Identification
- Summary
Ertapenem is a carbapenem antibiotic used for the treatment of moderate to severe infections caused by susceptible bacteria.
- Brand Names
- Invanz
- Generic Name
- Ertapenem
- DrugBank Accession Number
- DB00303
- Background
Ertapenem is a 1-β methyl-carbapenem that is structurally related to beta-lactam antibiotics.5 It was first authorized for use in the US in November 2001 and in Europe in April 2002.1 Shown to be effective against a wide range of Gram-positive and Gram-negative aerobic and anaerobic bacteria, ertapenem is used to treat various bacterial infections.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Ertapenem (DB00303)
- Weight
- Average: 475.515
Monoisotopic: 475.141320859 - Chemical Formula
- C22H25N3O7S
- Synonyms
- (1R,5S,6S,8R,2'S,4'S)-2-(2-(3-carboxyphenylcarbamoyl)pyrrolidin-4-ylthio)-6-(1-hydroxyethyl)-1-methylcarbapenem-3-carboxylic acid
- (4R,5S,6S)-3-((3S,5S)-5-((3-carboxyphenyl)carbamoyl)pyrrolidin-3-ylthio)-6-((R)-1-hydroxyethyl)-4-methyl-7-oxo-1-aza-bicyclo[3.2.0]hept-2-ene-2-carboxylic acid
- Ertapenem
Pharmacology
- Indication
Ertapenem is indicated to treat the following moderate to severe infections caused by susceptible bacteria in adult and pediatric patients (three months of age and older):5,6
- Complicated intra-abdominal infections.5,6
- Complicated skin and skin structure infections, including diabetic foot infections without osteomyelitis.5,6
- Community-acquired pneumonia.5,6
- Complicated urinary tract infections, including pyelonephritis.5
- Acute pelvic infections, including postpartum endomyometritis, septic abortion and post-surgical gynecologic infections.5
- Acute gynecological infections.6
Ertapenem is also used in adults for the prophylaxis of surgical site infection following elective colorectal surgery.5,6
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
- Acute Gynecological Infection
- Severe Community-acquired Pneumonia (sCAP)
- Surgical Site Infections
- Acute, moderate Pelvic Infections caused by susceptible bacteria
- Acute, severe susceptible bacteria Pelvic Infections
- Moderate Community acquired pneumonia
- Moderate Complicated Intra-Abdominal Infections (cIAIs) caused by susceptible bacteria
- Moderate Diabetic Foot Infection
- Moderate Gynaecological infection caused by susceptible bacteria
- Moderate Postpartum Endomyometritis caused by susceptible bacteria
- Moderate Septic Abortion caused by susceptible bacteria
- Moderate complicated Urinary Tract Infection caused by susceptible bacteria
- Moderate complicated skin and skin-structure infections caused by susceptible bacteria
- Severe Complicated Intra-Abdominal Infections (cIAIs) caused by susceptible bacteria
- Severe Diabetic Foot Infection
- Severe Gynaecological infection caused by susceptible bacteria
- Severe Postpartum Endomyometritis caused by susceptible bacteria
- Severe Septic Abortion caused by susceptible bacteria
- Severe complicated Urinary Tract Infection caused by susceptible bacteria
- Severe complicated skin and skin-structure infections caused by susceptible bacteria
- Contraindications & Blackbox Warnings
Avoid life-threatening adverse drug eventsImprove clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events & improve clinical decision support.- Pharmacodynamics
Ertapenem is a carbapenem antibiotic with time-dependent bactericidal activity.3,4 Its optimal bactericidal activity is achieved when drug concentrations exceed the minimal inhibitory concentrations (MIC) for a specified portion of the dosing interval.2,3,4
It works against Gram-positive and Gram-negative aerobic and anaerobic bacteria. It is stable against hydrolysis by various beta-lactamases, including penicillinases, cephalosporinases, and extended-spectrum beta-lactamases, but not metallo-beta-lactamases.5,6
- Mechanism of action
Ertapenem exhibits a bactericidal mode of action.2 It works by binding to and inhibiting bacterial penicillin-binding proteins (PBPs).5 In Escherichia coli, it has a strong affinity toward PBPs 1a, 1b, 2, 3, 4 and 5 with preferential binding to PBPs 2 and 3.5 Upon binding to PBPs, ertapenem inhibits bacterial cell wall synthesis by interfering with the lengthening and strengthening of the peptidoglycan portion of the cell wall, thereby inhibiting cell wall synthesis.3
Target Actions Organism APenicillin-binding protein 1A inhibitorEscherichia coli (strain K12) APenicillin-binding protein 1B inhibitorEscherichia coli (strain K12) APenicillin-binding protein 2 inhibitorHaemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd) APenicillin-binding protein 2 inhibitorEscherichia coli (strain K12) APeptidoglycan synthase FtsI inhibitorHaemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd) APeptidoglycan synthase FtsI inhibitorEscherichia coli (strain K12) AD-alanyl-D-alanine carboxypeptidase DacB inhibitorEscherichia coli (strain K12) AD-alanyl-D-alanine carboxypeptidase DacC inhibitorEscherichia coli (strain K12) - Absorption
Ertapenem is almost completely absorbed following intramuscular administration, with a mean bioavailability of approximately 90%.5
