Velcade

Velcade (originally PS-341 and marketed as Velcade by Millennium Pharmaceuticals) is the first therapeutic proteasome inhibitor to be tested in humans. It is approved in the U.S. for treating relapsed multiple myeloma and mantle cell lymphoma. In multiple myeloma, complete clinical responses have been obtained in patients with otherwise refractory or rapidly advancing disease.

Velcade - Pharmacology:

Velcade 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 active site of the proteasome has chymotrypsin-like, trypsin-like, and postglutamyl peptide hydrolysis activity. The 26S proteasome degrades various proteins critical to cancer cell survival, such as cyclins, tumor suppressors, BCL-2, and cyclin-dependent kinase inhibitors. Inhibition of these degradations sensitizes cells to apoptosis. Velcade is a potent inhibitor of 26S proteasome, which sensitizes activity in dividing multiple myeloma and leukemic cells, thus inducing apoptosis. In addition, bortezomib appears to increase the sensitivity of cancer cells to traditional anticancer agents (e.g., gemcitabine, cisplatin, paclitaxel, irinotecan, and radiation).

Velcade mini report

Velcade NDA
NDA - A product marketed under an approved New Drug Application
Velcade INTRAVENOUS; SUBCUTANEOUS
INTRAVENOUS; SUBCUTANEOUS
Velcade INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION
INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION
Velcade HUMAN PRESCRIPTION DRUG
HUMAN PRESCRIPTION DRUG
Start - Stop data
START DATA:
2003-May-13
Start - Stop data
STOP DATA
not occurred

Velcade for patients

VELCADE® (bortezomib) for Injection

PATIENT INFORMATION

VELCADE is intended for use under the guidance and supervision of a healthcare professional. Please discuss the possibility of the following side effects with your doctor:

Effects on Ability to Drive or Operate Machinery or Impairment of Mental Ability: VELCADE may cause low blood pressure that may lead to tiredness, dizziness, fainting, or blurred vision. Do not drive any vehicle or operate any dangerous tools or machinery if you experience these side effects. Even if you have not felt these effects previously, you must still be cautious.

Pregnancy/Nursing: Please use effective contraceptive measures to prevent pregnancy during treatment with VELCADE. It is advised that you are not given VELCADE if you are pregnant. You must make sure that you do not become pregnant while receiving VELCADE, but if you do, inform your doctor immediately. It is advised that you do not breast feed while you are receiving VELCADE. If you wish to restart breast feeding after your VELCADE treatment, you must discuss this with your doctor or nurse, who will tell you when it is safe to do so.

Dehydration/Hypotension: Following the use of VELCADE therapy, you may experience vomiting and/or diarrhea. Drink plenty of fluids. Speak with your doctor if these symptoms occur about what you should do to control or manage these symptoms. If you experience symptoms of dizziness or light-headedness, consult a healthcare professional. Seek immediate medical attention if you experience fainting spells.

Concomitant Medications: Please speak with your doctor about any other medication you are currently taking. Your doctor will want to be aware of any other medications.

Diabetic Patients: If you are a patient on oral antidiabetic medication while receiving VELCADE treatment, please check your blood sugar level frequently. Please call your doctor if you notice an unusual change.

Peripheral Neuropathy: Contact your doctor if you experience new or worsening symptoms of peripheral neuropathy such as tingling, numbness, pain, or a burning feeling in the feet or hands.

Congestive Heart Failure: Contact your doctor if you experience shortness of breath or swelling of the feet, ankles, or legs.

Velcade Interactions

No formal drug interaction studies have been conducted with VELCADE.

In vitro studies with human liver microsomes indicate that bortezomib is primarily a substrate for cytochrome P450 3A4, 2C19, and 1A2. Patients who are concomitantly receiving VELCADE and drugs that are inhibitors or inducers of cytochrome P450 3A4 should be closely monitored for either toxicities or reduced efficacy .

During clinical trials, hypoglycemia and hyperglycemia were reported in diabetic patients receiving oral hypoglycemics. Patients on oral antidiabetic agents receiving VELCADE treatment may require close monitoring of their blood glucose levels and adjustment of the dose of their antidiabetic medication.

Drug Laboratory Test Interactions

None known.

Velcade Contraindications

VELCADE is contraindicated in patients with hypersensitivity to bortezomib, boron, or mannitol.

Velcade tags categories:

Generic name, Overdose, Half Life Velcade, Food Interactions, Chemical, etc..

Velcade see also FDA report