Related Experiment Video

Updated: Feb 14, 2026

A New Technique for Treating Low-risk Prostate Cancer—Super Active Surveillance
05:19

A New Technique for Treating Low-risk Prostate Cancer—Super Active Surveillance

Published on: November 7, 2025

883

Pharmacokinetic/pharmacodynamic drug evaluation of enzalutamide for treating prostate cancer

Jeong Hee Hong1

  • 1a Department of Urology , Dankook University College of Medicine , Cheonan , Republic of Korea.

Expert Opinion on Drug Metabolism & Toxicology
|February 13, 2018
PubMed
Abstract

Insights

Enzalutamide is a key treatment for metastatic castration-resistant prostate cancer (mCRPC), showing good efficacy and safety. However, resistance can develop, necessitating further research for optimal patient selection and combination therapies.

Area of Science:

  • Oncology
  • Pharmacology

Background:

  • Enzalutamide is a second-generation androgen receptor (AR) antagonist.
  • It is approved for metastatic castration-resistant prostate cancer (mCRPC), with or without chemotherapy.
  • Recent years have seen extensive research into its clinical applications.

Purpose of the Study:

  • To review the pharmacology, efficacy, and tolerability of enzalutamide.
  • To discuss the future perspectives of enzalutamide in prostate cancer treatment.

Main Methods:

  • A comprehensive literature search was conducted.
  • Databases searched include PubMed, Embase, and Web of Science.
  • Relevant studies, including clinical trials and reviews, were selected.

Main Results:

  • Enzalutamide demonstrates favorable efficacy and safety profiles in mCRPC.
  • Primary or acquired resistance to enzalutamide is a significant clinical challenge.
  • The drug has significantly impacted the treatment paradigm for CRPC.

Conclusions:

  • Enzalutamide is a valuable therapeutic option for mCRPC.
  • Further research is crucial to overcome resistance mechanisms.
  • Identifying patient subgroups who benefit most from enzalutamide, alone or in combination, is essential.
Keywords:
Prostate cancerenzalutamidepharmacologysurvival

More Related Videos

A Computerized Test Battery to Study Pharmacodynamic Effects on the Central Nervous System of Cholinergic Drugs in Early Phase Drug Development07:02

A Computerized Test Battery to Study Pharmacodynamic Effects on the Central Nervous System of Cholinergic Drugs in Early Phase Drug Development

Published on: February 11, 2019

10.3K
An Orthotopic Murine Model of Human Prostate Cancer Metastasis06:48

An Orthotopic Murine Model of Human Prostate Cancer Metastasis

Published on: September 18, 2013

35.9K

Related Concept Videos

Pharmacokinetic–Pharmacodynamic Relationship: Problems01:24

Pharmacokinetic–Pharmacodynamic Relationship: Problems

The empirical approach to drug therapy optimization relies on correlating pharmacological response with administered dosage. Such an approach can be costly, time-consuming, and often yields poor correlation due to variables like formulation factors and drug elimination characteristics. A more precise approach correlates response with plasma drug concentration or the amount of drug in the body, rather than dosage. This is achieved through pharmacokinetic-pharmacodynamic (PK/PD) modeling, which...
17
Pharmacokinetic–Pharmacodynamic Relationship: Dose to Pharmacological Effect01:28

Pharmacokinetic–Pharmacodynamic Relationship: Dose to Pharmacological Effect

A drug’s dosage and pharmacokinetic properties determine how quickly it acts, how intense its effects are, and how long it lasts. Higher doses increase drug concentration at receptor sites, producing a hyperbolic curve when pharmacologic response is plotted against drug dose. Converting this scale to a log-linear format results in a sigmoidal curve, better representing dose–response relationships.For drugs following a one-compartment model, the pharmacologic response is directly...
16
Pharmacokinetic–Pharmacodynamic Relationship: Model Components01:14

Pharmacokinetic–Pharmacodynamic Relationship: Model Components

Pharmacokinetic-pharmacodynamic (PK–PD) modeling is essential in drug development and clinical pharmacology. It provides a quantitative framework to predict drug behavior and response over time. This approach integrates pharmacokinetics (PK), which describes the drug's absorption, distribution, metabolism, and excretion, with pharmacodynamics (PD), which characterizes the drug’s biological effects and mechanisms of action.The disposition kinetics of a drug determine its plasma...
20
Pharmacokinetic–Pharmacodynamic Relationship: Exposure, Response and Effect01:26

Pharmacokinetic–Pharmacodynamic Relationship: Exposure, Response and Effect

The pharmacokinetic-pharmacodynamic (PK-PD) relationship describes the intricate link between drug exposure, efficacy, and toxicity, forming the foundation for optimal dosing regimens. This relationship uses mathematical modeling to characterize drug concentration-effect dynamics, ensuring precise therapeutic outcomes.Exposure represents the pharmacokinetic aspect of the PK-PD relationship, denoting the drug amount that elicits a biological response. It is typically quantified by administered...
19
Pharmacokinetic–Pharmacodynamic Relationship: Duration of Dose-Effect Relationship01:14

Pharmacokinetic–Pharmacodynamic Relationship: Duration of Dose-Effect Relationship

For drugs producing a quantal response, onset occurs when plasma concentration reaches a minimum effective level (Cmin). The drug's action duration depends on how long the plasma concentration remains above Cmin.Two primary factors influence this duration: dose size and the rate of drug removal from the action site. Both depend on the drug's redistribution to poorly perfused tissues and elimination processes. A larger dose promotes rapid onset and prolongs the effect's duration.Consider a...
23
Pharmacokinetic–Pharmacodynamic Relationship: Intensity of Dose-Effect Relationship01:23

Pharmacokinetic–Pharmacodynamic Relationship: Intensity of Dose-Effect Relationship

Pharmacodynamics explores the relationship between drug concentration and its effect. In a quantal response drug, the duration of action better correlates with drug concentration, while for graded effect drugs, the intensity of response is more relevant. This intensity depends on the dose, drug removal rate, and the region of the concentration–response curve.The concentration–response curve can be divided into three regions. Region 3 (80–100% maximum response) demonstrates...
17