Antibiotics Drug Tacrolimus CAS: 109581-93-3

  • Model NO.: 109581-93-3
  • Customized: Non-Customized
  • Suitable for: Elderly, Adult
  • Purity: >99%
  • Mf: C44h69no12
  • Trademark: YC
  • Specification: ISO9001: 2008
  • HS Code: 3001909099
  • Powder: Yes
  • Certification: GMP, HSE, ISO 9001, USP, BP
  • State: Solid
  • CAS: 109581-93-3
  • MW: 804.02
  • Transport Package: Foil Bag/Tin or as Your Request
  • Origin: China
Product name: Tacrolimus
Synonyms: Tsukubaenolide hydrate
CAS Registry Number: 109581-93-3,104987-11-3
Molecular Formula: C44H69NO12
Molecular Weight: 804.02
Appearance: White to light yellow crystal powder
Purity:99%
Grade:Pharmaceutical Grade

Tacrolimus is an immunosuppressive drug used mainly after allogeneic organ transplant to lower the risk of organ rejection. It achieves this by inhibiting the production of interleukin-2, a molecule that promotes the development and proliferation of T cells, which are vital to the body's learned (or adaptive) immune response. Tacrolimus is also used in the treatment of other T cell-mediated diseases such as eczema (for which it is applied to the skin in a medicated ointment), severe refractory uveitis after bone marrow transplants, exacerbations of minimal change disease, Kimura's disease and the skin condition vitiligo.

Immunosuppression following transplantation

It has similar immunosuppressive properties to ciclosporin, but is much more potent. Immunosuppression with tacrolimus was associated with a significantly lower rate of acute rejection compared with ciclosporin-based immunosuppression (30.7% vs 46.4%) in one study.[8] Clinical outcome is better with tacrolimus than with ciclosporin during the first year of liver transplantation.[10][11] Long-term outcome has not been improved to the same extent. Tacrolimus is normally prescribed as part of a post-transplant cocktail including steroids, mycophenolate, and IL-2 receptor inhibitors. Dosages are titrated to target blood levels. Typical starting doses for once-daily tacrolimus are 0.15-0.20 mg/kg body weight.

Interactions

Also like ciclosporin, it has a wide range of interactions, including that with grapefruit which increases plasma-tacrolimus concentration. Several of the newer classes of antifungals, especially of the azole class (fluconazole, posaconazole) also increase drug levels by competing for degradative enzymes.

Ulcerative colitis

In recent years, tacrolimus has been used to suppress the inflammation associated with ulcerative colitis (UC), a form of inflammatory bowel disease. Although almost exclusively used in trial cases only, tacrolimus has shown to be significantly effective in the suppression of outbreaks of UC.

Dermatological use

As an ointment, tacrolimus is used in the treatment of eczema, in particular atopic dermatitis. It suppresses inflammation in a similar way to ste-roids, and is equally as effective as a mid-potency ste-roid. An important advantage of tacrolimus is that, unlike ste-roids, it does not cause skin thinning (atrophy), or other ste-roid related side effects.

It is applied on the active lesions until they heal off, but may also be used continuously in low doses (twice a week), and applied to the thinner skin over the face and eyelids.[citation needed] Clinical trials of up to one year have been conducted. Recently it has also been used to treat segmental vitiligo in children, especially in areas on the face.


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Antibiotics Drug Tacrolimus CAS: 109581-93-3
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