Bortezomib

Bortezomib is a reversible inhibitor of the chymotrypsin-like activity of the 26S proteasome in mammalian cells. The 26S proteasome is a large protein complex that degrades ubiquitinated proteins.

• Bortezomib for injection is a proteasome inhibitor indicated for: • treatment of adult patients with multiple myeloma ( 1.1 ) • treatment of adult patients with mantle cell lymphoma ( 1.2 ) 1.1 Multiple Myeloma Bortezomib for injection is indicated for the treatment of adult patients with multiple myeloma. 1.2 Mantle Cell Lymphoma Bortezomib for injection is indicated for the treatment of adult patients with mantle cell lymphoma.ICD-10: C85.90, C90.00

• Bortezomib is contraindicated in patients with hypersensitivity (not including local reactions) to bortezomib, boron, or mannitol. Reactions have included anaphylactic reactions [see Adverse Reactions ( 6.1 )].contraindicated

• For subcutaneous or intravenous use only. Each route of administration has a different reconstituted concentration. Exercise caution when calculating the volume to be administered. ( 2.1 , 2.10 ) • The recommended starting dose of bortezomib for injection is 1.3 mg/m 2 administered either as a 3 to 5 second bolus intravenous injection or subcutaneous injection. ( 2.2 , 2.4 , 2.6 ) • Retreatment for Multiple Myeloma: May retreat starting at the last tolerated dose. ( 2.6 ) • Hepatic Impairment: Use a lower starting dose for patients with moderate or severe hepatic impairment. ( 2.8 ) • Dose must be individualized to prevent overdose. ( 2.10 ) 2.1 Important Dosing Guidelines Bortezomib for injection is for intravenous or subcutaneous use only. Do not administer bortezomib for injection by any other route. Because each route of administration has a different reconstituted concentration, use caution when calculating the volume to be administered. The recommended starting dose of bortezomib for injection is 1.3 mg/m 2 . Bortezomib for injection is administered intravenously at a concentration of 1 mg/mL, or subcutaneously at a concentration of 2.5 mg/mL [see Dosage and Administration ( 2.10 )]. Bortezomib for injection retreatment may be considered for patients with multiple myeloma who had previously responded to treatment with bortezomib for injection and who have relapsed at least six months after completing prior bortezomib for injection treatment. Treatment may be started at the last tolerated dose [see Dosage and Administration ( 2.6 )].

• Peripheral Neuropathy: Manage with dose modification or discontinuation. ( 2.7 ) Patients with pre-existing severe neuropathy should be treated with bortezomib only after careful risk-benefit assessment. ( 2.7 , 5.1 ) • Hypotension: Use caution when treating patients taking anti hypertensives, with a history of syncope, or with dehydration. ( 5.2 ) • Cardiac Toxicity: Worsening of and development of cardiac failure has occurred. Closely monitor patients with existing heart disease or risk factors for heart disease. ( 5.3 ) • Pulmonary Toxicity: Acute respiratory syndromes have occurred. Monitor closely for new or worsening symptoms and consider interrupting bortezomib therapy. ( 5.4 ) • Posterior Reversible Encephalopathy Syndrome: Consider MRI imaging for onset of visual or neurological symptoms; discontinue bortezomib if suspected. ( 5.5 ) • Gastrointestinal Toxicity: Nausea, diarrhea, constipation, and vomiting may require use of antiemetic and antidiarrheal medications or fluid replacement. ( 5.6 ) • Thrombocytopenia and Neutropenia: Monitor complete blood counts regularly throughout treatment. ( 5.7 ) • Tumor Lysis Syndrome: Closely monitor patients with high tumor burden. ( 5.8 ) • Hepatic Toxicity: Monitor hepatic enzymes during treatment. Interrupt bortezomib therapy to assess reversibility. ( 5.9 ) • Thrombotic Microangiopathy: Monitor for signs and symptoms. Discontinue bortezomib if suspected. ( 5.10 ) • Embryo-Fetal Toxicity: Bortezomib can cause fetal harm.

The following clinically significant adverse reactions are also discussed in other sections of the labeling: • Peripheral Neuropathy [see Warnings and Precautions ( 5.1 )] • Hypotension [see Warnings and Precautions ( 5.2 )] • Cardiac Toxicity [see Warnings and Precautions ( 5.3 )] • Pulmonary Toxicity [see Warnings and Precautions ( 5.4 )] • Posterior Reversible Encephalopathy Syndrome (PRES) [see Warnings and Precautions ( 5.5 )] • Gastrointestinal Toxicity [see Warnings and Precautions ( 5.6 )] • Thrombocytopenia/Neutropenia [see Warnings and Precautions ( 5.7 )] • Tumor Lysis Syndrome [see Warnings and Precautions ( 5.8 )] • Hepatic Toxicity [see Warnings and Precautions ( 5.9 )] • Thrombotic Microangiopathy [see Warnings and Precautions ( 5.10 )] Most commonly reported adverse reactions (incidence ≥ 20%) in clinical studies include nausea, diarrhea, thrombocytopenia, neutropenia, peripheral neuropathy, fatigue, neuralgia, anemia, leukopenia, constipation, vomiting, lymphopenia, rash, pyrexia, and anorexia. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Hetero Labs Limited at 1-866-495-1995 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice.

