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[吉西他滨:从临床前到临床,药代动力学发挥重要作用]

[Gemcitabine: from preclinic to clinic passing by pharmacokinetics].

作者信息

Lokiec François, Lansiaux Amélie

机构信息

Service de Pharmacologie, Centre René Huguenin, 35, rue Dailly, 92210 Saint-Cloud.

出版信息

Bull Cancer. 2007;94 Spec No Actualites:S85-9.

PMID:17845976
Abstract

Gemcitabine or Gemzar forms part of the class of the anti-cancer drugs antimetabolites. Gemcitabine is a structural analogue of the deoxycytidine with 2 fluorine atoms. There is a strong analogy between gemcitabine and cytosine arabinoside (Aracytine or Depocyt), at the same time structural, mechanistic and metabolic. However, if the intracellular derivatives triphosphate of gemcitabine seem more stable than those of the cytarabine, the two molecules move away from share their therapeutic activity. Indeed, if the cytosine arabinoside finds its place in the treatment of hematologic diseases, myeloblastic or lymphoblastic acute leukaemia and in acute myeloid leukaemias and myelodysplasy, gemcitabine sees its indications in the treatment of solid tumours such as non small cell lung cancer, adenocarcinoma of the pancreas, cancer of the bladder and metastatic breast cancer.

摘要

吉西他滨(或健择)是抗癌药物抗代谢物类别的一部分。吉西他滨是一种带有2个氟原子的脱氧胞苷的结构类似物。吉西他滨与阿糖胞苷(阿糖胞嘧啶或Depocyt)在结构、机制和代谢方面存在很强的相似性。然而,如果吉西他滨的细胞内三磷酸衍生物似乎比阿糖胞苷的更稳定,那么这两种分子在治疗活性方面就有所不同。的确,如果阿糖胞苷在血液系统疾病、急性髓细胞性或淋巴细胞性白血病以及急性髓性白血病和骨髓发育异常的治疗中占有一席之地,那么吉西他滨则用于实体瘤的治疗,如非小细胞肺癌、胰腺癌、膀胱癌和转移性乳腺癌。

相似文献

1
[Gemcitabine: from preclinic to clinic passing by pharmacokinetics].[吉西他滨:从临床前到临床,药代动力学发挥重要作用]
Bull Cancer. 2007;94 Spec No Actualites:S85-9.
2
Gemcitabine in the treatment of metastatic pancreatic cancer.吉西他滨治疗转移性胰腺癌
Expert Rev Anticancer Ther. 2008 Apr;8(4):511-23. doi: 10.1586/14737140.8.4.511.
3
Pharmacogenomics of gemcitabine: can genetic studies lead to tailor-made therapy?吉西他滨的药物基因组学:基因研究能否带来个性化治疗?
Br J Cancer. 2007 Jul 16;97(2):145-51. doi: 10.1038/sj.bjc.6603860. Epub 2007 Jun 26.
4
Single-agent gemcitabine and gemcitabine/irinotecan combination (irimogem) in non-small cell lung cancer.
Semin Oncol. 1999 Oct;26(5 Suppl 16):43-50; discussion 71-2.
5
Clinical update of gemcitabine in pancreas cancer.
Gan To Kagaku Ryoho. 2000 May;27 Suppl 2:469-73.
6
[Gemzar (gemcitabine)--a new chemotherapeutic agent for pancreatic cancer].健择(吉西他滨)——一种用于胰腺癌的新型化疗药物
Harefuah. 1997 Sep;133(5-6):208-12.
7
Gemcitabine and the blood brain barrier.吉西他滨与血脑屏障
Aust N Z J Med. 1999 Dec;29(6):831-2. doi: 10.1111/j.1445-5994.1999.tb00795.x.
8
Capecitabine in carcinoma of the pancreas.卡培他滨用于胰腺癌治疗
Expert Opin Pharmacother. 2006 Aug;7(12):1633-9. doi: 10.1517/14656566.7.12.1633.
9
The role of gemcitabine in the treatment of other tumours.吉西他滨在其他肿瘤治疗中的作用。
Br J Cancer. 1998;78 Suppl 3(Suppl 3):21-5. doi: 10.1038/bjc.1998.750.
10
Gemcitabine in the treatment of bladder cancer.吉西他滨治疗膀胱癌
Expert Opin Pharmacother. 2000 Mar;1(3):547-53. doi: 10.1517/14656566.1.3.547.

引用本文的文献

1
An open-label phase 1 dose-escalation clinical trial of a single intravenous administration of gemcitabine in dogs with advanced solid tumors.一项关于吉西他滨单次静脉注射用于晚期实体瘤犬的开放标签1期剂量递增临床试验。
J Vet Intern Med. 2015 Mar-Apr;29(2):620-5. doi: 10.1111/jvim.12557.
2
Gemcitabine and arabinosylcytosin pharmacogenomics: genome-wide association and drug response biomarkers.吉西他滨和阿糖胞苷药物基因组学:全基因组关联和药物反应生物标志物。
PLoS One. 2009 Nov 9;4(11):e7765. doi: 10.1371/journal.pone.0007765.