General

Scientific Names: Taxus baccata

Common Names: Jiang Guo Zi Shan, Ou Zhou Zi Shan .

 

BOTANICAL:

来 源： 红豆杉科浆果红豆杉（Taxus baccata） 植物的树皮 。

 

 

 

 

Pharmacology

 

 

 

Efficacy

Docetaxel (Taxotere) is a taxoid derived from the European yew tree, taxus baccata. In 4 phase-II studies docetaxel has important single agent activity with an overall prostate-specific antigen response rate of 42% in hormone refractory prostate cancer. Other phase-II studies suggest that the addition of estramustine to docetaxel results in a higher response rate but also in an increased toxicity. At present Docetaxel with and without estramustine is being evaluated in phase-III studies that will provide definitive information about its role in hormone refractory prostate cancer. (source)

Docetaxel (Taxotere) is a taxoid derived from the needles of the European yew tree, Taxus baccata. With an overall prostate-specific antigen response rate of 42% in four Phase II studies, docetaxel has important single-agent activity in androgen-independent prostate cancer. Phase II studies suggest that the addition of estramustine (Emcyt) to docetaxel results in higher response rates but also increased toxicity. Docetaxel with and without estramustine is being evaluated in Phase III studies that will provide definitive information about its role in androgen-independent prostate cancer. Novel combinations of docetaxel with biologic response modifiers are in early stages of development. Similarly, a number of investigators are conducting exploratory trials that incorporate docetaxel into multimodality approaches to high-risk localized prostate cancer treatment. (source)

Docetaxel is a semisynthetic taxane derived from the needles of the European yew ( Taxus baccata) and it is an important chemotherapeutic agent in the treatment of recurrent ovarian, breast and non-small-cell lung cancers. Traditional dosing regimens with docetaxel involve doses of 60-100 mg/m(2) by infusion every 3 weeks. Now weekly low-dose (30-36 mg/m(2)) regimens are being evaluated in phase I trials. Such low-dose studies require a more sensitive, specific and rapid assay of docetaxel in biological fluids for the determination of pharmacokinetic parameters. Because docetaxel is primarily metabolized by CYP3A4 and is highly protein-bound in the plasma, there is potential for drug-drug interactions and high interpatient variability in pharmacokinetics. Therefore, pharmacokinetic studies are an important component to understanding the therapeutic variability of docetaxel-containing chemotherapeutic regimens. To this end, we developed an analytical assay for docetaxel based upon tandem LCMS and paclitaxel as an internal standard. The sensitivity of the new assay allowed us to monitor plasma levels of docetaxel out to 48 h after the end of the infusion in patients enrolled in a phase I trial of exisulind (orally, twice daily) receiving weekly docetaxel doses of 30 or 36 mg/m(2) where plasma docetaxel levels are below the lower limit of quantitation for traditional HPLC/UV-based assays at later time-points. The inclusion of the 48-h time-point had significant effects on the calculated pharmacokinetic parameters when using either a three-compartment or non-compartmental analysis. The terminal half-life was significantly increased when the 48-h time-point was included in the pharmacokinetic analysis, and the use of model parameters derived with the inclusion of the 48-h time-point were able to more accurately predict plasma levels at later times. The results reflect the importance of accurate and sensitive analytical methods for the determination of pharmacokinetic parameters and the effect of this later time-point on docetaxel pharmacokinetic modeling. Further, with the increased use of weekly docetaxel in combination with other agents, the inclusion of these later sampling time-points and sensitive methods for drug level determinations are important components in the description of pharmacokinetic drug interactions. (source)

紫杉醇对动物移植性肿瘤B16、Lewis肿瘤、P388和C38等癌细胞有较强抑制生长作用；对KB细胞集落形成的抑制强度超过长春新碱和秋水仙碱；还能使肝癌、乳腺癌、子宫癌、白血病、淋巴癌等癌细胞自然死亡，且癌细胞株自然死亡率随紫杉醇浓度升高而增加。

