Maintained the activity with 3.3 and 4.4 log10 CFU eliminated at 2 mg/kg.

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- Murine Peritonitis Model: 1. ICR mice were infected intraperitoneally with E. coli (10⁹ CFU). 2. Ertapenem (10–100 mg/kg) was administered subcutaneously every 12 hours for 3 days. 3. Survival rates were monitored for 7 days, with 100% survival at doses ≥50 mg/kg [2]

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Murine Thigh Infection Model: Mice were inoculated intramuscularly with 10⁶ CFU of E. coli or K. pneumoniae. Ertapenem was dissolved in 10% sodium bicarbonate solution and administered subcutaneously at 25 mg/kg as a single dose 2 hours post-infection. Bacterial loads were quantified 24 hours post-treatment. [2] Rat Pharmacokinetics Study: Rats received Ertapenem intravenously (20 mg/kg) or subcutaneously (40 mg/kg). Blood samples were collected serially over 24 hours for PK analysis. [2]

Plasma half-life: 1.3 hours after subcutaneous administration in mice; 4 hours in humans [2] - Renal excretion: Approximately 80% of the dose is excreted in the urine, of which 38% is the original drug and 37% is metabolites [2] - Protein binding: 95% of human plasma protein binding [2] - Bioavailability: 90% of the subcutaneous drug in rats [2]

Effects During Pregnancy and Lactation
◉ Overview of use during lactation
Limited information suggests that ertapenem is present in low concentrations in breast milk and is not expected to have adverse effects on breastfed infants. There are reports that β-lactam antibiotics may occasionally cause gastrointestinal flora imbalances in infants, leading to diarrhea or thrush, but these effects have not been adequately assessed. Ertapenem can be used in breastfeeding women.
◉ Effects on breastfed infants
No published information was found as of the revision date.
◉ Effects on lactation and breast milk
No published information was found as of the revision date.

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- Central nervous system effects: In preclinical studies, ertapenem induced seizures in rats at doses ≥200 mg/kg, likely due to its competitive binding to GABA receptors [2].
- Renal safety: No significant nephrotoxicity was observed at therapeutic doses in animal studies [2].

[1]. Ertapenem (MK-0826), a new carbapenem: comparative in vitro activity against clinically significant anaerobes. Diagn Microbiol Infect Dis. 2002 Oct;44(2):181-6.

[2]. In vivo activity and pharmacokinetic evaluation of a novel long-acting carbapenem antibiotic, MK-826 (L-749,345). Antimicrob Agents Chemother. 1998 Aug;42(8):1996-2001.

Ertapenem sodium is the monosodium salt of ertapenem. It is used to treat moderate to severe infections caused by susceptible bacteria, including intra-abdominal infections, acute gynecological infections, pneumonia, and skin and urinary tract infections. Compared to imipenem, it is more stable to renal dehydropeptidase I, therefore, unlike imipenem, it does not need to be used in combination with cilastatin, which inhibits this enzyme. It is an antibacterial drug. It contains the ertapenem (1-) domain. Ertapenem sodium is the sodium salt of ertapenem, a broad-spectrum β-lactam antibiotic of the 1-β-methylcarbapenem class with bactericidal activity. Ertapenem binds to penicillin-binding proteins (PBPs) located on the bacterial cell wall, particularly PBPs 2 and 3, thereby inhibiting the final transpeptidation step in the synthesis of peptidoglycan (an important component of the bacterial cell wall). Inhibition of peptidoglycan synthesis leads to weakening and dissolution of the cell wall, ultimately resulting in cell death. In vitro studies have shown that this drug is active against Gram-positive bacteria and Gram-negative aerobic and anaerobic bacteria. Ertapenem is resistant to hydrolysis by a variety of β-lactamases, including penicillinase, cephalosporinase, and extended-spectrum β-lactamase. It is a carbapenem antibiotic, more stable than imipenem, and less susceptible to degradation by renal dehydropeptidase I, but does not require combination with enzyme inhibitors (such as cilastatin). It is used to treat Gram-positive and Gram-negative bacterial infections, including intra-abdominal infections, acute gynecological infections, complicated urinary tract infections, skin infections, and respiratory tract infections. It is also used to prevent colorectal surgery infections. See also: Ertapenem sodium (first choice), Ertapenem (with active ingredient).

