Safety and efficacy of osimertinib 160 mg daily given concurrently with a strong CYP3A4 inducer

Introduction: Osimertinib remains the standard first-line therapy for patients with advanced EGFR-mutant NSCLC, at least in part due to its improved CNS penetrance compared to earlier generation EGFR TKIs. Strong CYP3A4-inducing medications are known to reduce the effective concentration of osimerti...

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Main Authors: Mostafa Aglan, Erin Spyropoulous, Joel Oster, Paul J. Hesketh, A.J. Piper-Vallillo
Format: Article
Language:English
Published: Elsevier 2025-01-01
Series:Respiratory Medicine Case Reports
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Online Access:http://www.sciencedirect.com/science/article/pii/S221300712500036X
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author Mostafa Aglan
Erin Spyropoulous
Joel Oster
Paul J. Hesketh
A.J. Piper-Vallillo
author_facet Mostafa Aglan
Erin Spyropoulous
Joel Oster
Paul J. Hesketh
A.J. Piper-Vallillo
author_sort Mostafa Aglan
collection DOAJ
description Introduction: Osimertinib remains the standard first-line therapy for patients with advanced EGFR-mutant NSCLC, at least in part due to its improved CNS penetrance compared to earlier generation EGFR TKIs. Strong CYP3A4-inducing medications are known to reduce the effective concentration of osimertinib, prompting the recommendation to double the standard osimertinib dose from 80 to 160 mg daily. However, little is known about the real-world safety and efficacy of osimertinib given in combination with long term CYP3A4 inducer use. We detail, to our knowledge, the first reported case of a patient receiving an escalated osimertinib dosage concurrent with a potent CYP3A4 inducer. Case presentation: A 69-year-old-female with a long-standing history of a seizure disorder was diagnosed with stage IV EGFR exon 19 deletion positive lung adenocarcinoma. After a failed trial to wean the patient off phenytoin, osimertinib at a dose of 160 mg in combination with phenytoin was recommended based on existing clinical guidelines. She achieved a partial response and continues with stable disease for more than 32 months from initiation of osimertinib. Additionally, she tolerated osimertinib well with minimal side effects although with persistent dyspnea of unclear etiology. Conclusion: Our case illustrates that 160 mg of osimertinib administered concurrently with a strong CYP3A4 inducer can be given safely and with retained efficacy in treating CNS metastatic EGFR-positive non-small cell lung cancer.
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spelling doaj-art-7d450370cf9e4576a948fd17490213a42025-08-20T02:56:07ZengElsevierRespiratory Medicine Case Reports2213-00712025-01-015510220010.1016/j.rmcr.2025.102200Safety and efficacy of osimertinib 160 mg daily given concurrently with a strong CYP3A4 inducerMostafa Aglan0Erin Spyropoulous1Joel Oster2Paul J. Hesketh3A.J. Piper-Vallillo4Department of Internal Medicine, Lahey Hospital and Medical Center, 41 Mall Road, Burlington, MA, 01805, USALahey Hospital and Medical Center, 41 Mall Road, Burlington, MA, 01805, USADepartment of Neurology, Tufts Medical Center, 260 Tremont Street, Boston, MA, 02116, USADivision of Hematology and Oncology, Lahey Hospital and Medical Center, 41 Mall Road, Burlington, MA, USADivision of Hematology and Oncology, Lahey Hospital and Medical Center, 41 Mall Road, Burlington, MA, USA; Corresponding author. Lahey Hospital and Medical Center, 41 Mall Rd, Burlington, MA, USA.Introduction: Osimertinib remains the standard first-line therapy for patients with advanced EGFR-mutant NSCLC, at least in part due to its improved CNS penetrance compared to earlier generation EGFR TKIs. Strong CYP3A4-inducing medications are known to reduce the effective concentration of osimertinib, prompting the recommendation to double the standard osimertinib dose from 80 to 160 mg daily. However, little is known about the real-world safety and efficacy of osimertinib given in combination with long term CYP3A4 inducer use. We detail, to our knowledge, the first reported case of a patient receiving an escalated osimertinib dosage concurrent with a potent CYP3A4 inducer. Case presentation: A 69-year-old-female with a long-standing history of a seizure disorder was diagnosed with stage IV EGFR exon 19 deletion positive lung adenocarcinoma. After a failed trial to wean the patient off phenytoin, osimertinib at a dose of 160 mg in combination with phenytoin was recommended based on existing clinical guidelines. She achieved a partial response and continues with stable disease for more than 32 months from initiation of osimertinib. Additionally, she tolerated osimertinib well with minimal side effects although with persistent dyspnea of unclear etiology. Conclusion: Our case illustrates that 160 mg of osimertinib administered concurrently with a strong CYP3A4 inducer can be given safely and with retained efficacy in treating CNS metastatic EGFR-positive non-small cell lung cancer.http://www.sciencedirect.com/science/article/pii/S221300712500036XEGFROsimertinib160 mgAEDDrug interaction
spellingShingle Mostafa Aglan
Erin Spyropoulous
Joel Oster
Paul J. Hesketh
A.J. Piper-Vallillo
Safety and efficacy of osimertinib 160 mg daily given concurrently with a strong CYP3A4 inducer
Respiratory Medicine Case Reports
EGFR
Osimertinib
160 mg
AED
Drug interaction
title Safety and efficacy of osimertinib 160 mg daily given concurrently with a strong CYP3A4 inducer
title_full Safety and efficacy of osimertinib 160 mg daily given concurrently with a strong CYP3A4 inducer
title_fullStr Safety and efficacy of osimertinib 160 mg daily given concurrently with a strong CYP3A4 inducer
title_full_unstemmed Safety and efficacy of osimertinib 160 mg daily given concurrently with a strong CYP3A4 inducer
title_short Safety and efficacy of osimertinib 160 mg daily given concurrently with a strong CYP3A4 inducer
title_sort safety and efficacy of osimertinib 160 mg daily given concurrently with a strong cyp3a4 inducer
topic EGFR
Osimertinib
160 mg
AED
Drug interaction
url http://www.sciencedirect.com/science/article/pii/S221300712500036X
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