临床应用：紫杉醇对卵巢癌、乳腺癌、头颈部癌、非小细胞性肺癌，前列腺癌等均有较好的良效。

IN VITRO:

  1. Fumoleau P, et al., Docetaxel: a new active agent in the therapy of metastatic breast cancer. Expert Opin Investig Drugs. 1997 Dec; 6(12):1853-65.
  2. Rosangkima G, et al., Antitumour activity of some plants from Meghalaya and Mizoram against murine ascites Dalton's lymphoma. Indian J Exp Biol. 2004 Oct; 42(10):981-8.
  3. Wolff JM, et al., [Significance of docetaxel in the chemotherapy of hormone-refractory prostate cancer]. Onkologie. 2003 Dec; 26 Suppl 7:37-40. Review. German.
  4. Beer TM, et al., Docetaxel (taxotere) in the treatment of prostate cancer. Expert Rev Anticancer Ther. 2003 Jun; 3(3):261-8. Review.
  5. Gustafson DL, et al., Analysis of docetaxel pharmacokinetics in humans with the inclusion of later sampling time-points afforded by the use of a sensitive tandem LCMS assay. Cancer Chemother Pharmacol. 2003 Aug; 52(2):159-66. Epub 2003 May 21.
  6. Georgoulias V. Docetaxel (taxotere) in the treatment of non-small cell lung cancer. Curr Med Chem. 2002 Apr; 9(8):869-77.
  7. Mantle D, et al., Therapeutic applications of medicinal plants in the treatment of breast cancer: a review of their pharmacology, efficacy and tolerability. Adverse Drug React Toxicol Rev. 2000 Aug; 19(3):223-40. Review.
  8. Vaishampayan U, et al., Taxanes: an overview of the pharmacokinetics and pharmacodynamics. Urology. 1999 Dec; 54(6A Suppl):22-9. Review.
  9. Strobel GA, et al., Glucosylation of the peptide leucinostatin A, produced by an endophytic fungus of European yew, may protect the host from leucinostatin toxicity. Chem Biol. 1997 Jul; 4(7):529-36.
  10. Adachi I, et al., A late phase II study of RP56976 (docetaxel) in patients with advanced or recurrent breast cancer. Br J Cancer. 1996 Jan; 73(2):210-6.
  11. Guo Y, et al., Immunoenzymatic methods applied to the search for bioactive taxoids from Taxus baccata. J Nat Prod. 1995 Jul; 58(7):1015-23.
  12. Lavelle F, et al., Preclinical evaluation of docetaxel (Taxotere). Semin Oncol. 1995 Apr; 22(2 Suppl 4):3-16. Review.
  13. Fumoleau P, et al., Current status of Taxotere (docetaxel) as a new treatment in breast cancer. Breast Cancer Res Treat. 1995; 33(1):39-46. Review.
  14. Karantanis E, et al., Taxotere inhibits in-vitro growth of human colonic cancer cell lines. Eur J Surg Oncol. 1994 Dec; 20(6):653-7.

 

CLINICAL:

  1. Aitini E, et al., [Current approaches in the medical treatment of advanced ovarian carcinoma]. Recenti Prog Med. 1994 Dec; 85(12):587-90. Review. Italian.
  2. ten Bokkel Huinink WW, et al., A phase II trial with docetaxel (Taxotere) in second line treatment with chemotherapy for advanced breast cancer. A study of the EORTC Early Clinical Trials Group. Ann Oncol. 1994 Jul; 5(6):527-32.
  3. Pazdur R, et al., Phase II trial of docetaxel (Taxotere) in metastatic colorectal carcinoma. Ann Oncol. 1994 May; 5(5):468-70.
  4. Lavelle F, et al., [Taxotere: from yew's needles to clinical practice]. Bull Cancer. 1993 Apr; 80(4):326-38. French.
  5. Bissery MC, et al., Experimental antitumor activity of taxotere (RP 56976, NSC 628503), a taxol analogue. Cancer Res. 1991 Sep 15; 51(18):4845-52.

 

 

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