Patients with diabetes may require close monitoring of blood glucose and adjustment of antidiabetic medication. ( 8.8 ) 8.1 Pregnancy Risk Summary Based on its mechanism of action [see Clinical Pharmacology ( 12.1 )] and findings in animals, bortezomib can cause fetal harm when administered to a pregnant woman. There are no studies with the use of bortezomib in pregnant women to inform drug-associated risks. Bortezomib caused embryo-fetal lethality in rabbits at doses lower than the clinical dose (see Data) . Advise pregnant women of the potential risk to the fetus. Adverse outcomes in pregnancy occur regardless of the health of the mother or the use of medications. The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. Data Animal Data Bortezomib was not teratogenic in nonclinical developmental toxicity studies in rats and rabbits at the highest dose tested (0.075 mg/kg; 0.5 mg/m 2 in the rat and 0.05 mg/kg; 0.6 mg/m 2 in the rabbit) when administered during organogenesis. These dosages are approximately 0.5 times the clinical dose of 1.3 mg/m 2 based on body surface area.

Metabolism

Following intravenous administration of 1 mg/m 2 and 1.3 mg/m 2 doses, the mean maximum plasma concentrations of bortezomib (C max ) after the first dose (Day 1) were 57 and 112 ng/mL, respectively. When administered twice weekly, the mean maximum observed plasma concentrations ranged from 67 to 106 ng/mL for the 1 mg/m 2 dose and 89 to 120 ng/mL for the 1.3 mg/m 2 dose.

There is no known specific antidote for bortezomib overdosage. In humans, fatal outcomes following the administration of more than twice the recommended therapeutic dose have been reported, which were associated with the acute onset of symptomatic hypotension (5.2) and thrombocytopenia (5.7). In the event of an overdosage, the patient's vital signs should be monitored and appropriate supportive care given. Studies in monkeys and dogs showed that intravenous bortezomib doses as low as two times the recommended clinical dose on a mg/m 2 basis were associated with increases in heart rate, decreases in contractility, hypotension, and death. In dog studies, a slight increase in the corrected QT interval was observed at doses resulting in death. In monkeys, doses of 3.0 mg/m 2 and greater (approximately twice the recommended clinical dose) resulted in hypotension starting at one hour postadministration, with progression to death in 12 to 14 hours following drug administration.

• May 13, 2003NDANDA021602Takeda Pharms Usa
• May 2, 2022NDANDA209191Hospira
• May 2, 2022ANDAANDA205533Apotex
• May 2, 2022ANDAANDA209659Fresenius Kabi Usa
• May 2, 2022ANDAANDA212825Eugia Pharma
• May 2, 2022ANDAANDA208392Pharmascience Inc
• Jul 27, 2022NDANDA215331Maia Pharms Inc
• Aug 26, 2024NDANDA212782Shilpa

Recent PubMed references pinned to Bortezomib as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

• Proteasomal inhibition compromises microvascular integrity via distinct effects on non-immune endothelial cells and immune cells.
  Frontiers in immunology · 2026 · Sawant P, Wolf H, Mathew A, et al.
  PMID 42253955DOI 10.3389/fimmu.2026.1759368
• A dual green chromatographic platform for bioanalytical quantification and pharmacokinetic characterization of the BBD antineoplastic regimen.
  Analytica chimica acta · 2026 · Sharkawi MMZ, Amin NH, Mohamed NR, et al.
  PMID 42218001DOI 10.1016/j.aca.2026.345652
• CD161⁺ NKT Cell Proportion as a Predictive Biomarker for Bortezomib Treatment Response in Newly Diagnosed Multiple Myeloma Patients.
  Clinical laboratory · 2026 · Zhou S, Xu X, Cuo J, et al.
  PMID 42159124DOI 10.7754/Clin.Lab.2025.250744
• ZNF750 loss defines an ESCC subtype with constitutive NF-κB activation and vulnerability to bortezomib.
  Biochimica et biophysica acta. Molecular basis of disease · 2026 · Bi Y, Wang M, Zhang Y, et al.
  PMID 42086128DOI 10.1016/j.bbadis.2026.168282
• ATF3/SLC31A1-Mediated Cuproptosis Contributes to Bortezomib-Induced Peripheral Neurotoxicity and Intervention by (-)-Epigallocatechin Gallate.
  International journal of molecular sciences · 2026 · Wang Y, Lu J, Feng X, et al.
  PMID 42074318DOI 10.3390/ijms27083680
• 6-O-Carboxypropyl-α-Tocotrienol Enhances the Anticancer Effects of Bortezomib Without Suppressing NRF1 and NRF3 in Colorectal Cancer Cells.
  Anticancer research · 2026 · Ishii K, Yano T
  PMID 42049351DOI 10.21873/anticanres.18124
• Icaritin Inhibits Malignant Progression and Enhances Ferroptosis and Bortezomib Sensitivity by Suppressing HSP90AA1 Expression in Multiple Myeloma.
  Chemical biology & drug design · 2026 · Shi L, Lv D, Wang X, et al.
  PMID 41973828DOI 10.1111/cbdd.70284
• Navigating the Post-BCMA/GPRC5D Landscape: Efficacy of Selinexor, Bortezomib, and Dexamethasone After Sequential Immunotherapy Failure in Penta-Refractory Multiple Myeloma-A Multicenter Analysis.
  American journal of hematology · 2026 · Al-Bazaz M, Alsdorf W, Leypoldt L, et al.
  PMID 41914448DOI 10.1002/ajh.70297

