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BORTEZOMIB Uses, Side Effects, and More

 BORTEZOMIB


BRAND NAME:- EGYBORT 3.5mg vial for inj 


BORTEZOMIB is an anti-cancer medication used to treat multiple myeloma and mantle cell lymphoma.This includes multiple myeloma in those who have and have not previously received treatment. It is generally used together with other medications. It is given by injection .

PHARMACODYNAMIC:-

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.
The pharmacodynamics of bortezomib are determined by quantifying proteasome inhibition in peripheral blood mononuclear cells taken from people receiving the drug. 

MECHANISM OF ACTION:-

Bortezomib is a proteasome inhibitor. The proteasomal system plays a vital role in cellular protein turnover, which is essential for the homeostasis of cells. Bortezomib reversibly binds to the chymotrypsin-like subunit of the 26S proteasome, resulting in its inhibition and preventing the degradation of various pro-apoptotic factors.[4][5] The accumulation will eventually activate the programmed cell death via caspase-mediated pathways in the neoplastic cells that are usually dependent on the suppression of pro-apoptotic pathways for their proliferation and survival. 

USED:-


Used in the treatment of multiple myeloma and mantle-cell lymphoma. It shows its working by stopping or slowing down the growth of cancer cells. 

SIDE EFFECTS:-


The most prominent adverse effects is peripheral neuropathy. Others are Diarrhoea, fatigue,bone marrow depression, especially thrombocytopenia.

DOSE:- 1.3mg/m² i .v. bolus injection,4 doses at 3 day intervals in cycles of 3 weeks.





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