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At a glance

Bortezomib is a proteasome inhibitor used in the treatment of multiple myeloma and mantle cell lymphoma. It stops or slows down the growth of cancer cells by blocking protein breakdown, leading to cell death.

Indications
  • Multiple myeloma
  • Mantle cell lymphoma
Pharmacology

Bortezomib is a reversible inhibitor of the chymotrypsin-like activity of the 26S proteasome. The 26S proteasome degrades ubiquitinated proteins. The ubiquitin-proteasome pathway regulates intracellular protein concentrations, maintaining cellular homeostasis. Proteasome inhibition prevents targeted proteolysis, affecting multiple signaling cascades and disrupting normal homeostatic mechanisms, leading to cell death. Bortezomib is 83% bound to human plasma proteins and is primarily metabolized by CYP3A4, CYP2C19, and CYP1A2. Half-life is 9-15 hours.

Dosage

Adults:
Mantle Cell Lymphoma (previously untreated): 1.3 mg/m² IV/SC twice weekly (Days 1, 4, 8, 11), 10-day rest (Days 12-21), for 6 cycles (3-week each). Given with R-CHOP (Rituximab, Cyclophosphamide, Doxorubicin, Prednisone).

Mantle Cell Lymphoma (relapsed): 1.3 mg/m² IV/SC twice weekly (Days 1, 4, 8, 11), 10-day rest (Days 12-21).

Multiple Myeloma (previously untreated, with Melphalan+Prednisone):
Cycles 1-4 (twice weekly): 1.3 mg/m² IV/SC on Days 1, 4, 8, 11, 22, 25, 29, 32
Cycles 5-9 (once weekly): 1.3 mg/m² IV/SC on Days 1, 8, 22, 29

Multiple Myeloma (relapsed): 1.3 mg/m² IV/SC twice weekly (Days 1, 4, 8, 11), 10-day rest (Days 12-21). Beyond 8 cycles: once weekly (Days 1, 8, 15, 22), 13-day rest (Days 23-35).

Re-treatment (Multiple Myeloma): Start at last tolerated dose. Twice weekly (Days 1, 4, 8, 11), 10-day rest (Days 12-21).

Hepatic impairment (Moderate-severe, bilirubin >1.5x ULN): Reduce to 0.7 mg/m² in first cycle; may escalate to 1 mg/m² or reduce to 0.5 mg/m² in subsequent cycles based on tolerability.

Renal impairment: No dose adjustment needed. Administer after dialysis.

Side effects

Common side effects:
Fatigue, nausea, vomiting, loss of appetite (anorexia), diarrhea, constipation, fever, anemia (low red blood cells), thrombocytopenia (low platelets), neutropenia (low white blood cells), peripheral neuropathy (tingling and numbness of hands and feet), psychiatric disturbances.

Serious: Hypotension, cardiac toxicity (heart failure), pulmonary toxicity (ARDS, pneumonitis), Posterior Reversible Encephalopathy Syndrome (PRES), tumor lysis syndrome, hepatic toxicity (liver toxicity), gastrointestinal hemorrhage.

Use in pregnancy

Unsafe during pregnancy (Category D). Definite evidence of risk to the developing baby. May be prescribed rarely in life-threatening situations if benefits outweigh risks. Women of childbearing potential should avoid becoming pregnant.

Pregnancy Category: D — always consult a doctor before taking during pregnancy.

Precautions & warnings
  • Monitor for peripheral neuropathy (burning sensation, hyperesthesia, paresthesia, neuropathic pain). Dose/schedule adjustment needed if pre-existing or worsening neuropathy.
  • Caution in patients with history of syncope, receiving antihypertensives, or dehydrated patients.
  • Monitor closely for heart failure in patients with cardiac risk factors or existing heart disease.
  • Gastrointestinal symptoms (nausea, diarrhea, constipation, vomiting) may require antiemetics and antidiarrheals; fluid and electrolyte replacement to prevent dehydration.
  • If new or worsening cardiopulmonary symptoms occur, interrupt Bortezomib for diagnostic evaluation.
  • Monitor CBC frequently; measure platelet count before each dose.
  • Monitor closely for tumor lysis syndrome in patients with high tumor burden.
  • If hepatic toxicity occurs, interrupt therapy to assess reversibility.
  • Do not use during pregnancy and lactation (Category D).
  • Avoid driving or operating machinery (fatigue, dizziness, fainting, blurred vision).
  • Drink plenty of fluids during treatment.
Overdose effects

Overdose more than twice the recommended dose may cause acute symptomatic hypotension and thrombocytopenia with fatal outcomes. No specific antidote. Monitor vital signs and provide supportive care (fluids, pressors, inotropic agents).

Storage conditions

Unopened vial: Do not store above 25°C. Keep in outer box to protect from light. Reconstituted solution: Store at 2-8°C; use within 8 hours. Do not use if particulate matter is observed or if solution is discolored.

Bortezomib — see the full informationPharmacology, precautions, pregnancy, overdose and the rest on the generic page
⚠️ This information is for educational purposes only — not a substitute for medical advice. Consult a registered physician before taking any medicine.