Sirolimus CAS No: 53123-88-9
First discovered in 1972 and approved by the FDA in 1999, sirolimus can be used for a variety of disorders and medical events, including organ transplant procedures, lung disease, and heart protection. By suppressing the immune system, patients who have recently received a new organ have a better chance of their body accepting their organ as a natural addition. It can also stop the production of harmful cells in the blood vessels and lungs. This API got its start as an antifungal medication but quickly pivoted when researchers started seeing success in other areas of study.
Immunosuppressant for Kidney Transplants
Sirolimus is derived from the bacteria Streptomyces hygroscopicus which was originally found on Easter Island. It stops the production of T and B cells by inhibiting the production of IL-2. While there are a number of immunosuppressants on the market, sirolimus seems to work particularly well for kidney transplants. It can be used alone or in combination with another similar API like tacrolimus, but there’s reason to believe sirolimus may be safer for patients. Traditional calcineurin inhibitors will work for a time with kidney transplant patients, but can ultimately lead to an impairment of kidney function (or even complete renal failure.) Those who have hemolytic-uremic syndrome have especially benefited from using sirolimus as opposed to alternatives on the market because their syndrome is far less likely to recur.
Sirolimus has been used to inhibit mTOR in normal cells that may threaten the efficacy of a stent. When a coronary stent is put in place after balloon angioplasty, the endothelial cells will flock to the site of trauma in order to protect it. The increased production of the cells can ultimately lead to restenosis, which can trigger another coronary event. To prevent this from happening, sirolimus is used to coat the stent and then release the substance into the body at regular intervals to keep the endothelial cells from narrowing the blood vessel. Those who used sirolimus saw better results than patients who used bare-metal stents, which resulted in fewer emergencies or additional procedures.
While sirolimus won’t treat most lung disorders, it has seen success in treating Lymphangioleiomyomatosis (LAM). This rare disease is the result of a mutation that invades the lungs and compromises their functionality. Normally occurring in young or middle-aged women, sirolimus stops the mutating cells from being able to continue their production. By inhibiting the mTOR of the mutations, those with LAM saw stabilized and even improved lung functionality. Before this incredible API was approved in 2015, the only options for those with LAM were to either a transplant or supportive care.
Side Effects of Sirolimus
General side effects of sirolimus include headaches, nausea, chest pain, or dizziness. Leg swelling has been known to occur in those treated for LAM and edema has been known to occur in those treated for kidney transplants. Sirolimus may also delay the healing of the would or cause thrombocytopenia in kidney transplant patients. Those who use sirolimus-coated stents may have an increased risk of vascular thrombosis. In certain cases, doctors will wait to administer sirolimus to patients so they have a better chance of immediate recovery from the surgery. In many ways, researchers are still figuring out exactly where sirolimus fits in terms of medical care, which is why there are a number of ongoing, long-term studies that should shed more light on its healing powers.
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