Pharmacokinetic Comparison and Bioequivalence of a New Generic Formulation of Lenalidomide 25 mg Capsules versus Revlimid in Healthy Volunteers under Fasting Conditions

Abstract

Lenalidomide is an immunomodulatory agent with direct antiproliferative, proapoptotic, and antiangiogenic effects, combined with long-term immunostimulatory effects which improve both cellular and humoral immune function. Lenalidomide is indicated for the treatment of patients with multiple myeloma, who are previously untreated and not eligible for transplant. Lenalidomide has dual effects, involving both direct tumoricidal properties and immunomodulatory activity. A single centre, open-label, single-dose, randomized, two-period, two-treatment, two sequence, crossover, comparative bioavailability study was conducted in 24 healthy volunteers to compare pharmacokinetics profile of a new lenalidomide generic formulation (lenalidomide capsules 25 mg, Hikma Pharmaceuticals) with those of the reference product (Revlimid, Celgene Gmbh, United Kingdom). The study was conducted at Pharma Medical Research Inc. (Canada) in accordance with Good Clinical Practices and the applicable regulatory requirements. One capsule of each formulation was administered with 240 mL of water after a 10 hr overnight fast. In each study period, eighteen (18) blood samples were collected by venepuncture in pre-cooled Vacutainers containing EDTA. First blood sample (2 × 6 mL) was collected prior to drug administration while the others (1 × 6 mL each) were collected at 0.167

Biopharmaceutics Classification System (BCS) Based Biowaiver Studies of Lenalidomide Capsules (25 mg) – An Alternative to In vivo Bioequivalence Studies for Generic Oncology Drug Products

“…This interaction was demonstrated to be related to the antitumor and the immunomodulatory properties of lenalidomide [6]. The empirical formula, the gram molecular weight and other chemical properties of lenalidomide are listed in Table 1 [7]. As shown in Figure 1, lenalidomide has an asymmetric carbon atom.…”