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Netilmicin | CAS No: 56391-56-1 | GMP-certified suppliers
A medication that treats serious aerobic Gram-negative bacterial infections such as bacteremia, respiratory, skin, soft tissue, burns, wounds, and peri-operative infections with reduced nephrotoxicity.
Therapeutic categories
Primary indications
- For the treatment of bacteremia, septicaemia, respiratory tract infections, skin and soft-tissue infection, burns, wounds, and peri-operative infections caused by susceptible strains
Product Snapshot
- Netilmicin is available as injectable and ophthalmic solutions, including parenteral formulations
- It is primarily utilized for the treatment of bacterial infections such as bacteremia, respiratory tract infections, and skin and soft tissue infections
- The product holds approval status in the Canadian market and includes both approved and investigational designations
Clinical Overview
Clinically, netilmicin is indicated for the treatment of serious infections caused by susceptible aerobic Gram-negative bacteria. These include bacteremia, septicaemia, respiratory tract infections, skin and soft tissue infections, burns, wounds, and peri-operative infections. It demonstrates potent in vitro activity against pathogens such as Escherichia coli, Klebsiella-Enterobacter-Serratia group, Proteus species including P. mirabilis, Pseudomonas aeruginosa, Neisseria gonorrhoeae, Hemophilus influenzae, Salmonella, Shigella, and both penicillinase-producing and non-penicillinase-producing Staphylococcus strains, including some methicillin-resistant variants.
The antibacterial effect of netilmicin arises from irreversible binding to the bacterial 30S ribosomal subunit. Specifically, netilmicin targets nucleotides within the 16S rRNA and the protein S12 component, disrupting the decoding site. This interferes with the initiation complex for protein synthesis, causing misreading of mRNA, insertion of incorrect amino acids, production of aberrant polypeptides, and disruption of polysome integrity. The resulting inhibition of protein synthesis leads to bacterial cell death.
Pharmacodynamically, netilmicin is effective primarily against aerobic Gram-negative organisms and exhibits synergy with beta-lactam antibiotics such as penicillin G, carbenicillin, and ticarcillin against certain strains. It is ineffective against anaerobic bacteria, fungi, and viruses.
Netilmicin is administered parenterally and is predominantly eliminated unchanged via the kidneys, necessitating careful dosing and monitoring due to its narrow therapeutic index and potential nephrotoxicity. Safety considerations include ototoxicity, nephrotoxicity, and neuromuscular blockade risks, especially at elevated plasma concentrations or in patients with renal impairment.
Notable clinical use of netilmicin includes treatment of infections resistant to other aminoglycosides and in settings requiring alternatives to gentamicin. It is marketed under various brand names globally, primarily in injectable formulations.
For API procurement, sourcing netilmicin requires adherence to stringent quality standards, including compliance with pharmacopoeial monographs and validation of manufacturing processes to ensure purity, consistent potency, and absence of impurities. Given its narrow therapeutic index and toxicity profile, stringent control of impurity levels and verification of physicochemical properties are critical to ensure clinical safety and efficacy.
