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Bortezomib(casno.179324-69-7) (BAN, INN and USAN. Originally codenamed PS-341; marketed as Velcade by Millennium Pharmaceuticals; Neomib by Getwell and Bortecad by Cadila Healthcare) is the first therapeutic proteasome inhibitor to be tested in humans. Proteasomes are cellular complexes that break down proteins. In some cancers, the proteins that normally kill cancer cells are broken down too quickly. Bortezomib(casno.179324-69-7) interrupts this process and lets those proteins kill the cancer cells. 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.
Origin and development of Bortezomib(casno.179324-69-7):
Bortezomib(casno.179324-69-7) was originally synthesized in 1995 at Myogenics. The drug (PS-341) was tested in a small Phase I clinical trial on patients with multiple myeloma. It was brought to further clinical trials by Millennium Pharmaceuticals in October 1999.
In May 2003, seven years after the initial synthesis, Bortezomib(casno.179324-69-7) (marketed as Velcade by Millennium Pharmaceuticals Inc.) was approved in the United States by the Food and Drug Administration (FDA) for use in multiple myeloma, based on the results from the SUMMIT Phase II trial. Bortezomib(casno.179324-69-7) is approved for initial treatment of patients with multiple myeloma by the U.S. FDA in 2008.
Later in August 2014, this Administration approved Velcade for the retreatment of adult patients with multiple myeloma who had previously responded to Velcade therapy and relapsed at least six months following completion of prior treatment.
Mechanism of Bortezomib(casno.179324-69-7):
The boron atom in Bortezomib(casno.179324-69-7) binds the catalytic site of the 26S proteasome with high affinity and specificity. In normal cells, the proteasome regulates protein expression and function by degradation of ubiquitylated proteins, and also cleanses the cell of abnormal or misfolded proteins. Clinical and preclinical data support a role in maintaining the immortal phenotype of myeloma cells, and cell-culture and xenograft data support a similar function in solid tumor cancers. While multiple mechanisms are likely to be involved, proteasome inhibition may prevent degradation of pro-apoptotic factors, permitting activation of programmed cell death in neoplastic cells dependent upon suppression of pro-apoptotic pathways. Recently, it was found that Bortezomib(casno.179324-69-7) caused a rapid and dramatic change in the levels of intracellular peptides that are produced by the proteasome. Some intracellular peptides have been shown to be biologically active, and so the effect of Bortezomib(casno.179324-69-7) on the levels of intracellular peptides may contribute to the biological and/or side effects of the drug.
Structure of Bortezomib(casno.179324-69-7):
The drug is an N-protected dipeptide and can be written as Pyz-Phe-boroLeu, which stands for pyrazinoic acid, phenylalanine and Leucine with a boronic acid instead of a carboxylic acid. Peptides are written N-terminus to C-terminus, and this convention is used here even though the "C-terminus" is a boronic acid instead of a carboxylic acid.
Bortezomib(casno.179324-69-7) Pharmacokinetics and Pharmacodynamics:
After subcutaneous administration, peak plasma levels are ~25-50 nM and this peak is sustained for 1-2 hrs. After intravenous injection, peak plasma levels are ~500 nM but only for ~5 minutes, after which the levels rapidly drop as the drug distributes to tissues (volume of distribution is ~500 L). Both routes provide equal drug exposures and generally comparable therapeutic efficacy. Elimination half life is 9–15 hours and the drug is primarily cleared by hepatic metabolism.
Pharmacodynamics are measured by measuring proteasome inhibition in peripheral blood mononuclear cells. The much greater sensitivity of myeloma cell lines and mantle cell lines to proteasome inhibition compared with normal peripheral blood mononuclear cells and most other cancer cell lines is poorly understood.
Adverse Effects of Bortezomib(casno.179324-69-7):
Bortezomib(casno.179324-69-7) is associated with peripheral neuropathy in 30% of patients; occasionally, it can be painful. This can be worse in patients with pre-existing neuropathy. In addition, myelosuppression causing neutropenia and thrombocytopenia can also occur and be dose-limiting. However, these side effects are usually mild relative to bone marrow transplantation and other treatment options for patients with advanced disease. Bortezomib(casno.179324-69-7) is associated with a high rate of shingles, although prophylactic acyclovir can reduce the risk of this. Acute interstitial nephritis has also been reported.
