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| Gene | FGFR2 |
| Variant | amp |
| Impact List | none |
| Protein Effect | no effect |
| Gene Variant Descriptions | FGFR2 amp indicates an increased number of copies of the FGFR2 gene. However, the mechanism causing the increase is unspecified. |
| Associated Drug Resistance | |
| Category Variants Paths |
| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| FGFR2 amp | colon cancer | sensitive | Fexagratinib | Preclinical - Cell culture | Actionable | In a preclinical study, AZD4547 inhibited survival of FGFR2 amplified colon cancer cells in culture (PMID: 27550940). | 27550940 |
| FGFR2 amp | endometrial cancer | sensitive | Fexagratinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, AZD4547 inhibited survival of FGFR2 amplified endometrial cancer cells in cell line xenograft models (PMID: 27550940). | 27550940 |
| FGFR2 amp | breast cancer | sensitive | Fexagratinib | Preclinical - Cell culture | Actionable | In a preclinical study, AZD4547 inhibited survival of FGFR2 amplified breast cancer cells in culture (PMID: 27550940). | 27550940 |
| FGFR2 amp | gastric adenocarcinoma | no benefit | Fexagratinib | Phase II | Actionable | In a Phase II trial (SHINE), AZD4547 treatment did not improve progression-free survival compared to Taxol (paclitaxel) (1.8 vs 3.5 months, p=0.9581) in advanced gastric adenocarcinoma patients with FGFR2 amplification (PMID: 29177434; NCT01457846). | 29177434 |
| FGFR2 amp | stomach cancer | sensitive | Fexagratinib | Phase II | Actionable | In a Phase II clinical trial, treatment with AZD4547 resulted in a 33% (3/9) response rate in patients with FGFR2-amplified gastroesophageal cancer, and high-level amplification was associated with clinical response (PMID: 27179038). | 27179038 |
| FGFR2 amp | stomach cancer | sensitive | Fexagratinib | Preclinical | Actionable | In a preclinical study, AZD4547 inhibited FGFR signaling, and decreased proliferation and induced cell-cycle arrest in gastric cancer cells with amplification and over expression of FGFR2 in culture (PMID: 22869148). | 22869148 |
| FGFR2 amp | stomach cancer | sensitive | Fexagratinib | Preclinical - Cell culture | Actionable | In a preclinical study, AZD4547 inhibited growth of a gastric cancer cell line harboring FGFR2 amplification in culture (PMID: 30045926). | 30045926 |
| FGFR2 amp | Advanced Solid Tumor | unknown | Fexagratinib | Case Reports/Case Series | Actionable | In a Phase II (MATCH) trial, AZD4547 treatment resulted in stable disease in 2 of 3 of patients with advanced solid tumors harboring FGFR2 amplification, with a 6-month progression-free survival rate of 0% (PMID: 32463741; NCT02465060). | 32463741 |
| FGFR2 amp | colon cancer | sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) reduced Myc expression, induced cell-cycle arrest, and inhibited growth of a colon cancer cell line with FGFR2 amplification in culture (PMID: 27401245). | 27401245 |
| FGFR2 amp | breast cancer | predicted - sensitive | Infigratinib | Case Reports/Case Series | Actionable | In a Phase I trial, a breast cancer patient harboring an FGFR2 amplification demonstrated stable disease when treated with Truseltiq (infigratinib) (PMID: 27870574). | 27870574 |
| FGFR2 amp | cholangiocarcinoma | sensitive | Infigratinib | Case Reports/Case Series | Actionable | In a clinical case study, treatment with Truseltiq (infigratinib) resulted in stable disease for 3.9 months in a patient with cholangiocarcinoma with amplification of FGFR2 (PMID: 34250419). | 34250419 |
| FGFR2 amp | cholangiocarcinoma | sensitive | Infigratinib | Case Reports/Case Series | Actionable | In a Phase II trial, Truseltiq (infigratinib) treatment demonstrated manageable toxicity, and resulted in a 27% tumor size reduction in a patient with advanced cholangiocarcinoma harboring FGFR2 amplification (PMID: 29182496; NCT02150967). | 29182496 |