Identification & chemistry
| Generic name | Netilmicin |
|---|---|
| Molecule type | Small molecule |
| CAS | 56391-56-1 |
| UNII | 4O5J85GJJB |
| DrugBank ID | DB00955 |
Pharmacology
| Summary | Netilmicin is an aminoglycoside antibiotic that targets the 30S ribosomal subunit by irreversibly binding to protein S12 and 16S rRNA, disrupting bacterial protein synthesis through interference with mRNA decoding. It exhibits bactericidal activity primarily against aerobic, Gram-negative pathogens and some Gram-positive bacteria, including strains resistant to other aminoglycosides. Its mechanism induces production of nonfunctional or toxic peptides, impairing bacterial growth and survival. |
|---|---|
| Mechanism of action | Aminoglycosides like netilmicin "irreversibly" bind to specific 30S-subunit proteins and 16S rRNA. Specifically netilmicin binds to four nucleotides of 16S rRNA and a single amino acid of protein S12. This interferes with decoding site in the vicinity of nucleotide 1400 in 16S rRNA of 30S subunit. This region interacts with the wobble base in the anticodon of tRNA. This leads to interference with the initiation complex, misreading of mRNA so incorrect amino acids are inserted into the polypeptide leading to nonfunctional or toxic peptides and the breakup of polysomes into nonfunctional monosomes, leaving the bacterium unable to synthesize proteins vital to its growth. |
| Pharmacodynamics | Netilmicin is a semisynthetic, water soluble antibiotic of the aminoglycoside group, produced by the fermentation of Micromonospora inyoensis, a species of actinomycete. Aminoglycosides are useful primarily in infections involving aerobic, Gram-negative bacteria, such as Pseudomonas, Acinetobacter, and Enterobacter. It is active at low concentrations against a wide variety of pathogenic bacteria including <i>Escherichia coli</i>, bacteria of the <i>Klebsiella-Enterobacter-Serratia </i>group, <i>Citrobacter </i>sp., <i>Proteus </i>sp. (indole-positive and indole-negative), including <i>Proteus mirabilis</i>, <i>P. morganii, P. rettgrei, P. vulgaris, Pseudomonas aeruginosa </i>and <i>Neisseria gonorrhoea</i>. Netilmicin is also active <i>in vitro </i>against isolates of <i>Hemophilus influenzae, Salmonella </i>sp., <i>Shigella </i>sp. and against penicillinase and non-penicillinase-producing <i>Staphylococcus </i>including methicillin-resistant strains. Some strains of <i>Providencia </i>sp., <i>Acinetobacter </i>sp. and <i>Aeromonas </i>sp. are also sensitive to netilmicin. Many strains of the above organisms which are found to be resistant to other aminoglycosides, such as kanamycin, gentamicin, tobramycin and sisomicin, are susceptible to netilmicin <i>in vitro</i>. Occasionally, strains have been identified which are resistant to amikacin but susceptible to netilmicin. The combination of netilmicin and penicillin G has a synergistic bactericidal effect against most strains of <i>Streptococcus faecalis</i> (enterococcus). The combined effect of netilmicin and carbenicillin or ticarcillin is synergistic for many strains of <i>Pseudomonas aeruginosa</i>. In addition, many isolates of <i>Serratia</i>, which are resistant to multiple antibiotics, are inhibited by synergistic combinations of netilmicin with carbenicillin, azlocillin, mezlocillin, cefamandole, cefotaxime or moxalactam. Aminoglycosides are mostly ineffective against anaerobic bacteria, fungi and viruses. |
Targets
| Target | Organism | Actions |
|---|---|---|
| 30S ribosomal protein S12 | Escherichia coli (strain K12) | inhibitor |
| 16S ribosomal RNA | Enteric bacteria and other eubacteria | inhibitor |
ADME / PK
| Absorption | Rapidly and completely absorbed after IM administration, peak serum levels were achieved within 30-60 minutes. Aminoglycosides are poorly absorbed orally. Topical absorption is also poor unless severe skin damage is present. |
|---|---|
| Half-life | 2.5 hours |
| Protein binding | Protein-binding of is low and depends on the test conditions (mainly the concentration of cations in the test medium). |
| Metabolism | No evidence of metabolic transformation, typically 80% is recoverable in the urine within 24 hours |
Formulation & handling
- Netilmicin is a small molecule aminoglycoside antibiotic primarily formulated for parenteral administration via intramuscular or intravenous injection.
- It is also available in ophthalmic formulations for topical use on the conjunctiva.
