福沙那韋

福沙那韋
臨床資料
商品名（英語：Drug nomenclature）	Lexiva, Telzir
其他名稱	Fosamprenavir calcium (USAN US)
AHFS/Drugs.com	Monograph
MedlinePlus	a604012
核准狀況	歐 EMA: yes;
懷孕分級	澳: B3 ; ;
給藥途徑	By mouth
ATC碼	J05AE07 (WHO) ;
法律規範狀態
法律規範	加：處方藥（℞-only）; 歐：Rx-only; 英：處方藥（℞-only） (POM); 美：處方藥（℞-only）;
藥物動力學數據
生物利用度	Unknown
血漿蛋白結合率	90%
藥物代謝	Hydrolysed to amprenavir and phosphate in GI tract epithelium
生物半衰期	7.7 hours
排泄途徑	Fecal (as metabolites of amprenavir)
識別資訊
	IUPAC命名法 {[(2R,3S)-1-[N-(2-methylpropyl)(4-aminobenzene)sulfonamido]-3-({[(3S)-oxolan-3-yloxy]carbonyl}amino)-4-phenylbutan-2-yl]oxy}phosphonic acid; ;
CAS號	226700-79-4 ; 226700-81-8
PubChem CID	131536; as salt: 131535;
DrugBank	DB01319 ; as salt: DBSALT001228;
ChemSpider	116245 ; as salt: 116244;
UNII	WOU1621EEG; as salt: ID1GU2627N ;
KEGG	D02497 ; as salt: D03835;
ChEBI	CHEBI:82941;
ChEMBL	ChEMBL1664 ; as salt: ChEMBL1200734;
NIAID ChemDB	082186;
CompTox Dashboard（英語：CompTox Chemicals Dashboard） (EPA)	DTXSID2048296 ;
化學資訊
化學式	C25H36N3O9PS
摩爾質量	585.61 g·mol−1
3D模型（JSmol（英語：JSmol））	交互式圖像;
	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 ; ; as salt: 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;

福沙那韋（英語：Fosamprenavir），商品名Lexiva和Telzir，是一種用於治療HIV/AIDS的藥物。^[3]^[4]它是蛋白酶抑制劑和抗逆轉錄病毒藥物安普那韋的前藥。^[5]它由ViiV醫療保健公司作為鈣鹽銷售。^[3]^[4]

福沙那韋於2003年10月在美國被批准用於醫療用途，^[6]並於2004年7月在歐盟獲得批准。^[4]人體代謝福沙那韋以形成作為活性成分的安普那韋。^[3]

一項與洛匹那韋的頭對頭研究表明，這兩種藥物具有相當的效力，但服用福沙那韋的患者往往具有更高的血清膽固醇。^[7]

醫療用途

福沙那韋用於治療HIV-1感染，通常但不一定與低劑量利托那韋或其他抗病毒藥物聯合使用。^[8]^[9]

副作用

最常見的不良反應是腹瀉。其他常見的副作用包括頭痛、頭暈和皮疹，這通常是短暫的。嚴重的過敏反應（史蒂文斯-約翰遜綜合症）很少見。^[8]

相互作用

安普那韋（福沙那韋的活性代謝物，存在於血漿、肝臟和其他器官中）通過肝酶CYP3A4代謝，並且對這種酶有微弱的抑制作用。這意味着與也被CYP3A4代謝的藥物聯合使用可以增加其血漿濃度，從而增加副作用；並與抑制CYP3A4的藥物合用可增加安普那韋的濃度。^[8]

當將福沙那韋與低劑量的CYP3A4抑制劑利托那韋聯合使用時，這種相互作用是有意的，因為它允許應用較低劑量的福沙那韋。^[8]

藥理學

福沙那韋甚至在到達循環系統之前就被迅速激活為安普那韋。安普那韋是一種 HIV 蛋白酶抑制劑。^[8]

參考文獻

^ Telzir Product information. Health Canada. 25 April 2012 [2 October 2022]. （原始內容存檔於14 June 2021）.
^ Telzir 700 mg film-coated tablets - Summary of Product Characteristics (SmPC). (emc). 22 June 2021 [2 October 2022]. （原始內容存檔於6 December 2021）.
^ ^3.0 ^3.1 ^3.2 ^3.3 Lexiva- fosamprenavir calcium tablet, film coated Lexiva- fosamprenavir calcium suspension. DailyMed. 1 October 2020 [2 October 2022]. （原始內容存檔於29 January 2022）.
^ ^4.0 ^4.1 ^4.2 ^4.3 Telzir EPAR. European Medicines Agency. 17 September 2018 [2 October 2022]. （原始內容存檔於15 May 2021）.
^ Archived copy. [2022-10-03]. （原始內容存檔於2021-06-28）.
^ Drug Approval Package: Lexiva (Fosamprenavir Calcium) NDA #021548. U.S. Food and Drug Administration (FDA). [2 October 2022]. （原始內容存檔於15 April 2021）.
^ 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. August 2006, 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 (編). Austria-Codex 62nd. Vienna: Österreichischer Apothekerverlag. 2007: 8009–17. ISBN 978-3-85200-181-4 （German）.
^ Lexiva. Drugs.com (報告). 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. September 2010, 277 (18): 3699–714. PMC 2975871 . PMID 20695887. doi:10.1111/j.1742-4658.2010.07771.x.

外部連結

Fosamprenavir. Drug Information Portal. U.S. National Library of Medicine. [2022-11-02]. （原始內容存檔於2021-02-25）.
Fosamprenavir calcium. Drug Information Portal. U.S. National Library of Medicine. [2022-11-02]. （原始內容存檔於2022-10-02）.

[1] Telzir Product information. Health Canada. 25 April 2012 [2 October 2022]. （原始內容存檔於14 June 2021）.

[2] Telzir 700 mg film-coated tablets - Summary of Product Characteristics (SmPC). (emc). 22 June 2021 [2 October 2022]. （原始內容存檔於6 December 2021）.

[Lexiva_FDA_label-3] 3.0 ^3.1 ^3.2 ^3.3 Lexiva- fosamprenavir calcium tablet, film coated Lexiva- fosamprenavir calcium suspension. DailyMed. 1 October 2020 [2 October 2022]. （原始內容存檔於29 January 2022）.

[Telzir_EPAR-4] 4.0 ^4.1 ^4.2 ^4.3 Telzir EPAR. European Medicines Agency. 17 September 2018 [2 October 2022]. （原始內容存檔於15 May 2021）.

[5] Archived copy. [2022-10-03]. （原始內容存檔於2021-06-28）.

[6] Drug Approval Package: Lexiva (Fosamprenavir Calcium) NDA #021548. U.S. Food and Drug Administration (FDA). [2 October 2022]. （原始內容存檔於15 April 2021）.

[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. August 2006, 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 (編). Austria-Codex 62nd. Vienna: Österreichischer Apothekerverlag. 2007: 8009–17. ISBN 978-3-85200-181-4 （German）.

[9] Lexiva. Drugs.com (報告). 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. September 2010, 277 (18): 3699–714. PMC 2975871 . PMID 20695887. doi:10.1111/j.1742-4658.2010.07771.x.

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