Drug Information

Drug (ID: DG00554) and It's Reported Resistant Information
Name
Erdafitinib
Synonyms
Erdafitinib; 1346242-81-6; JNJ-42756493; Balversa; UNII-890E37NHMV; 890E37NHMV; JNJ42756493; N'-(3,5-dimethoxyphenyl)-N'-[3-(1-methylpyrazol-4-yl)quinoxalin-6-yl]-N-propan-2-ylethane-1,2-diamine; N1-(3,5-dimethoxyphenyl)-N2-isopropyl-N1-(3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl)ethane-1,2-diamine; Erdafitinib [USAN:INN]; Balversa (TN); Erdafitinib (USAN/INN); GTPL9039; SCHEMBL2583760; CHEMBL3545376; Erdafitinib; JNJ-42756493; JNJ-42756493 (Erdafitinib); AMY31119; BCP20346; EX-A2564; BDBM50525939; MFCD28502040; NSC781556; s8401; compound 4 [WO2011135376]; ZINC168520308; CCG-269200; CS-4988; DB12147; NSC-781556; SB16854; NCGC00475735-01; 1,2-Ethanediamine, N1-(3,5-dimethoxyphenyl)-N2-(1-methylethyl)-N1-(3-(1-methyl-1H-pyrazol-4-yl)-6-quinoxalinyl)-; AC-30222; AS-35040; HY-18708; JNJ 42756493; D10927; A857165; Q27077213; B0084-470835; 5SF; N-(3,5-dimethoxyphenyl)-N'-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine; N-(3,5-dimethoxyphenyl)-N'-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine;Erdafitinib
    Click to Show/Hide
Indication
In total 4 Indication(s)
Bladder cancer [ICD-11: 2C94]
Approved
[1]
Lymphoma [ICD-11: 2A90- 2A85]
Phase 1/2
[1]
Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Phase 2
[1]
Ureteral cancer [ICD-11: 2C92]
Phase 2
[1]
Structure
Drug Resistance Disease(s)
Disease(s) with Clinically Reported Resistance for This Drug (2 diseases)
Breast cancer [ICD-11: 2C60]
[1]
Liver cancer [ICD-11: 2C12]
[1]
Click to Show/Hide the Molecular Information and External Link(s) of This Drug
Formula
C25H30N6O2
IsoSMILES
CC(C)NCCN(C1=CC2=NC(=CN=C2C=C1)C3=CN(N=C3)C)C4=CC(=CC(=C4)OC)OC
InChI
1S/C25H30N6O2/c1-17(2)26-8-9-31(20-10-21(32-4)13-22(11-20)33-5)19-6-7-23-24(12-19)29-25(15-27-23)18-14-28-30(3)16-18/h6-7,10-17,26H,8-9H2,1-5H3
InChIKey
OLAHOMJCDNXHFI-UHFFFAOYSA-N
PubChem CID
67462786
TTD Drug ID
D0EE8V
INTEDE ID
DR0595
DrugBank ID
DB12147
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
Click to Show/Hide the Resistance Disease of This Class
Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Click to Show/Hide
Drug Sensitivity Data Categorized by Their Corresponding Mechanisms
  Aberration of the Drug's Therapeutic Target (ADTT) Click to Show/Hide
Key Molecule: Fibroblast growth factor receptor 3 (FGFR3) [2]
Sensitive Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Molecule Alteration Missense mutation
p.K650E (c.1948A>G)
