Bortez is a proteasome inhibitor indicated for:
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Bortezomib is an antineoplastic drug available for intravenous (IV) and subcutaneous injection. It acts as a reversible inhibitor of the chymotrypsin-like activity of the 26S proteasome in mammalian cells. The 26S proteasome is a large protein complex responsible for degrading ubiquitinated proteins, crucial for regulating specific intracellular proteins and maintaining cellular homeostasis. Inhibition of this pathway disrupts normal cellular processes and can lead to cell death. Studies have shown that Bortezomib is cytotoxic to various cancer cell types and delays tumor growth in models of multiple myeloma.
The distribution volume of Bortezomib at the recommended dose in patients with multiple myeloma has not been assessed. The average binding of Bortezomib to human plasma proteins is 83% within the concentration range of 100–1000 ng/mL.
Bortezomib is primarily metabolized via cytochrome P450 enzymes (3A4, 2C19, and 1A2), with minor metabolism through CYP 2D6 and 2C9. The major metabolic route involves deboronation, resulting in two de-boronated metabolites, which are inactive as proteasome inhibitors.
The mean elimination half-life of Bortezomib ranges from 9 to 15 hours, with doses between 1.45 and 2.00 mg/m2 in patients with advanced cancers. The elimination pathways of Bortezomib in humans have not been fully characterized.
The recommended dose of Bortezomib is 1.3 mg/m2 per dose administered intravenously or subcutaneously as a 3 to 5-second bolus twice weekly for 2 weeks (Days 1, 4, 8, and 11), followed by a 10-day rest period (Days 12-21). For extended therapy beyond 8 cycles, Bortezomib may be administered weekly for 4 weeks (Days 1, 8, 15, and 22), followed by a 13-day rest period (Days 23-35).
Retreatment may be considered for patients who responded previously to Bortezomib and relapsed at least 6 months after prior treatment. The dose may be started at the last tolerated dose. Bortezomib is for intravenous or subcutaneous use only.
Take this medication only as directed by a registered physician.
No formal drug interaction studies have been conducted with Bortez. However, in vitro studies suggest Bortez is primarily a substrate of cytochrome P450 3A4, 2C19, and 1A2. It may inhibit the activity of 2C19 and increase exposure to drugs metabolized by this enzyme. Bortez is a poor inhibitor of several other cytochrome P450 enzymes.
Bortezomib is contraindicated in patients with hypersensitivity to Bortezomib, boron, or mannitol, and for intrathecal administration, as fatal reactions have occurred.
Overdosage may lead to symptomatic hypotension and thrombocytopenia with fatal outcomes. In the case of an overdose, monitor vital signs and provide supportive care.
Pregnancy Category D. Women of childbearing potential should avoid pregnancy during Bortezomib treatment. No studies have been conducted to assess placental transfer. Bortezomib may pose a risk to the fetus if used during pregnancy.
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