Skeletal effects of nilotinib on prepubertal and pubertal rats
Pharmacy Practice
Abstract
Background: Nilotinib belongs to a group of anti-cancer drugs called tyrosine kinase inhibitors (TKIs), which are currently the mainstay treatment of chronic myeloid leukemia (CML). Objectives: In this study, we aimed to investigate the effects of this drug on bones around puberty in vivo. Methods: Juvenile male Wistar rats were divided to three groups and were treated orally once a day. Group 1 was administered vehicle; group 2 was administered nilotinib at a low-dose (30.85 mg/kg) and group 3 was treated with a high-dose (41.13 mg/kg). The treatment continued from week 4 until week 7 of age (pre-pubertal and pubertal life). Methods: Serum calcium, insulin-like growth factor-1 (IGF-1) and procollagen type I (PINP) were measured by enzyme-linked immunosorbent assay (ELISA). Femur bone was collected for histopathological evaluation using Hematoxylin & Eosin stain, and Masson's trichrome (MTC) staining. Immunohistochemistry was performed, using the bone cellular markers antiosteopontin (OPN) and antitartrate-resistant acid phosphatase (TRAP). Results: Serum Calcium, IGF-1 and PINP declined in a dose-dependent manner (p < 0.05). Histopathological evaluation revealed dose-dependent degeneration of bone lamellae and disruption and disorganization of cellular components. Moreover, the study revealed a decrease in collagen, decrease in OPN, and increase in TRAP immunostaining. Conclusion: Nilotinib had deleterious skeletal effects around puberty, possibly requiring long-term monitoring of bone growth and mineralization.
Keywords
- Nilotinib
- Bone
- Calcification
- Puberty