Bortezomib

Bortezomib Brand Name– Velcade

What is Bortezomib

Bortezomib is a proteasome inhibitor; it was the first compound in this class to reach clinical trials and receive FDA-approval.

Bortezomib is approved for the treatment of multiple myeloma and mantle-cell lymphoma. It may be administered as an IV bolus injection; Velcade is the only formulation approved for subcutaneous and IV use.

Patients with pre-existing severe neuropathy should receive bortezomib only after careful risk-benefit assessment.

The subcutaneous route may be the preferred route of administration in patients with pre-existing peripheral neuropathy or who have a high risk of developing peripheral neuropathy.

Indications

  1. macroglobulinemia
  2. mantle cell lymphoma (MCL)
  3. multiple myeloma
  4. non-Hodgkin’s lymphoma (NHL)

For the treatment of multiple myeloma

NOTE: The FDA has designated bortezomib as an orphan drug for this indication.

Side Effects

  1. abdominal pain
  2. acute respiratory distress syndrome (ARDS)
  3. agitation
  4. alopecia
  5. anaphylactoid reactions
  6. anemia
  7. angina
  8. angioedema
  9. anorexia
  10. anxiety
  11. arthralgia
  12. ascites
  13. asthenia
  14. ataxia
  15. atrial fibrillation
  16. atrial flutter
  17. AV block
  18. back pain
  19. bladder spasm
  20. bleeding
  21. blepharitis
  22. blurred vision
  23. bone fractures
  24. bone pain
  25. bradycardia
  26. candidiasis
  27. cardiac arrest
  28. cardiac tamponade
  29. chalazion (meibomian cyst)
  30. chills
  31. cholestasis
  32. colitis
  33. coma
  34. confusion
  35. constipation
  36. cranial nerve palsies
  37. cystitis
  38. dehydration
  39. diarrhea
  40. diplopia
  41. disseminated intravascular coagulation (DIC)
  42. dizziness
  43. dysarthria
  44. dysesthesia
  45. dysgeusia
  46. dyspepsia
  47. dysphagia
  48. edema
  49. elevated hepatic enzymes
  50. encephalopathy
  51. epistaxis
  52. erythema
  53. fatigue
  54. fever
  55. gastritis
  56. gastroesophageal reflux
  57. GI bleeding
  58. GI obstruction
  59. GI perforation
  60. glomerulonephritis
  61. headache
  62. hearing loss
  63. heart failure
  64. hematemesis
  65. hematoma
  66. hematuria
  67. hemolytic-uremic syndrome
  68. hemoptysis
  69. hepatic failure
  70. hepatitis
  71. hyperbilirubinemia
  72. hyperglycemia
  73. hyperkalemia
  74. hypernatremia
  75. hypertension
  76. hyperuricemia
  77. hypocalcemia
  78. hypoesthesia
  79. hypoglycemia
  80. hypokalemia
  81. hyponatremia
  82. hypotension
  83. hypoxia
  84. ileus
  85. infection
  86. injection site reaction
  87. insomnia
  88. intracranial bleeding
  89. laryngeal edema
  90. leukoencephalopathy
  91. leukopenia
  92. lymphopenia
  93. malaise
  94. melena
  95. muscle paralysis
  96. myalgia
  97. myocardial infarction
  98. nausea
  99. neutropenia
  100. ocular infection
  101. ocular irritation
  102. orthostatic hypotension
  103. pancreatitis
  104. paresthesias
  105. pericardial effusion
  106. pericarditis
  107. peripheral edema
  108. peripheral neuropathy
  109. petechiae
  110. pharyngitis
  111. phlebitis
  112. pleural effusion
  113. pneumonitis
  114. pruritus
  115. psychosis
  116. pulmonary edema
  117. pulmonary embolism
  118. pulmonary hypertension
  119. QT prolongation
  120. rash
  121. renal failure (unspecified)
  122. seizures
  123. skin irritation
  124. Stevens-Johnson syndrome
  125. stomatitis
  126. stroke
  127. subdural hematoma
  128. suicidal ideation
  129. syncope
  130. thrombocytopenia
  131. thrombosis
  132. thrombotic microangiopathy
  133. thrombotic thrombocytopenic purpura (TTP)
  134. torsade de pointes
  135. toxic epidermal necrolysis
  136. tumor lysis syndrome (TLS)
  137. urinary incontinence
  138. urinary retention
  139. urticaria
  140. vasculitis
  141. ventricular tachycardia
  142. vertigo
  143. vomiting
  144. weakness
  145. weight loss