Plasma concentrations of ertapenem are similar whether given intramuscularly or intravenously; however, the peak concentrations are lower when given via the intramuscular route. The time to reach the Cmax (Tmax) is slightly longer when given via the intramuscular route.1 Following daily intramuscular administration of one gram of ertapenem, the Tmax was approximately 2.3 hours.5 In healthy young adults who received a single 30-minute intravenous infusion of one gram of ertapenem, the Cmax was 155 µG/mL at 0.5 hours postdose.6
- Volume of distribution
The apparent volume of distribution at steady state (Vss) of ertapenem is approximately 0.12 L/kg in adults, 0.2 L/kg in children three months to 12 years of age, and 0.16 L/kg in adolescents 13 to 17 years of age. Ertapenem does not accumulate.5
- Protein binding
Ertapenem binds to plasma proteins in a concentration-dependent manner. It is highly bound to human plasma proteins, primarily to albumin.5 Protein binding is saturable at higher doses, at which the unbound fraction of the drug increases disproportionately.3 In healthy young adults, the protein binding of ertapenem decreased as drug plasma concentrations increased. At an approximate plasma concentration of <100 micrograms (mcg)/mL, ertapenem was 95% bound, and this percentage dropped to 85% when the plasma concentration increased to 300 mcg/mL.5
- Metabolism
In healthy young adults, unchanged ertapenem accounted for most plasma radioactivity.5 The major metabolite of ertapenem is the ring-opened derivative formed by dehydropeptidase I-mediated hydrolysis of the beta-lactam ring.4,6 This metabolite is pharmacologically inactive.5 Dehydropeptidase I (DHP-I) is found predominantly in the kidneys.1 Hepatic metabolism is negligible.3
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- Route of elimination
Ertapenem predominantly undergoes renal elimination, where it undergoes glomerular filtration and net tubular secretion.1 In healthy young adults who received one gram of IV radiolabeled ertapenem, approximately 80% of the radioactivity was recovered in urine and 10% of the radioactivity was recovered in feces. The mean percentage of the administered dose excreted in urine was 17.4% during 0-2 hours postdose, 5.4% during 4-6 hours postdose, and 2.4% during 12-24 hours postdose.5
Of the 80% radioactivity in urine, about 38% accounted for unchanged ertapenem and 37% accounted for its ring-opened metabolite.5
- Half-life
The mean plasma half-life was approximately four hours in healthy young adults and adolescents and approximately 2.5 hours in children three to 12 years of age.5 The long half-life of ertapenem can be explained by its high protein binding.2
- Clearance
The mean plasma clearance in healthy young adults was approximately 1.8 L/hour.5 The mean renal clearance of intact ertapenem was 12.8 mL/min compared with a total clearance of 28.4 mL/min.1
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
The oral median lethal dose (LD50) in mouse is >500 mg/kg.7
Intravenous administration of ertapenem at a dose of 2 g over 30 min or 3 g over 1-2 hours in healthy adults resulted in increased incidence of nausea. In clinical trials in adults, inadvertent administration of three 1 g doses of ertapenem in a 24 hour period resulted in diarrhea and transient dizziness in one patient. As there is no known antidote for ertapenem overdose, the drug should be discontinued with the initiation of general supportive treatment until renal elimination takes place. Ertapenem can be removed by hemodialysis to some extent: the plasma clearance of the total fraction of ertapenem was increased by 30% in subjects with end-stage renal disease when hemodialysis was performed immediately following administration. However, no information is available on the use of hemodialysis to treat ertapenem overdosage.5
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbacavir Ertapenem may decrease the excretion rate of Abacavir which could result in a higher serum level. Aceclofenac Aceclofenac may decrease the excretion rate of Ertapenem which could result in a higher serum level. Acemetacin Acemetacin may decrease the excretion rate of Ertapenem which could result in a higher serum level. Acenocoumarol The risk or severity of bleeding can be increased when Ertapenem is combined with Acenocoumarol. Acetaminophen Ertapenem may decrease the excretion rate of Acetaminophen which could result in a higher serum level. Acetazolamide Acetazolamide may increase the excretion rate of Ertapenem which could result in a lower serum level and potentially a reduction in efficacy. Acetylsalicylic acid Acetylsalicylic acid may decrease the excretion rate of Ertapenem which could result in a higher serum level. Aclidinium Ertapenem may decrease the excretion rate of Aclidinium which could result in a higher serum level. Acrivastine Ertapenem may decrease the excretion rate of Acrivastine which could result in a higher serum level. Acyclovir Acyclovir may decrease the excretion rate of Ertapenem which could result in a higher serum level. 
