Sirolimus Continues to be Effective, Even When Thought to be Contraindicated

Sirolimus Continues to be Effective, Even When Thought to be Contraindicated


As an immunosuppressant drug used to prevent transplant rejection, Sirolimus, CAS number 53123-88-9, is a macrolide. Particularly useful for kidney transplant patients, sirolimus is also known as the brand name Rapamune, which is marketed by Pfizer. The first patent for Rapamune is set to expire in October 2012. An addtional patent will expire in July of 2013. Offered in either tablet or liquid form, sirolimus is typically taken once daily, either always with food or always without food. Derived from actinomycete Streptomyces hygroscopicus, sirolimus is usually used in combination with cyclosporine and corticosteroids to prevent the rejection of organ or tissue transplants. Extreme adverse events related to sirolimus are rare, but may include anemia, renal failure and pleural effusion. Side effects most reported by patients include nausea, vomiting, constipation, hypertension, insomnia, diarrhea, fever, urinary tract infections, tremors, headache and rash.

On January 6, 2012 Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy published a pilot study involving the use of sirolimus in conjunction with voriconazole.  As these drugs are typically contraindicated, researchers were interested in assessing the use and safety administering both sirolimus and  voriconazole concurrently, as many patients who receive both drugs are in need of optimal medication management. Study results were encouraging and indicated that both sirolimus and voriconazole can be safely coadministered, but consideration should be given as to which drug the patient receives first. Also to be considered by providers are the specific dosage of sirolimus, as well as information regarding CYP3A isoenzyme inhibitors. It was noted in this study that providers should be prudent and scrupulously monitor patients taking sirolimus before, during, and after the coadministration of voriconazole. Information gleaned from this study has lead toward the development of innovative protocols regarding medication management of this once thought contraindicated combination. LGM Pharma is a provider of API sirolimus, as well as voriconazole, for research and development purposes.

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