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Protein-bound paclitaxel, also known as nanoparticle albumin–bound paclitaxel or nab-paclitaxel, is an injectable formulation of paclitaxel used to treat breast cancer, lung cancer and pancreatic cancer, among others. Paclitaxel kills cancer cells by preventing the normal breakdown of microtubules during cell division.
Paclitaxel is one of several cytoskeletal drugs that target tubulin. Paclitaxel-treated cells have defects in mitotic spindle assembly, chromosome segregation, and cell division. Unlike other tubulin-targeting drugs, such as colchicine, that inhibit microtubule assembly, paclitaxel stabilizes the microtubule polymer and protects it from ...
In 2013, the U.S. Food and Drug Administration approved protein-bound paclitaxel (also known as nab-paclitaxel, sold as Abraxane) used with gemcitabine. This regimen may be less toxic—but perhaps less effective—alternative to FOLFIRINOX for treating late-stage pancreatic cancer.
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Paclitaxel has achieved great success as an anti-cancer drug, yet there has been continuous effort to improve its efficacy and develop analogues which are more active and have greater bioavailability and specificity. The importance of C-13 substituted phenylisoserine side chain to bioactivity of paclitaxel has been known for a long time.
It is highly bound to human plasma protein. Within a concentration range of 1-30 μM (0.87-26 μg/mL), the fraction unbound in plasma was less than 0.01. [7] Venetoclax is metabolized by CYP3A4/5 as proven by in-vitro studies. [7] Those using the drug should not consume grapefruit products because they contain CYP3A inhibitors. [7]
The drug is 95% protein bound and has a volume of distribution of 2230 L, which indicates distribution into tissues. Sunitinib is metabolised mostly by CYP3A4 and has a half life of 40–60 hours. [29] Nintedanib reaches maximum plasma concentration 2–4 hours post-dose. The drug is 97,8% protein bound and is preferentially distributed in plasma.