News - FGFR3 Y375C - LARVOL VERI

12ms

NCCH2006/MK010 Trial (FORTUNE Trial) (clinicaltrials.gov)

P2, N=46, Active, not recruiting, National Cancer Center, Japan | Recruiting --> Active, not recruiting

12 months ago

Enrollment closed • Metastases

EGFR (Epidermal growth factor receptor) • KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • ALK (Anaplastic lymphoma kinase) • NRAS (Neuroblastoma RAS viral oncogene homolog) • FGFR2 (Fibroblast growth factor receptor 2) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS) • FGFR4 (Fibroblast growth factor receptor 4) • NTRK (Neurotrophic receptor tyrosine kinase)

EGFR mutation • BRAF mutation • NRAS mutation • BRAF V600 • FGFR1 amplification • FGFR2 mutation • FGFR2 fusion • FGFR mutation • FGFR2 N549K • FGFR1 fusion • FGFR3 fusion • FGFR2 P253R • FGFR2 K310R • FGFR3 Y375C • FGFR2 C382R • FGFR2 N549D • FGFR2 N549H • FGFR2 S252W • FGFR2 Y375C • FGFR3 G380R • FGFR3 K650E • FGFR2 W290C

Tasfygo (tasurgratinib)

1year

Efficacy of futibatinib, an irreversible fibroblast growth factor receptor inhibitor, in FGFR-altered breast cancer. (PubMed, Sci Rep)

Per institutional and public databases, FGFR2 mutations and amplifications had a population frequency of 1.1%-2.6% and 1.5%-2.5%, respectively, in breast cancer patients. FGFR2 alterations in breast cancer may represent infrequent but highly promising targets for futibatinib.

1 year ago

Journal

FGFR2 (Fibroblast growth factor receptor 2) • FGFR3 (Fibroblast growth factor receptor 3)

FGFR2 mutation • FGFR2 amplification • FGFR2 overexpression • FGFR1 expression • FGFR2 expression • FGFR3 Y375C • FGFR2 Y375C

Lytgobi (futibatinib)

1year

Analysis of several common APOBEC-type mutations in bladder tumors suggests links to viral infection. (PubMed, Cancer Prev Res (Phila))

BKPyV tumor positivity in the NMIBC subset with FGFR3- or PIK3CA-mutated tumors was also associated with a higher risk of progression to MIBC (p=0.019). In conclusion, our results support smoking and BKPyV infection as risk factors contributing to bladder tumorigenesis in the general patient population through distinct molecular mechanisms.

1 year ago

Journal

PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • FGFR3 (Fibroblast growth factor receptor 3)

PIK3CA mutation • PIK3CA E545K • FGFR3 mutation • FGFR3 S249C • PIK3CA E542K • PIK3CA E545 • PIK3CA E542 • FGFR3 Y375C

over1year

Feasibility of ex vivo drug sensitivity testing in urothelial cancer: EVITA trial (ESMO 2023)

For ex vivo drug testing, tumor clusters were isolated, seeded, and exposed to single-agent chemotherapy: carboplatin, cisplatin, gemcitabine and targeted therapy (erdafitinib). A correlation with clinical response to chemotherapy could not be established due to a lack of successfully screened patients with matching clinical chemotherapy treatment. For NMIBC, however, differential ex vivo sensitivity to gemcitabine, and a preliminary correlation for ex vivo erdafitinib sensitivity and FGFR3 mutation status offers a potential solution to select NMIBC patients for effective (novel) treatment options.

over 1 year ago

Preclinical

PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • FGFR3 (Fibroblast growth factor receptor 3) • TERT (Telomerase Reverse Transcriptase)

PIK3CA mutation • FGFR3 mutation • TERT mutation • FGFR3 Y375C • FGFR wild-type

cisplatin • carboplatin • gemcitabine • Balversa (erdafitinib)

2years

Evaluation of a cytology-molecular co-test in urine of patients with non-muscle invasive urothelial cancer (EMUC 2022)

Thus, incorporation of urine molecular testing in THIN PREP material could enhance the diagnostic value of cytological assessment in clarification of atypical and suspicious cytological findings. This strategy, if prospectively validated, could potentially enable a more effective and timely management of these patients.

2 years ago

Clinical

FGFR3 (Fibroblast growth factor receptor 3) • TERT (Telomerase Reverse Transcriptase)

FGFR3 mutation • FGFR3 S249C • TERT mutation • TERT promoter mutation • FGFR3 Y375C

3years

Efficacy of futibatinib, an irreversible fibroblast growth factor receptor (FGFR) inhibitor, in breast cancer models with FGFR alterations (SABCS 2021)

Futibatinib had single agent activity of selected breast cancer PDX models. FGFR2 activating mutations and amplification may represent rare but promising therapeutic targets to FGFR inhibition.

