Information about Lenalidomide
Thalidomide and its analogue lenalidomide are immunomodulatory and antineoplastic agents that are used in the therapy of multiple myeloma.
Liver safety of Lenalidomide
Both agents are associated with a low rate of serum aminotransferase elevations during therapy and both have been implicated in causing rare instances of clinically apparent liver injury which can be severe.
Mechanism of action of Lenalidomide
Thalidomide (tha lid' oh mide) is a glutamic acid derivative that was introduced in Europe as a sedative in the late 1950s and subsequently withdrawn in 1961 when it was shown to be teratogenic, causing severe infant limb defects (phocomelia) when given to pregnant women. Several decades later, thalidomide was found to have potent activity in erythema nodosum leprosum, and subsequent studies found it beneficial in several autoimmune conditions and cancers. Thalidomide has immunomodulatory, antiinflammatory, antiangiogenic and anticancer properties that underlie its effects in inflammatory and malignant diseases. Thalidomide was approved for therapy of erythema nodosum leprosum (ENL) in the United States in 1998 and was subsequently approved for use in multiple myeloma (in combination with dexamethasone) in 2006.
FDA approval information for Lenalidomide
Lenalidomide (len" a lid' oh mide) is a thalidomide derivative that was found to be more potent as an antineoplastic agent, and was approved for use in selected myelodysplastic syndromes in 2005 and for multiple myeloma (combined with dexamethasone) in 2006. Thalidomide has also been used on an experimental basis for graft vs host disease, Kaposi sarcoma, AIDS associated wasting syndrome and several forms of autoimmune disease.
Dosage and administration for Lenalidomide
Thalidomide is available in capsules of 50, 100, 150 and 200 mg under the brand name Thalomid, and lenalidomide in capsules of 2.5, 5, 10, 15, 20 and 25 mg under the brand name Revlimid. The recommended doses vary by indication, and their use is restricted because of their proven teratogenicity.
Side effects of Lenalidomide
Side effects of thalidomide and lenalidomide are common and include sedation, dizziness, orthostatic hypotension, neutropenia, peripheral neuropathy, and venous thromboembolism (for which reason they are often given with anticoagulation).