Molecular Profile |
Indication/Tumor Type |
Response Type |
Therapy Name |
Approval Status |
Evidence Type |
Efficacy Evidence |
References |
FGFR2 act mut
|
Advanced Solid Tumor
|
sensitive
|
Debio 1347
|
Phase I |
Actionable |
In a Phase I trial, Debio 1347 (CH5183284) dosing regimen has been determined in solid tumor patients with activating FGFR2 alterations (JCO, Vol 33, No 15_suppl (May 20 Supplement), 2015: 2540).
|
detail...
|
FGFR2 act mut
|
Advanced Solid Tumor
|
predicted - sensitive
|
Erdafitinib
|
Phase I |
Actionable |
In a Phase I trial, Balversa (erdafitinib) treatment resulted in stable disease in 70% (16/23) and partial response in 22% (5/23) of patients with advanced solid tumors harboring FGFR 1-4 activating mutations (including amplifications, mutations and translocations), while no antitumor activity was observed in patients with unknown or no known changes in FGFR (PMID: 26324363; NCT01703481).
|
26324363
|
FGFR2 act mut
|
bladder urothelial carcinoma
|
sensitive
|
Erdafitinib
|
Guideline |
Actionable |
Balversa (erdafitinib) is included in guidelines for patients with advanced or metastatic bladder urothelial carcinoma harboring FGFR alterations (PMID: 34861372; ESMO.org).
|
detail...
34861372
|
FGFR2 act mut
|
Advanced Solid Tumor
|
decreased response
|
Nintedanib
|
Preclinical |
Actionable |
In a preclinical study, transformed cells expressing constitutively active FGFR2 demonstrated reduced sensitivity to Ofev (Nintedanib) in culture, when compared to other tyrosine kinase inhibitors (PMID: 22238366).
|
22238366
|
FGFR2 act mut
|
Advanced Solid Tumor
|
decreased response
|
Brivanib
|
Preclinical |
Actionable |
In a preclinical study, transformed cells expressing constitutively active FGFR2 demonstrated reduced sensitivity to inhibition of receptor phosphorylation and cell proliferation by Brivanib (BMS-540215) in culture, when compared to other tyrosine kinase inhibitors (PMID: 22238366).
|
22238366
|
FGFR2 act mut
|
stomach carcinoma
|
sensitive
|
S-49076
|
Preclinical - Cell line xenograft |
Actionable |
In a preclinical study, S-49076 inhibited Met activation, resulting in growth inhibition of gastric carcinoma cells harboring FGFR2 activating mutations in culture and in cell line xenograft models (PMID: 23804704).
|
23804704
|
FGFR2 act mut
|
Advanced Solid Tumor
|
decreased response
|
Cediranib
|
Preclinical |
Actionable |
In a preclinical study, transformed cells expressing constitutively active FGFR2 demonstrated reduced sensitivity to inhibition of receptor phosphorylation and cell proliferation by Cediranib (AZD-2171) in culture, when compared to other tyrosine kinase inhibitors (PMID: 22238366).
|
22238366
|
FGFR2 act mut
|
Advanced Solid Tumor
|
predicted - sensitive
|
AZD4547
|
Phase II |
Actionable |
In a Phase II (MATCH) trial, AZD4547 treatment resulted in an overall response rate of 10.5% (2/19) in patients with advanced solid tumors harboring FGFR2 or 3 activating single nucleotide variants and a 6-month progression-free survival rate of 6%, with a partial response in 1 and stable disease in 2 of 12 patients with FGFR2 activating mutations (PMID: 32463741; NCT02465060).
|
32463741
|
FGFR2 act mut
|
Advanced Solid Tumor
|
sensitive
|
Ponatinib
|
Preclinical |
Actionable |
In a preclinical study, Iclusig (ponatinib) inhibited receptor phosphorylation and cell growth in transformed cells expressing constitutively active FGFR2 in culture (PMID: 22238366).
|
22238366
|
FGFR2 act mut
|
Advanced Solid Tumor
|
sensitive
|
Dovitinib
|
Preclinical |
Actionable |
In a preclinical study, Dovitinib (TKI258) inhibited receptor phosphorylation and cell proliferation in transformed cells expressing constitutively active FGFR2 in culture (PMID: 22238366).
