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Related Concept Videos

Dose Size and Dosing Frequency: Determination Methods01:21

Dose Size and Dosing Frequency: Determination Methods

Determining the optimal dose size and dosing frequency in pharmacotherapy is crucial for achieving therapeutic effectiveness while minimizing adverse effects. This article explores the methodologies employed in determining these parameters, focusing on their significance and interplay to tailor dosing regimens.Dose Size: Dose size refers to the amount of a drug administered in a single dose. It is determined based on the drug's pharmacodynamics and pharmacokinetics properties and...
Determination of Multiple Dosing Parameters: Loading and Maintenance Doses01:25

Determination of Multiple Dosing Parameters: Loading and Maintenance Doses

A loading dose is an essential pharmacological strategy to rapidly achieve the target plasma drug concentration necessary for an immediate therapeutic effect. This approach is especially critical for drugs characterized by slow absorption or extended half-lives, where delaying therapeutic plasma levels could compromise treatment outcomes. By administering a loading dose, clinicians ensure a prompt onset of drug action, even for agents with complex pharmacokinetic profiles.Achieving steady-state...
Drug Dosing in Renal Diseases: Dose Adjustments Based on Drug Clearance and Elimination Rate Constant01:25

Drug Dosing in Renal Diseases: Dose Adjustments Based on Drug Clearance and Elimination Rate Constant

In patients with renal disease, dosage adjustments are necessary to maintain therapeutic plasma drug concentrations and prevent toxicity or subtherapeutic exposure. Renal impairment alters drug pharmacokinetics, especially in conditions like uremia, where changes such as prolonged elimination half-life and altered apparent volume of distribution can significantly affect drug disposition. These changes require careful modification of the dosing regimen to achieve the desired clinical...
Dosage Regimen: Fixed Dose01:01

Dosage Regimen: Fixed Dose

Fixed-dose regimens are a common approach to administer drugs to achieve and maintain desired levels of the drug in the body. In this dosing strategy, a specific amount of medication is given at regular intervals, often multiple times a day, to ensure a consistent drug concentration in the bloodstream.
Fixed-dose regimens can be used for various routes of administration, including intravenous (IV) injections and oral medications. For IV administration, a predetermined amount of the drug is...
Renal Failure: Dose Adjustments01:11

Renal Failure: Dose Adjustments

In patients with renal impairment, drugs undergo significant changes in their pharmacokinetics, which require dosage adjustments to ensure safe and effective therapy.
Reduced renal clearance and elimination rate are common outcomes of renal impairment. These alterations lead to a prolonged elimination half-life and an altered apparent volume of distribution for drugs. As a result, dosage adjustments are typically necessary to maintain optimal drug levels in the body.
However, dosage adjustments...
Dosage Regimen: Individualization01:24

Dosage Regimen: Individualization

Individualization in dosing regimens is the customization of medication doses for individual patients. Its necessity arises from the goal of maximizing therapeutic benefits while minimizing risks. This approach is pivotal because human responses to drugs can vary widely; what is effective for one person may be inadequate or excessive for another. Interpatient (intersubject) variability refers to differences in drug responses between individuals, while intrapatient (intrasubject) variability...

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Related Experiment Video

Updated: Jun 15, 2026

Identification of Rare Antigen-Specific T Cells from Mouse Lungs with Peptide:Major Histocompatibility Complex Tetramers
09:15

Identification of Rare Antigen-Specific T Cells from Mouse Lungs with Peptide:Major Histocompatibility Complex Tetramers

Published on: July 19, 2024

Dasatinib: is it all in the dose?

Fabrizio Condorelli1, Armando A Genazzani

  • 1DiSCAFF, Novara, Italy.

Biodrugs : Clinical Immunotherapeutics, Biopharmaceuticals and Gene Therapy
|March 13, 2010
PubMed
Summary

Dasatinib effectively treats chronic myeloid leukemia (CML) by inhibiting BCR/ABL. A 100 mg once-daily dose shows comparable efficacy and better tolerability than twice-daily dosing, suggesting potential for future pulse therapy.

Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • Dasatinib is an approved treatment for chronic myeloid leukemia (CML) in patients resistant or intolerant to imatinib.
  • Both imatinib and dasatinib target the BCR/ABL oncogenic fusion protein, a key driver in CML.
  • Understanding the pharmacokinetic, pharmacodynamic, and clinical profiles of dasatinib is crucial for optimizing CML treatment.

Purpose of the Study:

  • To review and highlight key pharmacokinetic, pharmacodynamic, and clinical data for dasatinib in CML treatment.
  • To compare the efficacy and tolerability of different dasatinib dosing regimens.
  • To explore the implications of dasatinib's mechanism of action for future therapeutic strategies.

Main Methods:

  • Review of pharmacokinetic, pharmacodynamic, and clinical trial data for dasatinib.

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Scaled-Up Preparation of an Intermediate of Upatinib, ACT051-3
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Scaled-Up Preparation of an Intermediate of Upatinib, ACT051-3

Published on: April 7, 2023

Related Experiment Videos

Last Updated: Jun 15, 2026

Identification of Rare Antigen-Specific T Cells from Mouse Lungs with Peptide:Major Histocompatibility Complex Tetramers
09:15

Identification of Rare Antigen-Specific T Cells from Mouse Lungs with Peptide:Major Histocompatibility Complex Tetramers

Published on: July 19, 2024

Scaled-Up Preparation of an Intermediate of Upatinib, ACT051-3
08:36

Scaled-Up Preparation of an Intermediate of Upatinib, ACT051-3

Published on: April 7, 2023

  • Comparison of dasatinib (100 mg once daily) versus dasatinib (70 mg twice daily) in a phase III trial.
  • Analysis of BCR/ABL inhibition, cytogenetic responses, and leukemic cell apoptosis.

    • Main Results:

    • Dasatinib is significantly more potent than imatinib in inhibiting BCR/ABL activity and has distinct inhibition profiles on other tyrosine kinases.
    • A once-daily dose of 100 mg dasatinib demonstrated similar efficacy and improved tolerability compared to 70 mg twice daily.
    • Cytogenetic responses correlate with BCR/ABL inhibition, and the 100 mg once-daily dose induces apoptosis in leukemic cells.

    Conclusions:

    • Dasatinib 100 mg once daily achieves sustained oncogenic shock and chronic inhibition of BCR/ABL activity.
    • The findings support the 100 mg once-daily regimen as an effective and well-tolerated option for CML treatment.
    • Pulse therapy with tyrosine kinase inhibitors (TKIs) may represent a future treatment option for select CML patients.