Gastro-intestinal (GI) effects and asthenia are the most common adverse events.
Experimental use of Bortezomib(casno.179324-69-7):
Bortezomib(casno.179324-69-7) has been trialled for SLE and appeared to reduce disease activity and plasma cell numbers, however 7 of 12 patients dropped out due to side effects, some of which were severe.
Bortezomib(casno.179324-69-7) is used for:
Bortezomib(casno.179324-69-7) is used to treat people with multiple myeloma (a type of cancer of the bone marrow) who have already been treated with at least one other medication. Bortezomib(casno.179324-69-7) is also used to treat people with mantle cell lymphoma (a fast-growing cancer that begins in the cells of the immune system) who have already been treated with at least one other medication. Bortezomib(casno.179324-69-7) is in a class of medications called antineoplastic agents. It works by killing cancer cells.
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How should Bortezomib(casno.179324-69-7) be used?
Bortezomib(casno.179324-69-7) comes as a solution (liquid) to inject into a vein. Bortezomib(casno.179324-69-7) is given by a doctor or nurse in a medical office or clinic. It is usually given on a rotating schedule that alternates 2 weeks when Bortezomib(casno.179324-69-7) is given twice a week with 10 days when the medication is not given. During the weeks that Bortezomib(casno.179324-69-7) is given, doses will always be at least 72 hours apart. The rotating schedule may be followed for up to eight cycles. After that, your doctor may decide to continue your treatment, but you will receive Bortezomib(casno.179324-69-7) less often.
Be sure to tell your doctor how you are feeling during your treatment. Your doctor may stop your treatment for a while or decrease your dose of Bortezomib(casno.179324-69-7) if you experience side effects of the medication.
Ask your pharmacist or doctor for a copy of the manufacturer's information for the patient.
How to use Bortezomib(casno.179324-69-7):
Use Bortezomib(casno.179324-69-7) as directed by your doctor. Check the label on the medicine for exact dosing instructions.
Drinking extra fluids while you are taking Bortezomib(casno.179324-69-7) is recommended. Check with your doctor for instructions.
Bortezomib(casno.179324-69-7) is given as an injection into a vein or under the skin at your doctor's office, hospital, or clinic. Bortezomib(casno.179324-69-7) is not intended to be injected into the spinal cord. Contact your health care provider if you have any questions.
It is very important that each dose is given at the scheduled time. If you miss a dose of Bortezomib(casno.179324-69-7), contact your doctor right away to establish a new dosing schedule. Do not use 2 doses at once.
Ask your health care provider any questions you may have about how to use Bortezomib(casno.179324-69-7).
Other uses for Bortezomib(casno.179324-69-7):
This medication may be prescribed for other uses; ask your doctor or pharmacist for more information.
Do not use Bortezomib(casno.179324-69-7) if:
You are allergic to any ingredient in Bortezomib(casno.179324-69-7), or to boron or mannitol
You are taking carbamazepine, efavirenz, enzalutamide, hydantoins (eg, phenytoin), oxcarbazepine, phenobarbital, primidone, rifamycins (eg, rifampin)
Contact your doctor or health care provider right away if any of these apply to you.
Bortezomib(casno.179324-69-7) may cause side effects. Tell your doctor if any of these symptoms, or those in the SPECIAL PRECAUTIONS section, are severe or do not go away:
general weakness
stomach pain
back pain
bone, joint, or muscle pain
muscle cramps
difficulty falling asleep or staying asleep
What should I know about storage and disposal of Bortezomib(casno.179324-69-7)?
Bortezomib(casno.179324-69-7) will be stored in the medical office or clinic.
What other information about Bortezomib(casno.179324-69-7) should I know?
Keep all appointments with your doctor and the laboratory. Your doctor will order certain lab tests to check your body's response to Bortezomib(casno.179324-69-7).
