Sirolimus
From Ganfyd
rINN: Sirolimus
Other Names
Rapamune®, rapamycin
Pharmacological Information
Pharmacology Images
Web information on Sirolimus
Metabolism & Interactions
Relevant Clinical Literature
UK Guidance
Regulatory Literature
Other Literature
Please read pharmacological data limitations
Other Wikis
Medpedia on Sirolimus (Less technical, good quality control)
Wikipedia on Sirolimus (Less technical, ? quality control)
Contents |
Introduction
A macrolide isolated from Streptomyces hygroscopicus that acts via the mTOR pathway to selectively block the transcriptional activation of cytokines.
Clinical Use
Indications
- Organ rejection prophylaxis in kidney allografts
Administration
Oral usually in range 2 to 6mg often adjusted with blood monitoring and taken diluted with water or orange juice
Clinical Issues
Contra-indications
- Pregnancy
- Breast feeding
Cautions and Interactions
Multiple interactions some of considerable importance such as with cyclosporin
Side effects
Multiple including hypersensitivity and immunosuppression
Special advice
Pharmacology
- Suppresses mTOR signaling by binding to a class of proteins actually first defined by its binding activity. It may thus be active from animal models in reducing malignant transformation in tuberous sclerosis and in prolonging life span. It inhibits:
- T lymphocyte activation and proliferation in response to antigenic and cytokine (IL-2, IL-4, and IL-15) stimulation
- Antibody production.
Sirolimus binds to serine/threonine-protein kinase mTOR, a key regulatory kinase which results in inhibition at the G1 to the S phase of the cell cycle suppressing cytokine-driven T-cell proliferation.
