Fibroblast growth factor receptor 2

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

Retrieved on: 
Thursday, September 3, 2020
Tyrosine kinase receptors, Clusters of differentiation, Fibroblast growth factor receptor 2

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.

Basilea announces completion of patient enrolment into first cohort of phase 2 study FIDES-01 with derazantinib in bile duct cancer (iCCA)

Retrieved on: 
Monday, July 20, 2020
Branches of biology, Medical specialties, Tyrosine kinase receptors, Hepatology, Medicine, Fibroblast growth factor receptor 2, Cholangiocarcinoma, Bile duct, Basilea Pharmaceutica, Fibroblast growth factor

Basilea Pharmaceutica Ltd. (SIX: BSLN) announced today the completion of patient enrolment into the first cohort of the phase 2 registrational study, FIDES-01, assessing the activity of the FGFR kinase inhibitor derazantinib in patients with intrahepatic cholangiocarcinoma (iCCA), a form of bile duct cancer.

Key Points: 
  • Basilea Pharmaceutica Ltd. (SIX: BSLN) announced today the completion of patient enrolment into the first cohort of the phase 2 registrational study, FIDES-01, assessing the activity of the FGFR kinase inhibitor derazantinib in patients with intrahepatic cholangiocarcinoma (iCCA), a form of bile duct cancer.
  • This first cohort enrolled patients with iCCA expressing fusions of the fibroblast growth factor receptor 2 (FGFR2) gene and reached its target enrolment of 100 patients.
  • This cohort is assessing the activity of derazantinib in patients with FGFR2 gene mutations or amplifications, thus broadening the range of investigated FGFR2-driven tumors.
  • The first study, FIDES-01, is a registrational phase 2 study in patients with inoperable or advanced iCCA.

 FDA Approves Incyte’s Pemazyre™ (pemigatinib) as First Targeted Treatment for Adults with Previously Treated, Unresectable Locally Advanced or Metastatic Cholangiocarcinoma

Retrieved on: 
Saturday, April 18, 2020
Oncology, FDA, Health, Clinical trials, Pharmaceutical, Biotechnology, Cancer, Medicine, Clinical medicine, Tyrosine kinase receptors, Cholangiocarcinoma, Hepatology, RTT, Fibroblast growth factor receptor 2, Protein kinase inhibitors, Treatment of lung cancer, Cancer, Medicine, Clinical medicine, Tyrosine kinase receptors, Cholangiocarcinoma, Hepatology, RTT, Fibroblast growth factor receptor 2, Protein kinase inhibitors, Treatment of lung cancer

The FDA approval was based on data from the FIGHT-202 study, a multi-center, open-label, single-arm study that evaluated Pemazyre as a treatment for adults with cholangiocarcinoma.

Key Points: 
  • The FDA approval was based on data from the FIGHT-202 study, a multi-center, open-label, single-arm study that evaluated Pemazyre as a treatment for adults with cholangiocarcinoma.
  • The FDA granted Pemazyre Breakthrough Therapy designation for the treatment of patients with previously treated advanced/metastatic or unresectable FGFR2 translocated cholangiocarcinoma.
  • Additionally, the FDA granted Pemazyre Orphan Drug designation for the treatment of cholangiocarcinoma, and the New Drug Application (NDA) for Pemazyre was reviewed under the FDAs Priority Review program.
  • Pemazyre is a kinase inhibitor indicated for the treatment of adults with previously treated, unresectable locally advanced or metastatic cholangiocarcinoma with a fibroblast growth factor receptor 2 (FGFR2) fusion or other rearrangement as detected by an FDA-approved test.

Basilea reports activity of derazantinib in preclinical models of gastric cancer at ASCO Gastrointestinal Cancers Symposium

Retrieved on: 
Thursday, January 23, 2020
Tyrosine kinase receptors, Fibroblast growth factor receptor 2, Pre-clinical development, Stomach cancer, Health, Branches of biology

Basel, Switzerland, January 23, 2020 Basilea Pharmaceutica Ltd. (SIX: BSLN) reported today that its oncology drug candidate derazantinib showed convincing activity in preclinical models of gastric cancer with FGFR genetic aberrations.