| FGFR2 amp | myxoid liposarcoma | sensitive | Infigratinib | Preclinical | Actionable | In a preclinical study, Truseltiq (infigratinib) increased apoptosis, and inhibited cell proliferation and migration of myxoid liposarcoma cell lines harboring FGFR2 amplification in culture (PMID: 26036639). | 26036639 |
| FGFR2 amp | stomach cancer | sensitive | Infigratinib | Phase II | Actionable | In a Phase II trial (LB1001-201), Truseltiq (infigratinib) treatment in patients with advanced or metastatic gastric cancer or gastroesophageal junction adenocarcinoma with FGFR2 amplification resulted in a response rate of 25%, disease control rate of 80%, median duration of response of 3.8 months, median progression-free survival of 3.3 months, median overall survival of 8 months, with 15 of 19 patients experiencing tumor shrinkage (Ann Oncol 34 (2023): S761-S762; NCT05019794). | detail... |
| FGFR2 amp | stomach cancer | sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) inhibited growth of a gastric cancer cell line harboring FGFR2 amplification in culture (PMID: 30045926). | 30045926 |
| FGFR2 amp | stomach cancer | sensitive | Infigratinib | Preclinical | Actionable | In a preclinical study, Truseltiq (infigratinib) inhibited proliferation of gastric cancer cell lines harboring FGFR2 amplification in culture (PMID: 26036639). | 26036639 |
| FGFR2 amp | colon cancer | sensitive | Dovitinib | Preclinical | Actionable | In a preclinical study, Dovitinib (TKI258) inhibited cell proliferation in colon cancer cells harboring FGFR2 amplification in culture (PMID: 22238366). | 22238366 |
| FGFR2 amp | breast cancer | sensitive | Dovitinib | Preclinical - Pdx & cell culture | Actionable | In a preclinical study, Dovitinib (TKI258) inhibited cell growth of an FGFR2 amplified breast cancer cell line in culture and prevented tumor growth and induced tumor regression in FGFR2 amplified breast cancer patient derived xenograft (PDX) models (PMID: 23658459). | 23658459 |
| FGFR2 amp | myxoid liposarcoma | sensitive | Dovitinib | Preclinical | Actionable | In a preclinical study, Dovitinib (TKI258) increased apoptosis, inhibited cell proliferation and migration of myxoid liposarcoma cell lines harbors FGFR2 amplification in culture (PMID: 26036639). | 26036639 |
| FGFR2 amp | stomach cancer | sensitive | Dovitinib | Preclinical | Actionable | In a preclinical study, Dovitinib (TKI258) inhibited cell proliferation in gastric cancer cell lines harboring FGFR2 amplification in culture (PMID: 22238366). | 22238366 |
| FGFR2 amp | Her2-receptor positive breast cancer | sensitive | Dovitinib | Phase I | Actionable | In a Phase I trial, Dovitinib (TKI258) displayed safety and preliminary efficacy resulting in tumor regression of 28.2% and 18.5% in two patients with FGFR2 amplified Erbb2 (Her2)-receptor positive breast cancer (PMID: 23658459). | 23658459 |
| FGFR2 amp | stomach cancer | no benefit | Pictilisib | Preclinical - Cell culture | Actionable | In a preclinical study, a gastric cancer cell line harboring an FGFR2 amplification was not sensitive to Pictilisib (GDC-0941) treatment in culture (PMID: 30045926). | 30045926 |
| FGFR2 amp | stomach cancer | no benefit | MK2206 | Preclinical - Cell culture | Actionable | In a preclinical study, a gastric cancer cell line harboring an FGFR2 amplification was not sensitive to MK2206 treatment in culture (PMID: 30045926). | 30045926 |
| FGFR2 amp | colon cancer | sensitive | Nintedanib | Preclinical | Actionable | In a preclinical study, Ofev (nintedanib) inhibited growth of colon cancer cells harboring FGFR2 amplification in culture (PMID: 22238366). | 22238366 |
| FGFR2 amp | colon cancer | sensitive | Ponatinib | Preclinical | Actionable | In a preclinical study, Iclusig (ponatinib) inhibited Fgfr phosphorylation and cell proliferation in colon cancer cells harboring FGFR2 amplification in culture (PMID: 22238366). | 22238366 |