|
22238366
|
FGFR2 act mut
|
endometrial cancer
|
sensitive
|
Dovitinib
|
Preclinical - Cell line xenograft |
Actionable |
In a preclinical study, both cell lines and cell line xenograft models of endometrial cancer with FGFR2 activating mutations showed greater sensitivity to Dovitinib (TKI258) as compared to FGFR2 wild-type (PMID: 23443805).
|
23443805
|
FGFR2 mutant
|
cholangiocarcinoma
|
sensitive
|
Infigratinib
|
Case Reports/Case Series |
Actionable |
In a Phase I trial, a patient with cholangiocarcinoma harboring an FGFR2 mutation demonstrated a decreased tumor burden when treated with Truseltiq (infigratinib) (PMID: 27870574).
|
27870574
|
FGFR2 mutant
|
bladder urothelial carcinoma
|
sensitive
|
Erdafitinib
|
FDA approved - Has Companion Diagnostic |
Actionable |
In a Phase II trial (BCL2001) that supported FDA approval, Balversa (erdafitinib) treatment resulted in an objective response rate of 40% (40/99, 3 complete response, 37 partial response) and a disease control rate of 80% in patients with metastatic or unresectable urothelial carcinoma harboring FGFR alterations (PMID: 31340094; NCT02365597).
|
detail...
31340094
detail...
|
FGFR2 mutant
|
bladder urothelial carcinoma
|
sensitive
|
Erdafitinib
|
Guideline |
Actionable |
Balversa (erdafitinib) is included in the guidelines for patients with advanced or metastatic urothelial carcinoma harboring Fgfr2 alterations after progression on platinum-based regimens (NCCN.org).
|
detail...
|
FGFR2 mutant
|
endometrial cancer
|
sensitive
|
Infigratinib
|
Preclinical |
Actionable |
In a preclinical study, Truseltiq (infigratinib) inhibited the growth of FGFR2-mutated endometrial cancer cells in vitro and in xenograft models (PMID: 23443805).
|
23443805
|
FGFR2 mutant
|
Advanced Solid Tumor
|
sensitive
|
Pemigatinib
|
Preclinical - Cell culture |
Actionable |
In a preclinical study, a variety of cancer cell lines harboring mutations in FGFR1, FGFR2, and/or FGFR3 demonstrated sensitivity to Pemazyre (pemigatinib) in culture and in cell line xenograft models, resulting in inhibition of tumor growth (Cancer Res 2015;75(15 Suppl):Abstract nr 771).
|
detail...
|
FGFR2 mutant
|
Advanced Solid Tumor
|
predicted - sensitive
|
Debio 1347
|
Phase I |
Actionable |
In a Phase I trial, Debio 1347 treatment resulted in partial response in 10.5% (6/57) and stable disease in 28.1% (16/57) of patients with advanced solid tumors harboring genomic alterations of FGFR1/2/3, including amplifications, fusions, and mutations (PMID: 30745300; NCT01948297).
|
30745300
|
FGFR2 mutant
|
endometrial cancer
|
sensitive
|
PRN1371
|
Preclinical - Cell culture |
Actionable |
In a preclinical study, PRN1371 inhibited proliferation of endometrial cancer cells harboring FGFR2 mutations in culture (AACR; Cancer Res 2016;76(14 Suppl):Abstract nr 1249).
|
detail...
|
FGFR2 mutant
|
cholangiocarcinoma
|
predicted - sensitive
|
Erdafitinib
|
Phase I |
Actionable |
In a Phase I trial, Balversa (erdafitinib) treatment resulted in an objective response rate of 27% (3/11) in patients with cholangiocarcinoma harboring FGFR genomic alterations, including 1 with FGFR2 mutation, 2 with FGFR3 mutations, and 8 with FGFR2 fusions (PMID: 31088831; NCT01703481).
|
31088831
|
FGFR2 mutant
|
Advanced Solid Tumor
|
predicted - sensitive
|
ICP-192
|
Phase I |
Actionable |
In a Phase I trial, ICP-192 (gunagratinib) was well-tolerated, and resulted in an overall response rate or 33.3% (4/12, 1 complete response, 3 partial response) and a disease control rate of 91.7% (11/12) in patients with advanced solid tumors harboring FGF/FGFR gene aberrations (J Clin Oncol 39, 2021 (suppl 15; abstr 4092); NCT03758664).