 Molecule Info 
Wild Type Structure Method: X-ray diffraction Resolution: 2.53  Å
PDB: 6LVM
Mutant Type Structure Method: X-ray diffraction Resolution: 2.34  Å
PDB: 4K33
   Download The Information of Sequence       Download The Structure File   
RMSD: 1.24
TM score: 0.96738
Amino acid change:
K650E
 : Wild Type Structure
 : Mutant Type Structure
  Mutation site(s) have been marked in red
-
-
M
-
G
-
S
-
S
-
H
440
|
-
H
-
H
-
H
-
H
-
H
-
S
-
Q
G
D
S
P
H
P
450
|
M
T
L
L
A
A
G
N
V
V
S
S
E
E
Y
L
E
E
L
L
460
|
P
P
E
A
D
D
P
P
K
K
W
W
E
E
F
L
P
S
R
R
470
|
D
A
K
R
L
L
T
T
L
L
G
G
K
K
P
P
L
L
G
G
480
|
E
E
G
G
C
A
F
F
G
G
Q
Q
V
V
V
V
M
M
A
A
490
|
E
E
A
A
I
I
G
G
I
I
D
D
K
K
D
D
R
R
A
A
500
|
A
A
K
K
P
P
V
V
T
T
V
V
A
A
V
V
K
K
M
M
510
|
L
L
K
K
D
D
D
D
A
A
T
T
D
D
K
K
D
D
L
L
520
|
S
S
D
D
L
L
V
V
S
S
E
E
M
M
E
E
M
M
M
M
530
|
K
K
M
M
I
I
G
G
K
K
H
H
K
K
N
N
I
I
I
I
540
|
N
N
L
L
L
L
G
G
A
A
C
C
T
T
Q
Q
G
G
G
G
550
|
P
P
L
L
Y
Y
V
V
L
L
V
V
E
E
Y
Y
A
A
A
A
560
|
K
K
G
G
N
N
L
L
R
R
E
E
F
F
L
L
R
R
A
A
570
|
R
R
R
R
P
P
P
P
G
G
L
L
D
D
Y
Y
S
S
F
F
580
|
D
D
T
T
C
S
K
K
P
P
P
P
E
E
E
E
Q
Q
L
L
590
|
T
T
F
F
K
K
D
D
L
L
V
V
S
S
C
C
A
A
Y
Y
600
|
Q
Q
V
V
A
A
R
R
G
G
M
M
E
E
Y
Y
L
L
A
A
610
|
S
S
Q
Q
K
K
C
C
I
I
H
H
R
R
D
D
L
L
A
A
620
|
A
A
R
R
N
N
V
V
L
L
V
V
T
T
E
E
D
D
N
N
630
|
V
V
M
M
K
K
I
I
A
A
D
D
F
F
G
G
L
L
A
A
640
|
R
R
D
D
V
V
H
H
N
N
L
L
D
D
Y
Y
Y
Y
K
K
650
|
K
E
T
T
T
T
N
N
G
G
R
R
L
L
P
P
V
V
K
K
660
|
W
W
M
M
A
A
P
P
E
E
A
A
L
L
F
F
D
D
R
R
670
|
V
V
Y
Y
T
T
H
H
Q
Q
S
S
D
D
V
V
W
W
S
S
680
|
F
F
G
G
V
V
L
L
L
L
W
W
E
E
I
I
F
F
T
T
690
|
L
L
G
G
G
G
S
S
P
P
Y
Y
P
P
G
G
I
I
P
P
700
|
V
V
E
E
E
E
L
L
F
F
K
K
L
L
L
L
K
K
E
E
710
|
G
G
H
H
R
R
M
M
D
D
K
K
P
P
A
A
N
N
C
C
720
|
T
T
H
H
D
D
L
L
Y
Y
M
M
I
I
M
M
R
R
E
E
730
|
C
C
W
W
H
H
A
A
A
A
P
P
S
S
Q
Q
R
R
P
P
740
|
T
T
F
F
K
K
Q
Q
L
L
V
V
E
E
D
D
L
L
D
D
750
|
R
R
V
V
L
L
T
T
V
V
T
T
S
S
T
T
D
D
E
E
Click to Show/Hide the Structure
Experimental Note Revealed Based on the Cell Line Data
In Vitro Model NIH3T3 cells Embryo Homo sapiens (Human) CVCL_0594
Experiment for
Drug Resistance		 Promega assay
Key Molecule: Fibroblast growth factor receptor 3 (FGFR3) [2]
Sensitive Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Molecule Alteration Missense mutation
p.N540K (c.1620C>G)
 Molecule Info 
Experimental Note Revealed Based on the Cell Line Data
In Vitro Model NIH3T3 cells Embryo Homo sapiens (Human) CVCL_0594
Experiment for
Drug Resistance		 Promega assay
Liver cancer [ICD-11: 2C12]
Click to Show/Hide