| FGFR2 amp | breast cancer | sensitive | Ponatinib | Preclinical | Actionable | In a preclinical study, Iclusig (ponatinib) inhibited Fgfr phosphorylation and cell proliferation in ER-negative breast cancer cells harboring FGFR2 amplification in culture (PMID: 22238366). | 22238366 |
| FGFR2 amp | stomach cancer | sensitive | Ponatinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Iclusig (ponatinib) inhibited proliferation of FGFR2-amplified gastric cancer cells in culture, and inhibited tumor growth in FGFR2-amplified gastric cancer cell line xenograft models (PMID: 22238366). | 22238366 |
| FGFR2 amp | colorectal cancer | predicted - sensitive | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, a colorectal cancer cell line with FGFR1 and FGFR2 amplification was sensitive to treatment with Stivarga (regorafenib), demonstrating inhibition of cell growth in culture (PMID: 33563752). | 33563752 |
| FGFR2 amp | colorectal cancer | predicted - sensitive | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Stivarga (regorafenib) inhibited Fgfr2 signaling and proliferation of FGFR2-amplified colorectal cancer cells in culture (PMID: 29573334). | 29573334 |
| FGFR2 amp | stomach cancer | sensitive | Regorafenib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Stivarga (regorafenib) inhibited Fgfr2 signaling and proliferation of FGFR2-amplified gastric cancer cell lines in culture, resulted in tumor growth inhibition in cell line xenograft models (PMID: 29573334). | 29573334 |
| FGFR2 amp | stomach cancer | sensitive | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, treatment with Stivarga (regorafenib) in gastric cancer cell lines harboring FGFR2 amplification resulted in decreased phosphorylation of Fgfr2 and Erk, and inhibition of cell growth in culture (PMID: 33563752). | 33563752 |
| FGFR2 amp | stomach carcinoma | no benefit | RO4987655 | Preclinical - Cell culture | Actionable | In a preclinical study, FGFR2 amplified gastric carcinoma cell lines were not sensitive to RO4987655 in culture (PMID: 26438159). | 26438159 |
| FGFR2 amp | colorectal adenocarcinoma | decreased response | RO4987655 | Preclinical - Cell culture | Actionable | In a preclinical study, FGFR2 amplified colorectal adenocarcinoma cells demonstrated decreased response to RO4987655 in culture (PMID: 26438159). | 26438159 |
| FGFR2 amp | stomach cancer | resistant | Selumetinib | Preclinical | Actionable | In a preclinical study, Selumetinib (AZD-6244) did not inhibit growth of gastric cancer cells with FGFR2 amplification in culture (PMID: 19755509). | 19755509 |
| FGFR2 amp | colorectal adenocarcinoma | no benefit | Selumetinib | Preclinical - Cell culture | Actionable | In a preclinical study, FGFR2 amplified colorectal adenocarcinoma cells were not sensitive to Selumetinib (AZD-6244) in culture (PMID: 26438159). | 26438159 |
| FGFR2 amp | breast cancer | no benefit | Sunitinib | Case Reports/Case Series | Actionable | In a Phase II trial (TAPUR), Sutent (sunitinib) treatment did not meet the predetermined efficacy criteria in metastatic breast cancer patients with FGFR2 amplification (n=2), FGFR2 mutation (including FGFR2 rearrangement) (n=6), or both (n=2), resulting in no objective responses or stable disease of at least 16 weeks, median progression-free survival of 8 weeks, and a median overall survival of 22 weeks (PMID: 38354330; NCT02693535). | 38354330 |
| FGFR2 amp | colon cancer | no benefit | Brivanib | Preclinical | Actionable | In a preclinical study, Brivanib (BMS-540215) did not inhibit growth of colon cancer cells harboring FGFR2 amplification in culture (PMID: 22238366). | 22238366 |
| FGFR2 amp | stomach cancer | no benefit | Brivanib | Preclinical | Actionable | In a preclinical study, Brivanib (BMS-540215) did not inhibit growth of gastric cancer cells harboring FGFR2 amplification in culture (PMID: 22238366). | 22238366 |
