Molecular Profile |
Indication/Tumor Type |
Response Type |
Relevant Treatment Approaches |
Therapy Name |
Approval Status |
Evidence Type |
Efficacy Evidence |
References |
FGFR1 amp
|
non-small cell lung carcinoma
|
sensitive |
FGFR1 Inhibitor
|
Debio 1347
|
Preclinical |
Actionable |
In a preclinical study, Debio 1347 inhibited proliferation of non-small cell lung cancer cell lines harboring FGFR1 amplification in culture (PMID: 25169980).
|
25169980
|
FGFR1 amp
|
lung squamous cell carcinoma
|
no benefit |
FGFR1 Inhibitor
|
AZD4547
|
Phase I |
Actionable |
In a Phase Ib trial, AZD4547 demonstrated limited efficacy in patients with squamous cell lung cancer with FGFR1 amplification, resulting in an overall response rate of 8% (1/15) and a median overall survival of 4.9 months (PMID: 28615371; NCT00979134).
|
28615371
|
FGFR1 amp
|
estrogen-receptor positive breast cancer
|
sensitive |
|
Cediranib
|
Preclinical |
Actionable |
In a preclinical study, Cediranib (AZD-2171) inhibited growth of estrogen receptor (ER)-positive breast cancer cells with FGFR1 amplification in culture (PMID: 22238366).
|
22238366
|
FGFR1 amp
|
lung squamous cell carcinoma
|
sensitive |
FGFR Inhibitor (Pan)
|
Ponatinib
|
Preclinical |
Actionable |
In a preclinical study, Iclusig (ponatinib) inhibited growth of squamous cell lung cancer cell lines harboring FGFR1 amplification (PMID: 22238366).
|
22238366
|
FGFR1 amp
|
lung large cell carcinoma
|
sensitive |
FGFR1 Inhibitor
|
AZD4547
|
Preclinical |
Actionable |
In a preclinical study, AZD4547 inhibited proliferation of a large cell lung cancer cell line harboring FGFR1 amplification in culture and induced tumor regression in xenograft models (PMID: 23082000).
|
23082000
|
FGFR1 amp
|
non-small cell lung carcinoma
|
sensitive |
GSK3052230
|
GSK3052230
|
Preclinical - Cell line xenograft |
Actionable |
In a preclinical study, GSK3052230 (FP-1039) treatment inhibited growth of FGFR1 amplified non-small cell lung carcinoma cell lines in culture and in cell line xenograft models (PMID: 23536011).
|
23536011
|
FGFR1 amp
|
non-small cell lung carcinoma
|
sensitive |
FGFR Inhibitor (Pan)
|
PRN1371
|
Preclinical - Pdx |
Actionable |
In a preclinical study, PRN1371 treatment resulted in 96.1% tumor growth inhibition in patient-derived xenograft models of FGFR1-amplified non-small cell lung cancer (PMID: 28978721).
|
28978721
|
FGFR1 amp
|
lung small cell carcinoma
|
no benefit |
|
RO5126766
|
Preclinical - Cell culture |
Actionable |
In a preclinical study, FGFR1 amplified lung small cell carcinoma cells were not sensitive to RO5126766 in culture (PMID: 26438159).
|
26438159
|
FGFR1 amp
|
estrogen-receptor positive breast cancer
|
sensitive |
FGFR1 Inhibitor
|
E7090
|
Preclinical - Cell culture |
Actionable |
In a preclinical study, an estrogen-receptor positive breast cancer cell line harboring FGFR1 amplification (PMID: 7506125) demonstrated sensitivity to E7090 in culture, resulting in decreased cell viability (PMID: 27535969).
|
7506125
27535969
|
FGFR1 amp
|
non-small cell lung carcinoma
|
sensitive |
FGFR1 Inhibitor
|
E7090
|
Preclinical - Cell line xenograft |
Actionable |
In a preclinical study, a non-small cell lung cancer cell line, harboring FGFR1 amplification, treated with E7090 demonstrated decreased cell viability in culture and antitumor activity in xenograft models (PMID: 27535969).
|
27535969
|
FGFR1 amp
|
synovial sarcoma
|
sensitive |
FGFR1 Inhibitor
|
AZD4547
|
Preclinical - Cell culture |
Actionable |
In a preclinical study, AZD4547 inhibited survival of FGFR1 amplified synovial sarcoma cells in culture (PMID: 27535980).
