Sitafloxacin

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An article about the antibiotic Sitafloxacin


Engineered Monoclonal Antibodies[edit source]

Diagram of engineered monoclonal antibodies

Engineered monoclonal antibodies are a class of biological therapies that are designed to target specific antigens on the surface of cells. These antibodies are produced using recombinant DNA technologies and are used in the treatment of various diseases, including cancer, autoimmune disorders, and infectious diseases.

Structure and Function[edit source]

Monoclonal antibodies are composed of two identical heavy chains and two identical light chains, forming a Y-shaped molecule. The tips of the "Y" contain the antigen-binding sites, which are highly specific to the target antigen. This specificity allows monoclonal antibodies to bind to their target with high affinity, blocking or modulating the function of the antigen.

Types of Engineered Monoclonal Antibodies[edit source]

There are several types of engineered monoclonal antibodies, each designed for specific therapeutic purposes:

  • Chimeric antibodies: These antibodies are composed of murine (mouse) variable regions and human constant regions. They are less immunogenic than fully murine antibodies.
  • Humanized antibodies: These antibodies are mostly human, with only the antigen-binding sites derived from murine sources. This reduces the risk of immune reactions.
  • Fully human antibodies: These are entirely human in origin, produced using transgenic mice or phage display technologies.
  • Bispecific antibodies: These antibodies are engineered to bind two different antigens simultaneously, offering unique therapeutic mechanisms.

Applications in Medicine[edit source]

Engineered monoclonal antibodies have revolutionized the treatment of many diseases:

  • Cancer therapy: Monoclonal antibodies can target specific tumor antigens, leading to direct tumor cell killing or recruitment of immune cells to attack the tumor.
  • Autoimmune diseases: By targeting specific components of the immune system, monoclonal antibodies can reduce inflammation and tissue damage in diseases such as rheumatoid arthritis and multiple sclerosis.
  • Infectious diseases: Monoclonal antibodies can neutralize pathogens or their toxins, providing passive immunity or enhancing the host's immune response.

Production[edit source]

The production of engineered monoclonal antibodies involves several steps:

1. Antigen identification: The target antigen is identified and characterized. 2. Hybridoma technology: B cells from immunized animals are fused with myeloma cells to create hybridomas that produce the desired antibody. 3. Recombinant DNA technology: Genes encoding the antibody are cloned and expressed in suitable host cells, such as Chinese hamster ovary cells. 4. Purification and formulation: The antibodies are purified and formulated for clinical use.

Challenges and Future Directions[edit source]

While engineered monoclonal antibodies have shown great promise, there are challenges such as high production costs, potential for immune reactions, and the development of resistance. Ongoing research aims to improve antibody design, reduce immunogenicity, and enhance therapeutic efficacy.

Related Pages[edit source]

Sitafloxacin is a fluoroquinolone antibiotic used in the treatment of various bacterial infections. It is known for its broad-spectrum activity against both Gram-positive and Gram-negative pathogens.

Mechanism of Action[edit | edit source]

Sitafloxacin works by inhibiting bacterial DNA gyrase and topoisomerase IV, enzymes critical for DNA replication and transcription. This inhibition leads to the disruption of bacterial DNA synthesis, ultimately resulting in bacterial cell death.

Pharmacokinetics[edit | edit source]

Sitafloxacin is well absorbed after oral administration, with a bioavailability of approximately 90%. It is widely distributed throughout the body, achieving therapeutic concentrations in various tissues and fluids. The drug is primarily excreted via the renal system, with a half-life of approximately 5 to 7 hours.

Clinical Uses[edit | edit source]

Sitafloxacin is indicated for the treatment of a variety of infections, including:

Adverse Effects[edit | edit source]

Common adverse effects of sitafloxacin include nausea, diarrhea, and headache. Like other fluoroquinolones, it may also cause more serious side effects such as tendonitis and tendon rupture, particularly in older adults and those on concurrent corticosteroid therapy.

Resistance[edit | edit source]

Bacterial resistance to sitafloxacin can occur through mutations in the gyrA and parC genes, which encode the target enzymes DNA gyrase and topoisomerase IV, respectively. Efflux pumps and reduced permeability of the bacterial cell wall can also contribute to resistance.

Related pages[edit | edit source]

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Contributors: Prab R. Tumpati, MD