| FGFR2 amp | estrogen-receptor negative breast cancer | no benefit | Brivanib | Preclinical | Actionable | In a preclinical study, Brivanib (BMS-540215) did not inhibit growth of estrogen receptor (ER)-negative breast cancer cells with FGFR2 amplification in culture (PMID: 22238366). | 22238366 |
| FGFR2 amp | colon cancer | sensitive | Cediranib | Preclinical | Actionable | In a preclinical study, Cediranib (AZD-2171) inhibited growth of colon cancer cells harboring FGFR2 amplification in culture (PMID: 22238366). | 22238366 |
| FGFR2 amp | stomach cancer | sensitive | Cediranib | Preclinical - Cell culture | Actionable | In a preclinical study, Cediranib (AZD-2171) inhibited growth of a gastric cancer cell line harboring FGFR2 amplification in culture (PMID: 30045926). | 30045926 |
| FGFR2 amp | stomach cancer | sensitive | Cediranib | Preclinical | Actionable | In a preclinical study, Cediranib (AZD-2171) inhibited growth of gastric cancer cells harboring FGFR2 amplification in culture (PMID: 22238366). | 22238366 |
| FGFR2 amp | uterine cancer | predicted - sensitive | Zoligratinib | Case Reports/Case Series | Actionable | In a Phase I trial, Debio 1347 treatment resulted in a stable disease with 3.9% change of tumor size and 60% decrease of DUSP6 score in a patient with uterine cancer harboring FGFR2 amplification (PMID: 30745300; NCT01948297). | 30745300 |
| FGFR2 amp | breast cancer | sensitive | Zoligratinib | Case Reports/Case Series | Actionable | In a Phase I trial, Debio 1347 treatment resulted in a stable disease with 19.4% reduction of tumor size and 41% decrease of DUSP6 score in a patient with lung squamous cell carcinoma harboring FGFR2 amplification (PMID: 30745300; NCT01948297). | 30745300 |
| FGFR2 amp | breast cancer | sensitive | Zoligratinib | Preclinical | Actionable | In a preclinical study, Debio 1347 inhibited proliferation of breast cancer cell lines harboring FGFR2 amplification in culture (PMID: 25169980). | 25169980 |
| FGFR2 amp | stomach carcinoma | sensitive | Zoligratinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Debio 1347 inhibited tumor growth in cell line xenograft models of FGFR2 amplified gastric carcinoma (PMID: 26438159). | 26438159 |
| FGFR2 amp | colorectal cancer | sensitive | Zoligratinib | Preclinical | Actionable | In a preclinical study, Debio 1347 inhibited proliferation of colorectal cancer cell lines harboring FGFR2 amplification in culture (PMID: 25169980). | 25169980 |
| FGFR2 amp | stomach cancer | sensitive | Zoligratinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Debio 1347 inhibited proliferation of FGFR-amplified gastric cancer cells in culture and inhibited tumor growth in cell line xenograft models of gastric cancer harboring FGFR2 amplification (PMID: 25169980). | 25169980 |
| FGFR2 amp | Advanced Solid Tumor | predicted - sensitive | Zoligratinib | 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 amp | colorectal cancer | sensitive | Erdafitinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Balversa (erdafitinib) inhibited tumor growth in an FGFR2-amplified colorectal cancer cell line xenograft model (PMID: 28341788). | 28341788 |
| FGFR2 amp | stomach cancer | sensitive | Erdafitinib | Preclinical - Cell culture | Actionable | In a preclinical study, Balversa (erdafitinib) inhibited growth of gastric cancer cell lines with FGFR2 amplification in culture (PMID: 33563752). | 33563752 |
| FGFR2 amp | stomach cancer | sensitive | Erdafitinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Balversa (erdafitinib) inhibited proliferation of a gastric cancer cell line with FGFR2 amplification in culture, and inhibited tumor growth in xenograft models (PMID: 28341788). | 28341788 |