Key Points: 
  • Basel, Switzerland, January 23, 2020 Basilea Pharmaceutica Ltd. (SIX: BSLN) reported today that its oncology drug candidate derazantinib showed convincing activity in preclinical models of gastric cancer with FGFR genetic aberrations.
  • Dr. Laurenz Kellenberger, Basileas Chief Scientific Officer, said: The preclinical data presented at the ASCO symposium show that derazantinib has the potential to provide clinical benefit in gastric cancer with FGFR genetic aberrations.
  • The preclinical data were generated in patient-derived mouse models of biliary, gastric and colorectal cancer with FGFR gene fusions, mutations and amplifications.
  • Derazantinib was well tolerated and led to strong responses in several animal models, particularly in gastric cancer models with FGFR2 gene fusions, where responses included complete tumor regression.

Innovent Biologics Announces FDA Acceptance of NDA for Pemigatinib in Patients with Previously Treated, Locally Advanced or Metastatic Cholangiocarcinoma with FGFR2 Fusions or Rearrangements

Retrieved on: 
Monday, December 2, 2019
Cancer, Medicine, Clinical medicine, Hepatology, Tyrosine kinase receptors, Cholangiocarcinoma, RTT, Fibroblast growth factor receptor 2

The NDA submission is based on data from Incyte's FIGHT-202 study evaluating pemigatinib as a treatment for patients with previously treated, locally advanced or metastatic cholangiocarcinoma.

Key Points: 
  • The NDA submission is based on data from Incyte's FIGHT-202 study evaluating pemigatinib as a treatment for patients with previously treated, locally advanced or metastatic cholangiocarcinoma.
  • FGFR2 fusions or rearrangements occur almost exclusively in iCCA, where they are observed in 10-16 percent of patients.
  • FIGHT-302 is a recently initiated Phase 3 study investigating pemigatinib as a first-line treatment for patients with cholangiocarcinoma with FGFR2 fusions or rearrangements.
  • The U.S. FDA has granted pemigatinib Breakthrough Therapy designation for the treatment of previously treated, advanced/metastatic or unresectable FGFR2 translocated cholangiocarcinoma.

Incyte Announces Acceptance and Priority Review of NDA for Pemigatinib as a Treatment for Patients with Cholangiocarcinoma

Retrieved on: 
Wednesday, November 27, 2019
Science, Biotechnology, Research, Pharmaceutical, Oncology, Health, FDA, Clinical trials, Health, Medical specialties, Medicine, Tyrosine kinase receptors, Cholangiocarcinoma, Hepatology, RTT, Priority review, Fibroblast growth factor receptor 2, Food and Drug Administration, FIGHT-202, FIGHT, FGFR and Pemigatinib, Incyte

The NDA submission is based on data from the FIGHT-202 study evaluating pemigatinib as a treatment for patients with previously treated, locally advanced or metastatic cholangiocarcinoma.

Key Points: 
  • The NDA submission is based on data from the FIGHT-202 study evaluating pemigatinib as a treatment for patients with previously treated, locally advanced or metastatic cholangiocarcinoma.
  • The FDA grants Priority Review to medicines that may offer a major advance in treatment where none currently exists.
  • This designation shortens the review period to eight months compared to 12 months for Standard Review.
  • FIGHT-302 is a recently initiated Phase 3 study investigating pemigatinib as a first-line treatment for patients with cholangiocarcinoma with FGFR2 fusions or rearrangements.

eFFECTOR Therapeutics Initiates Phase 1/2 Safety and Efficacy Study of Zotatifin (eFT226) in Patients with Advanced Solid Tumor Malignancies

Retrieved on: 
Tuesday, November 5, 2019
Tyrosine kinase receptors, Branches of biology, Cancer, Medicine, Fibroblast growth factor receptor 1, KRAS, Tyrosine kinase, Fibroblast growth factor receptor 2, ErbB, ERBB3, Pancreatic cancer, HER2/neu

The study will enroll patients with activating mutations, amplifications or fusions in HER2, ERBB3, FGFR1, or FGFR2 receptor tyrosine kinases, or any KRAS mutation subtype.