Drug Resistance Data Categorized by Their Corresponding Mechanisms
  Aberration of the Drug's Therapeutic Target (ADTT) Click to Show/Hide
Key Molecule: Fibroblast growth factor receptor 4 (FGFR4) [1]
Resistant Disease Intrahepatic cholangiocarcinoma [ICD-11: 2C12.1]
 Disease Info 
Molecule Alteration Missense mutation
p.V550L
 Molecule Info 
Wild Type Structure Method: X-ray diffraction Resolution: 2.35  Å
PDB: 5JKG
Mutant Type Structure Method: X-ray diffraction Resolution: 1.68  Å
PDB: 4QQJ
   Download The Information of Sequence       Download The Structure File   
RMSD: 1.26
TM score: 0.94767
Amino acid change:
V550L
 : Wild Type Structure
 : Mutant Type Structure
  Mutation site(s) have been marked in red
-
-
M
-
G
-
S
-
S
-
H
-
H
-
H
-
H
-
H
440
|
-
H
-
S
-
Q
G
D
P
P
L
L
L
L
A
A
G
G
L
L
450
|
V
V
S
S
L
L
D
D
L
L
P
P
L
L
D
D
P
P
L
L
460
|
W
W
E
E
F
F
P
P
R
R
D
D
R
R
L
L
V
V
L
L
470
|
G
G
K
K
P
P
L
L
G
G
E
E
G
G
A
A
F
F
G
G
480
|
Q
Q
V
V
V
V
R
R
A
A
E
E
A
A
F
F
G
G
M
M
490
|
D
D
P
P
A
A
R
R
P
P
D
D
Q
Q
A
A
S
S
T
T
500
|
V
V
A
A
V
V
K
K
M
M
L
L
K
K
D
D
N
N
A
A
510
|
S
S
D
D
K
K
D
D
L
L
A
A
D
D
L
L
V
V
S
S
520
|
E
E
M
M
E
E
V
V
M
M
K
K
L
L
I
I
G
G
R
R
530
|
H
H
K
K
N
N
I
I
I
I
N
N
L
L
L
L
G
G
V
V
540
|
C
C
T
T
Q
Q
E
E
G
G
P
P
L
L
Y
Y
V
V
I
I
550
|
V
L
E
E
C
C
A
A
A
A
K
K
G
G
N
N
L
L
R
R
560
|
E
E
F
F
L
L
R
R
A
A
R
R
R
R
P
P
P
P
G
G
570
|
P
P
D
D
L
L
S
S
P
P
D
D
G
G
P
P
R
R
S
S
580
|
S
S
E
E
G
G
P
P
L
L
S
S
F
F
P
P
V
V
L
L
590
|
V
V
S
S
C
C
A
A
Y
Y
Q
Q
V
V
A
A
R
R
G
G
600
|
M
M
Q
Q
Y
Y
L
L
E
E
S
S
R
R
K
K
C
C
I
I
610
|
H
H
R
R
D
D
L
L
A
A
A
A
R
R
N
N
V
V
L
L
620
|
V
V
T
T
E
E
D
D
N
N
V
V
M
M
K
K
I
I
A
A
630
|
D
D
F
F
G
G
L
L
A
A
R
R
G
G
V
V
H
H
H
H
640
|
I
I
D
D
Y
Y
Y
Y
K
K
K
K
T
T
S
S
N
N
G
G
650
|
R
R
L
L
P
P
V
V
K
K
W
W
M
M
A
A
P
P
E
E
660
|
A
A
L
L
F
F
D
D
R
E
V
V
Y
Y
T
T
H
H
Q
Q
670
|
S
S
D
D
V
V
W
W
S
S
F
F
G
G
I
I
L
L
L
L
680
|
W
W
E
E
I
I
F
F
T
T
L
L
G
G
G
G
S
S
P
P
690
|
Y
Y
P
P
G
G
I
I
P
P
V
V
E
E
E
E
L
L
F
F
700
|
S
S
L
L
L
L
R
R
E
E
G
G
H
H
R
R
M
M
D
D
710
|
R
R
P
P
P
P
H
H
C
C
P
P
P
P
E
E
L
L
Y
Y
720
|
G
G
L
L
M
M
R
R
E
E
C
C
W
W
H
H
A
A
A
A
730
|
P
P
S
S
Q
Q
R
R
P
P
T
T
F
F
K
K
Q
Q
L
L
740
|
V
V
E
E
A
A
L
L
D
D
K
K
V
V
L
L
L
L
A
A
750
|
V
V
S
S
E
E
E
E
Click to Show/Hide the Structure
Experimental Note Identified from the Human Clinical Data
Mechanism Description The mutations V550L and V550E in the FGFR4 kinase domain have been demonstrated to confer clinical resistance to erdafitinib in rhabdomyosarcoma, while V550M is associated with erdafitinib resistance in breast cancer.