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- No interactions found.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Ertapenem sodium 2T90KE67L0 153773-82-1 ZXNAQFZBWUNWJM-HRXMHBOMSA-M - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Ertapenem Injection, powder, lyophilized, for solution 1 g/1 Intramuscular; Intravenous Par Pharmaceutical Inc. 2018-11-01 Not applicable US 
Ertapenem for Injection Powder, for solution 1 g / vial Intramuscular; Intravenous Mantra Pharma Inc Not applicable Not applicable Canada 
Ertapenem for Injection Powder, for solution 1 g / vial Intramuscular; Intravenous Fresenius Kabi 2021-06-07 Not applicable Canada Ertapenem for Injection Powder, for solution 1 g / vial Intramuscular; Intravenous Dr Reddy's Laboratories Ltd 2021-01-27 Not applicable Canada Ertapenem for Injection Powder, for solution 1 g / vial Intramuscular; Intravenous Omega Laboratories Limited Not applicable Not applicable Canada Ertapenem for Injection Powder, for solution 1 g / vial Intramuscular; Intravenous Auro Pharma Inc 2021-10-08 Not applicable Canada Ertapenem for Injection Powder, for solution 1 g / vial Intramuscular; Intravenous Hikma Canada Limited Not applicable Not applicable Canada Ertapenem for Injection Powder, for solution 1 g / vial Intramuscular; Intravenous Eugia Pharma Inc. Not applicable Not applicable Canada Ertapenem for Injection Powder, for solution 1 g / vial Intramuscular; Intravenous Juno Pharmaceuticals Corp. 2020-02-10 Not applicable Canada Ertapenem Sun Injection, powder, for solution 1 g Intravenous Sun Pharmaceutical Industries (Europe) B.V. 2022-12-02 Not applicable EU 
- Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Ertapenem Injection 1 g/20mL Intramuscular; Intravenous Savior Lifetec Corporation 2019-03-19 Not applicable US Ertapenem Injection, powder, lyophilized, for solution 1 g/1 Intramuscular; Intravenous Fosun Pharma USA Inc 2021-11-01 Not applicable US Ertapenem Injection, powder, lyophilized, for solution 1 g/1 Intramuscular; Intravenous Hospira, Inc. 2020-10-19 Not applicable US Ertapenem Injection, powder, lyophilized, for solution 1 g/1 Intramuscular; Intravenous Fresenius Kabi USA, LLC 2019-10-10 Not applicable US Ertapenem Injection 1 g/1 Intramuscular; Intravenous Eugia US LLC 2018-06-25 Not applicable US Ertapenem Injection, powder, lyophilized, for solution 1 g/1 Intramuscular; Intravenous WG Critical Care, LLC 2020-01-07 Not applicable US Ertapenem Injection 1 g/20mL Intramuscular; Intravenous Apotex Corp 2019-04-02 Not applicable US Ertapenem Injection, powder, lyophilized, for solution 1 g/1 Intramuscular; Intravenous Gland Pharma Limited 2021-03-26 Not applicable US Ertapenem Injection 1 g/20mL Intramuscular; Intravenous BluePoint Laboratories 2019-08-29 Not applicable US Ertapenem Sodium Injection, powder, lyophilized, for solution 1 g/1 Intramuscular; Intravenous Dr.Reddys Laboratories Inc., 2021-04-29 Not applicable US
Categories
- ATC Codes
- J01DH03 — Ertapenem
- Drug Categories
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as thienamycins. These are beta-lactam antibiotics that differ from penicillins in having the thiazolidine sulfur atom replaced by carbon, the sulfur then becoming the first atom in the side chain.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Lactams
- Sub Class
- Beta lactams
- Direct Parent
- Thienamycins
- Alternative Parents
- Acylaminobenzoic acid and derivatives / Proline and derivatives / Alpha amino acid amides / Anilides / Benzoic acids / Pyrroline carboxylic acids / Pyrrolidinecarboxamides / Benzoyl derivatives / N-arylamides / Azepines show 16 more