Monitoring Parameters

  • CBC with differential
  • LFTs
  • pregnancy testing
  • serum creatinine/BUN
  • serum electrolytes
  • serum uric acid

Contraindications

  • anemia
  • bleeding
  • breast-feeding
  • cardiac disease
  • contraception requirements
  • dehydration
  • diabetes mellitus
  • GI bleeding
  • heart failure
  • hemolytic-uremic syndrome
  • hepatic disease
  • hepatitis
  • herpes infection
  • hypotension
  • infertility
  • intracranial bleeding
  • intrathecal administration
  • male-mediated teratogenicity
  • mannitol hypersensitivity
  • neutropenia
  • orthostatic hypotension
  • peripheral neuropathy
  • pregnancy
  • pregnancy testing
  • pulmonary disease
  • reproductive risk
  • syncope
  • thrombocytopenia
  • thrombotic microangiopathy
  • thrombotic thrombocytopenic purpura (TTP)
  • tumor lysis syndrome (TLS)

Interactions

  • Abacavir; Dolutegravir; Lamivudine
  • Abacavir; Lamivudine, 3TC
  • Abacavir; Lamivudine, 3TC; Zidovudine, ZDV
  • Acetaminophen; Butalbital
  • Acetaminophen; Butalbital; Caffeine
  • Acetaminophen; Butalbital; Caffeine; Codeine
  • Alogliptin; Metformin
  • Alpha-blockers
  • Alpha-glucosidase Inhibitors
  • Amiloride
  • Amiloride; Hydrochlorothiazide, HCTZ
  • Amiodarone
  • Amobarbital
  • Amoxicillin; Clarithromycin; Lansoprazole
  • Amoxicillin; Clarithromycin; Omeprazole
  • Amprenavir
  • Antithymocyte Globulin
  • Apalutamide
  • Aprepitant, Fosaprepitant
  • Aspirin, ASA; Butalbital; Caffeine
  • Aspirin, ASA; Butalbital; Caffeine; Codeine
  • Aspirin, ASA; Carisoprodol
  • Aspirin, ASA; Carisoprodol; Codeine
  • Aspirin, ASA; Omeprazole
  • Atazanavir
  • Atazanavir; Cobicistat
  • Atropine; Hyoscyamine; Phenobarbital; Scopolamine
  • Azelastine; Fluticasone
  • Barbiturates
  • Beclomethasone
  • Belladonna Alkaloids; Ergotamine; Phenobarbital
  • Betamethasone
  • Bismuth Subcitrate Potassium; Metronidazole; Tetracycline
  • Bismuth Subsalicylate; Metronidazole; Tetracycline
  • Boceprevir
  • Bosentan
  • Budesonide
  • Budesonide; Formoterol
  • Butabarbital
  • Calcium-channel blockers
  • Canagliflozin
  • Canagliflozin; Metformin
  • Carbamazepine
  • Carisoprodol
  • Central-acting adrenergic agents
  • Ceritinib
  • Chloramphenicol
  • Ciclesonide
  • Cimetidine
  • Ciprofloxacin
  • Clarithromycin
  • Clozapine
  • Cobicistat
  • Colchicine
  • Colchicine; Probenecid
  • Conivaptan
  • Corticosteroids
  • Corticotropin, ACTH
  • Cortisone
  • Cyclosporine
  • Dapagliflozin
  • Dapagliflozin; Metformin
  • Dapagliflozin; Saxagliptin
  • Dapsone
  • Darunavir
  • Darunavir; Cobicistat
  • Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
  • Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
  • Deflazacort
  • Delavirdine
  • Dexamethasone
  • Dexlansoprazole
  • Diazoxide
  • Didanosine, ddI
  • Digoxin
  • Dipeptidyl Peptidase-4 Inhibitors
  • Disulfiram
  • Docetaxel
  • Dolutegravir; Lamivudine
  • Doravirine; Lamivudine; Tenofovir disoproxil fumarate
  • Doxazosin
  • Echinacea
  • Efavirenz
  • Efavirenz; Emtricitabine; Tenofovir
  • Efavirenz; Lamivudine; Tenofovir Disoproxil Fumarate
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
