Therapy Detail
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| Therapy Name | Rogaratinib |
| Synonyms | |
| Therapy Description |
Rogaratinib (BAY 1163877) is a small molecule pan-FGFR inhibitor, which reduces downstream signaling, potentially resulting in decreased tumor cell proliferation (PMID: 27429073, PMID: 29451369, PMID: 30807645, PMID: 31405822). |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| Rogaratinib | BAY 1163877|BAY-1163877|BAY1163877 | FGFR Inhibitor (Pan) 26 | Rogaratinib (BAY 1163877) is a small molecule pan-FGFR inhibitor, which reduces downstream signaling, potentially resulting in decreased tumor cell proliferation (PMID: 27429073, PMID: 29451369, PMID: 30807645, PMID: 31405822). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| FGFR1 over exp | transitional cell carcinoma | no benefit | Rogaratinib | Phase II | Actionable | In a Phase II trial (FORT-1), Rogaratinib (BAY 1163877) treatment did not result in improved outcomes compared to chemotherapy in advanced or metastatic urothelial carcinoma patients with FGFR1 or FGFR3 overexpression, with similar median overall survival (8.3 mo vs 9.8 mo), median progression-free survival (2.7 mo vs. 3.2 mo), and objective response rate (20.7% (18/87) vs 19.3% (17/88)), failing to meet the predetermined criteria for continuation to Phase III (PMID: 36240478; NCT03410693). | 36240478 |
| FGFR1 amp FGFR1 over exp | lung cancer | sensitive | Rogaratinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, treatment with Rogaratinib (BAY 1163877) in a lung cancer cell line xenograft model with FGFR1 amplification and FGFR1 overexpression resulted in inhibition of tumor growth (PMID: 30807645). | 30807645 |
| FGFR1 amp | triple-receptor negative breast cancer | no benefit | Rogaratinib | Preclinical - Pdx | Actionable | In a preclinical study, Rogaratinib (BAY 1163877) treatment did not inhibit tumor growth in a patient-derived xenograft (PDX) model of triple-negative breast cancer with FGFR1 amplification (PMID: 34593528). | 34593528 |
| FGFR1 over exp | Advanced Solid Tumor | predicted - sensitive | Rogaratinib | Phase I | Actionable | In a Phase I trial, treatment with Rogaratinib (BAY 1163877) was well-tolerated and resulted in objective response rate (ORR) of 15% (15/100) in patients with FGFR1, FGFR2, or FGFR3-overexpressing advanced solid tumors, including urothelial cancer, head and neck squamous cell carcinoma, and non-small cell lung cancer, and led to an ORR of 67% (10/15) in patients with FGFR overexpression, but without an FGFR genetic aberration (PMID: 31405822; NCT01976741). | 31405822 |
| FGFR3 over exp | lung squamous cell carcinoma | no benefit | Rogaratinib | Phase II | Actionable | In a Phase II trial (SAKK 19/18), Rogaratinib (BAY 1163877) treatment did not meet its primary endpoint for 6-month progression-free survival (PFS) in patients with advanced lung squamous cell carcinoma with overexpression of FGFR1, FGFR2, or FGFR3, and resulted in only 6.7% (1/15) of patients achieving 6-month PFS, with no objective responses, a median PFS of 1.6 months, and a median overall survival of 3.5 months (PMID: 36099710; NCT03762122). | 36099710 |
| FGFR2 amp FGFR2 over exp | colon cancer | sensitive | Rogaratinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, a colon cancer cell line xenograft model with FGFR2 amplification and FGFR2 overexpression demonstrated antitumor efficacy when treated with Rogaratinib (BAY 1163877), with a partial response in one of eight at one dose and five of eight at a different dose (PMID: 30807645). | 30807645 |
| FGFR3 positive | lung squamous cell carcinoma | predicted - sensitive | Rogaratinib | Case Reports/Case Series | Actionable | In a Phase I trial, sensitivity to treatment with Rogaratinib (BAY 1163877) was demonstrated in patients with a variety of FGFR-expressing solid tumor types, including long lasting stable disease in a patient with FGFR3-positive lung squamous cell carcinoma (Ann Oncol 2017, Vol 28, Suppl 5, Abstract #379P; NCT01976741). | detail... |