|
27535980
|
FGFR1 amp
|
lung cancer
|
sensitive |
GSK3052230
|
GSK3052230
|
Preclinical - Cell line xenograft |
Actionable |
In a preclinical study, GSK3052230 (FP-1039) treatment resulted in greater tumor growth inhibition (56% vs 22%) in cell line xenograft models of FGFR1 amplified lung cancer compared to FGFR1 non-amplified models (PMID: 23536011).
|
23536011
|
FGFR1 amp
|
breast cancer
|
no benefit |
FGFR1 Inhibitor
|
AZD4547
|
Phase II |
Actionable |
In a Phase II clinical trial, treatment with AZD4547 resulted in a response rate of 12.5% (1/8) in patients with FGFR1-amplified breast cancer, and did not meet the predetermined criteria for efficacy (PMID: 27179038).
|
27179038
|
FGFR1 amp
|
Advanced Solid Tumor
|
predicted - sensitive |
FGFR1 Inhibitor
|
AZD4547
|
Phase II |
Actionable |
In a Phase II (MATCH) trial, AZD4547 treatment resulted in stable disease in 59% (10/17) of patients with advanced solid tumors harboring FGFR amplification, with a 6-month progression-free survival rate of 15% (J Clin Oncol 36, 2018 (suppl; abstr 2503); NCT02465060).
|
detail...
|
FGFR1 amp
|
lung squamous cell carcinoma
|
sensitive |
FGFR Inhibitor (Pan)
|
BGJ398
|
Phase I |
Actionable |
In a Phase I trial, patients with lung squamous cell carcinoma harboring an FGFR1 amplification demonstrated a disease control rate of 50% (18/36) when treated with BGJ398, resulting in 14 patients with stable disease and 4 patients with a partial response (PMID: 27870574).
|
27870574
|
FGFR1 amp
|
lung small cell carcinoma
|
sensitive |
FGFR1 Inhibitor
|
Debio 1347
|
Preclinical |
Actionable |
In a preclinical study, Debio 1347 inhibited proliferation of small cell lung cancer cell lines harboring FGFR1 amplification in culture (PMID: 25169980).
|
25169980
|
FGFR1 amp
|
estrogen-receptor positive breast cancer
|
resistant |
|
Alpelisib
|
Preclinical - Cell culture |
Actionable |
In a preclinical study, an estrogen-receptor positive breast cancer cell line harboring an FGFR1 amplification demonstrated resistance to Alpelisib (BYL719) in culture (PMID: 27126994).
|
27126994
|
FGFR1 amp
|
lung squamous cell carcinoma
|
sensitive |
FGFR1 Inhibitor
|
AZD4547 + BKM120
|
Preclinical - Cell culture |
Actionable |
In a preclinical study, the combination of AZD4547 and Buparlisib (BKM120) induced apoptosis in a squamous cell lung cancer cell line with amplification of FGFR1 in culture (PMID: 28108151).
|
28108151
|
FGFR1 amp
|
lung small cell carcinoma
|
sensitive |
FGFR1 Inhibitor
|
E7090
|
Preclinical - Cell culture |
Actionable |
In a preclinical study, a small cell lung cancer cell line harboring FGFR1 amplification demonstrated sensitivity to E7090, resulting in decreased cell viability in culture and antitumor activity in xenograft models (PMID: 27535969).
|
27535969
|
FGFR1 amp
|
lung squamous cell carcinoma
|
no benefit |
|
RO4987655
|
Preclinical - Cell culture |
Actionable |
In a preclinical study, FGFR1 amplified lung squamous cell carcinoma cells were not sensitive to RO4987655 in culture (PMID: 26438159).
|
26438159
|
FGFR1 amp
|
lung carcinoma
|
sensitive |
FGFR1 Inhibitor
|
Lucitanib
|
Preclinical - Cell line xenograft |
Actionable |
in a preclinical study, Lucitanib (E-3810) preferentially inhibited growth of FGFR1-amplified lung carcinoma cell lines in culture and in cell line xenograft models (PMID: 27988457).
|
27988457
|
FGFR1 amp
|
non-small cell lung carcinoma
|
no benefit |
|
RO5126766
|
Preclinical - Cell culture |
Actionable |
In a preclinical study, FGFR1 amplified non-small cell lung carcinoma cells were not sensitive to RO5126766 in culture (PMID: 26438159).