| FGFR2 amp | Advanced Solid Tumor | no benefit | Erdafitinib | Case Reports/Case Series | Actionable | In a Phase II trial (MATCH), Balversa (erdafitinib) treatment resulted in an objective response rate of 0% (0/18), median progression-free survival of 1.7 months, and median overall survival of 4.2 months in patients with advanced solid tumors with FGFR1 (n=12), FGFR2 (n=3), FGFR3 (n=2), or FGFR4 (n=1) amplification (PMID: 38603651; NCT02465060). | 38603651 |
| FGFR2 amp | breast cancer | sensitive | Futibatinib | Case Reports/Case Series | Actionable | In a Phase I trial, Lytgobi (futibatinib) treatment resulted in a partial response in a patient with breast cancer harboring FGFR2 amplification, with 37% tumor shrinkage (Annals of Oncology (2020) 31 (suppl_4): S475). | detail... |
| FGFR2 amp | breast cancer | sensitive | Futibatinib | Preclinical - Pdx | Actionable | In a preclinical study, Lytgoi (futibatinib) inhibited tumor growth and improved survival in a patient-derived xenograft (PDX) model of FGFR2-amplified breast cancer (PMID: 37980453). | 37980453 |
| FGFR2 amp | stomach cancer | predicted - sensitive | Futibatinib | Case Reports/Case Series | Actionable | In a Phase I trial, Lytgobi (futibatinib) treatment led to an overall objective response rate of 22% (2/9, 2 partial responses) and a disease control rate of 55.6% (5/9) in patients with gastric cancer harboring an FGFR2 amplification or FGFR3 rearrangement, including a progression-free survival of 4.8 months and a duration of response of 3.5 months in a patient with FGFR2 amplification (PMID: 34551969; NCT02052778). | 34551969 |
| FGFR2 amp | stomach cancer | predicted - sensitive | Futibatinib | Case Reports/Case Series | Actionable | In a Phase I trial, Lytgobi (futibatinib) treatment resulted in a partial response in 2 patients with gastric cancer harboring FGFR2 amplification, with 59% and 90% tumor shrinkage, respectively (Annals of Oncology (2020) 31 (suppl_4): S475). | detail... |
| FGFR2 amp | stomach cancer | predicted - sensitive | Futibatinib | Case Reports/Case Series | Actionable | In a Phase I trial, Lytgobi (futibatinib) treatment resulted in clinical response in a gastric cancer patient harboring FGFR2 amplification (Ann Oncol 2017, Vol 28, Suppl 5, Abstract # 372PD). | detail... |
| FGFR2 amp | stomach cancer | predicted - sensitive | Futibatinib | Preclinical - Cell culture | Actionable | In a preclinical study, Lytgobi (futibatinib) treatment inhibited growth of gastric cancer cells harboring FGFR2 amplification in culture (PMID: 33563752). | 33563752 |
| FGFR2 amp | triple-receptor negative breast cancer | predicted - sensitive | Futibatinib | Case Reports/Case Series | Actionable | In a Phase I trial, Lytgobi (futibatinib) treatment led to a partial response lasting 20.8 months and progression-free survival of 22.1 months in a triple-receptor negative breast cancer patient harboring an FGFR2 amplification (PMID: 34551969; NCT02052778). | 34551969 |
| FGFR2 amp | Advanced Solid Tumor | predicted - sensitive | Futibatinib | Phase I | Actionable | In a Phase I trial (FOENIX-101), Lytgobi (futibatinib) 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 5% (4/74) harbored FGFR2 amplification (PMID: 32622884; NCT02052778). | 32622884 |
| FGFR2 amp | stomach carcinoma | no benefit | RO5126766 | Preclinical - Cell culture | Actionable | In a preclinical study, FGFR2 amplified gastric carcinoma cell lines were not sensitive to RO5126766 in culture (PMID: 26438159). | 26438159 |
| FGFR2 amp | colorectal adenocarcinoma | predicted - sensitive | RO5126766 | Preclinical - Cell culture | Actionable | In a preclinical study, RO5126766 inhibited proliferation of FGFR2 amplified colorectal adenocarcinoma cells in culture (PMID: 26438159). | 26438159 |
| FGFR2 amp | stomach cancer | sensitive | FIIN-1 | Preclinical | Actionable | In a preclinical study, FIIN-1 inhibited Fgfr2-dependent cell proliferation of gastric cancer cell lines harboring FGFR2 amplification (PMID: 20338520). | 20338520 |
