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Tacrolimus is a macrolide calcineurin inhibitor. In T cells , activation of the T cell receptor normally increases intracellular calcium, which acts via calmodulin to activate calcineurin . Calcineurin then dephosphorylates the transcription factor nuclear factor of activated T cells (NF-AT), which moves to the nucleus of the T cell and ...
Although it is a structural analogue of tacrolimus, it acts somewhat differently and has different side-effects. Contrary to ciclosporin and tacrolimus, drugs that affect the first phase of T lymphocyte activation, sirolimus affects the second phase, namely signal transduction and lymphocyte clonal proliferation.
mTOR inhibitors are a class of drugs used to treat several human diseases, including cancer, autoimmune diseases, and neurodegeneration. They function by inhibiting the mammalian target of rapamycin (mTOR) (also known as the mechanistic target of rapamycin), which is a serine/threonine-specific protein kinase that belongs to the family of phosphatidylinositol-3 kinase (PI3K) related kinases ...
Pimecrolimus, like tacrolimus, belongs to the ascomycin class of macrolactam immunosuppressives, acting by the inhibition of T-cell activation by the calcineurin pathway and inhibition of the release of numerous inflammatory cytokines, thereby preventing the cascade of immune and inflammatory signals. [18]
A TNF inhibitor is a pharmaceutical drug that suppresses the physiologic response to tumor necrosis factor (TNF), which is part of the inflammatory response.TNF is involved in autoimmune and immune-mediated disorders such as rheumatoid arthritis, ankylosing spondylitis, inflammatory bowel disease, psoriasis, hidradenitis suppurativa and refractory asthma, so TNF inhibitors may be used in their ...
Serious side effects including hypersensitivity and swelling have been observed in renal transplant patients. [22] While sirolimus was considered for treatment of LAM, it received orphan drug designation status because LAM is a rare condition. [22] The safety of LAM treatment by sirolimus in people younger than 18 years old has not been tested.
Fortunately, most tadalafil side effects are mild and resolve on their own over time. ... which are known as phosphodiesterase 5 inhibitors (PDE5 inhibitors for short). 3. Heartburn.
Temsirolimus is a specific inhibitor of mTOR and interferes with the synthesis of proteins that regulate proliferation, growth, and survival of tumor cells. Though temsirolimus shows activity on its own, it is also known to be converted to sirolimus (rapamycin) in vivo; [4] therefore, its activity may be more attributed to its metabolite rather than the prodrug itself (despite claims to the ...