福巴替尼

福巴替尼
臨床資料
商品名（英語：Drug nomenclature）	Lytgobi
其他名稱	TAS-120，富替巴替尼
AHFS/Drugs.com	Micromedex詳細消費者藥物信息
核准狀況	美 DailyMed: Futibatinib;
給藥途徑	口服
藥物類別（英語：Drug class）	抗腫瘤藥物
ATC碼	L01EN04 (WHO) ;
法律規範狀態
法律規範	歐：Rx-only; 美：處方藥（℞-only）;
識別資訊
	IUPAC命名法 1-[(3S)-3-[4-amino-3-[2-(3,5-dimethoxyphenyl)ethynyl]pyrazolo[3,4-d]pyrimidin-1-yl]pyrrolidin-1-yl]prop-2-en-1-one; ;
CAS號	1448169-71-8
PubChem CID	71621331;
IUPHAR/BPS	9786;
DrugBank	DB15149;
ChemSpider	58877816;
UNII	4B93MGE4AL;
KEGG	D11725;
ChEMBL	ChEMBL3701238;
PDB配體ID	TZ0 (PDBe, RCSB PDB);
化學資訊
化學式	C22H22N6O3
摩爾質量	418.46 g·mol−1
3D模型（JSmol（英語：JSmol））	交互式圖像;
	SMILES COC1=CC(=CC(OC)=C1)C#CC1=NN([C@H]2CCN(C2)C(=O)C=C)C2=C1C(N)=NC=N2;
	InChI InChI=1S/C22H22N6O3/c1-4-19(29)27-8-7-15(12-27)28-22-20(21(23)24-13-25-22)18(26-28)6-5-14-9-16(30-2)11-17(10-14)31-3/h4,9-11,13,15H,1,7-8,12H2,2-3H3,(H2,23,24,25)/t15-/m0/s1; Key:KEIPNCCJPRMIAX-HNNXBMFYSA-N;

福巴替尼（INN：futibatinib^[6]），商品名Lytgobi，又稱富替巴替尼，是由日本大鵬製藥（Taiho Pharmaceutical）研製的一款治療膽管癌的口服藥^[1]^[3]^[7]。為成纖維細胞生長因子受體2（FGFR2）不可逆抑制劑，用於治療FGFR2基因融合的既往接受過治療且無法切除的局部晚期或轉移性肝內膽管癌的成年患者^[7]^[1]^[3]^[2]^[8]。

2022年9月通過美國FDA批准^[2]^[3]，2023年6月在日本獲批^[9]^[10]，並於同年7月在歐盟獲批^[4]^[11]。

參考文獻

^ ^1.0 ^1.1 ^1.2 Lytgobi- futibatinib tablet. DailyMed. 2 February 2023 [13 April 2023]. （原始內容存檔於12 April 2023）.
^ ^2.0 ^2.1 ^2.2 FDA grants accelerated approval to futibatinib for cholangiocarcinoma. U.S. Food and Drug Administration. 30 September 2022 [4 December 2022]. （原始內容存檔於4 December 2022）. 本文含有此來源中屬於公有領域的內容。
^ ^3.0 ^3.1 ^3.2 ^3.3 Drug Approval Package: Lytgobi. U.S. Food and Drug Administration (FDA). 8 November 2022 [18 November 2022]. （原始內容存檔於19 November 2022）.
^ ^4.0 ^4.1 Lytgobi. Union Register of medicinal products. 6 July 2023 [14 July 2023]. （原始內容存檔於14 July 2023）.
^ Lytgobi EPAR. European Medicines Agency. 18 July 2023 [25 August 2023]. （原始內容存檔於2024-10-07）.
^ World Health Organization. International nonproprietary names for pharmaceutical substances (INN): recommended INN: list 81. WHO Drug Information. 2019, 33 (1). hdl:10665/330896  .
^ ^7.0 ^7.1 許忠凱. 富替巴替尼(Futibatinib,Lytgobi). 中國藥物化學雜誌. 2023, 33 (4): 320. doi:10.14142/j.cnki.cn21-1313/r.2023.04.011.
^ Javle M, King G, Spencer K, Borad MJ. Futibatinib, an Irreversible FGFR1-4 Inhibitor for the Treatment of FGFR-Aberrant Tumors. The Oncologist. November 2023, 28 (11): 928–943. PMC 10628593  . PMID 37390492. doi:10.1093/oncolo/oyad149.
^ Taiho Pharmaceutical Obtains Approval in Japan to Manufacture and Market FGFR Inhibitor LYTGOBI® Tablets 4mg for Unresectable Biliary Tract Cancer Harboring FGFR2 Gene Fusions That Has Progressed After Chemotherapy. Taiho Pharmaceutical Co., Ltd. 26 June 2023 [17 August 2023]. （原始內容存檔於2024-10-07）.
^ Syed YY. Futibatinib: First Approval. Drugs. December 2022, 82 (18): 1737–1743 [2024-10-03]. PMID 36441501. doi:10.1007/s40265-022-01806-z. （原始內容存檔於2024-10-07）.
^ European Commission Grants Conditional Marketing Authorization for Taiho's Lytgobi Tablets for the Treatment of Adults With Cholangiocarcinoma (新聞稿). Taiho Oncology Europe. 4 July 2023 [14 July 2023]. （原始內容存檔於2024-10-07） –透過PR Newswire.

