Degradation-Driven Implications for the Pharmacology and Risk Profile ofFexofenadine

Introduction/Objective: Introduction/Objective: Understanding a drug’s degradation profile is essential for ensuring its stability, efficacy, and safety. This minireview summarizes the pharmacological characteristics of fexofenadine and predicts its degradation pathways, with an emphasis on quality assessment and regulatory implications. Methods: To build on the outlined objectives, a systematic search was conducted in PubMed and Scopus using keywords related to fexofenadine’s pharmacology, chemical structure, and degradation mechanisms. Of 368 records identified, 52 studies met the inclusion criteria and were critically analyzed. Results: Following this analysis, it was found that fexofenadine is susceptible to photolysis, hydrolysis, and N-nitrosation processes. Discussion: Fexofenadine’s vulnerabilities, which are corroborated by forced degradation studies, may compromise its stability and lead to nitrosamine formation. Notably, the drug is primarily excreted unchanged, indicating minimal metabolic transformation. Predicted metabolic routes include aromatic hydroxylation, Ndealkylation, and piperidine ring opening; however, its high polarity favors renal elimination. Phase II conjugation, particularly glucuronidation, may further contribute to its clearance and the absence of detectable metabolites. In addition, nanoformulations have been shown to enhance fexofenadine’s stability, bioavailability, and therapeutic performance Conclusion: Further investigation into fexofenadine’s stability is critical for optimizing formulation strategies, guiding quality control, and mitigating degradation-related risks. Theoretical and experimental insights can strengthen regulatory compliance and ensure sustained drug safety.

Authors

Institutions

Publication Details

Journal
Current Pharmaceutical Design
Published
2026-04-01
DOI
https://doi.org/10.2174/0113816128417080260218095837
Primary Topic
Analytical Methods in Pharmaceuticals
Type
article
Field-Weighted Citation Impact
0.00
Controls
|||
ALL TIME
JAN
FEB
MAR
APR
MAY
JUN
JUL
AUG
SEP
OCT
article

Degradation-Driven Implications for the Pharmacology and Risk Profile ofFexofenadine

Caroline Vitória de Lima Moreira, Camila Carlos Prado, Alessandro de Carvalho Cruz, James Oluwagbamigbe Fajemiroye et al.
Current Pharmaceutical Design
Analytical Methods in Pharmaceuticals
article

Degradation-Driven Implications for the Pharmacology and Risk Profile ofFexofenadine

Caroline Vitória de Lima Moreira, Camila Carlos Prado, Alessandro de Carvalho Cruz, James Oluwagbamigbe Fajemiroye, Gustavo Rodrigues Pedrino, John Ihayi Ogbu, Alberto Souza Sá Filho, Edeildo Ferreira da Silva-Júnior, Manuele Figueiredo da Silva
article en

Abstract

Introduction/Objective: Introduction/Objective: Understanding a drug’s degradation profile is essential for ensuring its stability, efficacy, and safety. This minireview summarizes the pharmacological characteristics of fexofenadine and predicts its degradation pathways, with an emphasis on quality assessment and regulatory implications. Methods: To build on the outlined objectives, a systematic search was conducted in PubMed and Scopus using keywords related to fexofenadine’s pharmacology, chemical structure, and degradation mechanisms. Of 368 records identified, 52 studies met the inclusion criteria and were critically analyzed. Results: Following this analysis, it was found that fexofenadine is susceptible to photolysis, hydrolysis, and N-nitrosation processes. Discussion: Fexofenadine’s vulnerabilities, which are corroborated by forced degradation studies, may compromise its stability and lead to nitrosamine formation. Notably, the drug is primarily excreted unchanged, indicating minimal metabolic transformation. Predicted metabolic routes include aromatic hydroxylation, Ndealkylation, and piperidine ring opening; however, its high polarity favors renal elimination. Phase II conjugation, particularly glucuronidation, may further contribute to its clearance and the absence of detectable metabolites. In addition, nanoformulations have been shown to enhance fexofenadine’s stability, bioavailability, and therapeutic performance Conclusion: Further investigation into fexofenadine’s stability is critical for optimizing formulation strategies, guiding quality control, and mitigating degradation-related risks. Theoretical and experimental insights can strengthen regulatory compliance and ensure sustained drug safety.

Current Pharmaceutical DesignVol. 32
Universidade Evangelica de Goiás (BR), Universidade Estadual de Goiás (BR), Fundação de Apoio a Pesquisa do Estado de Goiás (BR), Universidade Federal de Goiás (BR), Universidade Federal de Alagoas (BR)
Openalex Percentile: Top 27%
Analytical Methods in Pharmaceuticals
AI Navigator

Ask Laika to Summarize, Analyze, and Connect papers live on the map.

Summarize Papers & Methodologies

Extract key findings, datasets, and comparative methods across publications.

Benchmark Rankings & Visual Analytics

Rank top research institutions, authors, funders, topics, and journals by Field-Weighted Citation Impact (FWCI) and paper volume with instant charts.

Connect Distant Disciplines

Bridge topological clusters on the map to find hidden collaborative intersections.