The 10 most recently updated of 1,093 ClinicalTrials.gov registrations naming Bortezomib as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• All Japanese Population: Belantamab Mafodotin Plus Pomalidomide and Dexamethasone (Pd) Versus Bortezomib Plus Pd in Relapsed/Refractory Multiple Myeloma
  Active not recruiting · Phase 3 · Interventional · 21 enrolled · GlaxoSmithKline
  NCT06956170updated 2026-06-12
• Belantamab Mafodotin Plus Pomalidomide and Dexamethasone (Pd) Versus Bortezomib Plus Pd in Relapsed/Refractory Multiple Myeloma
  Active not recruiting · Phase 3 · Interventional · 302 enrolled · GlaxoSmithKline
  NCT04484623updated 2026-06-12
• Study Assessing Activity of Intravenous (IV) Etentamig Monotherapy Versus Standard Available Therapies in Adult Participants With Relapsed or Refractory Multiple Myeloma
  Recruiting · Phase 3 · Interventional · 380 enrolled · AbbVie
  NCT06158841updated 2026-06-12
• Lenalidomide and Dexamethasone With or Without Bortezomib in Treating Patients With Previously Untreated Multiple Myeloma
  Active not recruiting · Phase 3 · Interventional · 525 enrolled · National Cancer Institute (NCI)
  NCT00644228updated 2026-06-11
• A Study Comparing AZD0120, a Dual-targeted CAR-T Against B-cell Maturation Antigen (BCMA) and CD19, Versus Standard Regimens in Participants With Relapsed Refractory Multiple Myeloma (DURGA-4)
  Recruiting · Phase 3 · Interventional · 508 enrolled · AstraZeneca
  NCT07391657updated 2026-06-11
• A Study to Evaluate the Efficacy and Safety of Belantamab Mafodotin in Combination With Standard of Care in Participants With Relapsed-Refractory Multiple Myeloma (RRMM)
  Recruiting · Phase 2 · Interventional · 200 enrolled · GlaxoSmithKline
  NCT07227311updated 2026-06-10
• Comparing Combinations of Drugs to Treat Newly Diagnosed Multiple Myeloma (NDMM) When a Stem Cell Transplant is Not a Medically Suitable Treatment
  Recruiting · Phase 3 · Interventional · 510 enrolled · SWOG Cancer Research Network
  NCT05561387updated 2026-06-10
• A Study to Evaluate Mezigdomide, Bortezomib and Dexamethasone (MEZIVd) Versus Pomalidomide, Bortezomib and Dexamethasone (PVd) in Participants With Relapsed or Refractory Multiple Myeloma (RRMM)
  Recruiting · Phase 3 · Interventional · 810 enrolled · Celgene
  NCT05519085updated 2026-06-10
• Study to Evaluate Efficacy and Safety of Belantamab-based Combinations for Relapsed Multiple Myeloma
  Not yet recruiting · Observational · 100 enrolled · PETHEMA Foundation
  NCT07637526updated 2026-06-09
• Acalabrutinib Maleate and Bortezomib for Patients With HLA Antibodies
  Not yet recruiting · Phase 3 · Interventional · 42 enrolled · The First Affiliated Hospital of Soochow University
  NCT07635511updated 2026-06-09

Frequently asked questions

How does Bortezomib work?

Bortezomib is a reversible inhibitor of the chymotrypsin-like activity of the 26S proteasome in mammalian cells. The 26S proteasome is a large protein complex that degrades ubiquitinated proteins.

What is Bortezomib used for?

According to FDA labeling, Bortezomib carries indications including: Bortezomib for injection is a proteasome inhibitor indicated for: • treatment of adult patients with multiple myeloma ( 1.1 ) • treatment of adult patients with mantle cell lymphoma ( 1.2 ) 1.1 Multiple Myeloma Bortezomib for injection is indicated for the treatment of adult patients with multiple myeloma. 1.2 Mantle Cell Lymphoma Bortezomib for injection is indicated for the treatment of adult patients with mantle cell lymphoma.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Bortezomib?

Bortezomib is classified as Proteasome inhibitors, Proteasome Inhibitor, Proteasome Inhibitors, Ubiquitin Ligase Inhibitors, Increased Cellular Death.

What are the brand names for Bortezomib?

Bortezomib is marketed under brand names including Boruzu, Velcade.

What are the contraindications for Bortezomib?

Bortezomib labeling lists contraindications including: Bortezomib is contraindicated in patients with hypersensitivity (not including local reactions) to bortezomib, boron, or mannitol. Reactions have included anaphylactic reactions [see Adverse Reactions ( 6.1 )].. Always consult the full prescribing information and a clinician.