Futibatinib

Futibatinib
Clinical data
Trade names	Lytgobi
Other names	TAS-120
AHFS/Drugs.com	Micromedex Detailed Consumer Information
License data	US DailyMed: Futibatinib;
Routes of; administration	By mouth
Drug class	Antineoplastic
ATC code	L01EN04 (WHO) ;
Legal status
Legal status	US: ℞-only; EU: Rx-only;
Identifiers
	IUPAC name 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 Number	1448169-71-8;
PubChem CID	71621331;
IUPHAR/BPS	9786;
DrugBank	DB15149;
ChemSpider	58877816;
UNII	4B93MGE4AL;
KEGG	D11725;
ChEMBL	ChEMBL3701238;
PDB ligand	TZ0 (PDBe, RCSB PDB);
Chemical and physical data
Formula	C22H22N6O3
Molar mass	418.457 g·mol−1
3D model (JSmol)	Interactive image;
	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;

Futibatinib, sold under the brand name Lytgobi, is an anti-cancer medication used for the treatment of cholangiocarcinoma (bile duct cancer).^[1]^[3] It is a kinase inhibitor.^[1]^[6] It is taken by mouth.^[1]

Futibatinib was approved for medical use in the United States in September 2022,^[1]^[3]^[7]^[2] in Japan in June 2023^[8]^[9] and in the European Union in July 2023.^[4]^[10]

Medical uses

Futibatinib is indicated for the treatment of adults with previously treated, unresectable, locally advanced or metastatic intrahepatic cholangiocarcinoma harboring fibroblast growth factor receptor 2 (FGFR2) gene fusions or other rearrangements.^[1]^[3]^[2]^[11]

Society and culture

Legal status

On 26 April 2023, the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency (EMA) adopted a positive opinion, recommending the granting of a conditional marketing authorization for the medicinal product Lytgobi, intended for the second-line treatment of locally advanced or metastatic cholangiocarcinoma characterized by fusion or rearrangements of fibroblast growth factor receptor (FGFR) 2.^[12] The applicant for this medicinal product is Taiho Pharma Netherlands B.V.^[12] Futibatinib was approved for medical use in the European Union in July 2023.^[4]

Names

Futibatinib is the international nonproprietary name (INN).^[13]

References

^ ^a ^b ^c ^d ^e ^f "Lytgobi- futibatinib tablet". DailyMed. 2 February 2023. Archived from the original on 12 April 2023. Retrieved 13 April 2023.
^ ^a ^b ^c "FDA grants accelerated approval to futibatinib for cholangiocarcinoma". U.S. Food and Drug Administration. 30 September 2022. Archived from the original on 4 December 2022. Retrieved 4 December 2022. This article incorporates text from this source, which is in the public domain.
^ ^a ^b ^c ^d "Drug Approval Package: Lytgobi". U.S. Food and Drug Administration (FDA). 8 November 2022. Archived from the original on 19 November 2022. Retrieved 18 November 2022.
^ ^a ^b ^c "Lytgobi". Union Register of medicinal products. 6 July 2023. Archived from the original on 14 July 2023. Retrieved 14 July 2023.
^ "Lytgobi EPAR". European Medicines Agency. 18 July 2023. Retrieved 25 August 2023.
^ "Lytgobi (Futibatinib) FDA Approval History". Archived from the original on 4 October 2022. Retrieved 4 October 2022.
^ "FDA Approves Taiho's Lytgobi (futibatinib) Tablets for Previously Treated, Unresectable, Locally Advanced or Metastatic Intrahepatic Cholangiocarcinoma" (Press release). Taiho Oncology. 30 September 2022. Archived from the original on 4 October 2022. Retrieved 4 October 2022 – via PR Newswire.
^ "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. Retrieved 17 August 2023.
^ Syed YY (December 2022). "Futibatinib: First Approval". Drugs. 82 (18): 1737–1743. doi:10.1007/s40265-022-01806-z. PMID 36441501.
^ "European Commission Grants Conditional Marketing Authorization for Taiho's Lytgobi Tablets for the Treatment of Adults With Cholangiocarcinoma" (Press release). Taiho Oncology Europe. 4 July 2023. Retrieved 14 July 2023 – via PR Newswire.
^ Javle M, King G, Spencer K, Borad MJ (November 2023). "Futibatinib, an Irreversible FGFR1-4 Inhibitor for the Treatment of FGFR-Aberrant Tumors". The Oncologist. 28 (11): 928–943. doi:10.1093/oncolo/oyad149. PMC 10628593. PMID 37390492.
^ ^a ^b "Lytgobi: Pending EC decision". European Medicines Agency. 26 April 2023. Archived from the original on 27 April 2023. Retrieved 27 April 2023. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
^ World Health Organization (2019). "International nonproprietary names for pharmaceutical substances (INN): recommended INN: list 81". WHO Drug Information. 33 (1). hdl:10665/330896.

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[Lytgobi_FDA_label-1] ^ ^a ^b ^c ^d ^e ^f "Lytgobi- futibatinib tablet". DailyMed. 2 February 2023. Archived from the original on 12 April 2023. Retrieved 13 April 2023.

[FDA_futibatinib-2] "FDA grants accelerated approval to futibatinib for cholangiocarcinoma". U.S. Food and Drug Administration. 30 September 2022. Archived from the original on 4 December 2022. Retrieved 4 December 2022. This article incorporates text from this source, which is in the public domain.

[Lytgobi_Drug_Approval_Package-3] "Drug Approval Package: Lytgobi". U.S. Food and Drug Administration (FDA). 8 November 2022. Archived from the original on 19 November 2022. Retrieved 18 November 2022.

[Lytgobi_EU-4] "Lytgobi". Union Register of medicinal products. 6 July 2023. Archived from the original on 14 July 2023. Retrieved 14 July 2023.

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

[6] "Lytgobi (Futibatinib) FDA Approval History". Archived from the original on 4 October 2022. Retrieved 4 October 2022.

[7] "FDA Approves Taiho's Lytgobi (futibatinib) Tablets for Previously Treated, Unresectable, Locally Advanced or Metastatic Intrahepatic Cholangiocarcinoma" (Press release). Taiho Oncology. 30 September 2022. Archived from the original on 4 October 2022. Retrieved 4 October 2022 – via PR Newswire.

[8] "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. Retrieved 17 August 2023.

[pmid36441501-9] Syed YY (December 2022). "Futibatinib: First Approval". Drugs. 82 (18): 1737–1743. doi:10.1007/s40265-022-01806-z. PMID 36441501.

[10] "European Commission Grants Conditional Marketing Authorization for Taiho's Lytgobi Tablets for the Treatment of Adults With Cholangiocarcinoma" (Press release). Taiho Oncology Europe. 4 July 2023. Retrieved 14 July 2023 – via PR Newswire.

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

[Lytgobi:_Pending_EC_decision-12] "Lytgobi: Pending EC decision". European Medicines Agency. 26 April 2023. Archived from the original on 27 April 2023. Retrieved 27 April 2023. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.

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

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