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|Alias:||Rapamycin / Sirolimus||Water Solubility:||0.00173 Mg/mL|
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Sirolimus / Rapamycin Immunosuppressant Preventing Organ Rejection after a Kidney Transplant
Sirolimus is used for
Preventing organ rejection after a kidney transplant. It is used with other medicines. It may also be used for other conditions as determined by your doctor.Sirolimus is an immunosuppressant. It works by blocking the action of certain blood cells (eg, T lymphocytes) that can cause the body to reject the transplanted organ.
Do NOT use sirolimus if
Contact your doctor or health care provider right away if any of these apply to you.
Sirolimus is indicated for the prevention of organ transplant rejection and for the treatment oflymphangioleiomyomatosis (LAM).
Prevention of transplant rejection
The chief advantage sirolimus has over calcineurin inhibitors is its low toxicity toward kidneys. Transplant patients maintained on calcineurin inhibitors long-term tend to develop impaired kidney function or even chronic renal failure; this can be avoided by using sirolimus instead. It is particularly advantageous in patients with kidney transplants for hemolytic-uremic syndrome, as this disease is likely to recur in the transplanted kidney if a calcineurin-inhibitor is used.
However, on 7 October 2008, the FDA approved safety labeling revisions for sirolimus to warn of the risk for decreased renal function associated with its use. In 2009, the FDA notified healthcare professionals that a clinical trial conducted by Wyeth showed an increased mortality in stable liver transplant patients after switching from a calcineurin inhibitor-based immunosuppressive regimen to sirolimus.
Sirolimus can also be used alone, or in conjunction with a calcineurin inhibitor (such as tacrolimus), and/or mycophenolate mofetil, to provide steroid-free immunosuppression regimens. Impaired wound healing and thrombocytopenia are a possible side effects of sirolimus;
therefore, some transplant centers prefer not to use it immediately after the transplant operation, but instead administer it only after a period of weeks or months. Its optimal role in immunosuppression has not yet been determined, and it remains the subject of a number of ongoing clinical trials.
On May 28, 2015, the FDA approved sirolimus to treat lymphangioleiomyomatosis (LAM), a rare, progressive lung disease that primarily affects women of childbearing age. This made sirolimus the first drug approved to treat this disease. LAM involves lung tissue infiltration with smooth muscle-like cells with mutations of the tuberous sclerosis complex gene (TSC2). Loss of TSC2 gene function activates the mTORsignaling pathway, resulting in the release of lymphangiogenic growth factors. Sirolimus blocks this pathway.
The safety and efficacy of sirolimus treatment of LAM were investigated in clinical trials that compared sirolimus treatment with a placebo group in 89 patients for 12 months. The patients were observed for 12 months after the treatment had ended.
The most commonly reported side effect of sirolimus treatment of LAM were mouth and lip ulcers, diarrhea, abdominal pain, nausea, sore throat, acne, chest pain, leg swelling, upper respiratory tract infection, headache, dizziness, muscle pain and elevated cholesterol. Serious side effects including hypersensitivity and swelling (edema) have been observed in renal transplant patients.
While sirolimus was considered for treatment of LAM, it received orphan product designation status because LAM is a rare condition. Development for the product was partially supported by the FDA Orphan Products Grants Program, which provides grants for clinical studies on safety and/or effectiveness of products for use in rare diseases or conditions.The safety of LAM treatment by sirolimus in patients younger than 18 years old has not been tested.
Coronary stent coating
The antiproliferative effect of sirolimus has also been used in conjunction with coronary stents to prevent restenosis in coronary arteries following balloon angioplasty. The sirolimus is formulated in a polymer coating that affords controlled release through the healing period following coronary intervention. Several large clinical studies have demonstrated lower restenosis rates in patients treated with sirolimus
-eluting stents when compared to bare-metal stents, resulting in fewer repeat procedures. A sirolimus-eluting coronary stent was marketed by Cordis, a division ofJohnson & Johnson, under the tradename Cypher. However, this kind of stent may also increase the risk of vascular thrombosis.
|Description||off-white to yellow crystalline powder||Complies|
|The IR spectrum of Potassium Bromide preparation of the sample exhibits maxima at the same wavelengths as that of a similar preparation of in-house reference standard||Complies|
|The UV spectrum of 95% Ethanol preparation of the sample exhibits maxima at 267nm,277nm, 288nm that of similar preparation of in-house reference standard.||Complies|
|The retention times of the peaks for the Trans- and Cis-stereoisomers in the chromatogram of Assay preparation corresponds to that in the chromatogram of the standard preparation, as obtained in the Assay||Complies|
|Loss on drying||≤0.5%||0.16%|
|Cis-stereoisomer of Sirolimus||≤5.0%||2.4%|
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