  • Empagliflozin
  • Empagliflozin; Linagliptin
  • Empagliflozin; Linagliptin; Metformin
  • Empagliflozin; Metformin
  • Enzalutamide
  • Eplerenone
  • Epoprostenol
  • Ertugliflozin
  • Ertugliflozin; Metformin
  • Ertugliflozin; Sitagliptin
  • Erythromycin
  • Erythromycin; Sulfisoxazole
  • Esomeprazole
  • Esomeprazole; Naproxen
  • Ethotoin
  • Fenofibric Acid
  • Fenoldopam
  • Fluconazole
  • Fludrocortisone
  • Flunisolide
  • Fluoxetine
  • Fluoxetine; Olanzapine
  • Fluticasone
  • Fluticasone; Salmeterol
  • Fluticasone; Umeclidinium; Vilanterol
  • Fluticasone; Vilanterol
  • Formoterol; Mometasone
  • Fosamprenavir
  • Fosphenytoin
  • Glipizide; Metformin
  • Glyburide; Metformin
  • grapefruit juice
  • Green Tea
  • HMG-CoA reductase inhibitors
  • Hydantoins
  • Hydralazine
  • Hydralazine; Hydrochlorothiazide, HCTZ
  • Hydralazine; Isosorbide Dinitrate, ISDN
  • Hydrochlorothiazide, HCTZ; Spironolactone
  • Hydrochlorothiazide, HCTZ; Triamterene
  • Hydrocortisone
  • Idelalisib
  • Iloprost
  • Imatinib
  • Incretin Mimetics
  • Indinavir
  • Insulins
  • Iodoquinol
  • Isavuconazonium
  • Isoniazid, INH; Pyrazinamide, PZA; Rifampin
  • Isoniazid, INH; Rifampin
  • Itraconazole
  • Ketoconazole
  • Lamivudine, 3TC
  • Lamivudine, 3TC; Zidovudine, ZDV
  • Lamivudine; Tenofovir Disoproxil Fumarate
  • Lansoprazole
  • Lansoprazole; Naproxen
  • Letermovir
  • Linagliptin; Metformin
  • Lopinavir; Ritonavir
  • Luliconazole
  • Lumacaftor; Ivacaftor
  • Mecamylamine
  • Meglitinides
  • Mephobarbital
  • Metformin
  • Metformin; Pioglitazone
  • Metformin; Repaglinide
  • Metformin; Rosiglitazone
  • Metformin; Saxagliptin
  • Metformin; Sitagliptin
  • Methohexital
  • Methylprednisolone
  • Metronidazole
  • Mifepristone
  • Minoxidil
  • Mitotane
  • Mometasone
  • Nefazodone
  • Nelfinavir
  • Netupitant, Fosnetupitant; Palonosetron
  • Nevirapine
  • Nitrofurantoin
  • Nitroprusside
  • Ombitasvir; Paritaprevir; Ritonavir
  • Omeprazole
  • Omeprazole; Amoxicillin; Rifabutin
  • Omeprazole; Sodium Bicarbonate
  • Oritavancin
  • Paclitaxel
  • Palifermin
  • Pantoprazole
  • Pazopanib
  • Penicillamine
  • Pentobarbital
  • Phenicol Derivatives
  • Phenobarbital
  • Phenoxybenzamine
  • Phentolamine
  • Phenytoin
  • Posaconazole
  • Potassium-sparing diuretics
  • Pramlintide
  • Prazosin
  • Prednisolone
  • Prednisone
  • Primidone
  • Proton pump inhibitors
  • Rabeprazole
  • Reserpine
  • Ribociclib
  • Ribociclib; Letrozole
  • Rifabutin
  • Rifampin
  • Rifapentine
  • Ritonavir
  • Rufinamide
  • Saquinavir
  • Secobarbital
  • SGLT2 Inhibitors
  • Simeprevir
  • Spironolactone
  • St. John’s Wort, Hypericum perforatum
  • Stavudine, d4T
  • Sulfasalazine
  • Sulfonylureas
  • Tacrolimus
  • Telaprevir
  • Telithromycin
  • Telotristat Ethyl
  • Terazosin
  • Thalidomide
  • Thiazide diuretics
  • Thiazolidinediones
  • Thiopental
  • Tipranavir
  • Treprostinil
  • Triamcinolone
  • Triamterene
  • Tuberculin Purified Protein Derivative, PPD
  • Vemurafenib
  • Vinblastine
  • Vincristine
  • Vincristine Liposomal
  • Voriconazole
  • Zalcitabine, ddC
  • Zidovudine, ZDV