Key Molecule: Fibroblast growth factor receptor 4 (FGFR4) [1]
Resistant Disease Intrahepatic cholangiocarcinoma [ICD-11: 2C12.1]
 Disease Info 
Molecule Alteration Missense mutation
p.V550L
 Molecule Info 
Wild Type Structure Method: X-ray diffraction Resolution: 2.35  Å
PDB: 5JKG
Mutant Type Structure Method: X-ray diffraction Resolution: 1.68  Å
PDB: 4QQJ
   Download The Information of Sequence       Download The Structure File   
RMSD: 1.26
TM score: 0.94767
Amino acid change:
V550L
 : Wild Type Structure
 : Mutant Type Structure
  Mutation site(s) have been marked in red
-
-
M
-
G
-
S
-
S
-
H
-
H
-
H
-
H
-
H
440
|
-
H
-
S
-
Q
G
D
P
P
L
L
L
L
A
A
G
G
L
L
450
|
V
V
S
S
L
L
D
D
L
L
P
P
L
L
D
D
P
P
L
L
460
|
W
W
E
E
F
F
P
P
R
R
D
D
R
R
L
L
V
V
L
L
470
|
G
G
K
K
P
P
L
L
G
G
E
E
G
G
A
A
F
F
G
G
480
|
Q
Q
V
V
V
V
R
R
A
A
E
E
A
A
F
F
G
G
M
M
490
|
D
D
P
P
A
A
R
R
P
P
D
D
Q
Q
A
A
S
S
T
T
500
|
V
V
A
A
V
V
K
K
M
M
L
L
K
K
D
D
N
N
A
A
510
|
S
S
D
D
K
K
D
D
L
L
A
A
D
D
L
L
V
V
S
S
520
|
E
E
M
M
E
E
V
V
M
M
K
K
L
L
I
I
G
G
R
R
530
|
H
H
K
K
N
N
I
I
I
I
N
N
L
L
L
L
G
G
V
V
540
|
C
C
T
T
Q
Q
E
E
G
G
P
P
L
L
Y
Y
V
V
I
I
550
|
V
L
E
E
C
C
A
A
A
A
K
K
G
G
N
N
L
L
R
R
560
|
E
E
F
F
L
L
R
R
A
A
R
R
R
R
P
P
P
P
G
G
570
|
P
P
D
D
L
L
S
S
P
P
D
D
G
G
P
P
R
R
S
S
580
|
S
S
E
E
G
G
P
P
L
L
S
S
F
F
P
P
V
V
L
L
590
|
V
V
S
S
C
C
A
A
Y
Y
Q
Q
V
V
A
A
R
R
G
G
600
|
M
M
Q
Q
Y
Y
L
L
E
E
S
S
R
R
K
K
C
C
I
I
610
|
H
H
R
R
D
D
L
L
A
A
A
A
R
R
N
N
V
V
L
L
620
|
V
V
T
T
E
E
D
D
N
N
V
V
M
M
K
K
I
I
A
A
630
|
D
D
F
F
G
G
L
L
A
A
R
R
G
G
V
V
H
H
H
H
640
|
I
I
D
D
Y
Y
Y
Y
K
K
K
K
T
T
S
S
N
N
G
G
650
|
R
R
L
L
P
P
V
V
K
K
W
W
M
M
A
A
P
P
E
E
660
|
A
A
L
L
F
F
D
D
R
E
V
V
Y
Y
T
T
H
H
Q
Q
670
|
S
S
D
D
V
V
W
W
S
S
F
F
G
G
I
I
L
L
L
L
680
|
W
W
E
E
I
I
F
F
T
T
L
L
G
G
G
G
S
S
P
P
690
|
Y
Y
P
P
G
G
I
I
P
P
V
V
E
E
E
E
L
L
F
F
700
|
S
S
L
L
L
L
R
R
E
E
G
G
H
H
R
R
M
M
D
D
710
|
R
R
P
P
P
P
H
H
C
C
P
P
P
P
E
E
L
L
Y
Y
720
|
G
G
L
L
M
M
R
R
E
E
C
C
W
W
H
H
A
A
A
A
730
|
P
P
S
S
Q
Q
R
R
P
P
T
T
F
F
K
K
Q
Q
L
L
740
|
V
V
E
E
A
A
L
L
D
D
K
K
V
V
L
L
L
L
A
A
750
|
V
V
S
S
E
E
E
E
Click to Show/Hide the Structure
Experimental Note Identified from the Human Clinical Data
Mechanism Description The mutations V550L and V550E in the FGFR4 kinase domain have been demonstrated to confer clinical resistance to erdafitinib in rhabdomyosarcoma, while V550M is associated with erdafitinib resistance in breast cancer.