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[Lytgobi_FDA_label-1] 1.0 ^1.1 ^1.2 Lytgobi- futibatinib tablet. DailyMed. 2 February 2023 [13 April 2023]. （原始內容存檔於12 April 2023）.

[FDA_futibatinib-2] 2.0 ^2.1 ^2.2 FDA grants accelerated approval to futibatinib for cholangiocarcinoma. U.S. Food and Drug Administration. 30 September 2022 [4 December 2022]. （原始內容存檔於4 December 2022）. 本文含有此來源中屬於公有領域的內容。

[Lytgobi_Drug_Approval_Package-3] 3.0 ^3.1 ^3.2 ^3.3 Drug Approval Package: Lytgobi. U.S. Food and Drug Administration (FDA). 8 November 2022 [18 November 2022]. （原始內容存檔於19 November 2022）.

[Lytgobi_EU-4] 4.0 ^4.1 Lytgobi. Union Register of medicinal products. 6 July 2023 [14 July 2023]. （原始內容存檔於14 July 2023）.

[5] Lytgobi EPAR. European Medicines Agency. 18 July 2023 [25 August 2023]. （原始內容存檔於2024-10-07）.

[6] World Health Organization. International nonproprietary names for pharmaceutical substances (INN): recommended INN: list 81. WHO Drug Information. 2019, 33 (1). hdl:10665/330896  .

[:0-7] 7.0 ^7.1 許忠凱. 富替巴替尼(Futibatinib,Lytgobi). 中國藥物化學雜誌. 2023, 33 (4): 320. doi:10.14142/j.cnki.cn21-1313/r.2023.04.011.

[pmid37390492-8] Javle M, King G, Spencer K, Borad MJ. Futibatinib, an Irreversible FGFR1-4 Inhibitor for the Treatment of FGFR-Aberrant Tumors. The Oncologist. November 2023, 28 (11): 928–943. PMC 10628593  . PMID 37390492. doi:10.1093/oncolo/oyad149.

[9] Taiho Pharmaceutical Obtains Approval in Japan to Manufacture and Market FGFR Inhibitor LYTGOBI® Tablets 4mg for Unresectable Biliary Tract Cancer Harboring FGFR2 Gene Fusions That Has Progressed After Chemotherapy. Taiho Pharmaceutical Co., Ltd. 26 June 2023 [17 August 2023]. （原始內容存檔於2024-10-07）.

[pmid36441501-10] Syed YY. Futibatinib: First Approval. Drugs. December 2022, 82 (18): 1737–1743 [2024-10-03]. PMID 36441501. doi:10.1007/s40265-022-01806-z. （原始內容存檔於2024-10-07）.

[11] European Commission Grants Conditional Marketing Authorization for Taiho's Lytgobi Tablets for the Treatment of Adults With Cholangiocarcinoma (新聞稿). Taiho Oncology Europe. 4 July 2023 [14 July 2023]. （原始內容存檔於2024-10-07） –透過PR Newswire.

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