福巴替尼

福巴替尼
临床资料
商品名（英语：Drug nomenclature）	Lytgobi
其他名称	TAS-120，富替巴替尼
AHFS/Drugs.com	Micromedex详细消费者药物信息
核准状况	美 DailyMed: Futibatinib;
给药途径	口服
药物类别（英语：Drug class）	抗肿瘤药物
ATC码	L01EN04 (WHO) ;
法律规范状态
法律规范	欧：Rx-only; 美：处方药（℞-only）;
识别信息
	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号	1448169-71-8
PubChem CID	71621331;
IUPHAR/BPS	9786;
DrugBank	DB15149;
ChemSpider	58877816;
UNII	4B93MGE4AL;
KEGG	D11725;
ChEMBL	ChEMBL3701238;
PDB配体ID	TZ0 (PDBe, RCSB PDB);
化学信息
化学式	C22H22N6O3
摩尔质量	418.46 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
	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，又称富替巴替尼，是由日本大鹏制药（Taiho Pharmaceutical）研制的一款治疗局部晚期或转移性肝内胆管癌的口服药^[1]^[3]^[7]。为成纤维细胞生长因子受体2（FGFR2）不可逆抑制剂，用于治疗FGFR2基因融合的既往接受过治疗且无法切除的局部晚期或转移性肝内胆管癌的成年患者^[7]^[1]^[3]^[2]^[8]。

2022年9月通过美国FDA批准^[2]^[3]，2023年6月在日本获批^[9]^[10]，并于同年7月在欧盟获批^[4]^[11]。

参考文献

^ ^1.0 ^1.1 ^1.2 Lytgobi- futibatinib tablet. DailyMed. 2 February 2023 [13 April 2023]. （原始内容存档于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]. （原始内容存档于4 December 2022）. 本文含有此来源中属于公有领域的内容。
^ ^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]. （原始内容存档于19 November 2022）.
^ ^4.0 ^4.1 Lytgobi. Union Register of medicinal products. 6 July 2023 [14 July 2023]. （原始内容存档于14 July 2023）.
^ Lytgobi EPAR. European Medicines Agency. 18 July 2023 [25 August 2023].
^ 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 许忠凯. 富替巴替尼(Futibatinib,Lytgobi). 中国药物化学杂志. 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].
^ Syed YY. Futibatinib: First Approval. Drugs. December 2022, 82 (18): 1737–1743. PMID 36441501. doi:10.1007/s40265-022-01806-z.
^ European Commission Grants Conditional Marketing Authorization for Taiho's Lytgobi Tablets for the Treatment of Adults With Cholangiocarcinoma (新闻稿). Taiho Oncology Europe. 4 July 2023 [14 July 2023] –通过PR Newswire.

这是一篇与药学相关的小作品。您可以通过编辑或修订扩充其内容。

[Lytgobi_FDA_label-1] 1.0 ^1.1 ^1.2 Lytgobi- futibatinib tablet. DailyMed. 2 February 2023 [13 April 2023]. （原始内容存档于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]. （原始内容存档于4 December 2022）. 本文含有此来源中属于公有领域的内容。

[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]. （原始内容存档于19 November 2022）.

[Lytgobi_EU-4] 4.0 ^4.1 Lytgobi. Union Register of medicinal products. 6 July 2023 [14 July 2023]. （原始内容存档于14 July 2023）.

[5] Lytgobi EPAR. European Medicines Agency. 18 July 2023 [25 August 2023].

[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 许忠凯. 富替巴替尼(Futibatinib,Lytgobi). 中国药物化学杂志. 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].

[pmid36441501-10] Syed YY. Futibatinib: First Approval. Drugs. December 2022, 82 (18): 1737–1743. PMID 36441501. doi:10.1007/s40265-022-01806-z.

[11] European Commission Grants Conditional Marketing Authorization for Taiho's Lytgobi Tablets for the Treatment of Adults With Cholangiocarcinoma (新闻稿). Taiho Oncology Europe. 4 July 2023 [14 July 2023] –通过PR Newswire.

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