Key Molecule: Fibroblast growth factor receptor 4 (FGFR4) [1]
Resistant Disease Intrahepatic cholangiocarcinoma [ICD-11: 2C12.1]
 Disease Info 
Molecule Alteration Missense mutation
p.V550E
 Molecule Info 
Experimental Note Identified from the Human Clinical Data
Mechanism Description The mutations V550L and V550E in the FGFR4 kinase domain have been demonstrated to confer clinical resistance to erdafitinib in rhabdomyosarcoma, while V550M is associated with erdafitinib resistance in breast cancer.
Key Molecule: Fibroblast growth factor receptor 4 (FGFR4) [1]
Resistant Disease Intrahepatic cholangiocarcinoma [ICD-11: 2C12.1]
 Disease Info 
Molecule Alteration Missense mutation
p.V550E
 Molecule Info 
Experimental Note Identified from the Human Clinical Data
Mechanism Description The mutations V550L and V550E in the FGFR4 kinase domain have been demonstrated to confer clinical resistance to erdafitinib in rhabdomyosarcoma, while V550M is associated with erdafitinib resistance in breast cancer.
Breast cancer [ICD-11: 2C60]
Click to Show/Hide
Drug Resistance Data Categorized by Their Corresponding Mechanisms
  Aberration of the Drug's Therapeutic Target (ADTT) Click to Show/Hide
Key Molecule: Fibroblast growth factor receptor 4 (FGFR4) [1]
Resistant Disease Breast cancer [ICD-11: 2C60.3]
 Disease Info 
Molecule Alteration Missense mutation
p.V550M
 Molecule Info 
Wild Type Structure Method: X-ray diffraction Resolution: 2.35  Å
PDB: 5JKG
Mutant Type Structure Method: X-ray diffraction Resolution: 3.25  Å
PDB: 5XFJ
   Download The Information of Sequence       Download The Structure File   
RMSD: 0.43
TM score: 0.99507
Amino acid change:
V550M
 : Wild Type Structure
 : Mutant Type Structure
  Mutation site(s) have been marked in red
-
G
G
P
P
L
L
L
L
A
A
G
G
L
L
450
|
V
V
S
S
L
L
D
D
L
L
P
P
L
L
D
D
P
P
L
L
460
|
W
W
E
E
F
F
P
P
R
R
D
D
R
R
L
L
V
V
L
L
470
|
G
G
K
K
P
P
L
L
G
G
E
E
G
G
A
A
F
F
G
G
480
|
Q
Q
V
V
V
V
R
R
A
A
E
E
A
A
F
F
G
G
M
M
490
|
D
D
P
P
A
A
R
R
P
P
D
D
Q
Q
A
A
S
S
T
T
500
|
V
V
A
A
V
V
K
K
M
M
L
L
K
K
D
D
N
N
A
A
510
|
S
S
D
D
K
K
D
D
L
L
A
A
D
D
L
L
V
V
S
S
520
|
E
E
M
M
E
E
V
V
M
M
K
K
L
L
I
I
G
G
R
R
530
|
H
H
K
K
N
N
I
I
I
I
N
N
L
L
L
L
G
G
V
V
540
|
C
C
T
T
Q
Q
E
E
G
G
P
P
L
L
Y
Y
V
V
I
I
550
|
V
M
E
E
C
C
A
A
A
A
K
K
G
G
N
N
L
L
R
R
560
|
E
E
F
F
L
L
R
R
A
A
R
R
R
R
P
P
P
P
G
G
570
|
P
P
D
D
L
L
S
S
P
P
D
D
G
G
P
P
R
R
S
S
580
|
S
S
E
E
G
G
P
P
L
L
S
S
F
F
P
P
V
V
L
L
590
|
V
V
S
S
C
C
A
A
Y
Y
Q
Q
V
V
A
A
R
R
G
G
600
|
M
M
Q
Q
Y
Y
L
L
E
E
S
S
R
R
K
K
C
C
I
I
610
|
H
H
R
R
D
D
L
L
A
A
A
A
R
R
N
N
V
V
L
L
620
|
V
V
T
T
E
E
D
D
N
N
V
V
M
M
K
K
I
I
A
A
630
|
D
D
F
F
G
G
L
L
A
A
R
R
G
G
V
V
H
H
H
H
640
|
I
I
D
D
Y
Y
Y
Y
K
K
K
K
T
T
S
S
N
N
G
G
650
|
R
R
L
L
P
P
V
V
K
K
W
W
M
M
A
A
P
P
E
E
