福沙那韦

**福沙那韦**
系统（IUPAC）命名名称
	{[(2R,3S)-1-[N-(2-methylpropyl)(4-aminobenzene)sulfonamido]-3-({[(3S)-oxolan-3-yloxy]carbonyl}amino)-4-phenylbutan-2-yl]oxy}phosphonic acid
临床数据
商品名	Lexiva, Telzir
Drugs.com	Monograph
MedlinePlus	a604012
医疗法规	EU EMA: yes;
妊娠分级	AU: B3 ; ;
给药途径	By mouth
合法状态
合法状态	CA: 处方药（℞-only） ; UK: 处方药（℞-only） (POM) ; US: 处方药（℞-only） ; EU: Rx-only ;
药代动力学数据
生物利用度	Unknown
蛋白结合度	90%
代谢	Hydrolysed至amprenavir and phosphate in GI tract epithelium
生物半衰期	7.7 hours
排泄	Fecal (as metabolites of amprenavir)
识别信息
CAS注册号	226700-79-4 ; 226700-81-8
ATC代码	J05AE07
PubChem	CID 131536; CID 131535
DrugBank	DB01319 ; DBSALT001228
ChemSpider	116245 ; 116244
UNII	WOU1621EEG ; ID1GU2627N
KEGG	D02497 ; D03835
ChEBI	CHEBI:82941
ChEMBL	CHEMBL1664 ; CHEMBL1200734
NIAID ChemDB	082186
化学信息
化学式	C25H36N3O9PS
摩尔质量	585.61 g·mol−1
	SMILES O=C(O[C@H]1CCOC1)N[C@@H](Cc2ccccc2)[C@H](OP(=O)(O)O)CN(CC(C)C)S(=O)(=O)c3ccc(N)cc3; ;
	InChI InChI=1S/C25H36N3O9PS/c1-18(2)15-28(39(33,34)22-10-8-20(26)9-11-22)16-24(37-38(30,31)32)23(14-19-6-4-3-5-7-19)27-25(29)36-21-12-13-35-17-21/h3-11,18,21,23-24H,12-17,26H2,1-2H3,(H,27,29)(H2,30,31,32)/t21-,23-,24+/m0/s1 ; Key:MLBVMOWEQCZNCC-OEMFJLHTSA-N ; ; InChI=1S/C25H36N3O9PS.Ca/c1-18(2)15-28(39(33,34)22-10-8-20(26)9-11-22)16-24(37-38(30,31)32)23(14-19-6-4-3-5-7-19)27-25(29)36-21-12-13-35-17-21;/h3-11,18,21,23-24H,12-17,26H2,1-2H3,(H,27,29)(H2,30,31,32);/q;+2/p-2/t21-,23-,24+;/m0./s1; Key:PMDQGYMGQKTCSX-HQROKSDRSA-L;

福沙那韦（英语：Fosamprenavir），商品名Lexiva和Telzir，是一种用于治疗HIV/AIDS的药物。^[4]^[2]它是蛋白酶抑制剂和抗逆转录病毒药物安普那韦的前药。^[5]它由ViiV医疗保健公司作为钙盐销售。^[4]^[2]

福沙那韦于2003年10月在美国被批准用于医疗用途，^[6]并于2004年7月在欧盟获得批准。^[2]人体代谢福沙那韦以形成作为活性成分的安普那韦。^[4]

一项与洛匹那韦的头对头研究表明，这两种药物具有相当的效力，但服用福沙那韦的患者往往具有更高的血清胆固醇。^[7]

医疗用途

福沙那韦用于治疗HIV-1感染，通常但不一定与低剂量利托那韦或其他抗病毒药物联合使用。^[8]^[9]

副作用

最常见的不良反应是腹泻。其他常见的副作用包括头痛、头晕和皮疹，这通常是短暂的。严重的过敏反应（史蒂文斯-约翰逊综合征）很少见。^[8]

相互作用

安普那韦（福沙那韦的活性代谢物，存在于血浆、肝脏和其他器官中）通过肝酶CYP3A4代谢，并且对这种酶有微弱的抑制作用。这意味着与也被CYP3A4代谢的药物联合使用可以增加其血浆浓度，从而增加副作用；并与抑制CYP3A4的药物合用可增加安普那韦的浓度。^[8]

当将福沙那韦与低剂量的CYP3A4抑制剂利托那韦联合使用时，这种相互作用是有意的，因为它允许应用较低剂量的福沙那韦。^[8]