- Substituents
- Acylaminobenzoic acid or derivatives / Alcohol / Alpha-amino acid amide / Alpha-amino acid or derivatives / Amine / Amino acid / Amino acid or derivatives / Anilide / Aromatic heteropolycyclic compound / Azacycle show 37 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- pyrrolidinecarboxamide, carbapenemcarboxylic acid (CHEBI:404903)
- Affected organisms
- Enteric bacteria and other eubacteria
- Streptococcus pyogenes
- Streptococcus pneumoniae
- Streptococcus agalactiae
- Haemophilus influenzae
- Escherichia coli
- Staphylococcus aureus
- Moraxella catarrhalis
- Proteus mirabilis
- Bacteroides fragilis
- Peptostreptococcus
- Klebsiella pneumoniae
- Bacteroides thetaiotaomicron
- Bacteroides ovatus
- Bacteroides uniformis
- Parabacteroides distasonis
- Eubacterium spp.
- Clostridium clostridioforme
- Prevotella bivia
- Porphyromonas asaccharolytica
Chemical Identifiers
- UNII
- G32F6EID2H
- CAS number
- 153832-46-3
- InChI Key
- JUZNIMUFDBIJCM-ANEDZVCMSA-N
- InChI
- InChI=1S/C22H25N3O7S/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)/t9-,10-,13+,14+,15-,16-/m1/s1
- IUPAC Name
- (4R,5S,6S)-3-{[(3S,5S)-5-[(3-carboxyphenyl)carbamoyl]pyrrolidin-3-yl]sulfanyl}-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid
- SMILES
- [H][C@]12[C@@H](C)C(S[C@]3([H])CN[C@@]([H])(C3)C(=O)NC3=CC=CC(=C3)C(O)=O)=C(N1C(=O)[C@]2([H])[C@@H](C)O)C(O)=O
References
- Synthesis Reference
Ying Shi, Kun Li, Zan Xie, Xuebin Zhao, Jian Lv, Xiuqin Yu, "INTERMEDIATE OF ERTAPENEM, A COMPOSITION COMPRISING THE SAME AND PREPARATION METHODS THEREOF." U.S. Patent US20120095209, issued April 19, 2012.
US20120095209- General References
- Nix DE, Majumdar AK, DiNubile MJ: Pharmacokinetics and pharmacodynamics of ertapenem: an overview for clinicians. J Antimicrob Chemother. 2004 Jun;53 Suppl 2:ii23-8. [Article]
- Odenholt I: Ertapenem: a new carbapenem. Expert Opin Investig Drugs. 2001 Jun;10(6):1157-66. [Article]
- Congeni BL: Ertapenem. Expert Opin Pharmacother. 2010 Mar;11(4):669-72. doi: 10.1517/14656561003631397. [Article]
- Curran M, Simpson D, Perry C: Ertapenem: a review of its use in the management of bacterial infections. Drugs. 2003;63(17):1855-78. doi: 10.2165/00003495-200363170-00006. [Article]
- FDA Approved Drug Products: INVANZ (ertapenem) injection, for intravenous or intramuscular use [Link]
- EMA Approved Drug Products: Ertapenem SUN (ertapenem) Intravenous Infusion [Link]
- Merck: Ertapenem MSDS [Link]
- External Links
- Human Metabolome Database
- HMDB0014448
- KEGG Drug
- D07908
- PubChem Compound
- 150610
- PubChem Substance
- 46506508
- ChemSpider
- 132758
- 325642
- ChEBI
- 404903
- ChEMBL
- CHEMBL1359
- ZINC
- ZINC000003918453
- Therapeutic Targets Database
- DAP000431
- PharmGKB
- PA164777032
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Ertapenem
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Not Available Acute Renal Failure (ARF) 1 4 Completed Not Available Continuous ambulatory peritoneal dialysis therapy / End Stage Renal Disease (ESRD) 1 4 Completed Not Available Healthy Subjects (HS) 1 4 Completed Not Available Infection 1 4 Completed Prevention Benign Prostatic Hyperplasia (BPH) Requiring Surgical Resection 1 4 Completed Treatment Burn Patients 1 4 Completed Treatment Colon Neoplasm / Diverticulosis, Colonic / Rectal Neoplasms 1 4 Completed Treatment Complicated Intra-Abdominal Infections (cIAIs) 1 4 Completed Treatment Intraabdominal Infections 1 4 Completed Treatment Liver Abscess, Pyogenic 1
Pharmacoeconomics
- Manufacturers
- Merck and co inc
- Packagers
- Merck & Co.
