<unk>  is of the chemotherapy drug class; taxane, and is a semi-synthetic analogue of paclitaxel (Taxol), an extract from the bark of the rare Pacific yew tree, Taxus brevifolia. Due to scarcity of paclitaxel, extensive research was carried out leading to the formulation of<unk>  – an esterified product of 10-deacetyl baccatin III, which is extracted from the renewable and more readily available leaves of the European yew tree.<unk>  differs from paclitaxel at two positions in its chemical structure. It has a hydroxyl functional group on carbon 10, whereas paclitaxel has an acetate ester, and a tert-butyl carbamate ester exists on the phenylpropionate side chain instead of the benzamide in paclitaxel. The carbon 10 functional group change causes<unk>  to be more water-soluble than paclitaxel. Formulations and compositions<unk>  is a white powder and is the active ingredient available in 20 mg and 80 mg Taxotere single-dose vials of concentrated anhydrous<unk>  in polysorbate 80. The solution is a clear brown-yellow containing 40 mg<unk>  and 1040 mg polysorbate 80 per mL. 20 mg Taxotere is distributed in a blister carton containing one single-dose vial of Taxotere<unk>  preparation in 0.5 mL sterile pyrogen-free anhydrous polysorbate 80, and a single dose Taxotere solvent vial containing 1.5 mL 13% ethanol in saline to be combined and diluted in a 250 mL infusion bag containing 0.9% sodium chloride or 5% glucose for administration. 80 mg Taxotere is supplied identically but with 2.0 mL polysorbate 80 and 6.0 mL 13% ethanol in saline. The<unk>  and solvent vials are combined to give a solution of 10 mg/mL and the required dose is drawn from this solution. Vials have an overfill to compensate for liquid loss during preparation, foaming, adhesion to vial walls and the dead volume. 20 mg vials may be stored for 24 months below 25 °C away from light and 80 mg vials for 26 months in the same conditions. Recently Sanofi has got approval for one-vial formulation. With this one-vial formulation, the preparation of the infusion solution is simplified by eliminating the first dilution step. The two-vial and one-vial formulations contain the same drug substance,<unk>  trihydrate, and the same excipients (ethanol, polysorbate 80 and citric acid). The one-vial formulation is administered as an aqueous intravenous solution that contains the same drug substance in the same concentration as the already approved two-vial formulation. The same grade, quality, and quantity of polysorbate 80 are present in the infusion solution of both formulations. The only difference between these two formulations is the quantity of ethanol. Active regions A model based on electron crystallographic density and nuclear magnetic resonance deconvolution has been proposed to explain the binding of<unk>  to β-tubulin. In this T-shaped/butterfly model, a deep hydrophobic cleft exists near the surface of the β-tubulin where three potential hydrogen bonds and multiple hydrophobic contacts bind to<unk> . The hydrophobic pocket walls contain helices H1, H6, H7 and a loop between H6 and H7 that form hydrophobic interactions with the 3’-benzamido phenyl, 3’-phenyl, and the 2-benzoyl phenyl of<unk> . 3’-phenyl also has contact with β-sheets B8 and B10. The C-8 methyl of<unk>  has Van der Waals interactions with two residues, Thr-276 and Gln-281 near the C-terminal end of β-tubulin.<unk> 's O-21 experiences electrostatic attraction to Thr-276 and the C-12 methyl has proximity with Leu-371 on the loop between B9 and B10.
Docetaxel
Paclitaxel
Doxorubicin
Trastuzumab
Ifosfamide
Lipoplatin
Ribociclib
Cabazitaxel