Tacrolimus Chemische Eigenschaften,Einsatz,Produktion Methoden
R-Sätze Betriebsanweisung:
R25:Giftig beim Verschlucken.
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
S-Sätze Betriebsanweisung:
S45:Bei Unfall oder Unwohlsein sofort Arzt zuziehen (wenn möglich, dieses Etikett vorzeigen).
S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
Beschreibung
Tacrolimus, isolated from the microorganism Streptomyces tsukubaensis, is a
macrolide immunosuppressant developed by Fujisawa for organ transplantation. It displays
similar but more potent immunosuppressive activity than cyclosporin. It inhibits both cell
mediated and humoral immune responses. In animal models of organ transplantation,
tacrolimus has been shown to prolong survival of hepatic, renal, cardiac, small intestine,
pancreatic and skin allografts and to reverse cardiac and renal allograft rejection. It has been
used effectively in humans as rescue or primary immunosuppressant therapy in liver or kidney
transplantation. Compared to cyclosporin, tacrolimus causes reduced incidence of infectious
complications and of hypertension and hypercholesterolemia for the allograft recipients. In
common with cyclosporin, tacrolimus binds with high affinity to a family of cytoplasmic
immunosuppressant binding proteins, the immunophilins. This tight complex is proposed as
the biologically active moiety that interacts with intracellular molecules involved in signal
transduction.It inhibits phosphatase activity of calcineurin, an action that may impair the
generation and/or activation of nuclear transcription factors required for lymphokine
(particularly interleukin-2) gene expression. Tacrolimus has also been reported to have
potential in multiple sclerosis, psoriasis, rheumatoid arthritis and uveitis associated with
Behcet‘s disease.
Chemische Eigenschaften
White Crystalline Solid
Verwenden
FK-506 (Tacrolimus) is a macrolide immunosuppressive drug that is mainly used after allogeneic organ transplant to reduce the activity of the patient's immune system
Indications
Tacrolimus is a macrolide lactone originally derived
from Streptomyces tsukubaensis. Although structurally
unrelated to cyclosporine, tacrolimus has a very similar
mechanism of action; that is, it blocks the production of
proinflammatory cytokines by T lymphocytes by inhibiting
calcineurin.Tacrolimus, however, appears to be
10 to 100 times as potent as an immunosuppressive.
Oral tacrolimus (FK506) is used for prevention of organ
rejection in recipients of renal and hepatic transplants.
Definition
ChEBI: Tacrolimus is a macrolide containing a 23-membered lactone ring, originally isolated from the fermentation broth of a Japanese soil sample that contained the bacteria Streptomyces tsukubaensis.
Allgemeine Beschreibung
Immunosuppressant that blocks T-cell proliferation
in vitro by inhibiting the generation of several lymphokines, especially IL-2. Shown to inhibit the activity of FK-506 Binding Protein, thereby reversing its effects on sarcoplamic reticulum Ca
2+ release. Shown to inhibit the Ca
2+-dependent phosphatase, Calcineurin (Cat. No. 539565), as well as Na
+-K
+-ATPase in nephron segments. Also shown to inhibit aldosterone-induced synthesis of Giα-3 protein.
Clinical Use
A topical formulation (Protopic) has recently been approved
for treatment of moderate to severe atopic dermatitis
in children and adults who have not responded
to other therapies. Levels of systemic absorption are
low even when applied to a relatively large body surface
area.
Nebenwirkungen
Local irritant reactions (burning, stinging, erythema)
are a common side effect, but these usually resolve
within the first few days of treatment. The major
benefit of topical tacrolimus over topical corticosteroids
is that tacrolimus does not cause atrophy, striae, or
telangiectasia, even with chronic use.
Tacrolimus Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