- Dosage Forms
Form Route Strength Injection Intramuscular; Intravenous 1 g/20mL Injection Intramuscular; Intravenous 1 g/1 Injection, powder, lyophilized, for solution Intramuscular; Intravenous 1 g/1 Injection, powder, for solution Parenteral Injection, powder, for solution Intravenous 1 g/vial Injection, powder, for solution Injection, powder, for solution Intravenous Injection, powder, lyophilized, for solution Intravenous drip 1 G/VIAL Injection, powder, lyophilized, for solution Intravenous 1 g Powder Not applicable 1 kg/1kg Solution Intravenous 1.292 g Injection, powder, for solution 1213 mg Injection, powder, for solution Intravenous 1 g Injection, powder, for solution Intravenous; Parenteral 1 G Injection, powder, lyophilized, for solution Intravenous 1 g/1 Powder, for solution Intramuscular; Intravenous 1 g / vial Solution Parenteral 1.000 g Injection, powder, for solution Intramuscular; Intravenous 1 g Injection Intramuscular; Intravenous 1 g Injection, powder, lyophilized, for solution Intramuscular; Intravenous 1 g Solution Intravenous 1.046 g - Prices
Unit description Cost Unit Invanz 1 gm add-vantage vial 72.85USD vial Invanz 1 gm vial 69.4USD vial DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US5652233 No 1997-07-29 2013-02-02 US CA2106370 No 2003-11-25 2013-02-02 Canada US5478820 Yes 1995-12-26 2016-05-21 US US5952323 Yes 1999-09-14 2017-11-15 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 230-234 https://www.fishersci.com/store/msds?partNumber=AC460640010&productDescription=ERTAPENEM+SODIUM%2C+85%25+1GR&vendorId=VN00032119&countryCode=US&language=en logP 0.3 Not Available - Predicted Properties
Property Value Source Water Solubility 0.286 mg/mL ALOGPS logP -0.2 ALOGPS logP -3.2 Chemaxon logS -3.2 ALOGPS pKa (Strongest Acidic) 3.22 Chemaxon pKa (Strongest Basic) 9.03 Chemaxon Physiological Charge -1 Chemaxon Hydrogen Acceptor Count 8 Chemaxon Hydrogen Donor Count 5 Chemaxon Polar Surface Area 156.27 Å2 Chemaxon Rotatable Bond Count 7 Chemaxon Refractivity 121.8 m3·mol-1 Chemaxon Polarizability 48.77 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.5982 Blood Brain Barrier - 0.9811 Caco-2 permeable - 0.7052 P-glycoprotein substrate Substrate 0.7716 P-glycoprotein inhibitor I Non-inhibitor 0.917 P-glycoprotein inhibitor II Non-inhibitor 0.9955 Renal organic cation transporter Non-inhibitor 0.9253 CYP450 2C9 substrate Non-substrate 0.7891 CYP450 2D6 substrate Non-substrate 0.8229 CYP450 3A4 substrate Non-substrate 0.5 CYP450 1A2 substrate Non-inhibitor 0.8677 CYP450 2C9 inhibitor Non-inhibitor 0.867 CYP450 2D6 inhibitor Non-inhibitor 0.8964 CYP450 2C19 inhibitor Non-inhibitor 0.8511 CYP450 3A4 inhibitor Non-inhibitor 0.9658 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9695 Ames test Non AMES toxic 0.6766 Carcinogenicity Non-carcinogens 0.8052 Biodegradation Not ready biodegradable 0.9821 Rat acute toxicity 2.0803 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9947 hERG inhibition (predictor II) Non-inhibitor 0.8848
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS Not Available Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
Targets
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- Kind
- Protein
- Organism
- Escherichia coli (strain K12)
- Pharmacological action
- Yes
- Actions
- Inhibitor
- Curator comments
- The above was chosen as a representative target protein in a representative bacterium, and does not encompass all proteins/bacteria affected by this agent.
