Description
Erdafitinib is an oral pan-FGFR (1-4) inhibitor with has demonstrated promising activity in patients with metastatic or unresectable UC and other histologies (eg, cholangiocarcinoma) with FGFR alterations. It is used in the therapy of locally advanced, unresectable or metastatic urothelial carcinoma. Erdafitinib has been associated with a high rate of serum enzyme elevations during therapy, but has not been linked to cases of clinically apparent acute liver injury.
History
In early April of 2019, the US FDA approved Janssen Pharmaceutical Companies' brand name Balversa (erdafitinib) as the first-ever fibroblast growth factor receptor (FGFR) kinase inhibitor indicated for patients with locally advanced or metastatic urothelial carcinoma, with susceptible FGFR3 or FGFR2 genetic alterations, that has progressed during or following platinum-containing chemotherapy, including within 12 months of neoadjuvant or adjuvant platinum-containing chemotherapy. At the same time, the FDA also approved the therascreen FGFR RGQ RT-PCR Kit (Qiagen) for utilization as a companion diagnostic with erdafitinib for selecting patients for the indicated therapy.
Uses
Erdafitinib is a fibroblast growth factor receptor inhibitor.
General Description
Class: receptor tyrosine kinase;
Treatment: metastatic urothelial carcinoma;
Other name: JNJ-4275693;
Elimination half-life = 59 h;
Protein binding = 99.8%
Biological Activity
Erdafitinib binds to and inhibits the enzymatic activity of FGFR1−4, preventing phosphorylation and cell signaling. In addition, Erdafitinib also binds to Fms-related tyrosine kinase 4 (FLT4), tyrosine-protein kinase c-KIT, and vascular endothelial growth factor receptor 2 (VEGFR-2).
Synthesis
Synthesis of Erdafitinib
target
Primary targets: Pan-FGFR
References
[1] Patent: WO2011/135376, 2011, A1. Location in patent: Page/Page column 253