660
|
A
A
L
L
F
F
D
D
R
R
V
V
Y
Y
T
T
H
H
Q
Q
670
|
S
S
D
D
V
V
W
W
S
S
F
F
G
G
I
I
L
L
L
L
680
|
W
W
E
E
I
I
F
F
T
T
L
L
G
G
G
G
S
S
P
P
690
|
Y
Y
P
P
G
G
I
I
P
P
V
V
E
E
E
E
L
L
F
F
700
|
S
S
L
L
L
L
R
R
E
E
G
G
H
H
R
R
M
M
D
D
710
|
R
R
P
P
P
P
H
H
C
C
P
P
P
P
E
E
L
L
Y
Y
720
|
G
G
L
L
M
M
R
R
E
E
C
C
W
W
H
H
A
A
A
A
730
|
P
P
S
S
Q
Q
R
R
P
P
T
T
F
F
K
K
Q
Q
L
L
740
|
V
V
E
E
A
A
L
L
D
D
K
K
V
V
L
L
L
L
A
A
750
|
V
V
S
S
E
E
E
E
Click to Show/Hide the Structure
Experimental Note Identified from the Human Clinical Data
Mechanism Description The mutations V550L and V550E in the FGFR4 kinase domain have been demonstrated to confer clinical resistance to erdafitinib in rhabdomyosarcoma, while V550M is associated with erdafitinib resistance in breast cancer.
Key Molecule: Fibroblast growth factor receptor 4 (FGFR4) [1]
Resistant Disease Breast cancer [ICD-11: 2C60.3]
 Disease Info 
Molecule Alteration Missense mutation
p.V550M
 Molecule Info 
Wild Type Structure Method: X-ray diffraction Resolution: 2.35  Å
PDB: 5JKG
Mutant Type Structure Method: X-ray diffraction Resolution: 3.25  Å
PDB: 5XFJ
   Download The Information of Sequence       Download The Structure File   
RMSD: 0.43
TM score: 0.99507
Amino acid change:
V550M
 : Wild Type Structure
 : Mutant Type Structure
  Mutation site(s) have been marked in red
-
G
G
P
P
L
L
L
L
A
A
G
G
L
L
450
|
V
V
S
S
L
L
D
D
L
L
P
P
L
L
D
D
P
P
L
L
460
|
W
W
E
E
F
F
P
P
R
R
D
D
R
R
L
L
V
V
L
L
470
|
G
G
K
K
P
P
L
L
G
G
E
E
G
G
A
A
F
F
G
G
480
|
Q
Q
V
V
V
V
R
R
A
A
E
E
A
A
F
F
G
G
M
M
490
|
D
D
P
P
A
A
R
R
P
P
D
D
Q
Q
A
A
S
S
T
T
500
|
V
V
A
A
V
V
K
K
M
M
L
L
K
K
D
D
N
N
A
A
510
|
S
S
D
D
K
K
D
D
L
L
A
A
D
D
L
L
V
V
S
S
520
|
E
E
M
M
E
E
V
V
M
M
K
K
L
L
I
I
G
G
R
R
530
|
H
H
K
K
N
N
I
I
I
I
N
N
L
L
L
L
G
G
V
V
540
|
C
C
T
T
Q
Q
E
E
G
G
P
P
L
L
Y
Y
V
V
I
I
550
|
V
M
E
E
C
C
A
A
A
A
K
K
G
G
N
N
L
L
R
R
560
|
E
E
F
F
L
L
R
R
A
A
R
R
R
R
P
P
P
P
G
G
570
|
P
P
D
D
L
L
S
S
P
P
D
D
G
G
P
P
R
R
S
S
580
|
S
S
E
E
G
G
P
P
L
L
S
S
F
F
P
P
V
V
L
L
590
|
V
V
S
S
C
C
A
A
Y
Y
Q
Q
V
V
A
A
R
R
G
G
600
|
M
M
Q
Q
Y
Y
L
L
E
E
S
S
R
R
K
K
C
C
I
I
610
|
H
H
R
R
D
D
L
L
A
A
A
A
R
R
N
N
V
V
L
L
620
|
V
V
T
T
E
E
D
D
N
N
V
V
M
M
K
K
I
I
A
A
630
|
D
D
F
F
G
G
L
L
A
A
R
R
G
G
V
V
H
H
H
H
640
|
I
I
D
D
Y
Y
Y
Y
K
K
K
K
T
T
S
S
N
N
G
G
650
|
R
R
L
L
P
P
V
V
K
K
W
W
M
M
A
A
P
P
E
E
660
|
A
A
L
L
F
F
D
D
R
R
V
V
Y
Y
T
T
H
H
Q
Q
670
|
S
S
D
D
V
V
W
W
S
S
F
F
G
G
I
I
L
L
L
L
680
|
W
W
E
E
I
I
F
F
T
T
L
L
G
G
G
G
S
S
P
P
690
|
Y
Y
P
P
G
G
I
I
P
P
V
V
E
E
E
E
L
L
F
F
700
|
S
S
L
L
L
L
R
R
E
E
G
G
H
H
R
R
M
M
D
D
710
|
R
R
P
P
P
P
H
H
C
C
P
P
P
P
E
E
L
L
Y
Y
720
|
G
G
L
L
M
M
R
R
E
E
C
C
W
W
H
H
A
A
A
A
730
|
P
P
S
S
Q
Q
R
R
P
P
T
T
F
F
K
K
Q
Q
L
L
740
|
V
V
E
E
A
A
L
L
D
D
K
K
V
V
L
L
L
L
A
A
750
|
V
V
S
