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Regulatory Guidelines

The information shown here is Exprimo's best understanding of the current regulatory guidances with respect to the different topics presented. Only regulatory guidelines from ICH, USA and Europe are included here. The comments and interpretations given under each guidance/regulatory document are Exprimo's alone and do not reflect the opinion of the relevant regulatory agency. Exprimo will endeavour to ensure that the information presented here is as complete and as up to date as possible, but does not guarantee this.

The guidances are presented for three different topics, the population approach, PK/PD, and, modelling and simulation. The guidances that refer to PK/PD or modelling and simulation are presented below. Please click on the link 'What population PK analysis can be used for in drug development' for a presentation of the guidances that refer to population pharmacokinetics.

PK/PD Analyses
Modelling and Simulation
PK/PD Analyses

Knowledge of PK/PD relationships contributes to selection of the dose and dosing regimen of new compounds in different situations. Knowledge of PK/PD relationships is also crucial for the interpretation of pharmacokinetic data in relation to effect and safety. Many regulatory documents recommend that PK/PD relationships are characterised but provide sparse practical information as to the design and analysis of such studies.

ICH Final Guideline on dose response (E4). Released March 1994.

This guideline highlights the use of concentration-effect relationships for optimising dosing regimens and for adequate dosing instructions in the labelling.

FDA Final Guidance on pharmacokinetics in patients with impaired hepatic function. Released May 2003.

FDA Draft Guidance on PK in patients with impaired renal function. Released March 2010.

FDA Final Guidance for study and evaluation of gender differences. Released June 1993.

FDA Draft Guidance on paediatric PK studies. Released November 1998.

FDA Draft Guidance on drug interaction studies. Released September 2006.

The above five guidances make general statements with respect to PK/PD relationships along the theme of that information relating exposure to response can be used to adjust dosages and dosing regimens in the presence of influences on PK such as age, gender (demographic factors), impaired organ function (intrinsic factors) or concomitant medications or diet (extrinsic factors). In many circumstances where the assumption can be made that the exposure/response relationships are not disturbed by these factors, PK data alone can be used to guide dosages and dosing regimens.

FDA Final Guidance on population pharmacokinetics. Released February 1999.

The FDA guidance is on the subject ‘Population Pharmacokinetics' but makes a statement at the start of the guidance to say that the principles discussed are equally applicable to PK/PD analyses.

FDA Final Guidance on exposure-response relationships - study design, data analysis and regulatory applications. Released April 2003.

The guidance states that exposure can be dose or various measures of concentration. The major headings in the guidance are: Introduction, Background, Regulatory applications, Dose-concentration-response relationships and effects over time, Designs of exposure-response studies, Modelling of exposure-response relationships, and, Submission information.

Europe Final Guidance on pharmacokinetic studies in man. Released 1987.

This well established ‘pharmacokinetic studies in man' guideline mentions the value of PK/PD information.

CPMP Final Guidance on antiarrhythmics. Released November 1995.

The guidance states that pharmacodynamic studies should include “concentration dose-response studies with regard to a drug's haemodynamic and electrophysiological properties, in patients with non life-threatening arrhythmias and with no risk factors”.

CPMP Final Guidance on cardiac failure. Released December 1999.

The guidance states “Based on information from dose-concentration and concentration-response relationships, dose schedules should be clearly defined for patients with varying degrees of congestive heart failure, renal dysfunction and/or hepatic dysfunction”.

CPMP Final Guidance on the clinical investigation of medicinal products for the treatment of urinary incontinence. Released December 2002.

The guidance includes a short section on PK/PD studies.

EMA Draft Guidance on drug interactions. Released April 2010.

The guidance states that some knowledge of PK/PD relationships is required when interpreting the significance of drug-drug interactions.

CPMP Final Guidance on modified release oral and transdermal release forms. Released July 1999.

The guidance states that in rare cases, if there is a well-defined PK/PD relationship between plasma concentration and clinical response, then clinical trials may be considered unnecessary. An addendum to this guidance is under preparation and which will include a discussion on the clinical program if the PK/PD relationship is well defined.

Evaluation of Medicinal Products Indicated for Treatment of Bacterial Infections. Released October 2004.

This document has a paragraph on development of PK/PD relationships.

CPMP Final Guidance on evaluation of anticancer medicinal products in man. Released May 2001.

In this guideline, the PK/PD focus is towards the evaluation of the concentration-toxicity relationship in Phase I studies, and less so on efficacy.

CPMP Final Appendix to the Guidance for the treatment of schizophrenia concerning the development of depot preparations. Adopted February 2003.

The appendix states that clinical studies to compare the efficacy or oral and depot preparation and to justify the dosage interval are deemed necessary unless a clear PK/PD relationship has been demonstrated for the oral preparation.

EMA Final Guidance on the clinical development of medicinal products for the treatment of HIV infection. Released November 2008.

Multiple mentions of PK/PD, for dose selection, bridging to new formulations and for defining inter- and intra-subject variability in parameters.

CHMP Final Guidance on pharmacokinetic studies in patients with renal impairment. Released December 2004.

The final guidance for pharmacokinetic studies in renal impairment emphasizes knowledge of PK/PD so that appropriate dose adjustments can be made in this population. The guidance also says that knowledge of PK/PD relationships regarding the effect of renal impairment on relevant biomarkers for efficacy and safety may be important for developing dosing recommendations. It also stresses that consideration should be given to possible differences in the PK/PD relationship between patients with and without renal impairment.

Modelling and Simulation

FDA Draft Guidance on PK in patients with impaired renal function. Released March 2010.

The guidance includes the sentence "Simulations are encouraged as a means to identify doses and dosing intervals that achieve that goal for subjects with different levels of renal function".

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FDA Final Guidance on exposure-response relationships - study design, data analysis and regulatory applications. Released April 2003.

The guidance says “Creating a theory or rationale to explain exposure-response relationships through modelling and simulation allows interpolation and extrapolation to better doses and responses in the general population and to subpopulations defined by certain intrinsic and extrinsic factors.” The guidance also says “Exposure-response data can be derived from these clinical studies, as well as from other preclinical and clinical studies, and provide a basis for integrated model-based analysis and simulation. Simulation is a way of predicting expected relationships between exposure and response in situations where real data are sparse or absent.”

CHMP Final Guidance on pharmacokinetic studies in patients with renal impairment. Released December 2004.

The guidance includes a large paragraph on simulations and which includes that simulations can be used to identify doses and dosing intervals that achieve target exposure for patients with different degrees of renal impairment.