Pharmacologic class: Proteasome inhibitor

Therapeutic class: Antineoplastic

Pregnancy risk category D


Inhibits proteasomes (enzyme complexes that regulate protein homeostasis within cells). Reversibly inhibits chymotrypsin-like activity at 26S proteasome, leading to activation of signaling cascades, cell-cycle arrest, and apoptosis.


Powder for reconstitution (preservative-free): 3.5 mg (contains 35 mg of mannitol)

Indications and dosages

Multiple myeloma, patients with mantle cell lymphoma who have received at least one prior therapy

Adults: 1.3 mg/m2 I.V. or subcutaneously twice weekly for 2 weeks (days 1, 4, 8, and 11), followed by 10-day rest period (days 12 to 21). Allow at least 72 hours to elapse

between doses. One treatment cycle equals 21 days (3 weeks).

Dosage adjustment

• Moderate or severe hepatic impairment
• Peripheral neuropathy
• Grade 3 nonhematologic events
• Grade 4 hematologic events


• Hypersensitivity to drug, mannitol, or boron


Use cautiously in:
• peripheral neuropathy, dehydration, hepatic or renal impairment
• history of syncope or cardiovascular disorders
• pregnant or breastfeeding patients
• children.


• Be aware that drug is for I.V. or subcutaneous use only. Because each route of administration has a different reconstituted concentration, use caution when calculating volume to be administered.
• Reconstitute drug in vial with 3.5 ml of normal saline for injection to yield a concentration of 1 mg/ml for I.V. use.
• Reconstitute drug in vial with 1.4 ml of normal saline for injection to yield a concentration of 2.5 mg/ml for subcutaneous use.
• Give by I.V. push over 3 to 5 seconds or subcutaneously.
• Reconstituted solution must be used within 8 hours.

Adverse reactions

CNS: headache, insomnia, dizziness, anxiety, peripheral neuropathy, reversible posterior leukoen-cephalopathy syndrome

CV: tachycardia, hypotension

EENT: throat tightness

GI: nausea, vomiting, diarrhea, abdominal pain, dyspepsia

Hematologic: eosinophilia, anemia, thrombocytopenia, neutropenia

Hepatic: hyperbilirubinemia, hepatitis, acute liver failure

Metabolic: dehydration, pyrexia

Respiratory: cough, dyspnea, upper respiratory tract infection, acute diffuse infiltrative pulmonary disease (pneumonitis, interstitial pneumonia, acute respiratory distress syndrome)

Skin: rash, pruritus, urticaria

Other: altered taste, increased or decreased appetite, fever, chills, edema, tumor lysis syndrome


Drug-drug.CYP3A4 inducers (including amiodarone, carbamazepine, nevi-rapine, phenobarbital, phenytoin, and rifampin): possible decrease in bortezomid serum level and efficacy

CYP3A4 inhibitors (including amiodarone, cimetidine, clarithromycin, delavirdine, diltiazem, disulfiram, erythromycin, fluoxetine, fluvoxamine, nefazodone, nevirapine, propoxyphene, quinupristin, verapamil, zafirlukast, and zileuton): possible increase in bortezomib serum level and efficacy

Drug-diagnostic tests.Liver function

tests: increased levels

Drug-food.Grapefruit juice: increased bortezomib blood level, greater risk of toxicity

Patient monitoring

Monitor vital signs and temperature. Especially watch for tachycardia, fever, and hypotension.

Stay alert for and discontinue drug if posterior leukoencephalopathy (headache, seizures, lethargy, confusion, blindness) or tumor lysis syndrome occurs (irregular heartbeat, shortness of breath, high potassium level, high uric acid level, impairment of mental ability, kidney failure).

Closely monitor liver function tests and watch for signs and symptoms of hepatitis or liver failure.
• Monitor nutritional and hydration status for changes caused by GI adverse effects.
• Monitor CBC with white cell differential, and watch for signs and symptoms of blood dyscrasias.

Monitor respiratory status, watching for dyspnea, cough, and other signs and symptoms of upper respiratory tract infection.

Patient teaching

Inform patient that drug can cause serious blood dyscrasias. Teach him which signs and symptoms to report right away.
• Tell patient that drug may cause other significant adverse reactions. Reassure him he will be closely monitored.
• Instruct patient to move slowly when sitting or standing up to avoid dizziness or light-headedness from sudden blood pressure drop.
• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.
• Advise patient to minimize adverse GI effects by eating small frequent servings of healthy food and ensuring adequate fluid intake.
• Tell patient to immediately report signs and symptoms of upper respiratory tract infection.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs and foods mentioned above.


a trademark for bortezomib.


A proteasome inhibitor which induces apoptosis in cancer cells, and inhibits binding to stromal cells and production of growth and survival factors.

Treatment-refractory myeloma (35% response rate), mantle cell lymphoma.
Adverse effects
Thrombocytopaenia, fatigue, peripheral neuropathy, neutropaenia. 


A brand name for BORTEZOMIB.

Patient discussion about Velcade

Q. Has anyone out there taken the new drug Velcade?????? I've just started a JNJ Valcade trial and wonder if anyone out there has any experience this chemo treatment.

A. for a year and 2 months now. she is in pain but still alive and functioning.

More discussions about Velcade
References in periodicals archive ?
The CHMP has chosen a positive opinion recommending a label variation for the product to include updated overall survival data from the Phase three head-to-head ENDEAVOR trial in patients with relapsed or refractory multiple myeloma (KYPROLIS and dexamethasone compared with Velcade [bortezomib] and dexamethasone [Vd]).
Osaka JPN) are recalling batches of their Velcade blood-cancer medicine in the U.
Thalidomide and Velcade (bortezomib) will be made available for some patients with multiple myeloma, according to the National Institute Health and Clinical Excellence (Nice).
Thalidomide and Velcade (bortezomib) will be made available for some patients with multiple myeloma, according to guidance from the National Institute for Health and Clinical Excellence (Nice).
The breakthrough multiple myeloma drugs Velcade (bortezomib) and Revlimid (lenolidamide) could not prevent the cancer from recurring and failed to work at all on a large percentage of recurrent cancer.
The early stage trial combined elotuzumab with bortezomib, or Velcade, one of the novel chemotherapies approved to treat multiple myeloma, a cancer that arises in the plasma cells.
Other studies also indicated benefits with a wide range of Velcade combinations (including Velcade-Revlimid).
Merck and Multiple Myeloma Research Consortium (MMRC) initiated a Phase IIb study of Zolinza (Merck's vorinostat), an oral histone deacetylase (HDAC) inhibitor, in combination with Velcade (Millennium's bortezomib) for Injection, a proteasome inhibitor, in patients with relapsed and refractory multiple myeloma.
John McNamara, 47, was refused Velcade while other sufferers at the same hospital were given it because they lived in the "right" area.
VELCADE (bortezomib) for Injection, the market leader for multiple myeloma and mantle cell lymphoma patients, who have received at least one prior therapy, is the first and only marketed proteasome inhibitor.
Millennium markets VELCADE, a novel cancer product, and has a robust clinical development pipeline of product candidates.
Liam Lim, who celebrated his eighth birthday yesterday, raised pounds 182 for the so-called Velcade Three after seeing a TV report about their long-running battle to win equal access to a potentially life-saving drug for people with multiple myeloma.