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Fexofenadine dosing

Phase 1

Non Small Cell Lung Cancer | Small molecule | Oncology |AstraZeneca PLC|Trials Updated: Nov 14, 2022

Fexofenadine dosing target and mechanism

Molecular targetHRH1
Target classAntagonist
ModalitySmall molecule
ChEMBLCHEMBL914

Also known as Fexofenadine tablet dosing

Success Probability

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Market & Valuation

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Trial Design

UNCONTROLLEDBiomarker
Total Trials1
Total Enrollment24

FDA Designations

No designations recorded

Fexofenadine dosing clinical trials

Fexofenadine dosing · 1 trial · 1 indication

Phase 1 1
NCT02908750Study to Assess the Effect of Osimertinib (TAGRISSO™ ) on Blood Levels of Fexofenadine in Patients With EGFRm+ NSCLCNon Small Cell Lung Cancer
COMPLETED24 Analytics
PHASE1COMPLETED
Study to Assess the Effect of Osimertinib (TAGRISSO™ ) on Blood Levels of Fexofenadine in Patients With EGFRm+ NSCLC
Non Small Cell Lung CancerUnlock trial analytics

Study Endpoints

Primary Endpoints

Fexofenadine Cmax (alone and in combination with osimertinib)
Blood samples are collected pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 24, 36, 48, 60, 72 on Day 1 in Period 1 and Day 1 and Day 39 in Period 2

To characterize the pharmacokinetics of fexofenadine by assessment of maximum plasma fexofenadine concentration.

Fexofenadine AUC (alone and in combination with osimertinib)
Blood samples are collected pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 24, 36, 48, 60, 72 on Day 1 in Period 1 and Day 1 and Day 39 in Period 2.

To characterize the pharmacokinetics of fexofenadine by assessment of area under the plasma concentration time curve from zero to infinity

Secondary Endpoints

Fexofenadine tmax (alone and in combination with osimertinib)
Blood samples are collected pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 10 24, 36, 48, 60, 72 on Day 1 in Period 1 and Day 1 and Day 39 in Period 2
Fexofenadine AUC0-t (alone and in combination with osimertinib)
Blood samples are collected pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 10 24, 36, 48, 60, 72 on Day 1 in Period 1 and Day 1 and Day 39 in Period 2
Fexofenadine CL/F (alone and in combination with osimertinib)
Blood samples are collected pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 10 24, 36, 48, 60, 72 on Day 1 in Period 1 and Day 1 and Day 39 in Period 2
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Study Design & Arms

AllocationNON_RANDOMIZED
MaskingNONE
ModelSINGLE_GROUP
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
osimertinib and fexofenadineEXPERIMENTALSequential treatments of fexofenadine alone followed by osimertinib + fexofenadine, followed by osimertinib alone, followed by osimertinib + fexofenadine

Interventions

NameTypeDescription
Fexofenadine tablet dosingDRUGFexofenadine (P-gp substrate) 120mg taken once daily on Days 1 in Treatment Period 1 and Day 1 and Day 39 in Treatment Period 2
Osimertininb tablet dosingDRUGOsimertininb 80 mg taken once daily on Day 1 and Days 4 to 41 in Treatment Period 2
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Eligibility Criteria

Age Range18 Years to 130 Years
SexALL
Healthy VolunteersNo
Study Sites7

Inclusion Criteria: * Male or female, ≥18 years * Histological or cytological confirmation diagnosis of NSCLC * Radiological documentation of disease progression while receiving previous continuous treatment with an EGFR-TKI. * Confirmation that the tumour harbours an EGFR mutation known to be asso...

