Fibroblast growth factor receptor 2

Eisai: MHLW Grants Orphan Drug Designation in Japan to Novel FGF Receptor Selective Tyrosine Kinase Inhibitor E7090

Monday, February 22, 2021 - 6:40am

In Japan, a Phase I clinical trial of E7090 was conducted, and E7090 has been designated as the target drug for the SAKIGAKE Designation System of the MHLW for the treatment of unresectable biliary tract cancer.

Key Points: 
  • In Japan, a Phase I clinical trial of E7090 was conducted, and E7090 has been designated as the target drug for the SAKIGAKE Designation System of the MHLW for the treatment of unresectable biliary tract cancer.
  • Discovered in-house by Eisai's Tsukuba Research Laboratories, E7090 is an orally available novel tyrosine kinase inhibitor that demonstrates selective inhibitory activity against fibroblast growth factor receptors (FGFR) FGFR1, FGFR2 and FGFR3.
  • et al., "Biliary tract cancer registry in Japan from 2008 to 2013", J Hepatobiliary Pancreat Sci., 2016, 23, 149-157.
  • (6) Arai Y. et al., "Fibroblast growth factor receptor 2 tyrosine kinase fusions define a unique molecular subtype of cholangiocarcinoma", Hepatology, 2014, 59, 1427-1434.

Basilea reports positive topline results from phase 2 study FIDES-01 for derazantinib in FGFR2 gene fusion-positive patients with bile duct cancer (iCCA)

Wednesday, February 10, 2021 - 6:15am

Enrolment into cohort 2 of FIDES-01 is ongoing, assessing the activity of derazantinib in iCCA patients with FGFR2 gene mutations or amplifications.

Key Points: 
  • Enrolment into cohort 2 of FIDES-01 is ongoing, assessing the activity of derazantinib in iCCA patients with FGFR2 gene mutations or amplifications.
  • The disease control rate (DCR), reflecting the proportion of patients with a partial response or with stable disease, was 72.8%.
  • The results are not yet fully mature, as 12 patients are still ongoing, including 3 patients with a partial response.
  • The first study, FIDES-01, is a phase 2 study in patients with inoperable or advanced iCCA.

Incyte Announces Positive CHMP Opinion for Pemigatinib for the Treatment of Adults With Previously Treated, Unresectable Locally Advanced or Metastatic Cholangiocarcinoma With a Fibroblast Growth Factor Receptor 2 (FGFR2) Fusion or Rearrangement

Friday, January 29, 2021 - 6:36pm

The CHMP opinion is based on data from the FIGHT-202 study evaluating the safety and efficacy of pemigatinib in adult patients with previously treated, locally advanced or metastatic cholangiocarcinoma with documented FGF/FGFR status.

Key Points: 
  • The CHMP opinion is based on data from the FIGHT-202 study evaluating the safety and efficacy of pemigatinib in adult patients with previously treated, locally advanced or metastatic cholangiocarcinoma with documented FGF/FGFR status.
  • If approved, pemigatinib will be the first targeted treatment in the EU indicated for patients with unresectable locally advanced or metastatic cholangiocarcinoma with a fibroblast growth factor receptor 2 (FGFR2) fusion or rearrangement and would be commercialized under the brand name Pemazyre.
  • Patients with cholangiocarcinoma are often diagnosed at a late or advanced stage when the prognosis is poor1,2.
  • FIGHT-302 is a Phase 3 study investigating pemigatinib as a first-line treatment for patients with cholangiocarcinoma with FGFR2 fusions or rearrangements.

Phase 2 FIGHT Trial Results Presented at ASCO GI Validate Importance of FGFR2b Overexpression and Reinforce Potential of Bemarituzumab Plus Chemotherapy as a Frontline Targeted Treatment for FGFR2b+ Gastric and GEJ Cancers

Friday, January 15, 2021 - 11:55am

Stomatitis (31.6% vs 13.0%) and elevated transaminases (34.2% vs 19.5%) were also more common in the bemarituzumab arm.