| FGFR2 amp | breast cancer | sensitive | Derazantinib | Preclinical - Cell culture | Actionable | In a preclinical study, Derazantinib (ARQ 087) inhibited growth of breast cancer cells harboring FGFR2 amplification in culture (PMID: 27627808). | 27627808 |
| FGFR2 amp | intrahepatic cholangiocarcinoma | predicted - sensitive | Derazantinib | Phase II | Actionable | In a Phase II trial (FIDES-01), Derazantinib (ARQ 087) treatment resulted in an objective response rate of 6.5%, a disease control rate of 58.1%, median progression-free survival of 8.3 months, and a median overall survival of 15.9 months in patients with intrahepatic cholangiocarcinoma harboring an FGFR2 mutation or amplification (Ann Oncol (2022) 33 (suppl_7): S19-S26; NCT03230318). | detail... |
| FGFR2 amp | stomach cancer | sensitive | Derazantinib | Preclinical - Cell culture | Actionable | In a preclinical study, Derazantinib (ARQ 087) inhibited Fgfr signaling and growth of gastric cancer cells harboring FGFR2 amplification in culture (PMID: 27627808). | 27627808 |
| FGFR2 amp | ovarian cancer | sensitive | Aprutumab ixadotin | Preclinical - Pdx | Actionable | In a preclinical study, Aprutumab ixadotin (BAY1187982) inhibited tumor growth in patient-derived xenograft models of FGFR2 amplified ovarian cancer (PMID: 27543601). | 27543601 |
| FGFR2 amp | myxoid liposarcoma | sensitive | PD173074 | Preclinical | Actionable | In a preclinical study, PD173074 increased apoptosis, inhibited cell proliferation and migration of myxoid liposarcoma cell lines harboring FGFR2 amplification in culture (PMID: 26036639). | 26036639 |
| FGFR2 amp | stomach cancer | sensitive | PD173074 | Preclinical - Cell culture | Actionable | In a preclinical study, FGFR2-amplified gastric cancer cell lines demonstrated sensitivity to PD173074 in culture, with cell lines with high-level FGFR2 amplification displaying higher sensitivity compared to cell lines with low-level amplification (PMID: 27179038). | 27179038 |
| FGFR2 amp | stomach cancer | sensitive | PD173074 | Preclinical - Cell culture | Actionable | In a preclinical study, PD173074 inhibited growth of a gastric cancer cell line harboring FGFR2 amplification in culture (PMID: 30045926). | 30045926 |
| FGFR2 amp | stomach cancer | sensitive | PD173074 | Preclinical - Cell culture | Actionable | In a preclinical study, PD173074 inhibited proliferation of a gastric cancer cell line harboring FGFR2 amplification in culture (PMID: 26036639). | 26036639 |
| FGFR2 amp | myxoid liposarcoma | sensitive | Dovitinib + Trabectedin | Preclinical | Actionable | In a preclinical study, Dovitinib (TKI258) and Yondelis (trabectedin) worked synergistically to increase apoptosis, inhibit cell proliferation and migration of myxoid liposarcoma cell lines harbors FGFR2 amplification in culture (PMID: 26036639). | 26036639 |
| FGFR2 amp | myxoid liposarcoma | sensitive | PD173074 + Trabectedin | Preclinical | Actionable | In a preclinical study, PD173074 and Yondelis (trabectedin) worked synergistically to increase apoptosis, inhibit cell proliferation and migration of myxoid liposarcoma cell lines harboring FGFR2 amplification in culture (PMID: 26036639). | 26036639 |
| FGFR2 amp | myxoid liposarcoma | sensitive | Infigratinib + Trabectedin | Preclinical | Actionable | In a preclinical study, Truseltiq (infigratinib) and Yondelis (trabectedin) worked synergistically to increase apoptosis, inhibit cell proliferation and migration of myxoid liposarcoma cell lines harboring FGFR2 amplification in culture (PMID: 26036639). | 26036639 |
| FGFR2 amp | lung non-small cell carcinoma | sensitive | PRN1371 | Preclinical - Pdx | Actionable | In a preclinical study, PRN1371 treatment resulted in 67.5% tumor growth inhibition in patient-derived xenograft models of FGFR2-amplified non-small cell lung cancer (PMID: 28978721). | 28978721 |
