Exploring the Characterization of Erdafitinib

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Scientists from the National Institute of Pharmaceutical Education and Research (NIPER) in India used a variety of analytical techniques to characterize the medication erdafitinib. The team published their findings in a recent article in Chromatographia (1).

Erdafitinib is a type of tyrosine kinase receptor inhibitor used to treat a variety of diseases, most notably urothelial carcinoma. The study aimed to examine erdafitinib and its degradation behaviors when under different stress conditions as per the International Council for Harmonization of Technical Requirements for Pharmaceuticals for Human Use (ICH) (2). The scientists also wanted to test the compatibility with various excipients under accelerated stability conditions.

The scientists used a Phenomenex Gemini C18 column (250 × 4.6 mm; 5 μm) with 10 mM ammonium acetate (pH 4.50) buffer and methanol as mobile phase in gradient elution mode at a flow rate of 1 mL/min. Under hydrolytic, photolytic, and oxidative stress conditions, erdafitinib was found to be labile, meaning that it can change quickly and spontaneously (3). However, when exposed to accelerated stability conditions, it proved incompatible with polyethylene glycol-4000, polyvinyl pyrrolidone-K30, crospovidone, and carboxymethylcellulose. In total, eight novel degradation products and one interaction product were generated.

Two more methods were then used to analyze erdafitinib: liquid chromatography-quadrupole time-of-flight tandem mass spectrometry (LC–Q-TOF-MS/MS) and nuclear magnetic resonance (NMR) spectroscopy. LC–Q-TOF-MS/MS studies were conducted to propose the structures of degradation and interaction products formed by comparing with the fragmentation pattern of the drug, while the NMR study helped confirm the chemical structures of two degradation products (specifically DP7 and DP8).


From there, the degradation pathway of erdafitinib was laid down, and in silico toxicity and mutagenicity data was created using DEREK and Sarah software. All the while, DP1, DP4, DP5, DP6, DP7, and DP9 showed mutagenicity as an endpoint.


(1) Velip, L.; Dhiman, V.; Kushwah, B. S.; Samanthula, G. Characterization of Degradation Products and Drug–Excipient Interaction Products of Erdafitinib by LC–Q-TOF-MS/MS and NMR. Chromatographia 2023. DOI: https://doi.org/10.1007/s10337-023-04268-x

(2) ICH.Welcome to the ICH Official Website. ICH 2023. https://www.ich.org (accessed 2023-09-15)

(3) Amin, S. Medical News Today. What is labile hypertension? Medical News Today 2021. https://www.medicalnewstoday.com/articles/labile-hypertension (accessed 2023-09-15)