Classifications: antineoplastic agent; biologic response modifier; proteosome inhibitor; Therapeutic: antineoplastic agent; biologic response modifier
Pregnancy Category: D
3.5 mg powder for injection
Bortezomib is a reversible inhibitor of proteasome, which is responsible for regulation of protein expression and degradation
of damaged or obsolete proteins within the cell; its activity is critical to activation or suppression of cellular functions
including the cell cycle, oncogene expression, and apoptosis. Malignant cells are much more sensitive to the effects of
proteasome inhibition than normal cells.
Proteasome inhibition may reverse some of the changes that allow proliferation of malignant cells and suppress apoptosis
(programmed cell death) in malignant cells.
Treatment of relapsed or refractory multiple myeloma or mantle cell lymphoma in patients who have failed one prior therapy.
Hypersensitivity to bortezomib, boron, or mannitol; pregnancy (category D); lactation. Safety and effectiveness in children
are not established.
Peripheral neuropathy; history of syncope, dehydration, hypotension; concurrent antihypertensive drugs; history of allergies,
asthma; preexisting electrolyte or acid-base disturbances, especially hypokalemia or hyponatremia; liver disease; myelosuppression,
renal impairment; history of peripheral neuropathy or other neurologic disorders; GI toxicities.
Route & Dosage
|Multiple Myeloma/Mantle Cell Lymphoma
Adult: IV 1.3 mg/m2 twice weekly for 2 wk (days 1, 4, 8, and 11) followed by a 10-d rest period; at least 72 h should elapse between consecutive
doses; 3 wk period is a treatment cycle
Withhold dose with grade 3 or 4 hematologic toxicity, when symptoms resolve dose may be reduced 25% and restarted.
- Wear protective gloves and prevent contact with skin.
PREPARE: Direct: Reconstitute 3.5 mg vial with 3.5 mL of NS for injection to yield 1 mg/mL. Discard if not clear and colorless. Give within
8 h of reconstitution.
ADMINISTER: Direct: Give as a bolus dose over 35 sec. Flush before/after with NS. ??Store unopened vials at 15°30° C (59°86° F). Protect from light.??Store reconstituted vials at 15°30° C (59°86° F). Give within 8 h of reconstitution. May store
up to 3 h in a syringe; however, total storage time must not exceed 8 h when exposed to normal indoor lighting.
INCOMPATIBILITIES Solution/additive: No data available. Do not recommend mixing or injecting with any other drugs.
Adverse Effects (≥1%) Body as a Whole: Asthenia, weakness, fatigue, malaise, fever, dehydration, peripheral neuropathy, rigors, herpes zoster. CNS: Insomnia, headache, paresthesia, dizziness, anxiety. CV: Edema, hypotension, orthostatic hypotension. GI: Nausea, vomiting, diarrhea, anorexia, abdominal pain, constipation, dyspepsia, dysphagia. Hematologic: Thrombocytopenia, neutropenia, anemia. Musculoskeletal: Arthralgia, musculoskeletal pain, bone pain, myalgia, back pain, muscle cramps. Respiratory: Dyspnea, cough, upper respiratory infection. Skin: Rash, pruritus. Special Senses: Blurred vision, diplopia.
Interactions Drug: Hypoglycemia
and hyperglycemia have been reported with antidiabetic agents
; antihypertensive agents
may exacerbate hypotension; anticoagulants
, antithymocyte globulin, nsaids
, platelet inhibitors
, aspirin, thrombolytic agents
may increase risk of bleeding. Food: Grapefruit juice
may increase drug levels.
In the liver primarily by CYP3A4. Half-Life:
Assessment & Drug Effects
- Monitor for and report S&S of neuropathy (e.g., hyperesthesia, hypoesthesia, paresthesia, discomfort or neuropathic pain).
- Monitor postural vital signs for orthostatic hypotension.
- Monitor I&O and assess for S&S of dehydration or electrolyte imbalance if vomiting and/or diarrhea develop.
- Lab tests: Frequent CBC with platelet count; baseline and periodic LFTs; frequent blood glucose in diabetics.
Patient & Family Education
- Report promptly any of the following: dizziness, light-headedness or fainting spells; numbness, tingling, or other unusual
sensations; signs of infection (e.g., fever, chills, cough, sore throat); bruising, pinpoint red spots on the skin; black,
tarry stools, nosebleeds, or any other sign of bleeding.
- Do not drive or engage in other hazardous activities until reaction to drug is known.
- Females should use reliable methods of contraception to avoid pregnancy while on this drug.