|
26438159
|
FGFR1 amp
|
estrogen-receptor positive breast cancer
|
no benefit |
FGFR1 Inhibitor
|
Brivanib
|
Preclinical |
Actionable |
In a preclinical study, Brivanib (BMS-540215) did not inhibit growth of estrogen receptor (ER)-positive breast cancer cells with FGFR2 amplification in culture (PMID: 22238366).
|
22238366
|
FGFR1 amp
|
synovial sarcoma
|
sensitive |
FGFR Inhibitor (Pan)
|
BGJ398
|
Preclinical - Cell culture |
Actionable |
In a preclinical study, BGJ398 inhibited survival of FGFR1 amplified synovial sarcoma cells in culture (PMID: 27535980).
|
27535980
|
FGFR1 amp
|
synovial sarcoma
|
sensitive |
FGFR1 Inhibitor
|
PD173074
|
Preclinical - Cell culture |
Actionable |
In a preclinical study, PD173074 inhibited survival of FGFR1 amplified synovial sarcoma cells in culture (PMID: 27535980).
|
27535980
|
FGFR1 amp
|
lung cancer
|
sensitive |
FGFR1 Inhibitor
|
AZD4547
|
Preclinical |
Actionable |
In a preclinical study, AZD4547 inhibited proliferation of lung cancer cell lines harboring FGFR1 amplification in culture and induced tumor regression in xenograft models (PMID: 23082000).
|
23082000
|
FGFR1 amp
|
non-small cell lung carcinoma
|
sensitive |
FGFR Inhibitor (Pan)
|
BGJ398 + Trametinib
|
Preclinical - Cell culture |
Actionable |
In a preclinical study, BGJ398 and Mekinist (trametinib) combination treatment inhibited Erk signaling and growth of FGFR1-amplified non-small cell lung carcinoma cells in culture (PMID: 28630215).
|
28630215
|
FGFR1 amp
|
non-small cell lung carcinoma
|
sensitive |
FGFR1 Inhibitor
|
AZD4547
|
Preclinical - Pdx |
Actionable |
In a preclinical study, AZD4547 inhibited FGFR1 signaling and resulted in tumor regression in patient-derived xenograft models of non-small cell lung carcinoma harboring FGFR1 amplification, wild-type for EGFR, K-Ras and negative for EML4-ALK fusion (PMID: 23082000).
|
23082000
|
FGFR1 amp
|
estrogen-receptor positive breast cancer
|
sensitive |
FGFR1 Inhibitor
|
Lucitanib
|
Preclinical - Cell culture |
Actionable |
In a preclinical study, an estrogen-receptor positive breast cancer cell line harboring FGFR1 amplification demonstrated sensitivity to treatment with Lucitanib (E-3810) in culture (PMID: 27126994).
|
27126994
|
FGFR1 amp
|
lung squamous cell carcinoma
|
no benefit |
|
Selumetinib
|
Preclinical - Cell culture |
Actionable |
In a preclinical study, FGFR1 amplified lung squamous cell carcinoma cells were not sensitive to Selumetinib (AZD-6244) in culture (PMID: 26438159).
|
26438159
|
FGFR1 amp
|
Her2-receptor negative breast cancer
|
sensitive |
FGFR1 Inhibitor
|
Pazopanib
|
Clinical Study |
Actionable |
In a clinical case study, a patient with ERBB2 (HER2)-receptor negative breast cancer harboring FGFR1 amplification demonstrated antitumor activity when treated with Votrient (pazopanib), including a near complete loss of brain lesions and improved function of the liver (PMID: 29223982).
|
29223982
|
FGFR1 amp
|
lung cancer
|
no benefit |
FGFR1 Inhibitor
|
Brivanib
|
Preclinical |
Actionable |
In a preclinical study, Brivanib (BMS-540215) did not inhibit growth of lung cancer cells with FGFR1 amplification in culture (PMID: 22238366).
|
22238366
|
FGFR1 amp
|
non-small cell lung carcinoma
|
sensitive |
FGFR Inhibitor (Pan)
|
BGJ398
|
Preclinical - Cell culture |
Actionable |
In a preclinical study, BGJ398 inhibited Erk signaling and growth of FGFR1-amplified non-small cell lung carcinoma cells in culture (PMID: 28630215).