|
detail...
|
FGFR2 mutant
|
transitional cell carcinoma
|
sensitive
|
Erdafitinib
|
Guideline |
Actionable |
Balversa (erdafitinib) is included in the guidelines for patients with advanced or metastatic urothelial carcinoma harboring Fgfr2 alterations after progression on platinum-based regimens (NCCN.org).
|
detail...
|
FGFR2 mutant
|
transitional cell carcinoma
|
sensitive
|
Erdafitinib
|
FDA approved - Has Companion Diagnostic |
Actionable |
In a Phase II trial (BCL2001) that supported FDA approval, Balversa (erdafitinib) treatment resulted in an objective response rate of 40% (40/99, 3 complete response, 37 partial response) and a disease control rate of 80% in patients with metastatic or unresectable urothelial carcinoma harboring FGFR alterations (PMID: 31340094; NCT02365597).
|
detail...
31340094
detail...
|
FGFR2 fusion
|
cholangiocarcinoma
|
sensitive
|
Pemigatinib
|
Guideline |
Actionable |
Pemazyre (pemigatinib) is included in guidelines as subsequent-line therapy for patients with cholangiocarcinoma harboring FGFR2 fusions or rearrangements (NCCN.org).
|
detail...
|
FGFR2 fusion
|
cholangiocarcinoma
|
sensitive
|
Pemigatinib
|
FDA approved - On Companion Diagnostic |
Actionable |
In a Phase II (FIGHT-202) trial, Pemazyre (pemigatinib) treatment resulted in an objective response in 35.5% (38/107, 3 complete response, 35 partial response) of patients with advanced cholangiocarcinoma harboring FGFR2 fusions or rearrangements, with a disease control rate of 82% (88/107), median time-to-response of 2.7 months, and a median progression-free survival of 6.9 months (PMID: 32203698; NCT02924376).
|
detail...
32203698
detail...
|
FGFR2 fusion
|
intrahepatic cholangiocarcinoma
|
predicted - sensitive
|
Futibatinib
|
Phase II |
Actionable |
In a Phase II trial (FOENIX-CCA2), Futibatinib (TAS-120) demonstrated manageable toxicity profile, resulted in an objective response rate (ORR) of 37.3% (25/67), a median duration of response of 8.3 months, and a disease control rate of 82% in patients with intrahepatic cholangiocarcinoma harboring FGFR2 fusions (82%) or other rearrangements (18%), ORR was 36.2% (21/58) in patients harboring FGFR2 fusions (Annals of Oncology (2020) 31 (suppl_4): S261-S262; NCT02052778).
|
detail...
|
FGFR2 fusion
|
Advanced Solid Tumor
|
predicted - sensitive
|
Futibatinib
|
Phase I |
Actionable |
In a Phase I trial (FOENIX-101), Futibatinib (TAS-120) treatment demonstrated manageable safety profile, and resulted in a partial response in 6% (5/86) and stable disease in 48% (41/86) of patients with advanced solid tumors harboring FGF/FGFR aberrations, among whom 20% (15/74) harbored FGFR2 fusions (PMID: 32622884; NCT02052778).
|
32622884
|
FGFR2 fusion
|
transitional cell carcinoma
|
predicted - sensitive
|
Erdafitinib
|
Phase I |
Actionable |
In a Phase I trial, Balversa (erdafitinib) treatment resulted in an objective response rate of 46% (12/26) in patients with urothelial carcinoma harboring FGFR genomic alterations, including 17 with FGFR3 mutations, and 11 with FGFR2 and/or FGFR3 fusions (PMID: 31088831; NCT01703481).
|
31088831
|
FGFR2 fusion
|
stomach cancer
|
predicted - sensitive
|
RLY-4008
|
Preclinical - Cell line xenograft |
Actionable |
In a preclinical study, RLY-4008 treatment led to tumor regression in a cell line xenograft model of gastric cancer harboring an FGFR2 fusion (Cancer Res 2021;81(13_Suppl):Abstract nr 1455).
|
detail...