- Due to its hydrophilic nature and water solubility, parenteral formulations require careful handling to maintain stability and avoid degradation.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient (API) has experienced patent expiry in Canada, allowing for generic competition and a mature market landscape characterized by established product availability. |
|---|
| Markets | Canada |
|---|
Supply Chain
| Supply chain summary | Netilmicin is primarily manufactured by originator companies such as Schering Corp under Schering Plough Corp, with branded products available in the Canadian market. The presence of multiple branded formulations, including Netildex and Netromycin injections, indicates established market offerings. Patent expiration status is not specified, but the availability of generics would depend on local regulatory approvals and market demand. |
|---|
Safety
| Toxicity | Netilmicin has nephrotoxic and ototoxic potential. Nephrotoxicity occurs via drug accumulation in renal proximal tubular cells resulting in cellular damage. Tubular cells may regenerate despite continued exposure and nephrotoxicity is usually mild and reversible. Netilmicin is less nephrotoxic than neomycin, gentamicin, tobramycin, and amikacin, likely due to a reduced number of cationic amino groups in its structure. Otoxicity occurs as a result of irreversible damage to hair cells of the cochlea and/or summit of the ampullar cristae in the vestibular complex caused drug accumulation in the endolymph and perilymph of the inner ear. Otoxicity appears to be correlated to total exposure and may be cumulative with further doses of aminoglycosides or other ototoxic drugs (e.g. cisplatin, furosemide). High frequency hearing loss is followed by low frequency hearing loss, which may be followed by retrograde degeneration of the auditory nerve. Vestibular toxicity may cause vertigo, nausea and vomiting, dizziness and loss of balance. |
|---|
- Netilmicin exhibits nephrotoxicity due to accumulation in renal proximal tubular cells
- Effects are generally mild and reversible
- Ototoxicity results from accumulation in inner ear fluids causing irreversible cochlear and vestibular hair cell damage
Netilmicin is a type of Aminoglycosides
Aminoglycosides are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that play a crucial role in combating bacterial infections. These powerful antibiotics are primarily used to treat severe infections caused by gram-negative bacteria. Aminoglycosides are characterized by their unique chemical structure, consisting of amino sugars and a glycosidic bond.
These antibiotics exert their therapeutic effects by inhibiting bacterial protein synthesis, leading to the disruption of essential cellular functions in the bacteria. This mechanism of action makes aminoglycosides highly effective against a wide range of bacteria, including those that have developed resistance to other classes of antibiotics.
Key examples of aminoglycosides include gentamicin, amikacin, and tobramycin. These drugs are typically administered intravenously or intramuscularly to ensure optimal absorption and distribution throughout the body. Due to their limited oral bioavailability, aminoglycosides are not commonly administered orally.
Although aminoglycosides possess potent antimicrobial properties, they are associated with some potential adverse effects, including nephrotoxicity and ototoxicity. Regular monitoring of kidney function and therapeutic drug monitoring are often recommended during aminoglycoside therapy to minimize the risk of these complications.
In summary, aminoglycosides are an important subcategory of pharmaceutical APIs that have significant therapeutic value in the treatment of severe bacterial infections. Their unique mechanism of action and broad spectrum of activity make them valuable tools in the fight against antibiotic-resistant bacteria.
Netilmicin (Aminoglycosides), classified under Antibacterials
Antibacterials, a category of pharmaceutical active pharmaceutical ingredients (APIs), play a crucial role in combating bacterial infections. These APIs are chemical compounds that target and inhibit the growth or kill bacteria, helping to eliminate harmful bacterial pathogens from the body.
Antibacterials are essential for the treatment of various bacterial infections, including respiratory tract infections, urinary tract infections, skin and soft tissue infections, and more. They are commonly prescribed by healthcare professionals to combat both mild and severe bacterial infections.
Within the category of antibacterials, there are different classes and subclasses of APIs, each with distinct mechanisms of action and target bacteria. Some commonly used antibacterials include penicillins, cephalosporins, tetracyclines, macrolides, and fluoroquinolones. These APIs work by interfering with various aspects of bacterial cellular processes, such as cell wall synthesis, protein synthesis, DNA replication, or enzyme activity.
The development and production of antibacterial APIs require stringent quality control measures to ensure their safety, efficacy, and purity. Pharmaceutical manufacturers must adhere to Good Manufacturing Practices (GMP) and follow rigorous testing protocols to guarantee the quality and consistency of these APIs.
As bacterial resistance to antibiotics continues to be a significant concern, ongoing research and development efforts aim to discover and develop new antibacterial APIs. The evolution of antibacterials plays a crucial role in combating emerging bacterial strains and ensuring effective treatment options for infectious diseases.
In summary, antibacterials are a vital category of pharmaceutical APIs used to treat bacterial infections. They are designed to inhibit or kill bacteria, and their development requires strict adherence to quality control standards. By continually advancing research in this field, scientists and pharmaceutical companies can contribute to the ongoing battle against bacterial infections.
Netilmicin API manufacturers & distributors
Compare qualified Netilmicin API suppliers worldwide. We currently have 2 companies offering Netilmicin API, with manufacturing taking place in 1 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Zhejiang Kangle Pharma | Producer | China | China | CoA, WC | 3 products |
| Zhejiang Zhenyuan | Producer | China | China | CEP, CoA, GMP | 3 products |
When sending a request, specify which Netilmicin API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
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