Key Points: 
  • The study will enroll patients with activating mutations, amplifications or fusions in HER2, ERBB3, FGFR1, or FGFR2 receptor tyrosine kinases, or any KRAS mutation subtype.
  • It will also include pancreatic adenocarcinoma with no molecular typing since the large majority of those patients harbor a KRAS mutation.
  • Zotatifin will be administered as a monotherapy in weekly intravenous infusions in subjects with advanced solid tumor malignancies.
  • The drug is currently being evaluated in a Phase 1/2 clinical trial in patients with solid tumors.

Basilea reports at ESMO meeting that drug candidate derazantinib showed clinical benefit in intrahepatic cholangiocarcinoma (iCCA) patients with various FGFR2 genetic aberrations

Retrieved on: 
Monday, September 30, 2019
Tyrosine kinase receptors, Fibroblast growth factor receptor 2, Organ systems, Syndromes, Medical specialties, Beare–Stevenson cutis gyrata syndrome

The analysis shows that derazantinib provided clinically meaningful anti-tumor activity, not only in iCCA patients with FGFR2 gene fusions, but also in iCCA patients with FGFR2 gene mutations and amplifications.

Key Points: 
  • The analysis shows that derazantinib provided clinically meaningful anti-tumor activity, not only in iCCA patients with FGFR2 gene fusions, but also in iCCA patients with FGFR2 gene mutations and amplifications.
  • Activity of derazantinib in patients with FGFR2 gene mutations and amplifications could be an important differentiation factor in this indication and would address an important unmet medical need."
  • DCRs were 67% for patients with FGFR2 gene mutations or amplifications compared to 83% for patients with FGFR2 gene fusions.
  • ICCA patients without any FGFR2 genetic aberration did not respond to treatment with derazantinib, which is consistent with previous reports.

Incyte Announces Positive Updated Results from Phase 2 Trial of Pemigatinib in Patients with Previously Treated, Advanced Cholangiocarcinoma

Retrieved on: 
Friday, September 27, 2019
Biotechnology, General Health, Health, Pharmaceutical, Oncology, Research, Science, Clinical trials, Hepatology, Medicine, RTT, Infectious causes of cancer, Tyrosine kinase receptors, Cholangiocarcinoma, Clinical medicine, Fibroblast growth factor receptor 2, Health, Biotechnology, General Health, Health, Pharmaceutical, Oncology, Research, Science, Clinical trials, Hepatology, Medicine, RTT, Infectious causes of cancer, Tyrosine kinase receptors, Cholangiocarcinoma, Clinical medicine, Fibroblast growth factor receptor 2, Health, FIGHT-202, FIGHT, FGFR and Pemigatinib, Incyte

The safety analysis, including 146 patients, showed that pemigatinib was generally well tolerated.

Key Points: 
  • The safety analysis, including 146 patients, showed that pemigatinib was generally well tolerated.
  • Serious retinal detachment was observed in 4 percent of patients (Grade 3, 1 percent) with none of the cases resulting in clinical sequelae.
  • FIGHT-302 is a recently initiated Phase 3 study investigating pemigatinib as a first-line treatment for patients with cholangiocarcinoma with FGFR2 fusions or rearrangements.
  • The U.S. Food and Drug Administration (FDA) has granted pemigatinib Breakthrough Therapy designation for the treatment of previously treated, advanced/metastatic or unresectable FGFR2 translocated cholangiocarcinoma.

Incyte Announces First Patient Treated in Phase 3 Clinical Trial of Pemigatinib as a First-Line Therapy for Cholangiocarcinoma

Retrieved on: 
Tuesday, June 4, 2019
Health, Biotechnology, Clinical trials, Oncology, Pharmaceutical, Research, Other Science, Science, Hepatology, Cancer, Medical specialties, Medicine, RTT, Cholangiocarcinoma, Tyrosine kinase receptors, Fibroblast growth factor receptor 2, Erdafitinib

It is most common in those over 70 years old and is more common in men than women.

Key Points: 
  • It is most common in those over 70 years old and is more common in men than women.
  • FGFR2 fusion genes are drivers of the disease occurring almost exclusively in patients with intrahepatic cholangiocarcinoma (iCCA), a subset of the disease.
  • The incidence of cholangiocarcinoma with FGFR2 rearrangements is increasing and is currently estimated at 2,000-3,000 patients in the U.S., Europe and Japan.
  • The U.S. Food and Drug Administration (FDA) has granted pemigatinib Breakthrough Therapy designation for the second-line treatment of cholangiocarcinoma.