S
E
E
E
E
Click to Show/Hide the Structure
Experimental Note Identified from the Human Clinical Data
Mechanism Description The mutations V550L and V550E in the FGFR4 kinase domain have been demonstrated to confer clinical resistance to erdafitinib in rhabdomyosarcoma, while V550M is associated with erdafitinib resistance in breast cancer.
Bladder cancer [ICD-11: 2C94]
Click to Show/Hide
Drug Sensitivity Data Categorized by Their Corresponding Mechanisms
  Aberration of the Drug's Therapeutic Target (ADTT) Click to Show/Hide
Key Molecule: Fibroblast growth factor receptor 3 (FGFR3) [3]
Sensitive Disease Bladder cancer [ICD-11: 2C94.0]
 Disease Info 
Molecule Alteration Missense mutation
p.G370C (c.1108G>T)
 Molecule Info 
Experimental Note Identified from the Human Clinical Data
Key Molecule: Fibroblast growth factor receptor 3 (FGFR3) [3]
Sensitive Disease Bladder cancer [ICD-11: 2C94.0]
 Disease Info 
Molecule Alteration Missense mutation
p.Y373C (c.1118A>G)
 Molecule Info 
Experimental Note Identified from the Human Clinical Data
Key Molecule: Fibroblast growth factor receptor 3 (FGFR3) [3]
Sensitive Disease Bladder cancer [ICD-11: 2C94.0]
 Disease Info 
Molecule Alteration Missense mutation
p.R248C (c.742C>T)
 Molecule Info 
Experimental Note Identified from the Human Clinical Data
Key Molecule: Fibroblast growth factor receptor 3 (FGFR3) [4]
Sensitive Disease Bladder cancer [ICD-11: 2C94.0]
 Disease Info 
Molecule Alteration Missense mutation
p.S371C (c.1111A>T)
 Molecule Info 
Experimental Note Identified from the Human Clinical Data
Key Molecule: Fibroblast growth factor receptor 3 (FGFR3) [4]
Sensitive Disease Bladder cancer [ICD-11: 2C94.0]
 Disease Info 
Molecule Alteration Missense mutation
p.G380R (c.1138G>A)
 Molecule Info 
Experimental Note Identified from the Human Clinical Data
Key Molecule: Fibroblast growth factor receptor 3 (FGFR3) [4]
Sensitive Disease Bladder cancer [ICD-11: 2C94.0]
 Disease Info 
Molecule Alteration Synonymous
p.K650K (c.1950G>A)
 Molecule Info 
Experimental Note Identified from the Human Clinical Data
Key Molecule: Fibroblast growth factor receptor 3 (FGFR3) [3]
Sensitive Disease Bladder cancer [ICD-11: 2C94.0]
 Disease Info 
Molecule Alteration Missense mutation
p.G370C (c.1108G>T)
 Molecule Info 
Experimental Note Identified from the Human Clinical Data
Key Molecule: Fibroblast growth factor receptor 3 (FGFR3) [3]
Sensitive Disease Bladder cancer [ICD-11: 2C94.0]
 Disease Info 
Molecule Alteration Missense mutation
p.Y373C (c.1118A>G)
 Molecule Info 
Experimental Note Identified from the Human Clinical Data
Key Molecule: Fibroblast growth factor receptor 3 (FGFR3) [3]
Sensitive Disease Bladder cancer [ICD-11: 2C94.0]
 Disease Info 
Molecule Alteration Missense mutation
