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Pharmacokinetics of selective estrogen receptor modulators
Karla C Morello1, Gregory T Wurz, Michael W DeGregorio
1Department of Internal Medicine, University of California, Davis, Sacramento, California 95817, USA.
Clinical Pharmacokinetics
|March 22, 2003
Summary
Selective estrogen receptor modulators (SERMs) treat and prevent breast cancer and osteoporosis. This review covers SERM pharmacokinetics, including metabolism, half-life, and drug interactions, crucial for patient care.
Area of Science:
- Pharmacology
- Oncology
- Endocrinology
Background:
- Selective estrogen receptor modulators (SERMs) are vital in treating and preventing breast cancer and osteoporosis.
- Approved SERMs include tamoxifen, toremifene, and raloxifene, generally well-tolerated with common side effects like hot flashes.
- New SERMs, such as ospemifene and arzoxifene, are under development for similar therapeutic applications.
Purpose of the Study:
- To review the pharmacokinetic properties of currently approved and developing Selective estrogen receptor modulators (SERMs).
- To highlight key aspects of SERM metabolism, bioavailability, protein binding, and elimination half-lives.
- To discuss the clinical implications of SERM pharmacokinetics, including effects of hepatic impairment and potential drug interactions.
Main Methods:
- Literature review of pharmacokinetic data for established and investigational SERMs.
- Analysis of drug metabolism pathways, including cytochrome P450 and glucuronide conjugation.
- Examination of factors influencing SERM pharmacokinetics, such as bioavailability, protein binding, and elimination half-life.
Main Results:
- SERMs exhibit variable bioavailability (e.g., tamoxifen ~100%, raloxifene ~2%) and high plasma protein binding (>95%).
- Metabolism differs, with tamoxifen and toremifene utilizing the cytochrome P450 system, while raloxifene undergoes glucuronide conjugation.
- Pharmacokinetics are impacted by hepatic impairment but not renal impairment; drug interactions are noted with agents like warfarin and rifampicin.
Conclusions:
- Understanding SERM pharmacokinetics is essential for optimizing treatment efficacy and safety in patients with breast cancer and osteoporosis.
- Hepatic function significantly influences SERM pharmacokinetics, necessitating careful consideration in patients with liver conditions.
- Potential drug interactions with SERMs require vigilant monitoring and management in clinical practice.