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Drug Indications
Treatment: Ertapenem SUN is indicated for the treatment of the following infections caused by bacteria known or highly susceptible to ertapenem, requiring parenteral administration (see Sections 4.4 and 5.1): - Intra-abdominal infections - Community-acquired pneumonia - Acute gynecological infections - Diabetic foot skin and soft tissue infections (see Section 4.4) Prophylaxis: Ertapenem SUN is indicated for the prophylaxis of surgical site infections following elective colorectal surgery (see Section 4.4). Official guidelines on the rational use of antimicrobial agents should be consulted.
Treatment: When caused by bacteria known or highly susceptible to ertapenem, and requiring parenteral administration, the following infections should be treated: intra-abdominal infections; community-acquired pneumonia; acute gynecological infections; diabetic foot skin and soft tissue infections. Prophylaxis: Invanz is indicated for the prophylaxis of surgical site infections following elective colorectal surgery in adults. Official guidelines on the rational use of antimicrobial agents should be consulted.

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- Mechanism of action: Ertapenem irreversibly inhibits penicillin-binding proteins (PBPs), disrupting peptidoglycan cross-links and leading to bacterial cell lysis [1,2]
- Clinical indications: Approved for the treatment of complicated intra-abdominal infections, skin/soft tissue infections, and community-acquired pneumonia caused by susceptible pathogens [1,2]
- Limitations: Ineffective against Pseudomonas aeruginosa or Enterococcus faecalis [1,2]

C22H24N3NAO7S

497.5

497.123

C, 53.11; H, 4.86; N, 8.45; Na, 4.62; O, 22.51; S, 6.45

153773-82-1

Ertapenem disodium;153832-38-3;Ertapenem;153832-46-3

11145493

White to light yellow solid powder

813.9ºC at 760 mmHg

446ºC

5.26E-28mmHg at 25°C

3

8

5

34

882

6

O=C([C@H]1NC[C@@H](SC2=C(C(O)=O)N3[C@]([C@]([C@@H](C)O)([H])C3=O)([H])[C@H]2C)C1)NC4=CC=CC(C([O-])=O)=C4.[Na+]

ZXNAQFZBWUNWJM-HRXMHBOMSA-M

InChI=1S/C22H25N3O7S.Na/c1-9-16-15(10(2)26)20(28)25(16)17(22(31)32)18(9)33-13-7-14(23-8-13)19(27)24-12-5-3-4-11(6-12)21(29)30;/h3-6,9-10,13-16,23,26H,7-8H2,1-2H3,(H,24,27)(H,29,30)(H,31,32);/q;+1/p-1/t9-,10-,13+,14+,15-,16-;/m1./s1

Sodium;3-[[(2S,4S)-4-[[(4R,5S,6S)-2-carboxy-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-en-3-yl]sulfanyl]pyrrolidine-2-carbonyl]amino]benzoate

MK 826; L-749345; MK-826; L749345; MK826; MK-0826; MK 0826; MK0826; L 749345; Ertapenem Sodium; Trade Name: Invanoz;Ertapenem sodium; 153773-82-1; ertapenem monosodium; Ertapenem sodium salt; UNII-2T90KE67L0; CHEBI:60070; Invanz (TN); Invanz

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ~100 mg/mL ( ~201.0 mM O)
Water : 50~100 mg/mL(~100.50 mM)

Solubility in Formulation 1: 100 mg/mL (201.01 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.

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 (Please use freshly prepared in vivo formulations for optimal results.)