| FGFR2 over exp | lung squamous cell carcinoma | no benefit | Rogaratinib | Phase II | Actionable | In a Phase II trial (SAKK 19/18), Rogaratinib (BAY 1163877) treatment did not meet its primary endpoint for 6-month progression-free survival (PFS) in patients with advanced lung squamous cell carcinoma with overexpression of FGFR1, FGFR2, or FGFR3, and resulted in only 6.7% (1/15) of patients achieving 6-month PFS, with no objective responses, a median PFS of 1.6 months, and a median overall survival of 3.5 months (PMID: 36099710; NCT03762122). | 36099710 |
| FGFR1 positive | hemangioma | predicted - sensitive | Rogaratinib | Case Reports/Case Series | Actionable | In a Phase I trial, sensitivity to treatment with Rogaratinib (BAY 1163877) was demonstrated in patients with a variety of FGFR-expressing solid tumor types, including long lasting stable disease with resolution of edema in a patient with FGFR1-positive hemangioendothelioma (Ann Oncol 2017, Vol 28, Suppl 5, Abstract #379P; NCT01976741). | detail... |
| FGFR3 positive | lung adenocarcinoma | predicted - sensitive | Rogaratinib | Case Reports/Case Series | Actionable | In a Phase I trial, sensitivity to treatment with Rogaratinib (BAY 1163877) was demonstrated in patients with a variety of FGFR-expressing solid tumor types, including long lasting stable disease in a patient with FGFR3-positive lung adenocarcinoma (Ann Oncol 2017, Vol 28, Suppl 5, Abstract #379P; NCT01976741). | detail... |
| FGFR3 over exp | transitional cell carcinoma | no benefit | Rogaratinib | Phase II | Actionable | In a Phase II trial (FORT-1), Rogaratinib (BAY 1163877) treatment did not result in improved outcomes compared to chemotherapy in advanced or metastatic urothelial carcinoma patients with FGFR1 or FGFR3 overexpression, with similar median overall survival (8.3 mo vs 9.8 mo), median progression-free survival (2.7 mo vs. 3.2 mo), and objective response rate (20.7% (18/87) vs 19.3% (17/88)), failing to meet the predetermined criteria for continuation to Phase III (PMID: 36240478; NCT03410693). | 36240478 |
| FGFR3 positive | head and neck squamous cell carcinoma | predicted - sensitive | Rogaratinib | Case Reports/Case Series | Actionable | In a Phase I trial, sensitivity to treatment with Rogaratinib (BAY 1163877) was demonstrated in patients with a variety of FGFR-expressing solid tumor types, including a partial response in a patient with FGFR3-positive head and neck squamous cell carcinoma (PMID: 31405822; NCT01976741). | 31405822 |
| FGFR2 positive | breast cancer | predicted - sensitive | Rogaratinib | Case Reports/Case Series | Actionable | In a Phase I trial, sensitivity to treatment with Rogaratinib (BAY 1163877) was demonstrated in patients with a variety of FGFR-expressing solid tumor types, including long lasting stable disease in a patient with FGFR2-positive breast cancer (Ann Oncol 2017, Vol 28, Suppl 5, Abstract #379P; NCT01976741). | detail... |
| FGFR3 positive | stomach cancer | predicted - sensitive | Rogaratinib | Case Reports/Case Series | Actionable | In a Phase I trial, sensitivity to treatment with Rogaratinib (BAY 1163877) was demonstrated in patients with a variety of FGFR-expressing solid tumor types, including long lasting stable disease in a patient with FGFR3-positive gastric cancer (Ann Oncol 2017, Vol 28, Suppl 5, Abstract #379P; NCT01976741). | detail... |
| FGFR1 over exp | lung squamous cell carcinoma | no benefit | Rogaratinib | Phase II | Actionable | In a Phase II trial (SAKK 19/18), Rogaratinib (BAY 1163877) treatment did not meet its primary endpoint for 6-month progression-free survival (PFS) in patients with advanced lung squamous cell carcinoma harboring overexpression of FGFR1, FGFR2, or FGFR3, and resulted in only 6.7% (1/15) of patients achieving 6-month PFS, with no objective responses, a median PFS of 1.6 months, and a median overall survival of 3.5 months (PMID: 36099710; NCT03762122). | 36099710 |
| FGFR1 positive | salivary gland adenoid cystic carcinoma | predicted - sensitive | Rogaratinib | Case Reports/Case Series | Actionable | In a Phase I trial, sensitivity to treatment with Rogaratinib (BAY 1163877) was demonstrated in patients with a variety of FGFR-expressing solid tumor types, including a partial response in a patient with FGFR1-positive adenoid cystic carcinoma of the tongue (PMID: 31405822; NCT01976741). | 31405822 |
