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Medicine overview
Indications of Velcade 1 mg/vial
Velcade 1 mg/vial is a proteasome inhibitor indicated for:
Treatment of patients with multiple myeloma
Treatment of patients with mantle cell lymphoma who have received at least 1 prior therapy
Theropeutic Class
Targeted Cancer Therapy
Pharmacology
Velcade 1 mg/vial 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. The ubiquitin-proteasome pathway plays an essential role in regulating the intracellular concentration of specific proteins, thereby maintaining homeostasis within cells. Inhibition of the 26S proteasome prevents this targeted proteolysis, which can affect multiple signaling cascades within the cell. This disruption of normal homeostatic mechanisms can lead to cell death. Experiments have demonstrated that Velcade 1 mg/vial is cytotoxic to a variety of cancer cell types in vitro. Velcade 1 mg/vial causes a delay in tumor growth in vivo in nonclinical tumor models, including multiple myeloma.
Dosage & Administration of Velcade 1 mg/vial
The recommended dose of Velcade 1 mg/vial is 1.3 mg/m2 administered as a 3 to 5 second bolus intravenous injection. Dose adjustment may be used to manage adverse events that occur during treatment
Dosage of Velcade 1 mg/vial
The recommended dose of Velcade 1 mg/vial is 1.3 mg/m2 administered as a 3 to 5 second bolus intravenous injection. Dose adjustment may be used to manage adverse events that occur during treatment
Interaction of Velcade 1 mg/vial
Ketoconazole: Co-administration of ketoconazole, a potent CYP3A inhibitor, increased the exposure of Velcade 1 mg/vial. Therefore, patients should be closely monitored when given Velcade 1 mg/vial in combination with potent CYP3A4 inhibitors (e.g. ketoconazole, ritonavir).Melphalan-Prednisone: Co-administration of melphalan prednisone increased the exposure of Velcade 1 mg/vial. However, this increase is unlikely to be clinically relevant.Omeprazole: Co-administration of omeprazole, a potent inhibitor of CYP2C19, had no effect on the exposure of Velcade 1 mg/vial.Cytochrome P450: Patients who are concomitantly receiving Velcade 1 mg/vial and drugs that are inhibitors or inducers of cytochrome P450 3A4 should be closely monitored for either toxicities or reduced efficacy
Contraindications
Velcade 1 mg/vial is contraindicated in patients with hypersensitivity to Velcade 1 mg/vial, boron, or mannitol
Side Effects of Velcade 1 mg/vial
Most commonly reported adverse reactions (incidence ≥30%) in clinical studies include asthenic conditions, diarrhea, nausea, constipation, peripheral neuropathy, vomiting, pyrexia, thrombocytopenia, psychiatric disorders, anorexia and decreased appetite, neutropenia, neuralgia, leukopenia and anemia. Other adverse reactions, including serious adverse reactions, have been reported
Pregnancy & Lactation
Pregnancy Category D. Women of childbearing potential should avoid becoming pregnant while being treated with Velcade 1 mg/vial. Velcade 1 mg/vial administered to rabbits during organogenesis at a dose approximately 0.5 times the clinical dose of 1.3 mg/m2 based on body surface area caused post implantation loss and a decreased number of live fetuses.
Precautions & Warnings
Women should avoid becoming pregnant while being treated with Velcade 1 mg/vial. Pregnant women should be apprised of the potential harm to the fetusPeripheral neuropathy, including severe cases, may occur - manage with dose modification or discontinuation. Patients with preexisting severe neuropathy should be treated with Velcade 1 mg/vial only after careful risk-benefit assessment.Hypotension can occur. Caution should be used when treating patients receiving antihypertensives, those with a history of syncope, and those who are dehydrated. Patients with risk factors for, or existing heart disease, should be closely monitored.Acute diffuse infiltrative pulmonary disease has been reported.Nausea, diarrhea, constipation, and vomiting have occurred and may require use of antiemetic and antidiarrheal medications or fluid replacement.Thrombocytopenia or neutropenia can occur; complete blood counts should be regularly monitored throughout treatment.Tumor Lysis Syndrome, Reversible Posterior Leukoencephalopathy Syndrome, and acute hepatic failure have been reported.
Storage Conditions
Unopened vials may be stored at controlled room temperature 25º C
Drug Classes
Targeted Cancer Therapy
Mode Of Action
Velcade 1 mg/vial 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. The ubiquitin-proteasome pathway plays an essential role in regulating the intracellular concentration of specific proteins, thereby maintaining homeostasis within cells. Inhibition of the 26S proteasome prevents this targeted proteolysis, which can affect multiple signaling cascades within the cell. This disruption of normal homeostatic mechanisms can lead to cell death. Experiments have demonstrated that Velcade 1 mg/vial is cytotoxic to a variety of cancer cell types in vitro. Velcade 1 mg/vial causes a delay in tumor growth in vivo in nonclinical tumor models, including multiple myeloma.
Pregnancy
Pregnancy Category D. Women of childbearing potential should avoid becoming pregnant while being treated with Velcade 1 mg/vial. Velcade 1 mg/vial administered to rabbits during organogenesis at a dose approximately 0.5 times the clinical dose of 1.3 mg/m2 based on body surface area caused post implantation loss and a decreased number of live fetuses.
Frequently Asked Questions
What is Velcade 1 mg/vial used for?
Velcade 1 mg/vial is a proteasome inhibitor indicated for: Treatment of patients with multiple myeloma Treatment of patients with mantle cell lymphoma who have received at least 1 prior therapy
What is the dosage of Velcade 1 mg/vial?
The recommended dose of Velcade 1 mg/vial is 1.3 mg/m2 administered as a 3 to 5 second bolus intravenous injection. Dose adjustment may be used to manage adverse events that occur during treatment
What are the side effects of Velcade 1 mg/vial?
Most commonly reported adverse reactions (incidence ≥30%) in clinical studies include asthenic conditions, diarrhea, nausea, constipation, peripheral neuropathy, vomiting, pyrexia, thrombocytopenia, psychiatric disorders, anorexia and decreased appetite, neutropenia, neuralgia, leukopenia and anemia. Other adverse reactions, including serious adverse reactions, have been reported
Who should not take Velcade 1 mg/vial?
Velcade 1 mg/vial is contraindicated in patients with hypersensitivity to Velcade 1 mg/vial, boron, or mannitol
What precautions should be taken with Velcade 1 mg/vial?
Women should avoid becoming pregnant while being treated with Velcade 1 mg/vial. Pregnant women should be apprised of the potential harm to the fetusPeripheral neuropathy, including severe cases, may occur - manage with dose modification or discontinuation. Patients with preexisting severe neuropathy should be treated with Velcade 1 mg/vial only after careful risk-benefit assessment.Hypotension ca…
Is Velcade 1 mg/vial safe during pregnancy and breastfeeding?
Pregnancy Category D. Women of childbearing potential should avoid becoming pregnant while being treated with Velcade 1 mg/vial. Velcade 1 mg/vial administered to rabbits during organogenesis at a dose approximately 0.5 times the clinical dose of 1.3 mg/m2 based on body surface area caused post implantation loss and a decreased number of live fetuses.
Disclaimer
The information provided is accurate to our best practices, but it does not replace professional medical advice. We cannot guarantee its completeness or accuracy. The absence of specific information about a drug should not be seen as an endorsement. We are not responsible for any consequences resulting from this information, so consult a healthcare professional for any concerns or questions.