Drug Information

Drug (ID: DG00581) and It's Reported Resistant Information

• Name: TAS-120
• Synonyms: Futibatinib; TAS-120; 1448169-71-8; FGFR-IN-1; TAS120; UNII-4B93MGE4AL; 4B93MGE4AL; TAS 120; 1-[(3S)-3-[4-amino-3-[2-(3,5-dimethoxyphenyl)ethynyl]-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-pyrrolidinyl]-2-propen-1-one; 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; 1-[(3S)-3-{4-amino-3-[(3,5-dimethoxyphenyl)ethynyl]-1H-pyrazolo[3,4-d]pyrimidin-1-yl}pyrrolidin-1-yl]prop-2-en-1-one; Futibatinib [USAN]; Futibatinib (JAN/USAN/INN); GTPL9786; CHEMBL3701238; SCHEMBL15345470; TAS 120 [WHO-DD]; BDBM161389; AMY16930; BCP17213; EX-A1862; NSC813488; WHO 10879; ZINC207800318; CS-6031; DB15149; Example 2 [WO2013108809]; NSC-813488; (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pyrrolidin-1-yl)prop-2-en-1-one; BS-15425; HY-100818; D11725; D77976; US9108973, 2; 2-Propen-1-one, 1-((3S)-3-(4-amino-3-(2-(3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo(3,4-d)pyrimidin-1-yl)-1-pyrrolidinyl)-
• Indication:
  In total 3 Indication(s)
  Cholangiocarcinoma [ICD-11: 2C12]; Investigative; [1]
  Multiple myeloma [ICD-11: 2A83]; Investigative; [1]
  Solid tumour/cancer [ICD-11: 2A00-2F9Z]; Investigative; [1]
• Drug Resistance Disease(s):
  Disease(s) with Clinically Reported Resistance for This Drug (1 diseases)
  Liver cancer [ICD-11: 2C12]; [1]
• Target: Fibroblast growth factor (FGF); NOUNIPROTAC; [1]
• Target: Fibroblast growth factor receptor (FGFR); NOUNIPROTAC; [1]
• Formula: C22H22N6O3
• IsoSMILES: COC1=CC(=CC(=C1)C#CC2=NN(C3=NC=NC(=C23)N)[C@H]4CCN(C4)C(=O)C=C)OC
• 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
• InChIKey: KEIPNCCJPRMIAX-HNNXBMFYSA-N
• PubChem CID: 71621331
• TTD Drug ID: D01ZLU
• DrugBank ID: DB15149

Type(s) of Resistant Mechanism of This Drug

  ADTT: Aberration of the Drug's Therapeutic Target

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-02: Benign/in-situ/malignant neoplasm

Liver cancer [ICD-11: 2C12]

Drug Resistance Data Categorized by Their Corresponding Mechanisms

Aberration of the Drug's Therapeutic Target (ADTT)

Key Molecule: Fibroblast growth factor receptor 2 (FGFR2) [1]

• Molecule Alteration: Missense mutation; p.V565F
• Resistant Disease: Intrahepatic cholangiocarcinoma [ICD-11: 2C12.1]
• Experimental Note: Identified from the Human Clinical Data
• Experiment for Molecule Alteration: ctDNA analysis
• Mechanism Description: TAS-120 overcomes resistance to atp-competitive fgfr inhibitors in patients with fgfr2 fusion-positive intrahepatic cholangiocarcinoma.

Key Molecule: Fibroblast growth factor receptor 2 (FGFR2) [1]

• Molecule Alteration: Missense mutation; p.V565F
• Resistant Disease: Intrahepatic cholangiocarcinoma [ICD-11: 2C12.1]
• Experimental Note: Identified from the Human Clinical Data
• Experiment for Molecule Alteration: ctDNA analysis
• Mechanism Description: TAS-120 overcomes resistance to atp-competitive fgfr inhibitors in patients with fgfr2 fusion-positive intrahepatic cholangiocarcinoma.

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Aberration of the Drug's Therapeutic Target (ADTT)

Key Molecule: Fibroblast growth factor receptor 2 (FGFR2) [1]

• Molecule Alteration: Missense mutation; p.V565I
• Sensitive Disease: Intrahepatic cholangiocarcinoma [ICD-11: 2C12.1]
• Experimental Note: Identified from the Human Clinical Data
• Experiment for Molecule Alteration: ctDNA analysis
• Mechanism Description: TAS-120 overcomes resistance to atp-competitive fgfr inhibitors in patients with fgfr2 fusion-positive intrahepatic cholangiocarcinoma.

Key Molecule: Fibroblast growth factor receptor 2 (FGFR2) [1]

• Molecule Alteration: Missense mutation; p.N550H
• Sensitive Disease: Intrahepatic cholangiocarcinoma [ICD-11: 2C12.1]
• Experimental Note: Identified from the Human Clinical Data
• Experiment for Molecule Alteration: ctDNA analysis
• Mechanism Description: TAS-120 overcomes resistance to atp-competitive fgfr inhibitors in patients with fgfr2 fusion-positive intrahepatic cholangiocarcinoma.

Key Molecule: Fibroblast growth factor receptor 2 (FGFR2) [1]

• Molecule Alteration: Missense mutation; p.E566A
• Sensitive Disease: Intrahepatic cholangiocarcinoma [ICD-11: 2C12.1]
• Experimental Note: Identified from the Human Clinical Data
• Experiment for Molecule Alteration: ctDNA analysis
• Mechanism Description: TAS-120 overcomes resistance to atp-competitive fgfr inhibitors in patients with fgfr2 fusion-positive intrahepatic cholangiocarcinoma.

Key Molecule: Fibroblast growth factor receptor 2 (FGFR2) [1]

• Molecule Alteration: Missense mutation; p.V565I
• Sensitive Disease: Intrahepatic cholangiocarcinoma [ICD-11: 2C12.1]
• Experimental Note: Identified from the Human Clinical Data
• Experiment for Molecule Alteration: ctDNA analysis
• Mechanism Description: TAS-120 overcomes resistance to atp-competitive fgfr inhibitors in patients with fgfr2 fusion-positive intrahepatic cholangiocarcinoma.

Key Molecule: Fibroblast growth factor receptor 2 (FGFR2) [1]

• Molecule Alteration: Missense mutation; p.N550H
• Sensitive Disease: Intrahepatic cholangiocarcinoma [ICD-11: 2C12.1]
• Experimental Note: Identified from the Human Clinical Data
• Experiment for Molecule Alteration: ctDNA analysis
• Mechanism Description: TAS-120 overcomes resistance to atp-competitive fgfr inhibitors in patients with fgfr2 fusion-positive intrahepatic cholangiocarcinoma.

Key Molecule: Fibroblast growth factor receptor 2 (FGFR2) [1]

• Molecule Alteration: Missense mutation; p.E566A
• Sensitive Disease: Intrahepatic cholangiocarcinoma [ICD-11: 2C12.1]
• Experimental Note: Identified from the Human Clinical Data
• Experiment for Molecule Alteration: ctDNA analysis
• Mechanism Description: TAS-120 overcomes resistance to atp-competitive fgfr inhibitors in patients with fgfr2 fusion-positive intrahepatic cholangiocarcinoma.

References

• Ref 1: TAS-120 Overcomes Resistance to ATP-Competitive FGFR Inhibitors in Patients with FGFR2 Fusion-Positive Intrahepatic Cholangiocarcinoma .Cancer Discov. 2019 Aug;9(8):1064-1079. doi: 10.1158/2159-8290.CD-19-0182. Epub 2019 May 20. 10.1158/2159-8290.CD-19-0182