- General Function
- Serine-type d-ala-d-ala carboxypeptidase activity
- Specific Function
- Cell wall formation. Synthesis of cross-linked peptidoglycan from the lipid intermediates. The enzyme has a penicillin-insensitive transglycosylase N-terminal domain (formation of linear glycan str...
- Gene Name
- mrcA
- Uniprot ID
- P02918
- Uniprot Name
- Penicillin-binding protein 1A
- Molecular Weight
- 93635.545 Da
References
- Kohler J, Dorso KL, Young K, Hammond GG, Rosen H, Kropp H, Silver LL: In vitro activities of the potent, broad-spectrum carbapenem MK-0826 (L-749,345) against broad-spectrum beta-lactamase-and extended-spectrum beta-lactamase-producing Klebsiella pneumoniae and Escherichia coli clinical isolates. Antimicrob Agents Chemother. 1999 May;43(5):1170-6. [Article]
- Curran M, Simpson D, Perry C: Ertapenem: a review of its use in the management of bacterial infections. Drugs. 2003;63(17):1855-78. doi: 10.2165/00003495-200363170-00006. [Article]
- Congeni BL: Ertapenem. Expert Opin Pharmacother. 2010 Mar;11(4):669-72. doi: 10.1517/14656561003631397. [Article]
- FDA Approved Drug Products: INVANZ (ertapenem) injection, for intravenous or intramuscular use [Link]
- Kind
- Protein
- Organism
- Escherichia coli (strain K12)
- Pharmacological action
- Yes
- Actions
- Inhibitor
- Curator comments
- The above was chosen as a representative target protein in a representative bacterium, and does not encompass all proteins/bacteria affected by this agent.
- General Function
- Serine-type d-ala-d-ala carboxypeptidase activity
- Specific Function
- Cell wall formation. Synthesis of cross-linked peptidoglycan from the lipid intermediates. The enzyme has a penicillin-insensitive transglycosylase N-terminal domain (formation of linear glycan str...
- Gene Name
- mrcB
- Uniprot ID
- P02919
- Uniprot Name
- Penicillin-binding protein 1B
- Molecular Weight
- 94291.875 Da
References
- Kohler J, Dorso KL, Young K, Hammond GG, Rosen H, Kropp H, Silver LL: In vitro activities of the potent, broad-spectrum carbapenem MK-0826 (L-749,345) against broad-spectrum beta-lactamase-and extended-spectrum beta-lactamase-producing Klebsiella pneumoniae and Escherichia coli clinical isolates. Antimicrob Agents Chemother. 1999 May;43(5):1170-6. [Article]
- Congeni BL: Ertapenem. Expert Opin Pharmacother. 2010 Mar;11(4):669-72. doi: 10.1517/14656561003631397. [Article]
- Curran M, Simpson D, Perry C: Ertapenem: a review of its use in the management of bacterial infections. Drugs. 2003;63(17):1855-78. doi: 10.2165/00003495-200363170-00006. [Article]
- FDA Approved Drug Products: INVANZ (ertapenem) injection, for intravenous or intramuscular use [Link]
- Kind
- Protein
- Organism
- Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd)
- Pharmacological action
- Yes
- Actions
- Inhibitor
- Curator comments
- The above was chosen as a representative target protein in a representative bacterium, and does not encompass all proteins/bacteria affected by this agent.
- General Function
- Penicillin binding
- Specific Function
- Cell wall formation; PBP-2 is responsible for the determination of the rod shape of the cell. Its synthesize cross-linked peptidoglycan from the lipid intermediates (By similarity).