It is important for you to keep a written list of all of the prescription and nonprescription (over-the-counter) medicines you are taking, as well as any products such as vitamins, minerals, or other dietary supplements. You should bring this list with you each time you visit a doctor or if you are admitted to a hospital. It is also important information to carry with you in case of emergencies.
Important safety information:
Bortezomib(casno.179324-69-7) may cause dizziness, fatigue, fainting, or vision changes. These effects may be worse if you take it with alcohol or certain medicines. Use Bortezomib(casno.179324-69-7) with caution. Do not drive or perform other possibly unsafe tasks until you know how you react to it.
Bortezomib(casno.179324-69-7) may cause dizziness, light-headedness, or fainting; alcohol, hot weather, exercise, or fever may increase these effects. To prevent them, sit up or stand slowly, especially in the morning. Sit or lie down at the first sign of any of these effects.
Bortezomib(casno.179324-69-7) may reduce the number of clot-forming cells (platelets) in your blood. Avoid activities that may cause bruising or injury. Tell your doctor if you have unusual bruising or bleeding. Tell your doctor if you have dark, tarry, or bloody stools.
Use caution with sharp objects like safety razors or nail cutters and avoid activities such as contact sports to lower your chance of getting cut, bruised, or injured.
Bortezomib(casno.179324-69-7) may lower the ability of your body to fight infection. Avoid contact with people who have colds or infections. Tell your doctor if you notice signs of infection like fever, sore throat, rash, or chills.
Contact your doctor if you experience new or worsening nerve problems (eg, tingling, numbness, pain, or burning in the feet or hands; weakness in the arms or legs). Your dose may need to be changed.
A serious and possibly fatal condition called tumor lysis syndrome (TLS) has been reported in certain patients taking Bortezomib(casno.179324-69-7). Contact your doctor right away if you develop symptoms, such as fast or irregular heartbeat; fainting; decreased urination; muscle weakness or cramps; nausea, vomiting, diarrhea, or loss of appetite; or sluggishness. Discuss any questions or concerns with your doctor.
Heart failure, as well as heart failure that has gotten worse in people who already have it, has happened with Bortezomib(casno.179324-69-7). Tell your doctor if you have heart disease. Call your doctor right away if you have shortness of breath, a big weight gain, irregular heartbeat, or swelling in the arms or legs that is new or worse.
Serious and sometimes fatal lung problems have happened with Bortezomib(casno.179324-69-7). Call your doctor right away if you have lung or breathing problems (eg, trouble breathing, shortness of breath, a cough that is new or worse).
A serious and sometimes fatal brain problem called posterior reversible encephalopathy syndrome (PRES) has happened with Bortezomib(casno.179324-69-7). Call your doctor right away if you have confusion, seizures, severe headache, sluggishness, or vision changes (eg, vision loss).
Carry an ID card at all times that says you take Bortezomib(casno.179324-69-7).
If vomiting or diarrhea occurs, you will need to take care not to become dehydrated. Contact your doctor for instructions. Contact your doctor right away if you experience dizziness, light-headedness, or fainting.
Diabetes patients - Bortezomib(casno.179324-69-7) may affect your blood sugar. Check blood sugar levels closely. Ask your doctor before you change the dose of your diabetes medicine.
Women who may become pregnant should avoid becoming pregnant while being treated with Bortezomib(casno.179324-69-7). Be sure to use effective birth control while using Bortezomib(casno.179324-69-7). If you have questions about effective birth control, talk with your doctor.
Lab tests may be performed while you use Bortezomib(casno.179324-69-7). These tests may be used to monitor your condition or check for side effects. Be sure to keep all doctor and lab appointments.
PREGNANCY and BREAST-FEEDING: Bortezomib(casno.179324-69-7) may cause harm to the fetus. Do not become pregnant while you are using it. If you think you may be pregnant, contact your doctor. You will need to discuss the benefits and risks of using Bortezomib(casno.179324-69-7) while you are pregnant. It is not known if this medicine is found in breast milk. Do not breast-feed while using Bortezomib(casno.179324-69-7).