Related Experiment Video

Updated: Aug 13, 2026

Evaluating the Effectiveness of Cancer Drug Sensitization In Vitro and In Vivo
09:19

Evaluating the Effectiveness of Cancer Drug Sensitization In Vitro and In Vivo

Published on: February 6, 2015

Biochemical pharmacological determinants of drug action in cancer therapeutics

E Mihich

    Oncology
    |January 1, 1980
    PubMed

    Insights

    Drug selectivity for cancer treatment depends on various factors. Understanding pharmacokinetics and target cell interactions can lead to more effective chemotherapy strategies.

    Area of Science:

    • Pharmacology
    • Oncology
    • Biochemistry

    Background:

    • Antitumor drug selectivity is influenced by systemic and target cell factors.
    • Pharmacokinetics and biotransformation are crucial for drug bioavailability.
    • Arabinosylcytosine and methotrexate serve as examples for target cell determinants.

    Purpose of the Study:

    • To discuss the role of pharmacokinetics and target cell factors in antitumor drug selectivity.
    • To explore the determinants of arabinosylcytosine and methotrexate action.
    • To highlight approaches for developing more selective chemotherapy.

    Main Methods:

    • Literature review and discussion of existing hypotheses.
    • Analysis of pharmacokinetic and biotransformation data.
    • Examination of target cell determinants for antimetabolites.

    Main Results:

    • Drug bioavailability is significantly impacted by pharmacokinetics and biotransformation.
    • Target cell characteristics play a key role in the efficacy of antimetabolites like arabinosylcytosine and methotrexate.
    • Modulating metabolite bioavailability offers a potential strategy for enhancing chemotherapy selectivity.

    Conclusions:

    • Selective chemotherapy requires a comprehensive understanding of drug disposition and target cell biology.
    • Pharmacokinetic optimization and targeting specific metabolic pathways are promising avenues for improving cancer treatment.
    • Further research into antimetabolite mechanisms can lead to the development of superior anticancer agents.

    More Related Videos

    Utilizing Functional Genomics Screening to Identify Potentially Novel Drug Targets in Cancer Cell Spheroid Cultures07:48

    Utilizing Functional Genomics Screening to Identify Potentially Novel Drug Targets in Cancer Cell Spheroid Cultures

    Published on: December 26, 2016

    Potentiation of Anticancer Antibody Efficacy by Antineoplastic Drugs: Detection of Antibody-drug Synergism Using the Combination Index Equation15:04

    Potentiation of Anticancer Antibody Efficacy by Antineoplastic Drugs: Detection of Antibody-drug Synergism Using the Combination Index Equation

    Published on: January 19, 2019

    Related Concept Videos

    Targeted Cancer Therapies02:57

    Targeted Cancer Therapies

    The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
    There are several types of targeted therapies against specific...
    Combination Therapies and Personalized Medicine02:50

    Combination Therapies and Personalized Medicine

    Combining two or more treatment methods increases the life span of cancer patients while reducing damage to vital organs or tissue from the overuse of a single treatment. Combination therapy also targets different cancer-inducing pathways, thus reducing the chances of developing resistance to treatment.
    The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
    Principles of Drug Action01:24

    Principles of Drug Action

    Drugs are chemical substances that modify biological responses by interacting with macromolecular targets such as receptors, ion channels, transporters, and enzymes. Pharmacodynamics describes the course of action of drugs leading to the physiological effect at a specific site in the body.
    Drugs can be agonists or antagonists. Like the endogenous ligands, agonists always bind and activate the target to produce a cellular response. Agonist binding induces a conformational change which in turn...
    Targets for Drug Action: Overview01:26

    Targets for Drug Action: Overview

    Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
    Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
    Pharmacogenetic Phenotypes: Alterations in Pharmacokinetics, Drug Targets and Biologic Milieu01:29

    Pharmacogenetic Phenotypes: Alterations in Pharmacokinetics, Drug Targets and Biologic Milieu

    Genetic variations significantly influence drug response through pharmacokinetics, receptor interactions, and biologic milieu modifications. Pharmacokinetic alterations impact drug metabolism and clearance, affecting efficacy and toxicity. Variants in drug-metabolizing enzymes, such as CYP2C9 and CYP2C19, alter drug activation and elimination. For example, CYP2C9 loss-of-function variants require lower warfarin doses to prevent excessive bleeding, while CYP2C19 variants reduce clopidogrel...
    Pharmacogenomics: Identification of New Drug Targets01:29

    Pharmacogenomics: Identification of New Drug Targets

    Advances in genomics have profoundly influenced drug discovery by increasing both the speed and accuracy of pharmaceutical development. Pharmacogenomics, which examines how genetic variation influences drug response, facilitates the identification of novel therapeutic targets and enables patient stratification for personalized treatment. These strategies contribute to improved drug efficacy, minimized adverse effects, and more efficient clinical trial design.Mapping genetic differences...