Tedizolid API CAS 856866-72-3

What is Torezolid ?

Tedizolid API is a similar substance to Linezolid and is a protein synthesis inhibitor. It belongs to the second-generation Oxadixyl class of antibiotics and acts on the 50S subunit of bacterial ribosomes, interfering with the synthesis of bacterial proteins. Compared with Linezolid, the effects of the two are not significantly different, but Linezolid needs to be used continuously for 10 days, twice a day. While Torezolid only needs to be used once a day and for 6 consecutive days. On June 20, 2014, the US FDA approved the new antibacterial product Torezolid (trade name: Sivextro) for the treatment of adult patients with skin infections. Sivextro was approved for the treatment of acute bacterial skin and skin structure infections caused by certain sensitive bacteria, such as Staphylococcus aureus (including methicillin-resistant strains and methicillin-sensitive strains), various streptococci, and Enterococcus faecalis.  
Tedizolid Impurity 47 is a second-generation Oxadixyl antibiotic developed by Dong-A Pharmaceutical. It has been licensed to Cubist Pharmaceuticals and Bayer for commercial development. The purpose of DA-7157 is to treat severe or life-threatening infections. Its marketing application has been granted Qualified Infectious Disease Product (QIDP) status and has received accelerated review from the FDA. The QIDP status of Tedizolid enables this product to have not only the market exclusivity granted by the Food, Pruduct and Cosmetic Act, but also an additional five-year market exclusivity. The effectiveness, safety and stability of the free base form of Tedizolid were evaluated in two clinical trials involving 1,315 adult patients with ABSSSI. The subjects were randomly assigned to Tedizolid free base or another approved antibacterial product for the treatment of acute bacterial skin and skin structure infections (ABSSSI). The results showed that its clinical efficacy was comparable to Linezolid, with fewer adverse reactions in the gastrointestinal tract and thrombocytopenia, and a lower incidence of tolerability. Some trials have shown that the tolerance of DA-7157 is also better than Vancomycin. The most common side effects confirmed in the clinical trials were nausea, headache, diarrhea, vomiting and dizziness.

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Why can Torezolid inhibit bacteria?

Many antibacterial substances work by interfering with bacterial protein synthesis, thereby preventing bacterial proliferation. Proteins are crucial for bacterial growth and reproduction; if synthesis is blocked, bacterial division and spread are severely hampered. For example, the DERMASEPTIN PHYLLOMEDUSA SAUVAGII shown in the image first penetrates the cell membrane and then targets genetic material to inhibit protein synthesis. Torezolid, a new generation of Oxadixyl derivatives, has a more precise mechanism of action. The Tedizolid API binds directly to bacterial ribosomes, effectively cutting off protein synthesis at its source. Because of this clearly defined target, Torezolid exhibits more stable inhibitory effects against Gram-positive bacteria, and bacteria are less likely to develop tolerance, making it well-suited for various applications, from basic research to the development of bioactive compounds.

 

What are the structural advantages of the Tedizolid free base?

The structural advantages of Torezolid are mainly reflected in three aspects: First, DA-7157 retains the C-5 hydroxymethyl structure of the Oxadixyl core, enabling precise binding to the 50S subunit of bacterial ribosomes and controlling protein synthesis. Second, the Tedizolid API transforms the morpholine ring of Linezolid into a pyridine-tetrazole ring structure. This change allows the active compound to form 2-4 additional hydrogen bonds with the ribosomal target, increasing antibacterial activity by 4-16 times, while reducing the inhibition of human mitochondrial protein synthesis and the affinity for AMINE:OXYGEN OXIDOREDUCTASE [DEAMINATING], thus significantly reducing the risk of side effects such as myelosuppression. Finally, by phosphated a calcium hydroxy compound in the molecule to form an activating precursor, water solubility is greatly improved (exceeding 50 mg/mL), resulting in an oral bioavailability of up to 91% and enabling a convenient once-daily administration.

MF of Torezolid

Melting point	201 °C
Boiling point Density	614.5±65.0 °C(Predicted)
Storage conditions	1.57
Solubility	Refrigerator
Molecular weight	370.34
EINECS Number	815-370-6
Acidity coefficient(pKa)	14.05±0.10(Predicted)

Specification

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FAQ:

Q1: What type of antibiotic is Torezolid?
Torezolid belongs to the Oxadixyl class and is in the same family as Linezolid. They have a somewhat similar structure. It mainly targets Gram-positive bacteria, especially those resistant to multiple products, and shows excellent efficacy. Its mechanism of action is to interfere with the bacterial protein synthesis, thereby preventing their growth and reproduction. In summary, it is highly active and has a wide range of applications. It is often used in product structure research, scientific experiments, or as a standard reference for comparison.
Q2: Is Torezolid better than Linezolid?
Tedizolid Impurity 47 is a new generation of Oxadixyl compound derived from Linezolid. It possesses stronger inhibitory activity, better safety performance, and lower risk of causing bacterial resistance compared to Linezolid. Compared to Linezolid, it exhibits superior inhibitory effect on Gram-positive bacteria.
Q3: How effective is TEDIZOLID?

Tedizolid API (also known as Torezolid856866-72-3) is an antibiotic. It has excellent efficacy, especially showing significant potent effects on certain difficult-to-treat bacteria. Its effectiveness can be divided into three key aspects: its potency, its clinical success rate, and the comparison with standard treatments.

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