|
FGFR2 fusion
|
cholangiocarcinoma
|
predicted - sensitive
|
Futibatinib
|
Phase I |
Actionable |
In a Phase I trial, TAS-120 treatment resulted in an objective response rate of 25% (7/28, 7 partial responses) in patients with cholangiocarcinoma harboring FGFR2 fusions, with 71% of patients experienced tumor shrinkage, 54% (15/28) achieved stable disease (Annals of Oncology, Volume 29, Issue suppl_5).
|
detail...
|
FGFR2 fusion
|
intrahepatic cholangiocarcinoma
|
sensitive
|
Derazantinib
|
Phase I |
Actionable |
In a Phase Ib/II trial, Derazantinib (ARQ 087) treatment resulted in an overall response rate of 20.7% (6/29), a disease control rate of 82.8% (24/29), and a median progression-free survival of 5.7 months in patients with intrahepatic cholangiocarcinoma harboring FGFR2 fusions (PMID: 30420614; NCT01752920).
|
30420614
|
FGFR2 fusion
|
cholangiocarcinoma
|
sensitive
|
Infigratinib
|
Guideline |
Actionable |
Truseltiq (infigratinib) is included in guidelines as a subsequent-line therapy for patients with cholangiocarcinoma harboring an FGFR2 fusion or rearrangement (NCCN.org).
|
detail...
|
FGFR2 fusion
|
cholangiocarcinoma
|
sensitive
|
Infigratinib
|
FDA approved - On Companion Diagnostic |
Actionable |
In a Phase II trial that supported FDA approval, Truseltiq (infigratinib) treatment demonstrated manageable toxicity, resulted in an objective response rate of 23.1% (25/108, 1 complete response, 24 partial responses) in patients with previously treated advanced cholangiocarcinoma harboring an FGFR2 fusion or rearrangement, with a median duration of response of 5.0 months and a median progression-free survival of 7.3 months (J Clin Oncol 39, no. 3_suppl (January 20, 2021) 265-265; NCT02150967).
|
detail...
detail...
detail...
|
FGFR2 fusion
|
cholangiocarcinoma
|
sensitive
|
Infigratinib
|
Case Reports/Case Series |
Actionable |
In a Phase I trial, two patients with cholangiocarcinoma harboring FGFR2 fusions demonstrated a decreased tumor burden when treated with Truseltiq (infigratinib) (PMID: 27870574).
|
27870574
|
FGFR2 fusion
|
Advanced Solid Tumor
|
predicted - sensitive
|
Pemigatinib
|
Case Reports/Case Series |
Actionable |
In a Phase I trial (FIGHT-101), Pemazyre (pemigatinib) treatment led to an objective response rate of 25% (5/20, all partial responses) in patients harboring FGFR rearrangements, with all 5 partial responses in patients with FGFR2 fusions, stable disease in 50% (10/20) of patients, and a median progression-free survival of 5.7 months (PMID: 35176457; NCT02393248).
|
35176457
|
FGFR2 fusion
|
lung cancer
|
predicted - sensitive
|
RLY-4008
|
Preclinical - Cell line xenograft |
Actionable |
In a preclinical study, RLY-4008 treatment led to tumor regression in a cell line xenograft model of lung cancer harboring an FGFR2 fusion (Cancer Res 2021;81(13_Suppl):Abstract nr 1455).
|
detail...
|
FGFR2 fusion
|
cholangiocarcinoma
|
predicted - sensitive
|
Erdafitinib
|
Phase I |
Actionable |
In a Phase I trial, Balversa (erdafitinib) treatment resulted in an objective response rate of 27% (3/11) in patients with cholangiocarcinoma harboring FGFR genomic alterations, including 1 with FGFR2 mutation, 2 with FGFR3 mutations, and 8 with FGFR2 fusions (PMID: 31088831; NCT01703481).
|
31088831
|
FGFR2 fusion
|
bladder urothelial carcinoma
|
sensitive
|
Erdafitinib
|
Guideline |
Actionable |
Balversa (erdafitinib) is included in guidelines for patients with advanced or metastatic bladder urothelial carcinoma harboring FGFR alterations (PMID: 34861372; ESMO.org).
|
detail...
