Product Information
Registration Status: ActiveREVLIMID CAPSULE 15mg is approved to be sold in Singapore with effective from 2009-06-23. It is marketed by CELGENE PTE LTD, with the registration number of SIN13664P.
This product contains Lenalidomide 15mg in the form of CAPSULE. It is approved for ORAL use.
This product is manufactured by Penn Pharmaceutical Services Limited in SWITZERLAND, andCelgene International Sarl in UNITED KINGDOM.
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
Lenalidomide (initially known as CC-5013 and marketed as Revlimid® by Celgene) is a derivative of thalidomide introduced in 2004. It was initially intended as a treatment for multiple myeloma, for which thalidomide is an accepted therapeutic modality, but has also shown efficacy in the hematological disorders known as the myelodysplastic syndromes. FDA approved on December 27, 2005.
Indication
Lenalidomide is indicated for the treatment of multiple myeloma in combination with dexamethasone. It is also indicated for the treatment of patients with transfusion-dependent anemia due to low- or intermediate- risk myelodysplastic syndromes (MDS) associated with a deletion 5q cytogenetic abnormality with or without additional cytogenetic abnormalities.
Mechanism of Action
The mechanism of action of lenalidomide remains to be fully characterized, however it has been demonstrated that lenalidomide inhibits the expression of cyclooxygenase-2 (COX-2), but not COX-1, in vitro. In vivo it induces tumor cell apoptosis directly and indirectly by inhibition of bone marrow stromal cell support, by anti-angiogenic and anti-osteoclastogenic effects, and by immunomodulatory activity
Pharmacokinetics
- Absorption
- Rapidly absorbed following oral administration, with maximum plasma concentrations occurring between 0.625 and 1.5 hours post-dose. Co-administration with food does not alter the extent of absorption (AUC) but does reduce the maximal plasma concentration (Cmax) by 36%. The pharmacokinetic disposition of lenalidomide is linear. Accumulation does not occur following multiple doses.
- Distribution
- Metabolism
- Lenalidomide undergoes limited metabolism. Unchanged lenalidomide is the predominant circulating component in humans. Two identified metabolites are hydroxy-lenalidomide and N-acetyl-lenalidomide; each constitutes less than 5% of parent levels in circulation. The cytochrome P450 enzyme system is not involved with the metabolism of lenalidomide.
- Elimination
Clearance
The renal clearance of lenalidomide exceeds the glomerular filtration rate.
Toxicity
The most frequently reported adverse events were related to blood and lymphatic system disorders, skin and subcutaneous tissue disorders, gastrointestinal disorders, and general disorders and administrative site conditions.
Active Ingredient/Synonyms
1-oxo-2-(2,6-Dioxopiperidin-3-yl)-4-aminoisoindoline | 3-(4-Amino-1-oxoisoindolin-2-yl)piperidine-2,6-dione | CC-5013 | CDC 501 | IMid-1 | IMiD3 | Lenalidomide |
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.