Key Points: 
  • Stomatitis (31.6% vs 13.0%) and elevated transaminases (34.2% vs 19.5%) were also more common in the bemarituzumab arm.
  • Ocular events are common in therapies targeting FGFR and were also reported in the FIGHT trial.
  • To participate in the conference call, please dial (877) 878-2269 (domestic) or (253) 237-1188 (international) and refer to conference ID: 2063209.
  • Bemarituzumab is being developed in gastric and GEJ cancer as a targeted therapy for tumors that overexpress FGFR2b.

SEngine Precision Medicine Presents Data Summarizing Predictive Value of PARIS® Test in Breast Cancer Patients at 2020 San Antonio Breast Cancer Symposium

Wednesday, December 9, 2020 - 2:00pm

SEATTLE, Dec. 09, 2020 (GLOBE NEWSWIRE) -- SEngine Precision Medicine , a precision oncology company revolutionizing cancer therapies by pre-testing drugs on patient-derivedtumor organoids, today presented data from a study summarizing the predictive value of the PARIS Test in breast cancer tumors as a poster session (PS04/01) at the 2020 San Antonio Breast Cancer Symposium, taking place virtually from December 8-11, 2020.

Key Points: 
  • SEATTLE, Dec. 09, 2020 (GLOBE NEWSWIRE) -- SEngine Precision Medicine , a precision oncology company revolutionizing cancer therapies by pre-testing drugs on patient-derivedtumor organoids, today presented data from a study summarizing the predictive value of the PARIS Test in breast cancer tumors as a poster session (PS04/01) at the 2020 San Antonio Breast Cancer Symposium, taking place virtually from December 8-11, 2020.
  • This study highlighted the utility of the PARIS Test, a CLIA certified functional drug sensitivity assay, to support clinical decision making in heterogeneous disease such as breast cancer.
  • Showed high genomic concordance between known actionable biomarkers, such as PIK3CA and FGFR1/FGFR2, and PARIS Test organoid drug sensitivity.
  • This commitment is exemplified by this exciting data utilizing our PARIS Test across the breast cancer spectrum that showed a very strong predictive value between PARIS Test drug responses and clinical benefit.

LianBio Announces Clearance to Initiate in China the Phase 2a Trial of Infigratinib in Patients with Locally Advanced or Metastatic Gastric Cancer or Gastroesophageal Junction Adenocarcinoma with FGFR2 Gene Amplification

Tuesday, December 1, 2020 - 12:00pm

The Phase 2a trial is a multicenter, single-arm study designed to explore and evaluate the pharmacokinetic profile, efficacy and safety of infigratinib in patients with locally advanced or metastatic gastric cancer or gastroesophageal junction adenocarcinoma with FGFR2 gene amplification.

Key Points: 
  • The Phase 2a trial is a multicenter, single-arm study designed to explore and evaluate the pharmacokinetic profile, efficacy and safety of infigratinib in patients with locally advanced or metastatic gastric cancer or gastroesophageal junction adenocarcinoma with FGFR2 gene amplification.
  • Infigratinib is also currently under Phase 3 global development by LianBio and BridgeBio for patients with FGFR2 fusion positive cholangiocarcinoma.
  • Gastric cancer is the third most common cancer in China, causing approximately 300,000 deaths every year.
  • This clearance by the China NMPA to conduct the Phase 2a trial of infigratinib in gastric cancer will enable LianBio to work towards addressing the significant unmet medical need for this growing patient population.

LianBio Announces Clearance to Initiate the Phase 3 PROOF Trial of Infigratinib in Patients with Locally Advanced or Metastatic Unresectable Cholangiocarcinoma with FGFR2 Gene Fusions in China

Tuesday, November 3, 2020 - 9:30pm

In a separate clinical trial investigating infigratinib for patients with FGFR2-fusion positive cholangiocarcinoma who had progressed on gemcitabine-based therapy, infigratinib demonstrated an overall response rate of 27% [1].

Key Points: 
  • In a separate clinical trial investigating infigratinib for patients with FGFR2-fusion positive cholangiocarcinoma who had progressed on gemcitabine-based therapy, infigratinib demonstrated an overall response rate of 27% [1].
  • The Phase 3 PROOF trial is a multicenter, randomized and controlled study designed to evaluate the pharmacokinetic profile, efficacy, and safety of infigratinib in patients with locally advanced or metastatic unresectable cholangiocarcinoma with FGFR2 gene fusions.
  • This clearance by the China NMPA highlights the efficiency of LianBios operational model to bring cutting-edge technology to China, said Dr. Bing Li, Chief Executive Officer of LianBio.
  • A phase II study of infigratinib (BGJ398), an FGFR-selective tyrosine kinase inhibitor (TKI), in patients with previously-treated advanced cholangiocarcinoma containing FGFR2 fusions; ESMO 2018 Annual Meeting.

