In recent years, new medications like proteasome inhibitors (PIs) have significantly improved cancer patients' response rate and overall survival. Carfilzomib (CFZ), a second-generation proteasome inhibitor, has shown promising results in clinical trials for treating multiple myeloma patients. In the current study, a Fe-Co metal-organic framework (MOF) was developed as a drug delivery system for targeted therapy of cancer cells. CFZ-loaded Fe-Co MOFs were synthesized and characterized using DLS, VSM, SEM-EDS, and BET analyses. The in vivo effects of CFZ-loaded Fe-Co MOFs were compared with standard drugs using a male Wistar rat model. Based on the results, DLS revealed a polydisperse size distribution, while VSM showed strong magnetic properties with 20 emu/g saturation magnetization. SEM-EDS confirmed a well-defined crystalline structure with uniform elemental distribution, and BET analysis indicated a mesoporous structure with a surface area of 84.984 m/g. The MOFs demonstrated a high drug loading efficiency of 74.86% and a controlled release profile, with an initial burst followed by sustained release. When administered intravenously to rats, free CFZ at doses of 0.4 mg/kg and 0.8 mg/kg led to significant increases in serum liver enzymes, kidney function markers, and liver malondialdehyde content. Furthermore, high doses of CFZ-loaded Fe-Co MOFs caused significant histopathological changes in the rats. These findings provide a basis for further research on using Fe-Co MOFs as carriers of proteasome inhibitors like CFZ for targeted drug delivery.