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
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
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
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
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
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
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
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...
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
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 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 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...
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
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 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
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...
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
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 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 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...
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
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...

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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries
NCT04040725 Phase II Rogaratinib Rogaratinib for BCG Refractory High Risk Non-Muscle Invasive Bladder Cancer With FGFR1/2 Overexpression Withdrawn 0
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
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
NCT01976741 Phase I Rogaratinib Phase I Dose Escalation Pan-FGFR (Fibroblast Growth Factor Receptor) Inhibitor Completed USA | FRA | ESP | DEU 3
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


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