p.R248C (c.742C>T)
 Molecule Info 
Experimental Note Identified from the Human Clinical Data
Key Molecule: Fibroblast growth factor receptor 3 (FGFR3) [3]
Sensitive Disease Bladder cancer [ICD-11: 2C94.0]
 Disease Info 
Molecule Alteration Missense mutation
p.S249C (c.746C>G)
 Molecule Info 
Experimental Note Identified from the Human Clinical Data
Key Molecule: Fibroblast growth factor receptor 3 (FGFR3) [3]
Sensitive Disease Bladder cancer [ICD-11: 2C94.0]
 Disease Info 
Molecule Alteration Missense mutation
p.S249C (c.746C>G)
 Molecule Info 
Experimental Note Identified from the Human Clinical Data
Transitional cell carcinoma [ICD-11: 2C9Z]
Click to Show/Hide
Drug Sensitivity Data Categorized by Their Corresponding Mechanisms
  Aberration of the Drug's Therapeutic Target (ADTT) Click to Show/Hide
Key Molecule: Fibroblast growth factor receptor 3 (FGFR3) [3]
Sensitive Disease Transitional cell carcinoma [ICD-11: 2C9Z.0]
 Disease Info 
Molecule Alteration Missense mutation
p.S249C (c.746C>G)
 Molecule Info 
Experimental Note Identified from the Human Clinical Data
Key Molecule: Fibroblast growth factor receptor 3 (FGFR3) [3]
Sensitive Disease Transitional cell carcinoma [ICD-11: 2C9Z.0]
 Disease Info 
Molecule Alteration Missense mutation
p.G370C (c.1108G>T)
 Molecule Info 
Experimental Note Identified from the Human Clinical Data
Key Molecule: Fibroblast growth factor receptor 3 (FGFR3) [3]
Sensitive Disease Transitional cell carcinoma [ICD-11: 2C9Z.0]
 Disease Info 
Molecule Alteration Missense mutation
p.Y373C (c.1118A>G)
 Molecule Info 
Experimental Note Identified from the Human Clinical Data
Key Molecule: Fibroblast growth factor receptor 3 (FGFR3) [3]
Sensitive Disease Transitional cell carcinoma [ICD-11: 2C9Z.0]
 Disease Info 
Molecule Alteration Missense mutation
p.R248C (c.742C>T)
 Molecule Info 
Experimental Note Identified from the Human Clinical Data
References
Ref 1 Fibroblast growth factor receptors in cancer: genetic alterations, diagnostics, therapeutic targets and mechanisms of resistance .Br J Cancer. 2021 Mar;124(5):880-892. doi: 10.1038/s41416-020-01157-0. Epub 2020 Dec 3. 10.1038/s41416-020-01157-0
Ref 2 Landscape of activating cancer mutations in FGFR kinases and their differential responses to inhibitors in clinical useOncotarget. 2016 Apr 26;7(17):24252-68. doi: 10.18632/oncotarget.8132.
Ref 3 Erdafitinib in Locally Advanced or Metastatic Urothelial CarcinomaN Engl J Med. 2019 Jul 25;381(4):338-348. doi: 10.1056/NEJMoa1817323.
Ref 4 Small molecule FGF receptor inhibitors block FGFR-dependent urothelial carcinoma growth in vitro and in vivoBr J Cancer. 2011 Jan 4;104(1):75-82. doi: 10.1038/sj.bjc.6606016. Epub 2010 Nov 30.

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