- Gene Name
- mrdA
- Uniprot ID
- P44469
- Uniprot Name
- Penicillin-binding protein 2
- Molecular Weight
- 73812.47 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
- Odenholt I: Ertapenem: a new carbapenem. Expert Opin Investig Drugs. 2001 Jun;10(6):1157-66. [Article]
- Kohler J, Dorso KL, Young K, Hammond GG, Rosen H, Kropp H, Silver LL: In vitro activities of the potent, broad-spectrum carbapenem MK-0826 (L-749,345) against broad-spectrum beta-lactamase-and extended-spectrum beta-lactamase-producing Klebsiella pneumoniae and Escherichia coli clinical isolates. Antimicrob Agents Chemother. 1999 May;43(5):1170-6. [Article]
- FDA Approved Drug Products: INVANZ (ertapenem) injection, for intravenous or intramuscular use [Link]
- Kind
- Protein
- Organism
- Escherichia coli (strain K12)
- Pharmacological action
- Yes
- Actions
- Inhibitor
- Curator comments
- The above was chosen as a representative target protein in a representative bacterium, and does not encompass all proteins/bacteria affected by this agent.
- General Function
- Serine-type d-ala-d-ala carboxypeptidase activity
- Specific Function
- Cell wall formation; PBP-2 is responsible for the determination of the rod shape of the cell. It synthesizes cross-linked peptidoglycan from lipid intermediates.
- Gene Name
- mrdA
- Uniprot ID
- P0AD65
- Uniprot Name
- Penicillin-binding protein 2
- Molecular Weight
- 70856.1 Da
References
- Kohler J, Dorso KL, Young K, Hammond GG, Rosen H, Kropp H, Silver LL: In vitro activities of the potent, broad-spectrum carbapenem MK-0826 (L-749,345) against broad-spectrum beta-lactamase-and extended-spectrum beta-lactamase-producing Klebsiella pneumoniae and Escherichia coli clinical isolates. Antimicrob Agents Chemother. 1999 May;43(5):1170-6. [Article]
- Curran M, Simpson D, Perry C: Ertapenem: a review of its use in the management of bacterial infections. Drugs. 2003;63(17):1855-78. doi: 10.2165/00003495-200363170-00006. [Article]
- FDA Approved Drug Products: INVANZ (ertapenem) injection, for intravenous or intramuscular use [Link]
- Kind
- Protein
- Organism
- Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd)
- Pharmacological action
- Yes
- Actions
- Inhibitor
- Curator comments
- The above was chosen as a representative target protein in a representative bacterium, and does not encompass all proteins/bacteria affected by this agent.
- General Function
- Peptidoglycan glycosyltransferase activity
- Specific Function
- Essential cell division protein that is required for the synthesis of peptidoglycan at the division septum. Catalyzes the synthesis of cross-linked peptidoglycan from the lipid-linked precursors.
- Gene Name
- ftsI
- Uniprot ID
- P45059
- Uniprot Name
- Peptidoglycan synthase FtsI
- Molecular Weight
- 67165.845 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
- Kohler J, Dorso KL, Young K, Hammond GG, Rosen H, Kropp H, Silver LL: In vitro activities of the potent, broad-spectrum carbapenem MK-0826 (L-749,345) against broad-spectrum beta-lactamase-and extended-spectrum beta-lactamase-producing Klebsiella pneumoniae and Escherichia coli clinical isolates. Antimicrob Agents Chemother. 1999 May;43(5):1170-6. [Article]
- Curran M, Simpson D, Perry C: Ertapenem: a review of its use in the management of bacterial infections. Drugs. 2003;63(17):1855-78. doi: 10.2165/00003495-200363170-00006. [Article]
- FDA Approved Drug Products: INVANZ (ertapenem) injection, for intravenous or intramuscular use [Link]
- Kind
- Protein
- Organism
- Escherichia coli (strain K12)
- Pharmacological action
- Yes
- Actions
- Inhibitor
- Curator comments
- The above was chosen as a representative target protein in a representative bacterium, and does not encompass all proteins/bacteria affected by this agent.
- General Function
- Peptidoglycan glycosyltransferase activity
- Specific Function
- Essential cell division protein that is required for the synthesis of peptidoglycan at the division septum (PubMed:1103132, PubMed:9614966). Catalyzes the synthesis of cross-linked peptidoglycan fr...
