Product Information
Registration Status: ActiveRAPAMUNE TABLET 2mg is approved to be sold in Singapore with effective from 2005-03-03. It is marketed by PFIZER PTE LTD, with the registration number of SIN12647P.
This product contains Sirolimus 2mg in the form of TABLET, SUGAR-COATED. It is approved for ORAL use.
This product is manufactured by PFIZER BIOTECH CORPORATION (Primary and Secondary Packager) in TAIWAN, andPfizer Ireland Pharmaceuticals in IRELAND.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
A macrolide compound obtained from Streptomyces hygroscopicus that acts by selectively blocking the transcriptional activation of cytokines thereby inhibiting cytokine production. It is bioactive only when bound to immunophilins. Sirolimus is a potent immunosuppressant and possesses both antifungal and antineoplastic properties.
Indication
For the prophylaxis of organ rejection in patients receiving renal transplants.
Mechanism of Action
Sirolimus inhibits T lymphocyte activation and proliferation that occurs in response to antigenic and cytokine (Interleukin IL-2, IL-4, and IL-15) stimulation by a mechanism that is distinct from that of other immunosuppressants. Sirolimus also inhibits antibody production. In cells, sirolimus binds to the immunophilin, FK Binding Protein-12 (FKBP-12), to generate an immunosuppressive complex. The sirolimus:FKBP-12 complex has no effect on calcineurin activity. This complex binds to and inhibits the activation of the mammalian Target Of Rapamycin (mTOR), a key regulatory kinase. This inhibition suppresses cytokine-driven T-cell proliferation, inhibiting the progression from the G1 to the S phase of the cell cycle.
Active Ingredient/Synonyms
(-)-Rapamycin | Rapamycin | sirolimús | sirolimus | sirolimusum | Sirolimus |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.