Countries:FranceSouth KoreaSpain
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Competitive Landscape -Non-Small Cell Lung Cancer 544 trials (matched to "Non Small Cell Lung Cancer")

Top 20 of 90 competitors

CompanyTickerTrialsLead PhaseDrugs
Merck & Co., Inc.MRK37PHASE3Pembrolizumab, Olaparib, Sacituzumab tirumotecan, Intismeran autogene, Pembrolizumab Berahyaluronidase alfa
Revolution Medicines, Inc.RVMD9PHASE3Daraxonrasib, Zoldonrasib, Elironrasib, RMC-5127
Eli Lilly and CompanyLLY18PHASE3Selpercatinib, Pemetrexed, Abemaciclib, Olomorasib, LY3537982
AbbVie, Inc.ABBV12PHASE3Telisotuzumab vedotin, ABBV-1480, Livmoniplimab, Budigalimab, Telisotuzumab Adizutecan
AstraZeneca PLCAZN68PHASE3Datopotamab deruxtecan, Durvalumab, Oleclumab, Monalizumab, Tremelimumab
Gilead Sciences, Inc.GILD7PHASE3Sacituzumab govitecan, Zimberelimab, Domvanalimab, Etrumadenant, TUB-040- Dose escalation
Bristol-Myers Squibb CompanyBMY24PHASE3Repotrectinib, Nivolumab, Pumitamig, Relatlimab, Adagrasib
Johnson & JohnsonJNJ19PHASE3Lazertinib, Amivantamab, JNJ-90301900, JNJ-86974680, Cetrelimab
BioNTech SE Sponsored ADRBNTX7PHASE3Gotistobart, Pumitamig, BNT326, BNT116, BNT324
Pfizer Inc.PFE20PHASE3Lorlatinib, Crizotinib, Avelumab, Talazoparib, Axitinib
ArriVent BioPharma, Inc.AVBP9PHASE3Firmonertinib
Amgen Inc.AMGN4PHASE3ABP 234, Sotorasib, Anvumetostat
Novartis AG Sponsored ADRNVS11PHASE3Opnurasib, TNO155, DKY709, Spartalizumab, KFA115
GSK plc Sponsored ADRGSK3PHASE3Dostarlimab, Belrestotug, Nelistotug, Cobolimab
Summit Therapeutics IncSMMT2PHASE3Ivonescimab
Nuvation Bio, Inc. Class ANUVB4PHASE3Taletrectinib
Genmab A/S Sponsored ADRGMAB4PHASE3Acasunlimab, Rina-S, GEN1042
Regeneron Pharmaceuticals, Inc.REGN7PHASE2Cemiplimab, Marlotamig, Fianlimab, REGN5093
Nuvalent, Inc. Class ANUVL1PHASE3Neladalkib
BeOne Medicines Ltd. Sponsored ADRONC7PHASE3Tislelizumab, BGB-A445, LBL-007, BGB-15025, BGB-43395
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Frequently asked questions about Fexofenadine dosing

What is Fexofenadine dosing?

Fexofenadine dosing refers to the administration of fexofenadine, an HRH1 antagonist small molecule. In this context, it was studied as a probe substrate to assess drug-drug interactions in patients with EGFR-mutant non-small cell lung cancer. It is also known as fexofenadine tablet dosing.

What does Fexofenadine dosing target?

Fexofenadine dosing targets HRH1, the histamine H1 receptor, acting as an antagonist. This mechanism is well established for fexofenadine, and in the oncology setting it was used to evaluate transporter-mediated interactions.

Who is developing Fexofenadine dosing?

Fexofenadine dosing is being developed by AstraZeneca PLC, ticker AZN. The company sponsored a Phase 1 trial to study the effect of osimertinib on fexofenadine blood levels in patients with EGFR-mutant non-small cell lung cancer.

What phase is Fexofenadine dosing in?

Fexofenadine dosing is in Phase 1 clinical development. The only listed trial, NCT02908750, is a completed Phase 1 study. It is investigational and has not been approved for the oncology indication studied.

What clinical trials is Fexofenadine dosing in?

Fexofenadine dosing has been evaluated in one clinical trial: NCT02908750, titled "Study to Assess the Effect of Osimertinib (TAGRISSO™) on Blood Levels of Fexofenadine in Patients With EGFRm+ NSCLC." This Phase 1 trial was completed and enrolled 24 patients across France, South Korea, and Spain.

Is Fexofenadine dosing the same as Fexofenadine tablet dosing?

Yes, Fexofenadine dosing is also known as fexofenadine tablet dosing. Both terms refer to the same HRH1 antagonist small molecule developed by AstraZeneca PLC for study in non-small cell lung cancer.