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