Bortezomib Application Scope

Bortezomib is indicated for the treatment of adult patients with multiple myeloma (MM). Also approved for mantle cell lymphoma (MCL).
(In some regions) used for the re-treatment of multiple myeloma patients.

Bortezomib Characteristics

Ingredients: Bortezomib
Properties: A white to off-white cake or powder for reconstitution into a sterile solution
Packaging Specification: Single-dose vials containing 3.5 mg of bortezomib as a sterile lyophilized powder
Storage: Store in the original package at 25°C (77°F). Excursions are permitted between 15-30°C (59-86°F)
Expiry Date: As stated on the vial and outer packaging
Executive Standard: Complies with the specifications of the current approved product labeling
Approval Number: Specific to each country; see local product labeling
Date of Revision: For the latest version, check the official package insert
Manufacturer: Pfizer (Velcade)

Guidelines for the Use of Bortezomib

Dosage and Administration:
- Recommended Dose:
  - The standard starting dose for many regimens: 1.3 mg/m² per dose.
  - Cycle scheduling depends on the treatment protocol (e.g., on days 1, 4, 8, and 11 in a 21-day cycle for some myeloma regimens).
- Administration:
  - Intravenous (IV): Typically 3–5 second bolus injection.
  - Subcutaneous (SC): Alternative route; some regimens prefer SC because of lower neuropathy risk.
  - Reconstitution: e.g., for 3.5 mg vial, add 3.5 mL of 0.9% NaCl to make 1 mg/mL (for some Velcade formulations)
- Missed Dose: If a dose is missed, the re-treatment or “catch-up” depends on the specific cycle schedule.
Adverse Reactions:
- Common Adverse Reactions:
  
  Based on clinical studies/prescribing information: Nausea
  - Diarrhea
  - Thrombocytopenia
  - Neutropenia
  - Peripheral neuropathy
  - Fatigue
  - Neuralgia
  - Anemia
  - Leukopenia
  - Constipation
  - Vomiting
  - Lymphopenia
  - Rash
  - Fever (pyrexia)
  - Anorexia
- Serious Adverse Reactions:
  - Peripheral neuropathy, including severe sensory and motor neuropathy.
  - Cardiovascular: heart failure, pulmonary edema, QT-interval prolongation (isolated cases)
  - Pulmonary toxicity: acute respiratory distress syndrome (ARDS), interstitial lung disease, pneumonitis.
  - Hematologic toxicity: cyclic thrombocytopenia / neutropenia.
  - Thrombotic microangiopathy (per more recent label updates)
  - Tumor lysis syndrome in patients with high tumor burden.
  - Embryo-fetal toxicity: potential fetal harm; advise females of reproductive potential to avoid pregnancy.
  - Posterior Reversible Encephalopathy Syndrome (PRES) (in some reported cases)
Contraindications:
- Hypersensitivity to bortezomib, boron, or mannitol (some formulations contain mannitol).
- Intrathecal administration (into the spine) is absolutely contraindicated—fatal events have occurred.
Precautions:
- Patients with pre-existing peripheral neuropathy should be monitored closely; dose modification or discontinuation may be required if neuropathy worsens.
- Cardiac monitoring: patients with heart disease or risk factors may need close monitoring (risk of heart failure, fluid overload).
- Pulmonary symptoms: new or worsening dyspnea/infiltrates → interrupt therapy and evaluate.
- Hematologic parameters: frequent CBC monitoring because of thrombocytopenia/neutropenia.
- Hepatic impairment: In moderate/severe liver dysfunction, dose adjustment may be needed.
- Pregnancy: may cause fetal harm; counsel women of childbearing potential.
- Hypotension: caution in patients with dehydration, those on antihypertensives, history of syncope.
- Tumor lysis: monitor high-burden disease for tumor lysis syndrome.

Bortezomib Interactions

CYP3A4 inhibitors (e.g., ketoconazole) can increase bortezomib exposure.
PMCCYP3A4 inducers (e.g., rifampin) can decrease bortezomib exposure; use with caution/avoid.
PMC: Because bortezomib is metabolized by multiple CYPs, other drugs affecting CYP pathways may interact.
Proper handling: Cytotoxic drug handling procedures should be followed during preparation/administration.

Note:

If there is a new packaging for the drug, the new packaging shall prevail. The above information is sourced from DengYue Medicine.
This content is for reference only. Prescription drugs must be used under a doctor’s guidance and purchased from authorized sources.