Basilea reports pooled efficacy data for derazantinib in iCCA patients with FGFR2 gene mutations and amplifications presented at ESMO MAP Virtual Congress 2020

Monday, October 12, 2020 - 6:15am

FGFR inhibitors, including derazantinib, have demonstrated clinical antitumor activity in patients with FGFR2 gene fusion-positive iCCA.

Key Points: 
  • FGFR inhibitors, including derazantinib, have demonstrated clinical antitumor activity in patients with FGFR2 gene fusion-positive iCCA.
  • However, to date there is limited clinical evidence for the benefit of FGFR inhibitors in iCCA patients with FGFR2 gene mutations and amplifications.
  • The data presented at the MAP congress show that derazantinib is active in this group of patients and underscore the broad therapeutic potential of derazantinib in FGFR2-positive iCCA.
  • The following e-poster was presented at the ESMO MAP Virtual Congress 2020:
    Efficacy of derazantinib in intrahepatic cholangiocarcinoma patients with FGFR2 mutations or amplifications: Pooled analysis of clinical trials and early access programs.

Taiho Oncology To Present Futibatinib (TAS-120) Data In Advanced Intrahepatic Cholangiocarcinoma at ESMO Virtual Congress 2020

Tuesday, September 15, 2020 - 1:00pm

PRINCETON, N.J., Sept.15, 2020 /PRNewswire/ -- Taiho Oncology, Inc. today announced data from three abstracts for futibatinib (TAS-120) in intrahepatic cholangiocarcinoma (iCCA) and in advanced solid tumors will be presented during the European Society for Medical Oncology (ESMO) Virtual Congress 2020 from September 19-21, 2020.

Key Points: 
  • PRINCETON, N.J., Sept.15, 2020 /PRNewswire/ -- Taiho Oncology, Inc. today announced data from three abstracts for futibatinib (TAS-120) in intrahepatic cholangiocarcinoma (iCCA) and in advanced solid tumors will be presented during the European Society for Medical Oncology (ESMO) Virtual Congress 2020 from September 19-21, 2020.
  • Key presentations include:
    Efficacy and Safety of Futibatinib in Intrahepatic Cholangiocarcinoma (iCCA) Harboring FGFR2 Fusions/Other Rearrangements: Subgroup Analyses of a Phase 2 Study (FOENIX-CCA2) (Abstract 4493).
  • The abstract for this presentation is available on the ESMO website: https://cslide.ctimeetingtech.com/esmo2020/attendee/confcal_2/presentati...
    Quality of Life (QOL) Outcomes With Futibatinib Treatment in FOENIX-CCA2, a Phase 2 Study in Patients (Pts) With Intrahepatic Cholangiocarcinoma (iCCA) Harboring FGFR2 Gene Fusions/Rearrangements (Abstract 4513).
  • In May 2018, the U.S. Food and Drug Administration Office of Orphan Drug Development granted futibatinib orphan drug status for the treatment of cholangiocarcinoma.

Relay Therapeutics Announces Dosing of First Patient in First-in-Human Clinical Trial of RLY-4008, a Highly Selective FGFR2 Inhibitor

Thursday, September 3, 2020 - 9:05pm

RLY-4008 is the only selective small molecule inhibitor of FGFR2 in clinical development.

Key Points: 
  • RLY-4008 is the only selective small molecule inhibitor of FGFR2 in clinical development.
  • We are excited to bring RLY-4008, our second targeted therapeutic, into clinical development, said Don Bergstrom, M.D., Ph.D., executive vice president of R&D of Relay Therapeutics.
  • The first-in-human trial is designed to evaluate the safety and tolerability of RLY-4008 in patients with advanced or metastatic solid tumors.
  • The trial will predominantly enroll patients with molecularly identified FGFR2 fusions, mutations and amplifications during the dose escalation phase.