3 years ago

Clinical • Preclinical

FGFR2 (Fibroblast growth factor receptor 2) • FGFR3 (Fibroblast growth factor receptor 3) • FGFR (Fibroblast Growth Factor Receptor) • FGFR4 (Fibroblast growth factor receptor 4) • BICC1 (BicC Family RNA Binding Protein 1)

FGFR2 mutation • FGFR2 fusion • FGFR2 amplification • FGFR2-BICC1 fusion • FGFR1 expression • FGFR2 expression • FGFR2b expression • FGFR4 expression • FGFR3 Y375C • FGFR2 Y375C

Lytgobi (futibatinib)

3years

The frequency and somatic mutation landscape of Fibroblast growth factor receptor ( FGFR ) alterations in breast cancer (SABCS 2021)

High-level FGFR amplifications are observed in >11% of breast cancers, especially the ER+/HER2- subtype, while mutations/fusions are rare. These data support the ongoing studies evaluating targeted therapies for FGFR amplified ER + breast cancer. Correlations with clinical information (MC cohort) and associations with actionable alterations are ongoing and may inform potential combination strategies.

3 years ago

Tumor Mutational Burden • BRCA Biomarker • MSi-H Biomarker

HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • TP53 (Tumor protein P53) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • TMB (Tumor Mutational Burden) • BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • MSI (Microsatellite instability) • FGFR2 (Fibroblast growth factor receptor 2) • PTEN (Phosphatase and tensin homolog) • FGFR3 (Fibroblast growth factor receptor 3) • FGFR1 (Fibroblast growth factor receptor 1) • FGFR (Fibroblast Growth Factor Receptor) • CCND1 (Cyclin D1) • TACC3 (Transforming acidic coiled-coil containing protein 3) • FGFR4 (Fibroblast growth factor receptor 4) • CDK4 (Cyclin-dependent kinase 4) • PIK3R1 (Phosphoinositide-3-Kinase Regulatory Subunit 1) • BAG4 (BAG Cochaperone 4) • EMSY (EMSY Transcriptional Repressor BRCA2 Interacting) • TACC1 (Transforming Acidic Coiled-Coil Containing Protein 1)

MSI-H/dMMR • HER-2 amplification • HER-2 negative • HER-2 mutation • FGFR1 amplification • FGFR2 mutation • FGFR2 fusion • FGFR mutation • FGFR fusion • FGFR2 N549K • FGFR1 fusion • FGFR3 fusion • FGFR3 Y375C • FGFR2 Y375C

4years

[VIRTUAL] Identification of FGFR Mutations in Chinese Lung Cancer Patients by Next-Generation Sequencing (IASLC-WCLC 2020)

Food and Drug Administration (FDA) has approved Balversa (erdafitinib) for metastatic bladder cancer treatment, and more FGFR inhibitors are currently being evaluated clinically in many other cancer types, including lung cancer...Hopefully, more patients with other FGFR mutations may benefit from FGFR inhibitors as well, which needs further clinical investigation. Meanwhile, the exclusive relationship between druggable FGFR mutations and other actionable variations in lung cancers defines a unique molecular subtype, extending the number of patients who can benefit from targeted therapy.

4 years ago

Clinical • Next-generation sequencing

EGFR (Epidermal growth factor receptor) • BRAF (B-raf proto-oncogene) • ALK (Anaplastic lymphoma kinase) • FGFR2 (Fibroblast growth factor receptor 2) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS) • NTRK1 (Neurotrophic tyrosine kinase, receptor, type 1) • NTRK3 (Neurotrophic tyrosine kinase, receptor, type 3) • FGFR3 (Fibroblast growth factor receptor 3) • FGFR1 (Fibroblast growth factor receptor 1) • FGFR (Fibroblast Growth Factor Receptor) • FGFR4 (Fibroblast growth factor receptor 4)

BRAF V600E • EGFR mutation • BRAF V600 • FGFR1 amplification • FGFR2 mutation • FGFR2 fusion • ALK fusion • FGFR mutation • FGFR1 mutation • ROS1 fusion • FGFR3 S249C • FGFR3 Y373C • FGFR3 fusion • FGFR3 G370C • FGFR3 R248C • NTRK1 mutation • FGFR3 Y375C • FGFR2 S252W

Balversa (erdafitinib)

over4years

A novel ultra-sensitive method for the detection of FGFR3 mutations in urine of bladder cancer patients - Design of the Urodiag® PCR kit for surveillance of patients with non-muscle-invasive bladder cancer (NMIBC). (PubMed, BMC Med Genet)

"We developed and clinically validated the MASO-PCR assay, generating cost-effective, simple, fast and clinically applicable assay for the detection of FGFR3 mutations in urine. We also designed the Urodiag® PCR Kit, which includes the MASO-PCR and QM-MSPCR assays. Adapted to routine clinical laboratory (simplicity, accuracy), the kit will be a great help to urologists for recurrence surveillance in patients at low-, intermediate- and high-risk NMIBC. Reducing the number of unnecessary cystoscopies, it will have extremely beneficial effects for patients (painless) and for the healthcare systems (low cost)."

over 4 years ago

Journal • Clinical

FGFR3 (Fibroblast growth factor receptor 3) • SLIT2 (Slit Guidance Ligand 2)

FGFR3 mutation • FGFR3 S249C • FGFR3 R248C • FGFR3 Y375C

Urodiag®