|
28630215
|
FGFR1 amp
|
lung small cell carcinoma
|
no benefit |
|
RO4987655
|
Preclinical - Cell culture |
Actionable |
In a preclinical study, FGFR1 amplified lung small cell carcinoma cells were not sensitive to RO4987655 in culture (PMID: 26438159).
|
26438159
|
FGFR1 amp
|
lung small cell carcinoma
|
sensitive |
GSK3052230
|
GSK3052230
|
Preclinical - Cell line xenograft |
Actionable |
In a preclinical study, GSK3052230 (FP-1039) treatment inhibited growth of FGFR1 amplified lung small cell carcinoma cell lines in culture and in cell line xenograft models (PMID: 23536011).
|
23536011
|
FGFR1 amp
|
lung small cell carcinoma
|
sensitive |
|
Cisplatin + Etoposide + GSK3052230
|
Preclinical - Cell line xenograft |
Actionable |
In a preclinical study, addition of GSK3052230 (FP-1039) to Platinol (cisplatin) and Vepesid (etoposide) resulted in improved tumor growth inhibition in cell line xenograft models of FGFR1 amplified lung small cell carcinoma (PMID: 23536011).
|
23536011
|
FGFR1 amp
|
breast cancer
|
sensitive |
FGFR Inhibitor (Pan)
|
Ponatinib
|
Preclinical |
Actionable |
In a preclinical study, Iclusig (ponatinib) inhibited Fgfr phosphorylation and cell proliferation in ER-positive breast cancer cells harboring FGFR1 amplification in culture (PMID: 22238366).
|
22238366
|
FGFR1 amp
|
Her2-receptor positive breast cancer
|
sensitive |
FGFR Inhibitor (Pan)
|
Dovitinib
|
Phase I |
Actionable |
In a Phase I trial, Dovitinib (TKI258) promoted 6-month stable disease in Erbb2 (Her2)-positive breast cancer patients with FGFR1 amplification (PMID: 23658459).
|
23658459
|
FGFR1 amp
|
non-small cell lung carcinoma
|
no benefit |
|
RO4987655
|
Preclinical - Cell culture |
Actionable |
In a preclinical study, FGFR1 amplified non-small cell lung carcinoma cells were not sensitive to RO4987655 in culture (PMID: 26438159).
|
26438159
|
FGFR1 amp
|
lung small cell carcinoma
|
sensitive |
FGFR1 Inhibitor
|
AZD4547 + BKM120
|
Preclinical - Cell culture |
Actionable |
In a preclinical study, the combination of AZD4547 and Buparlisib (BKM120) induced apoptosis in a small cell lung cancer cell line with amplification of FGFR1 in culture (PMID: 28108151).
|
28108151
|
FGFR1 amp
|
Ewing sarcoma
|
predicted - sensitive |
FGFR Inhibitor (Pan)
|
Ponatinib
|
Preclinical - Cell culture |
Actionable |
In a preclinical study, Iclusig (ponatinib) inhibited proliferation of Ewing’s sarcoma cell lines with FGFR1 copy number gain in culture (PMID: 26179511).
|
26179511
|
FGFR1 amp
|
lung cancer
|
sensitive |
FGFR1 Inhibitor
|
PD173074
|
Preclinical - Cell culture |
Actionable |
In a preclinical study, lung cancer cells harboring FGFR1 amplification were sensitive to PD173074 treatment in culture, demonstrating inhibition of cell growth (PMID: 30140389).
|
30140389
|
FGFR1 amp
|
breast cancer
|
sensitive |
FGFR Inhibitor (Pan)
|
BGJ398
|
Phase I |
Actionable |
In a Phase I trial, 28% (9/32) of breast cancer patients harboring FGFR1 amplification demonstrated stable disease when treated with BGJ398 (PMID: 27870574).
|
27870574
|
FGFR1 amp
|
lung squamous cell carcinoma
|
no benefit |
|
RO5126766
|
Preclinical - Cell culture |
Actionable |
In a preclinical study, FGFR1 amplified lung squamous cell carcinoma cells were not sensitive to RO5126766 in culture (PMID: 26438159).
|
26438159
|
FGFR1 amp
|
adrenocortical carcinoma
|
sensitive |
FGFR1 Inhibitor
|
Derazantinib
|
Phase I |
Actionable |
In a Phase I trial, ARQ 087 treatment resulted in stable disease with a tumor reduction of 20% in an adrenocortical carcinoma patient harboring FGFR1 amplification, who remained on study for 3.5 years (PMID: 28972963; NCT01752920).
