SIROLIMUS

Product Description

Sirolimus (Rapamycin) is being supplied by MedicaPharma Sirolimus, also known asrapamycin, is amacrolidecompound that is used to coatcoronary stents, preventorgan transplant rejectionand treat a rare lung disease calledlymphangioleiomyomatosis.It hasimmunosuppressantfunctions in humans and is especially useful in preventing the rejection ofkidneytransplants. It inhibits activation ofT cellsandB cellsby reducing their sensitivity tointerleukin-2(IL-2) throughmTORinhibition. It is produced by thebacteriumStreptomyces hygroscopicusand was isolated for the first time in 1972 bySurendra Nath Sehgaland colleagues from samples ofStreptomyces hygroscopicusfound onEaster Island. The compound was originally named rapamycin after the native name of the island, Rapa Nui.Sirolimus was initially developed as anantifungalagent. However, this use was abandoned when it was discovered to have potent immunosuppressive and antiproliferative properties due to itsability to inhibit mTOR. It was approved by the USFood and Drug Administrationin September 1999 and is marketed under the trade nameRapamunebyPfizer(formerly byWyeth).

Venous malformations

Sirolimus is used to treat venous malformations. Treatment with it can decrease pain and the fullness of venous malformations, improve coagulation levels, and slow the growth of abnormal lymphatic vessels. Sirolimus is a relatively new medical therapy for the treatment of vascular malformations,in recent years, sirolimus has emerged as a new medical treatment option for both vascular tumors and vascular malformations, as a mammalian target of rapamycin (mTOR), capable of integrating signals from the PI3K/AKT pathway to coordinate proper cell growth and proliferation. Hence, sirolimus is ideal for proliferative vascular tumors through the control of tissue overgrowth disorders caused by inappropriate activation of the PI3K/AKT/mTOR pathway as an antiproliferative agent.Sirolimus is used especially to treat lymphatic malformation.

Adverse effects

The most common adverse reactions (30% occurrence, leading to a 5% treatment discontinuation rate) observed with sirolimus in clinical studies of organ rejection prophylaxis in individuals with kidney transplants include:peripheral edema,hypercholesterolemia, abdominal pain, headache, nausea, diarrhea, pain, constipation,hypertriglyceridemia,hypertension, increasedcreatinine, fever,urinary tract infection,anemia,arthralgia, andthrombocytopenia. The most common adverse reactions (20% occurrence, leading to an 11% treatment discontinuation rate) observed with sirolimus in clinical studies for the treatment of lymphangioleiomyomatosis are: peripheral edema, hypercholesterolemia, abdominal pain, headache, nausea, diarrhea, chest pain,stomatitis,nasopharyngitis, acne,upper respiratory tract infection, dizziness, andmyalgia. The following adverse effects occurred in 320% of individuals taking sirolimus for organ rejection prophylaxis following a kidney transplant.  

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