Bioequivalence between tofacitinib Tolvar and tofacitinib Xeljanz: a healthy volunteers trial

Autores: Camilo Lis, Sabrina Tedesco, Gabriela Nicotera, Pablo Quiroga, Alejandro Schamun

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Background: Rheumatoid arthritis is a chronic inflammatory disease that significantly impacts quality of life. Tofacitinib is a selective Janus kinase (JAK) inhibitor approved for multiple therapeutic indications.

Objective: To evaluate the bioequivalence between tofacitinib Tolvar® 5 mg, the product under study, and tofacitinib Xeljanz® 5 mg, the reference product.

Methods: An open-label, randomized, two-period, two-sequence crossover study was conducted in 27 healthy volunteers, with an 8-day washout period. Primary pharmacokinetic parameters (Cmax, AUC0-t, AUC0-∞) were determined using LC-MS/MS, and statistical analysis was based on ANOVA of log-transformed data, applying Schuirmann’s two one-sided tests.

Results: The 90% CI for Cmax, AUC0-t, and AUC0-∞ was within the acceptance range (80–125%). No adverse events were observed.

Conclusions: Tofacitinib Tolvar® 5 mg was shown to be bioequivalent to tofacitinib Xeljanz® 5 mg and demonstrated a comparable safety profile.