Revlimid®
Active ingredient: Lenalidomide
Marketing authorisation holder: Celgene Europe Ltd
Availability: Private Sector and National Health Service
Variations: The pharmacokinetics section of the SmPC was updated regarding absorption of lenalidomide in
both the fed and fasted state based on data from phase I studies in healthy volunteers and a phase II study in
patients with multiple myeloma. Further amendments were made to the information regarding metabolism and
excretion of lenalidomide in both healthy participants and patients suffering from multiple myeloma.
After oral administration, lenalidomide is rapidly absorbed in healthy participants, the plasma concentrations
occurred within 2 hours post-dose under fasting conditions. AUC and Cmax in both healthy participants and
patients suffering from multiple myeloma increases proportionally with the dose. No marked drug accumulation
occurs in multiple dosing. The relative exposures S- and R- enantiomers of lenalidomide are about 56% and
44% respectively in the plasma.
Although lenalidomide can be administered irrespective of mealtimes, when it was co-administered with a high
fat and high calorie meal in healthy participants, both the AUC and Cmax decreased by 20% and 50%
respectively. Hence it had affected negatively the extent of absorption. In pivotal trials carried out in participants
suffering from multiple myeloma, lenalidomide was administered irrespective of food intake.
Lenalidomide is eliminated mainly through the urinary system 90% (in subjects with normal renal function) and
4% in faeces. The active ingredient undergoes poor metabolism with 82% per dose excreted unchanged in urine.
Hydroxy-lenalidomide and N-acetyl-lenalidomide form 4.59% and 1.83% of the excreted dose respectively. The
half life in plasma is about 3 hours both in healthy participants and patients suffering from multiple myeloma at
recommended doses (5 to 25mg/day).
Reference: European Medicines Agency. Revlimid. [online]. 2011July 25 [cited 2011 Aug 23]; Available from: URL:
http://www.ema.europa.eu/ema/index.jsp?curl=pages/medicines/human/medicines/000717/human_med_001034.jsp&murl=menus/medicine
s/medicines.jsp&mid=WC0b01ac058001d124