| FGFR1 over exp | lung cancer | predicted - sensitive | Rogaratinib | Preclinical - Pdx | Actionable | In a preclinical study, a lung cancer patient-derived xenograft (PDX) model with FGFR1 overexpression demonstrated decreased tumor volume when treated with Rogaratinib (BAY 1163877) (PMID: 30807645). | 30807645 |
| FGFR3 over exp | Advanced Solid Tumor | predicted - sensitive | Rogaratinib | Phase I | Actionable | In a Phase I trial, treatment with Rogaratinib (BAY 1163877) was well-tolerated and resulted in objective response rate (ORR) of 15% (15/100) in patients with FGFR1, FGFR2, or FGFR3-overexpressing advanced solid tumors, including urothelial cancer, head and neck squamous cell carcinoma, and non-small cell lung cancer, and led to an ORR of 67% (10/15) in patients with FGFR overexpression, but without an FGFR genetic aberration (PMID: 31405822; NCT01976741). | 31405822 |
| FGFR1 over exp | colon cancer | sensitive | Rogaratinib | Preclinical | Actionable | In a preclinical study, syngeneic colon cancer mouse models with FGFR1 over expression demonstrated antitumor activity when treated with Rogaratinib (BAY 1163877), with a partial response observed in 22% (2/9) and stable disease in one (PMID: 30807645). | 30807645 |
| FGFR3 act mut FGFR3 over exp | transitional cell carcinoma | predicted - sensitive | Rogaratinib | Phase II | Actionable | In a Phase II trial (FORT-1), Rogaratinib (BAY 1163877) treatment resulted in a higher objective response rate of 52.4% (11/21) compared to 26.7% (4/15) with chemotherapy in advanced or metastatic urothelial carcinoma patients with FGFR3 overexpression and an FGFR3 alteration (including FGFR3 G370C, FGFR3 R248C, FGFR3 S249C, FGFR3 Y373C, FGFR3-TACC3v1, and FGFR3-TACC3v3) (PMID: 36240478; NCT03410693). | 36240478 |
| FGFR1 W4C FGFR1 amp | estrogen-receptor positive breast cancer | no benefit | Rogaratinib | Preclinical - Pdx | Actionable | In a preclinical study, Rogaratinib (BAY 1163877) treatment did not inhibit tumor growth in an ER-positive breast cancer patient-derived xenograft (PDX) model with FGFR1 W4C and FGFR1 amplification (PMID: 34593528). | 34593528 |
| FGFR3 over exp | head and neck squamous cell carcinoma | sensitive | Rogaratinib | Preclinical | Actionable | In a preclinical study, Rogaratinib (BAY 1163877) inhibited tumor growth in a head and neck squamous cell carcinoma xenograft model with FGFR3 overexpression (Cancer Res August 1, 2015 75:772). | detail... |
| FGFR2 over exp | Advanced Solid Tumor | predicted - sensitive | Rogaratinib | Phase I | Actionable | In a Phase I trial, treatment with Rogaratinib (BAY 1163877) was well-tolerated and resulted in objective response rate (ORR) of 15% (15/100) in patients with FGFR1, FGFR2, or FGFR3-overexpressing advanced solid tumors, including urothelial cancer, head and neck squamous cell carcinoma, and non-small cell lung cancer, and led to an ORR of 67% (10/15) in patients with FGFR overexpression, but without an FGFR genetic aberration (PMID: 31405822; NCT01976741). | 31405822 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|---|---|---|---|---|---|
| NCT03410693 | Phase II | Docetaxel Vinflunine Paclitaxel Rogaratinib | Study of Rogaratinib (BAY1163877) vs Chemotherapy in Patients With FGFR (Fibroblast Growth Factor Receptor)-Positive Locally Advanced or Metastatic Urothelial Carcinoma (FORT-1) | Completed | USA | NLD | ITA | GBR | FRA | ESP | DEU | CAN | BEL | AUT | AUS | 18 |
| NCT04040725 | Phase II | Rogaratinib | Rogaratinib for BCG Refractory High Risk Non-Muscle Invasive Bladder Cancer With FGFR1/2 Overexpression | Withdrawn | 0 | |
| NCT03088059 | Phase II | Niraparib Durvalumab + Monalizumab Methotrexate Carboplatin Rogaratinib Mitomycin C Docetaxel Afatinib Paclitaxel Durvalumab Monalizumab Palbociclib Bleomycin Gemcitabine Fluorouracil | Biomarker-based Study in R/M SCCHN (UPSTREAM) | Active, not recruiting | ITA | GBR | FRA | ESP | BEL | 0 |
| NCT01976741 | Phase I | Rogaratinib | Phase I Dose Escalation Pan-FGFR (Fibroblast Growth Factor Receptor) Inhibitor | Completed | USA | FRA | ESP | DEU | 3 |
| NCT04595747 | Phase II | Rogaratinib | Testing the Anti-cancer Drug, Rogaratinib (BAY 1163877), for Treatment of Advanced Sarcoma With Alteration in Fibroblast Growth Factor Receptor (FGFR 1-4), and in Patients With SDH-deficient Gastrointestinal Stromal Tumor (GIST) | Active, not recruiting | USA | 0 |
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