| FGFR2 amp | stomach carcinoma | sensitive | PRN1371 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, PRN1371 inhibited proliferation of FGFR2 amplified gastric carcinoma cells in culture and tumor growth in cell line xenograft models (PMID: 28978721). | 28978721 |
| FGFR2 amp | stomach cancer | sensitive | Pemigatinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Pemazyre (pemigatinib) inhibited viability in a gastric cancer cell line with FGFR2 amplification in culture, and inhibited tumor growth in a cell line xenograft model (PMID: 32315352). | 32315352 |
| FGFR2 amp | stomach cancer | sensitive | Infigratinib + Trametinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the addition of Mekinist (trametinib) restored sensitivity of gastric cancer cells with FGFR2 amplification to Truseltiq (infigratinib) treatment, demonstrating decreased Erk phosphorylation and reduced cell proliferation in culture and inhibition of tumor growth in cell line xenograft models (PMID: 33563752). | 33563752 |
| FGFR2 amp | Cancer of Unknown Primary | sensitive | Infigratinib + Trametinib | Preclinical - Pdx & cell culture | Actionable | In a preclinical study, the combination of Truseltiq (infigratinib) and Mekinist (trametinib) inhibited Akt and Mapk signaling, induced apoptosis, and synergistically decreased proliferation in FGFR2-amplified cell lines derived from patients with cancer of unknown primary in culture and decreased tumor volume in patient-derived xenograft (PDX) models (PMID: 39033323). | 39033323 |
| FGFR2 amp | gastric signet ring cell adenocarcinoma | sensitive | M-COPA | Preclinical - Cell culture | Actionable | In a preclinical study, treatment with M-COPA resulted in decreased Fgfr2 cell surface expression and phosphorylation and reduced growth of an FGFR2-amplified signet cell gastric cancer cell line in culture (PMID: 27197184). | 27197184 |
| FGFR2 amp | stomach cancer | predicted - sensitive | PRN1109 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, PRN1109 treatment resulted in tumor regression in gastric cancer cell line xenograft models harboring FGFR2 amplification (Eu J Cancer 2014 Vol 50, Suppl 6:157). | detail... |
| FGFR2 amp | stomach cancer | sensitive | E7090 | Case Reports/Case Series | Actionable | In a Phase I trial, treatment with E7090 demonstrated safety and was well-tolerable in patients with advanced solid tumors, and led to a partial response including a 71% decrease in diameter of the target lesion in a patient with gastric cancer previously treated with three lines of chemotherapy and harboring FGFR2 amplification (PMID: 31797489; NCT02275910). | 31797489 |
| FGFR2 amp | stomach cancer | sensitive | E7090 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, a gastric cancer cell line harboring FGFR2 amplification demonstrated decreased cell viability in culture and antitumor activity in xenograft models when treated with E7090 (PMID: 27535969). | 27535969 |
| FGFR2 amp | stomach cancer | sensitive | ODM-203 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, ODM-203 inhibited FGFR signaling and proliferation in a gastric cancer cell line with amplification of FGFR2, and inhibited tumor growth in xenograft models (PMID: 30301864). | 30301864 |
| FGFR2 amp | Advanced Solid Tumor | predicted - sensitive | Olverembatinib | Preclinical - Cell culture | Actionable | In a preclinical study, Olverembatinib (HQP1351) inhibited growth of FGFR2 amplified cell lines in culture (PMID: 34114373). | 34114373 |
| FGFR2 amp | colorectal cancer | sensitive | Zotatifin | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Zotatifin (eFT226) inhibited cell growth, and induced apoptosis in a FGFR2-amplified colorectal cancer cell line in culture, and inhibited tumor growth, and induced regression in a cell line xenograft model (Mol Cancer Ther 2019;18(12 Suppl):Abstract nr B133). | detail... |