34861372
|
FGFR2 fusion
|
Advanced Solid Tumor
|
predicted - sensitive
|
Debio 1347
|
Phase I |
Actionable |
In a Phase I trial, Debio 1347 treatment resulted in partial response in 10.5% (6/57) and stable disease in 28.1% (16/57) of patients with advanced solid tumors harboring genomic alterations of FGFR1/2/3, including amplifications, fusions, and mutations (PMID: 30745300; NCT01948297).
|
30745300
|
FGFR2 fusion
|
biliary tract cancer
|
predicted - sensitive
|
Futibatinib
|
Phase I |
Actionable |
In a Phase I trial, TAS-120 treatment resulted in stable disease over 24 weeks in two biliary tract cancer patients harboring FGFR2 fusions (Ann Oncol 2017, Vol 28, Suppl 5, Abstract # 372PD).
|
detail...
|
FGFR2 fusion
|
cholangiocarcinoma
|
predicted - sensitive
|
ICP-192
|
Case Reports/Case Series |
Actionable |
In a Phase I trial, ICP-192 (gunagratinib) treatment resulted in a complete response in a patient with cholangiocarcinoma harboring FGFR2 fusion (J Clin Oncol 39, 2021 (suppl 15; abstr 4092); NCT03758664).
|
detail...
|
FGFR2 rearrange
|
intrahepatic cholangiocarcinoma
|
predicted - sensitive
|
Futibatinib
|
Case Reports/Case Series |
Actionable |
In a Phase II trial (FOENIX-CCA2), Futibatinib (TAS-120) demonstrated manageable toxicity profile, resulted in an objective response rate (ORR) of 37.3% (25/67), a median duration of response of 8.3 months, and a disease control rate of 82% in patients with intrahepatic cholangiocarcinoma harboring FGFR2 fusions (82%) or other rearrangements (18%), ORR was 44.4% (4/9) in patients harboring FGFR2 rearrangements (Annals of Oncology (2020) 31 (suppl_4): S261-S262; NCT02052778).
|
detail...
|
FGFR2 rearrange
|
cholangiocarcinoma
|
predicted - sensitive
|
Futibatinib
|
Phase I |
Actionable |
In a Phase I trial, TAS-120 treatment resulted in partial response in 2 patients with cholangiocarcinoma harboring FGFR2 rearrangements (Annals of Oncology, Volume 29, Issue suppl_5).
|
detail...
|
FGFR2 rearrange
|
cholangiocarcinoma
|
sensitive
|
Pemigatinib
|
Guideline |
Actionable |
Pemazyre (pemigatinib) is included in guidelines as subsequent-line therapy for patients with cholangiocarcinoma harboring FGFR2 fusions or rearrangements (NCCN.org).
|
detail...
|
FGFR2 rearrange
|
cholangiocarcinoma
|
sensitive
|
Pemigatinib
|
FDA approved - On Companion Diagnostic |
Actionable |
In a Phase II (FIGHT-202) trial, Pemazyre (pemigatinib) treatment resulted in an objective response in 35.5% (38/107, 3 complete response, 35 partial response) of patients with advanced cholangiocarcinoma harboring FGFR2 fusions or rearrangements, with a disease control rate of 82% (88/107), median time-to-response of 2.7 months, and a median progression-free survival of 6.9 months (PMID: 32203698; NCT02924376).
|
detail...
32203698
detail...
|
FGFR2 rearrange
|
cholangiocarcinoma
|
sensitive
|
Infigratinib
|
FDA approved - On Companion Diagnostic |
Actionable |
In a Phase II trial that supported FDA approval, Truseltiq (infigratinib) treatment demonstrated manageable toxicity, resulted in an objective response rate of 23.1% (25/108, 1 complete response, 24 partial responses) in patients with previously treated advanced cholangiocarcinoma harboring an FGFR2 fusion or rearrangement, with a median duration of response of 5.0 months and a median progression-free survival of 7.3 months (J Clin Oncol 39, no. 3_suppl (January 20, 2021) 265-265; NCT02150967).
|
detail...
detail...
detail...
|
FGFR2 rearrange
|
cholangiocarcinoma
|
sensitive
|
Infigratinib
|
Guideline |
Actionable |
Truseltiq (infigratinib) is included in guidelines as a subsequent-line therapy for patients with cholangiocarcinoma harboring an FGFR2 fusion or rearrangement (NCCN.org).
|
detail...
|