|
28972963
|
FGFR1 amp
|
lung cancer
|
predicted - sensitive |
FGFR Inhibitor (Pan)
|
Erdafitinib
|
Preclinical - Cell line xenograft |
Actionable |
In a preclinical study, Erdafitinib (JNJ-42756493) inhibited FGFR downstream signaling and proliferation of several lung cancer cell lines with FGFR1 amplification in culture, and inhibited tumor growth in an FGFR1-amplified lung cancer cell line xenograft model (PMID: 28341788).
|
28341788
|
FGFR1 amp
|
estrogen-receptor positive breast cancer
|
sensitive |
FGFR Inhibitor (Pan)
|
Nintedanib
|
Preclinical |
Actionable |
In a preclinical study, Ofev (nintedanib) inhibited the growth of ER-positive breast cancer cells harboring FGFR1 amplification in culture (PMID: 22238366).
|
22238366
|
FGFR1 amp
|
transitional cell carcinoma
|
sensitive |
FGFR1 Inhibitor
|
AZD4547 + BKM120
|
Preclinical - Cell culture |
Actionable |
In a preclinical study, the combination of AZD4547 and Buparlisib (BKM120) worked synergistically to induce apoptosis and inhibit growth of a urothelial cell carcinoma cell line with FGFR1 amplification in culture, with increased efficacy over either agent alone (PMID: 28108151).
|
28108151
|
FGFR1 amp
|
lung small cell carcinoma
|
sensitive |
FGFR1 Inhibitor
|
AZD4547
|
Preclinical |
Actionable |
In a preclinical study, AZD4547 inhibited proliferation of a small cell lung cancer cell line harboring FGFR1 amplification in culture (PMID: 23082000).
|
23082000
|
FGFR1 amp
|
lung small cell carcinoma
|
no benefit |
|
Selumetinib
|
Preclinical - Cell culture |
Actionable |
In a preclinical study, FGFR1 amplified lung small cell carcinoma cells were not sensitive to Selumetinib (AZD-6244) in culture (PMID: 26438159).
|
26438159
|
FGFR1 amp
|
non-small cell lung carcinoma
|
predicted - sensitive |
|
NGI-1
|
Preclinical - Cell culture |
Actionable |
In a preclinical study, NGI-1 inhibited FGFR1 phosphorylation and proliferation of a FGFR1-amplified cell line dependent on FGFR1 signaling in culture, however, did not inhibit proliferation of an FGFR1-amplified cell line not dependent on FGFR1 signaling (PMID: 27694802).
|
27694802
|
FGFR1 amp
|
lung adenocarcinoma
|
sensitive |
FGFR Inhibitor (Pan)
|
PRN1371
|
Preclinical - Pdx |
Actionable |
In a preclinical study, PRN1371 treatment resulted in 64.6% tumor growth inhibition in patient-derived xenograft models of FGFR1-amplified lung adenocarcinoma (PMID: 28978721).
|
28978721
|
FGFR1 amp
|
lung squamous cell carcinoma
|
no benefit |
FGFR Inhibitor (Pan)
|
Dovitinib
|
Phase II |
Actionable |
In a Phase II clinical trial, dovitinib treatment resulted in a objective response rate of 11.5% (3/26, all partial responses) and disease control rate of 50% (13/26), and a median progression-free survival of 2.9 months in lung squamous cell carcinoma patients with FGFR1 amplification, and FGFR1 amplification was not determined to be a predictive biomarker for sensitivity (PMID: 27315356).
|
27315356
|
FGFR1 amp
|
non-small cell lung carcinoma
|
no benefit |
|
Selumetinib
|
Preclinical - Cell culture |
Actionable |
In a preclinical study, FGFR1 amplified non-small cell lung carcinoma cells were not sensitive to Selumetinib (AZD-6244) in culture (PMID: 26438159).
|
26438159
|
FGFR1 amp
|
estrogen-receptor positive breast cancer
|
sensitive |
FGFR Inhibitor (Pan)
|
Dovitinib
|
Preclinical |
Actionable |
In a preclinical study, Dovitinib (TKI258) inhibited cell proliferation in estrogen receptor (ER)-positive breast cancer cells harboring FGFR1 amplification in culture (PMID: 22238366).
|
22238366
|