| FGFR2 amp | prostate adenocarcinoma | predicted - sensitive | Tinengotinib | Case Reports/Case Series | Actionable | In a Phase I trial, Tinengotinib (TT-00420) treatment was well tolerated and resulted in stable disease in 53.3% (23/43) and partial response in 16.3% (7/43) of patients with advanced solid tumors, including a partial response in a patient with castration-resistant prostate adenocarcinoma with amplification of FGFR2 (PMID: 38297981; NCT03654547). | 38297981 |
| FGFR2 amp | stomach cancer | sensitive | Lirafugratinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Lirafugratinib treatment inhibited proliferation of gastric carcinoma cell lines with an FGFR2 amplification in culture, and led to tumor regression in a cell line xenograft model (PMID: 37270847). | 37270847 |
| FGFR2 amp | colorectal adenocarcinoma | sensitive | Lirafugratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Lirafugratinib inhibited proliferation of a colorectal adenocarcinoma cell line with FGFR2 amplification in culture (PMID: 37270847). | 37270847 |
| FGFR2 amp | stomach cancer | sensitive | Regorafenib + Trametinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the addition of Mekinist (trametinib) restored sensitivity of gastric cancer cells with FGFR2 amplification to Stivarga (regorafenib) treatment, demonstrating decreased Erk phosphorylation and reduced cell proliferation in culture, and in cell line xenograft models led to inhibition of tumor growth (PMID: 33563752). | 33563752 |
| FGFR2 amp | endometrial cancer | sensitive | CPL304110 | Preclinical - Cell culture | Actionable | In a preclinical study, CPL304110 inhibited viability of an FGFR2-amplified endometrial cancer cell line in culture (PMID: 38282676). | 38282676 |
| FGFR2 amp | lung non-small cell carcinoma | sensitive | CPL304110 | Preclinical - Pdx | Actionable | In a preclinical study, CPL304110 inhibited tumor growth in a patient-derived xenograft (PDX) model of FGFR2-amplified non-small cell lung cancer, however, regrowth was observed after treatment was stopped (PMID: 38282676). | 38282676 |
| FGFR2 amp | stomach carcinoma | sensitive | CPL304110 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, CPL304110 treatment inhibited downstream signaling and proliferation of a gastric carcinoma cell line harboring FGFR2 amplification in culture and inhibited tumor growth in cell line xenograft models (PMID: 33199155). | 33199155 |
| FGFR2 amp | stomach cancer | sensitive | CPL304110 | Preclinical - Pdx & cell culture | Actionable | In a preclinical study, CPL304110 inhibited Erk phosphorylation and viability in an FGFR2-amplified gastric cancer cell line in culture, inhibited growth in a cell line xenograft model, and induced tumor regression in a patient-derived xenograft (PDX) model (PMID: 38282676). | 38282676 |
| FGFR2 amp | colorectal cancer | sensitive | 3D185 | Preclinical - Cell culture | Actionable | In a preclinical study, 3D185 inhibited proliferation of a colorectal cancer cell line harboring FGFR2 amplification in culture (PMID: 31438996). | 31438996 |
| FGFR2 amp | stomach cancer | sensitive | 3D185 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, 3D185 inhibited downstream signaling and proliferation of gastric cancer cell lines harboring FGFR2 amplification in culture and induced dose-dependent tumor growth inhibition in a cell line xenograft model (PMID: 31438996). | 31438996 |
| FGFR2 amp | triple-receptor negative breast cancer | sensitive | 3D185 | Preclinical - Cell culture | Actionable | In a preclinical study, 3D185 inhibited proliferation of a triple-negative breast cancer cell line harboring FGFR2 amplification in culture (PMID: 31438996). | 31438996 |
| FGFR2 amp | stomach cancer | predicted - sensitive | 3HP-2827 | Preclinical - Pdx | Actionable | In a preclinical study, 3HP-2827 treatment demonstrated antitumor activity in a patient-derived xenograft (PDX) model of gastric cancer with FGFR2 amplification (Cancer Res (2024) 84 (6_Supplement): 1965). | detail... |