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A Relative Bioavailability Study of Vepdegestrant Tablets in Healthy Adult Participants.
Derek Z Yang1, Kyle T Matschke2, Jennifer A Kimberly C WintonLee3
1Pfizer Inc., 11202 El Camino Real, San Diego, CA, 92130, USA. Derek.Yang@pfizer.com.
European Journal of Drug Metabolism and Pharmacokinetics
|June 29, 2026
Summary
Commercially representative vepdegestrant tablets are bioequivalent to the pivotal phase 3 formulation. This study confirms that different vepdegestrant tablet strengths are well-tolerated and suitable for breast cancer treatment.
Area of Science:
- Pharmacology and Drug Development
- Oncology
- Clinical Pharmacology
Background:
- Vepdegestrant is an oral PROTAC estrogen receptor (ER) degrader for ER-positive, HER2-negative advanced breast cancer.
- Development of new drug formulations is crucial for patient treatment accessibility.
Purpose of the Study:
- To assess the relative bioavailability of commercially representative vepdegestrant tablets compared to pivotal phase 3 tablets.
- To establish bioequivalence between different vepdegestrant tablet strengths (2x100mg and 1x200mg) and the reference formulation.
Main Methods:
- Phase 1, randomized, open-label, crossover study in healthy adults.
- Single 200-mg dose administration of three vepdegestrant tablet formulations.
- Pharmacokinetic sampling up to 168 hours post-dose to determine plasma concentrations.
Main Results:
- Vepdegestrant plasma concentration-time profiles were nearly superimposable between test and reference tablets.
- Bioequivalence was demonstrated, with 90% confidence intervals for key pharmacokinetic parameters falling within the 80.00-125.00% range.
- Similar adverse event rates were observed across all tested vepdegestrant tablet formulations.
Conclusions:
- Commercially representative vepdegestrant tablets are bioequivalent to the pivotal phase 3 formulation.
- All tested 200 mg vepdegestrant tablet formulations were well-tolerated in healthy adults.
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