Bortezomib

Indications
 Intravenous
Multiple myeloma
Adult: Patients without symptoms or with Grade 1 peripheral neuropathy symptoms: 1.3 mg/m2 as IV bolus over 3-5 sec on days 1, 4, 8 and 11 of a 21-day cycle, followed by a 10-day rest period (days 12-21). At least 72 hr should elapse between consecutive doses.

Special Populations: Onset of any Grade 3 non-haematological or Grade 4 haematological toxicities excluding neuropathy: Withhold therapy until toxicities symptoms resolved, then reinitiate at 25% reduced dose. Grade 1 with pain or Grade 2 peripheral neuropathy symptoms: 1 mg/m2 2x wkly for 2 wk (days 1, 4, 8, 11), then a 10-day rest period (days 12-21). At least 72 hrs elapse between consecutive dose. Grade 2 with pain or Grade 3 peripheral neuropathy symptoms: Withhold therapy until toxicity resolves, then reduce dose to 0.7 mg/m2 weekly. Grade 4 peripheral neuropathy symptoms: Discontinue.
Contraindications
 Hypersensitivity. Child. Pregnancy and lactation.
Warnings / Precautions
 Hepatic or renal impairment; history of syncope, orthostatic hypotension; dehydration. Impairs ability to drive or operate machinery. Monitor for symptoms of peripheral neuropathy. Monitor closely the blood glucose levels in patients receiving oral antidiabetic agents.
Adverse Reactions
 Asthenic conditions; pyrexia; GI disturbances, anorexia; dehydration; peripheral neuropathy; thrombocytopenia, neutropenia, anaemia; hypotension; cardiac disorders; bone and body pain; cough, dyspnoea; rash, oedema; hypersensitivity reactions; painful or difficult urination.
Potentially Fatal: Pneumonia, pyrexia, diarrhoea, vomiting, dehydration and nausea.
Overdose Reactions
 Symptoms include hypotension and thrombocytopenia. Monitor vital signs and admin appropriate supportive care.
Drug Interactions
 Concurrent use of amiodarone, antivirals, isoniazid, nitrofurantoin, statins may increase the chance of peripheral neuropathy. Concurrent use of antihypertensives increases the chance of hypotension.
See Below for More bortezomib Drug Interactions
Mechanism of Actions
 Bortezomib is a reversible inhibitor of the chymotrypsin-like activity of the 26-S proteasome. It prevents targeted proteolysis that affects multiple signaling cascades responsible for normal homeostatic functions within the cell, leading to cell death.
Distribution: Protein binding: >80%.
Metabolism: Mainly metabolised via the cytochrome P450 isoenzymes CYP3A4, CYP2C19 and CYP1A2.
ATC Classification
 L01XX32 - bortezomib ; Belongs to the class of other antineoplastic agents. Used in the treatment of cancer.
Available As
  • Bortezomib 2 mg
  • Bortezomib 3.5 mg

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