药理学

福沙那韦甚至在到达循环系统之前就被迅速激活为安普那韦。安普那韦是一种 HIV 蛋白酶抑制剂。^[8]

参考文献

↑ Telzir Product information. Health Canada. 2012-04-25 [2022-10-02].
↑ ^2.0 ^2.1 ^2.2 ^2.3 Telzir EPAR. European Medicines Agency. 2018-09-17 [2022-10-02].
↑ Telzir 700 mg film-coated tablets - Summary of Product Characteristics (SmPC). (emc). 2021-06-22 [2022-10-02].
↑ ^4.0 ^4.1 ^4.2 ^4.3 Lexiva- fosamprenavir calcium tablet, film coated Lexiva- fosamprenavir calcium suspension. DailyMed. 2020-10-01 [2022-10-02].
↑ Archived copy. [2022-10-03].
↑ Drug Approval Package: Lexiva (Fosamprenavir Calcium) NDA #021548. U.S. Food and Drug Administration (FDA). [2022-10-02].
↑ Eron J, Yeni P, Gathe J, Estrada V, DeJesus E, Staszewski S, et al. The KLEAN study of fosamprenavir-ritonavir versus lopinavir-ritonavir, each in combination with abacavir-lamivudine, for initial treatment of HIV infection over 48 weeks: a randomised non-inferiority trial. Lancet. 2006-08, 368 (9534): 476–82. PMID 16890834. S2CID 33612672. doi:10.1016/S0140-6736(06)69155-1.
↑ ^8.0 ^8.1 ^8.2 ^8.3 ^8.4 Jasek W (编). Austria-Codex 62nd. Vienna: Österreichischer Apothekerverlag. 2007: 8009–17. ISBN 978-3-85200-181-4 （German）.
↑ Lexiva. Drugs.com. Monograph.
↑ Shen CH, Wang YF, Kovalevsky AY, Harrison RW, Weber IT. Amprenavir complexes with HIV-1 protease and its drug-resistant mutants altering hydrophobic clusters. The FEBS Journal. 2010-09, 277 (18): 3699–714. PMC 2975871 . PMID 20695887. doi:10.1111/j.1742-4658.2010.07771.x.

外部链接

Fosamprenavir. Drug Information Portal. U.S. National Library of Medicine. [2022-11-02].
Fosamprenavir calcium. Drug Information Portal. U.S. National Library of Medicine. [2022-11-02].

[1] Telzir Product information. Health Canada. 2012-04-25 [2022-10-02].

[Telzir_EPAR-2] 2.0 ^2.1 ^2.2 ^2.3 Telzir EPAR. European Medicines Agency. 2018-09-17 [2022-10-02].

[3] Telzir 700 mg film-coated tablets - Summary of Product Characteristics (SmPC). (emc). 2021-06-22 [2022-10-02].

[Lexiva_FDA_label-4] 4.0 ^4.1 ^4.2 ^4.3 Lexiva- fosamprenavir calcium tablet, film coated Lexiva- fosamprenavir calcium suspension. DailyMed. 2020-10-01 [2022-10-02].

[5] Archived copy. [2022-10-03].

[6] Drug Approval Package: Lexiva (Fosamprenavir Calcium) NDA #021548. U.S. Food and Drug Administration (FDA). [2022-10-02].

[7] Eron J, Yeni P, Gathe J, Estrada V, DeJesus E, Staszewski S, et al. The KLEAN study of fosamprenavir-ritonavir versus lopinavir-ritonavir, each in combination with abacavir-lamivudine, for initial treatment of HIV infection over 48 weeks: a randomised non-inferiority trial. Lancet. 2006-08, 368 (9534): 476–82. PMID 16890834. S2CID 33612672. doi:10.1016/S0140-6736(06)69155-1.

[Austria-Codex-8] 8.0 ^8.1 ^8.2 ^8.3 ^8.4 Jasek W (编). Austria-Codex 62nd. Vienna: Österreichischer Apothekerverlag. 2007: 8009–17. ISBN 978-3-85200-181-4 （German）.

[9] Lexiva. Drugs.com. Monograph.

[10] Shen CH, Wang YF, Kovalevsky AY, Harrison RW, Weber IT. Amprenavir complexes with HIV-1 protease and its drug-resistant mutants altering hydrophobic clusters. The FEBS Journal. 2010-09, 277 (18): 3699–714. PMC 2975871 . PMID 20695887. doi:10.1111/j.1742-4658.2010.07771.x.

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