bortezomib

Contraindicated in:

Hypersensitivity to bortezomib, boron, or mannitol
Intrathecal administration (may cause death)
OB: Pregnancy
Lactation: Lactation.

Use Cautiously in:

Moderate to severe hepatic impairment
History of or risk factors for HF
Rep: Women of reproductive potential and men with female partners of reproductive potential
Pedi: Safety and effectiveness not established in children.

Adv. Reactions/Side Effects ⬆ ⬇

CV: hypotension, HF.

Derm: STEVENS-JOHNSON SYNDROME, TOXIC EPIDERMAL NECROLYSIS.

EENT: blurred vision, diplopia.

GI: anorexia, constipation, diarrhea, nausea, vomiting, LIVER FAILURE.

Hemat: anemia, neutropenia, thrombocytopenia, BLEEDING, THROMBOTIC THROMBOCYTOPENIC PURPURA/HEMOLYTIC UREMIC SYNDROME.

Neuro: fatigue, malaise, peripheral neuropathy, weakness, dizziness, POSTERIOR REVERSIBLE ENCEPHALOPATHY SYNDROME (PRES), syncope.

Resp: pneumonia.

Misc: fever, tumor lysis syndrome.

Interactions ⬆ ⬇

Drug-Drug:

Concurrent neurotoxic medications including amiodarone, some antivirals, nitrofurantoin, isoniazid, or HMG-CoA reductase inhibitors may ↑ risk of peripheral neuropathy.

Availability ⬆ ⬇

(Generic available)

Lyophilized powder for injection: 3.5 mg/vial;
Solution for injection: 1 mg/mL; 2.5 mg/mL;

Route/Dosage ⬆ ⬇

Previously Untreated Multiple Myeloma

IV, SC (Adults): 1.3 mg/m² twice weekly for Cycles 1–4 (days 1, 4, 8, 11, 22, 25, 29, and 32; no treatment during cycle 3), then once weekly for Cycles 5–9 (days 1, 8, 22, and 29; no treatment during Cycle 7); further cycles/doses depend on response and toxicity.

Hepatic Impairment

IV (Adults): Moderate or severe hepatic impairment: 0.7 mg/m² per injection for the first cycle, then may ↑ to 1 mg/m² per injection or ↓ further to 0.5 mg/m² per injection, based on tolerability.

Previously Untreated Mantle Cell Lymphoma

IV, SC (Adults): 1.3 mg/m² twice weekly on days 1, 4, 8, and 11, followed by a 10-day rest (days 12–21); repeat for 5 additional cycles; further cycles/doses depend on response and toxicity.

Hepatic Impairment

IV (Adults): Moderate or severe hepatic impairment: 0.7 mg/m² per injection for the first cycle, then may ↑ to 1 mg/m² per injection or ↓ further to 0.5 mg/m² per injection, based on tolerability.

Relapsed Multiple Myeloma and Mantle Cell Lymphoma

IV, SC (Adults): 1.3 mg/m² twice weekly for 2 wk (days 1, 4, 8, and 11), followed by a 10-day rest; further cycles/doses depend on response and toxicity. Patients with multiple myeloma who have previously responded to bortezomib therapy and who have relapsed ≥6 mo after prior bortezomib therapy can be started on their last tolerated dose; dose should be given twice weekly (days 1, 4, 8, and 11) every 3 wk for a maximum of 8 cycles.

Hepatic Impairment

IV (Adults): Moderate or severe hepatic impairment: 0.7 mg/m² per injection for the first cycle, then may ↑ to 1 mg/m² per injection or ↓ further to 0.5 mg/m² per injection, based on tolerability.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Inhibits proteasome, a regulator of intracellular protein catabolism, resulting in disruption of various intracellular processes.
Cytotoxic to a variety of cancerous cells.

Therapeutic Effects:

Decreased progression and improved survival in multiple myeloma and mantle cell lymphoma.

Classifications ⬆ ⬇

Therapeutic Classification: antineoplastics

Pharmacologic Classification: proteasome inhibitors

Pharmacokinetics ⬆ ⬇

Absorption: IV administration results in complete bioavailability.

Distribution: Widely distributed to tissues.

Metabolism/Excretion: Mostly metabolized by the liver via the CYP2C19, CYP3A4, and CYP1A2 isoenzymes, and to a lesser extent by the CYP2D6 and CYP2C9 isoenzymes; excretion pathway unknown.

Half-life: 9–15 hr.

Time/Action Profile ⬆ ⬇

ROUTE	ONSET	PEAK	DURATION
IV	unknown	38 days*	unknown

*Median time to response based on clinical parameters.

Patient/Family Teaching ⬆ ⬇

Caution the patient that dehydration may occur with vomiting or diarrhea. Advise patient to maintain fluid intake and to notify health care professional if dizziness or fainting occurs.
Instruct patient to contact health care professional if they experience new or worsening signs of peripheral neuropathy (tingling, numbness, pain, burning feeling in the feet or hands, weakness in the arms or legs), PML (progressive weakness on one side of the body or clumsiness of limbs; disturbance of vision; changes in thinking, memory, and orientation leading to confusion and personality changes), or if symptoms of dehydration (dizziness, fainting) due to vomiting or diarrhea; rash; shortness of breath; cough; swelling of feet, ankles, or legs; bleeding, infection, convulsions; persistent headache; reduced eyesight; increase in BP or blurred vision occur.
May cause dizziness and blurred vision. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking Rx, OTC, or herbal products, especially St. John's wort.
Advise diabetic patients taking oral hypoglycemic agents to monitor blood glucose frequently and notify health care professional of changes in blood sugar.
Rep: Advise females of reproductive potential to use effective contraception during and for 7 mo after last dose and to avoid breast feeding during therapy and for 2 mo after therapy. Advise males with female partner of reproductive potential to use effective contraception for 4 mo after last dose of bortezomib. Patient should notify health care professional immediately if pregnancy is suspected. May impair fertility for male and female patients.

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Indications ⬇

Contraind./Precautions ⬆ ⬇

Adv. Reactions/Side Effects ⬆ ⬇

Interactions ⬆ ⬇

Availability ⬆ ⬇

Route/Dosage ⬆ ⬇

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Classifications ⬆ ⬇

Pharmacokinetics ⬆ ⬇

Time/Action Profile ⬆ ⬇

Patient/Family Teaching ⬆ ⬇

Pronunciation ⬆ ⬇

Code ⬆