[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › [Other antineoplastics (differentiating agents, asparaginases, proteasome inhibitors)](https://durgical.com/en/pharmacology/classes/other-antineoplastics/) › Bortezomib # Bortezomib ## Other antineoplastics (differentiating agents, asparaginases, proteasome inhibitors)? Other antineoplastics (differentiating agents, asparaginases, proteasome inhibitors) ## High alert? An error with this medicine can cause serious harm: double checks and protocols are used. The first proteasome inhibitor, a cornerstone of multiple myeloma and also used in mantle cell lymphoma. Its main toxicity is peripheral neuropathy. Updated Nov 1, 2026 ## Quick facts **Group** [Other antineoplastics (differentiating agents, asparaginases, proteasome inhibitors)](https://durgical.com/en/pharmacology/classes/other-antineoplastics/) **Target** 26S proteasome, chymotrypsin-like site (β5 subunit) **Used for** Multiple myeloma · Mantle cell lymphoma **Key effects** Peripheral neuropathy · Nausea · Thrombocytopenia **Monitor** Neuropathy symptoms before each dose · Blood counts **ATC** L01XG01 No doses: the clinician sets them by the current guideline. On this page - The basics Mechanism of action - Indications - Adverse effects - Pharmacokinetics - Memory aid - Clinical What the labels mean - Safety Contraindications - Key interactions - What is monitored - Administration and safety - Pregnancy and breastfeeding - Nursing care - Study Test yourself - Connections Connections ## Mechanism of action ✂**26S proteasome, chymotrypsin-like site (β5 subunit)**Bortezomib ⓘ The crystal shows the human 20S proteasome core with bortezomib in the active sites of its catalytic subunits. **Target in 3D:** 26S proteasome, chymotrypsin-like site (β5 subunit). PDB structure 5LF3 (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/5LF3) · Drag to rotate · pinch to zoom The proteasome destroys proteins tagged with ubiquitin, including misfolded proteins and regulators of cell signalling. Bortezomib, a boronic acid dipeptide, reversibly inhibits its chymotrypsin-like activity. Myeloma cells make huge amounts of antibody protein and are very dependent on this disposal system: when it is blocked, misfolded and regulatory proteins pile up, stress pathways switch on and the cell dies by apoptosis. - Ubiquitin-tagged proteins go to the proteasome - Bortezomib blocks its chymotrypsin-like site - Misfolded and regulatory proteins accumulate - Protein-loaded myeloma cells die (apoptosis) ## Indications - Multiple myeloma, newly diagnosed or relapsed, usually with other drugs (dexamethasone, lenalidomide, thalidomide). [Multiple myeloma →](https://durgical.com/en/conditions/multiple-myeloma/) - Mantle cell lymphoma. [Non-Hodgkin lymphoma →](https://durgical.com/en/conditions/non-hodgkin-lymphoma/) ## Adverse effects ### Common - Peripheral neuropathy: burning, numbness, pain in hands and feet - Nausea, diarrhoea, constipation, vomiting - Thrombocytopenia, neutropenia, anaemia - Fatigue, fever, loss of appetite - Rash ### Serious (rare, important) - Severe peripheral and autonomic neuropathy - Low blood pressure and fainting - Heart failure - Acute lung toxicity - Posterior reversible encephalopathy syndrome - Herpes zoster reactivation - Tumour lysis syndrome - Hepatotoxicity and thrombotic microangiopathy ## Contraindications - Allergy to bortezomib, boron or mannitol - Intrathecal administration (never given into the spinal canal) ## Key interactions **Strong CYP3A4 inhibitors (e.g. ketoconazole)** Raise bortezomib exposure; the patient is watched closely for toxicity. **Strong CYP3A4 inducers (rifampicin, St John's wort)** Lower its effect; avoided. **Oral antidiabetic drugs** Both low and high glucose have been reported; glucose is followed and treatment adjusted. **Antihypertensives** Add to bortezomib's low blood pressure. ## What is monitored - Neuropathy symptoms before each dose - Blood counts, especially platelets, before each dose - Blood pressure and hydration - Liver tests - Glucose in people with diabetes - Uric acid and potassium when tumour burden is high ## Administration and safety - Subcutaneous or intravenous only; never intrathecal (wrong-route deaths have occurred with this class of mistakes). - The reconstituted concentration differs for the subcutaneous and intravenous routes, so the volume is checked carefully for the intended route. - Subcutaneous injection sites are rotated. - Hazardous drug: prepared and disposed of following cytotoxic handling procedures. ## Pregnancy and breastfeeding Can harm the fetus; effective contraception is used by women and by men with female partners during treatment. ## Nursing care - Ask about tingling, burning or pain in hands and feet before each dose and report new or worse symptoms. - Check blood pressure, lying and standing if dizzy; encourage fluids if dehydrated. - Review platelet count and look for bleeding. - Confirm antiviral prophylaxis against herpes zoster if ordered. - Teaching: rise slowly, report fainting, rash with blisters, breathlessness or sudden vision change; avoid driving until the effect is known. ## Pharmacokinetics **Absorption** Subcutaneous or intravenous injection. **Distribution** Large volume of distribution; moderately bound to plasma proteins. **Metabolism** Oxidised by liver CYP enzymes (CYP3A4, CYP2C19, CYP1A2) to inactive metabolites. **Elimination** The routes of elimination in humans are not well characterised. ## Memory aid «BORtezomib BORes into the proteasome» (boron). Myeloma cells drown in their own proteins. Watch the feet (neuropathy) and the platelets. ## Test yourself Think of the answer, then tap the question to see it. ## What does bortezomib inhibit? The chymotrypsin-like activity of the 26S proteasome. ## Why are myeloma cells especially sensitive to proteasome inhibition? They produce large amounts of immunoglobulin and depend on the proteasome to clear misfolded proteins. ## Which route of administration is absolutely contraindicated for bortezomib? Intrathecal. ## Which viral infection prophylaxis is commonly given with bortezomib? Antiviral prophylaxis against herpes zoster reactivation. [Add to my cards (4)](https://durgical.app/estudiar/?add=/en/pharmacology/bortezomib/) [More Pharmacology questions →](https://durgical.com/en/practice/?f=pharmacology) ## What the labels mean **High alert** An error with this medicine can cause serious harm: double checks and protocols are used. ## Connections ## Related drugs 1 - [Rituximab](https://durgical.com/en/pharmacology/rituximab/) ## Related conditions 2 - [Multiple myeloma](https://durgical.com/en/conditions/multiple-myeloma/) - [Non-Hodgkin lymphoma](https://durgical.com/en/conditions/non-hodgkin-lymphoma/) [← Back to the class: Other antineoplastics (differentiating agents, asparaginases, proteasome inhibitors)](https://durgical.com/en/pharmacology/classes/other-antineoplastics/) Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given. Sources: [DailyMed - BORTEZOMIB injection, powder, lyophilized, for solution](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=decb5d94-2ea2-48d8-b08b-3196b24c0ed3) (DailyMed (U.S. National Library of Medicine), 2026); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=L01XG01) (WHO Collaborating Centre for Drug Statistics Methodology, 2026); [eEML - Electronic Essential Medicines List](https://list.essentialmeds.org/) (World Health Organization, 2025). ## **Spotted a mistake?** We are always improving for the community. Tell us what is wrong and our team will review it. Report a mistake Representative model, for educational purposes only. --- Source: https://durgical.com/en/pharmacology/bortezomib/ License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/bortezomib/