- Gene Name
- ftsI
- Uniprot ID
- P0AD68
- Uniprot Name
- Peptidoglycan synthase FtsI
- Molecular Weight
- 63876.925 Da
References
- Kohler J, Dorso KL, Young K, Hammond GG, Rosen H, Kropp H, Silver LL: In vitro activities of the potent, broad-spectrum carbapenem MK-0826 (L-749,345) against broad-spectrum beta-lactamase-and extended-spectrum beta-lactamase-producing Klebsiella pneumoniae and Escherichia coli clinical isolates. Antimicrob Agents Chemother. 1999 May;43(5):1170-6. [Article]
- Curran M, Simpson D, Perry C: Ertapenem: a review of its use in the management of bacterial infections. Drugs. 2003;63(17):1855-78. doi: 10.2165/00003495-200363170-00006. [Article]
- FDA Approved Drug Products: INVANZ (ertapenem) injection, for intravenous or intramuscular use [Link]
- Kind
- Protein
- Organism
- Escherichia coli (strain K12)
- Pharmacological action
- Yes
- Actions
- Inhibitor
- Curator comments
- The above was chosen as a representative target protein in a representative bacterium, and does not encompass all proteins/bacteria affected by this agent.
- General Function
- Serine-type d-ala-d-ala carboxypeptidase activity
- Specific Function
- Not involved in transpeptidation but exclusively catalyzes a DD-carboxypeptidase and DD-endopeptidase reaction.
- Gene Name
- dacB
- Uniprot ID
- P24228
- Uniprot Name
- D-alanyl-D-alanine carboxypeptidase DacB
- Molecular Weight
- 51797.85 Da
References
- Kohler J, Dorso KL, Young K, Hammond GG, Rosen H, Kropp H, Silver LL: In vitro activities of the potent, broad-spectrum carbapenem MK-0826 (L-749,345) against broad-spectrum beta-lactamase-and extended-spectrum beta-lactamase-producing Klebsiella pneumoniae and Escherichia coli clinical isolates. Antimicrob Agents Chemother. 1999 May;43(5):1170-6. [Article]
- Curran M, Simpson D, Perry C: Ertapenem: a review of its use in the management of bacterial infections. Drugs. 2003;63(17):1855-78. doi: 10.2165/00003495-200363170-00006. [Article]
- FDA Approved Drug Products: INVANZ (ertapenem) injection, for intravenous or intramuscular use [Link]
- Kind
- Protein
- Organism
- Escherichia coli (strain K12)
- Pharmacological action
- Yes
- Actions
- Inhibitor
- Curator comments
- The above was chosen as a representative target protein in a representative bacterium, and does not encompass all proteins/bacteria affected by this agent.
- General Function
- Serine-type d-ala-d-ala carboxypeptidase activity
- Specific Function
- Removes C-terminal D-alanyl residues from sugar-peptide cell wall precursors.
- Gene Name
- dacC
- Uniprot ID
- P08506
- Uniprot Name
- D-alanyl-D-alanine carboxypeptidase DacC
- Molecular Weight
- 43608.595 Da
References
- Kohler J, Dorso KL, Young K, Hammond GG, Rosen H, Kropp H, Silver LL: In vitro activities of the potent, broad-spectrum carbapenem MK-0826 (L-749,345) against broad-spectrum beta-lactamase-and extended-spectrum beta-lactamase-producing Klebsiella pneumoniae and Escherichia coli clinical isolates. Antimicrob Agents Chemother. 1999 May;43(5):1170-6. [Article]
- Curran M, Simpson D, Perry C: Ertapenem: a review of its use in the management of bacterial infections. Drugs. 2003;63(17):1855-78. doi: 10.2165/00003495-200363170-00006. [Article]
- FDA Approved Drug Products: INVANZ (ertapenem) injection, for intravenous or intramuscular use [Link]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Zinc ion binding
- Specific Function
- Hydrolyzes a wide range of dipeptides. Implicated in the renal metabolism of glutathione and its conjugates. Converts leukotriene D4 to leukotriene E4; it may play an important role in the regulati...
- Gene Name
- DPEP1
- Uniprot ID
- P16444
- Uniprot Name
- Dipeptidase 1
- Molecular Weight
- 45673.48 Da
References
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Binder
- General Function
- Toxic substance binding
- Specific Function
- Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
- Gene Name
- ALB
- Uniprot ID
- P02768
- Uniprot Name
- Serum albumin
- Molecular Weight
- 69365.94 Da
References
- FDA Approved Drug Products: INVANZ (ertapenem) injection, for intravenous or intramuscular use [Link]
Drug created at June 13, 2005 13:24 / Updated at September 21, 2023 08:43