CCR1 antagonists: what have we learned from clinical trials

Related Experiment Video

Updated: Jun 12, 2026

Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs
10:44

Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs

Published on: May 15, 2019

Ronald P Gladue1, Matthew F Brown, Samuel H Zwillich

  • 1Pfizer Global Research and Development,Eastern Point Road,Groton, CT 06340, USA. Ronald.P.Gladue@Pfizer.com

Current Topics in Medicinal Chemistry
|June 12, 2010
PubMed

Insights

Chemokine receptor CCR1 plays a role in inflammatory diseases. CCR1 antagonists show therapeutic potential, with several drugs entering clinical trials for conditions like rheumatoid arthritis and multiple sclerosis.

Area of Science:

  • Immunology
  • Pharmacology
  • Pathogenesis of inflammatory diseases

Background:

  • Chemokines and their receptors mediate leukocyte infiltration, suggesting a role in disease.
  • CCR1 is upregulated in various human diseases, with animal models showing benefits from CCR1 inhibition.
  • CCR1 antagonists are being investigated for therapeutic applications in inflammatory conditions.

Purpose of the Study:

  • To review evidence supporting CCR1's role in inflammatory diseases.
  • To summarize results from clinical trials of CCR1 antagonists.
  • To provide insights for future chemokine receptor antagonist studies.

Main Methods:

  • Review of scientific literature on chemokines, CCR1, and inflammatory diseases.
  • Analysis of data from clinical trials involving CCR1 antagonists.
  • Synthesis of findings to inform future research directions.

Main Results:

  • Evidence supports CCR1's involvement in rheumatoid arthritis, multiple sclerosis, and COPD.
  • Several CCR1 antagonists (e.g., CP-481,715, MLN3897, BX471, AZD-4818) have advanced to clinical trials.
  • Clinical trial outcomes provide valuable lessons for developing future chemokine receptor antagonists.

Conclusions:

  • CCR1 antagonists hold therapeutic promise for inflammatory diseases.
  • Clinical trial experiences offer critical insights for optimizing the development of novel chemokine receptor antagonists.
  • Further research is warranted to fully leverage the therapeutic potential of targeting the CCR1 pathway.

More Related Videos

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators07:41

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators

Published on: February 20, 2018

An Analytical Tool that Quantifies Cellular Morphology Changes from Three-dimensional Fluorescence Images10:00

An Analytical Tool that Quantifies Cellular Morphology Changes from Three-dimensional Fluorescence Images

Published on: August 31, 2012

Related Concept Videos

Antianginal Drugs: Calcium Channel Blockers and Ranolazine01:25

Antianginal Drugs: Calcium Channel Blockers and Ranolazine

Angina pectoris, a primary symptom of ischemic heart disease, requires careful pharmacological interventions. In this context, calcium channel blockers (CCBs) and ranolazine have emerged as crucial pharmacotherapeutic agents, providing deep insights into the complexities of angina management.
CCBs, a diverse class that includes dihydropyridines (nifedipine) and diphenylalkylamines (verapamil and diltiazem), exert their effect by blocking calcium channels in cardiac and smooth muscle cells. This...
Clinical Trials: Overview01:11

Clinical Trials: Overview

Clinical development focuses on how the drug will interact with the human body and encompasses four key phases of clinical trials, each serving a specific purpose in assessing the safety and effectiveness of new drugs. These phases overlap and build upon one another. Phase I involves a small group of healthy volunteers (typically 20-80 individuals) or, in cases where significant toxicity is expected, patients with the targeted disease, such as cancer or AIDS. The volunteers are tested for...
Clinical Trials01:16

Clinical Trials

Clinical trials are prospective experimental studies conducted on humans to determine the safety and efficacy of treatments, drugs, diet methods, and medical devices. Using statistics in clinical trials enables researchers to derive reasonable and accurate conclusions from the collected data, allowing them to make wise decisions in uncertain situations. In medical research, statistical methods are crucial for preventing errors and bias.
There are four phases in a clinical trial. A phase one...
Adrenergic Antagonists: Pharmacological Actions of ɑ-Receptor Blockers01:22

Adrenergic Antagonists: Pharmacological Actions of ɑ-Receptor Blockers

α-Adrenergic antagonists, known as α-blockers, exert their effects by inhibiting α-adrenoceptors, leading to specific physiological actions. α1-blockers and α2-blockers have distinct pharmacological actions and therapeutic applications.
α1-blockers: These drugs inhibit α1-adrenoceptors on smooth muscle cells, resulting in vasodilation. This vasodilation lowers blood pressure, making α1-blockers valuable in treating hypertension. Additionally, α1-blockers effectively address urinary obstruction...
Drug-Receptor Interaction: Antagonist01:28

Drug-Receptor Interaction: Antagonist

An antagonist is a drug that binds strongly to a receptor without activating it. An antagonist prevents other molecules, such as neurotransmitters or hormones, from binding to the receptor and triggering a cellular response. Such interaction effectively hinders the normal physiological processes mediated by the receptor, resulting in various pharmacological effects depending on the specific receptor targeted.
Antagonists can be classified as competitive or noncompetitive based on their...
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...