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Safety and Pharmacokinetics of JAK/ROCK Inhibitor in Healthy Volunteers

NCT04670757 · Status: COMPLETED · Phase: PHASE1 · Type: INTERVENTIONAL · Enrollment: 65

Last updated 2022-05-16

No results posted yet for this study

Summary

The aim of the following clinical trial is to determine safety an pharmacokinetic parameters in healthy volunteers after oral administration of Janus kinases and Rho-kinases inhibitor (JAK/ROCKi), called CPL409116.Janus kinase (JAK) inhibitors are a new class of small molecule drugs that modulate inflammatory pathways by blocking one or more JAK receptors. In recent years, JAK inhibitors have emerged as a new option for the treatment of various inflammatory diseases, including rheumatoid arthritis, psoriatic arthritis, spondyloarthritis, skin disorders and others. CPL409116 inhibits JAK1 and JAK3 with less inhibitory activity against JAK2 and Tyk2. Inhibition of these kinases decreases inflammatory cytokine release which in turn decreases lymphocyte activation and proliferation. Moreover, CPL409116 blocks Rho-kinases (ROCKs), which are involved in diverse cellular processes including actin cytoskeleton organization, cell adhesion and motility, proliferation, apoptosis as well as smooth muscle contraction. ROCKs signalling is one of the major pathways implicated in the pathogenesis of cardiovascular, renal as well as fibrotic diseases. However recent data indicate their role in immune cell regulation and inflammatory disease development. CPL409116 was designed predominantly for the therapy of immune-related diseases: rheumatoid arthritis, psoriasis and because antifibrotic therapies are needed. Dual inhibition of JAK/ROCK kinases may be beneficial for patients suffering from fibrotic complications of inflammatory disease.

Rheumatoid arthritis (RA) is a chronic systemic autoimmune disease characterised by persistent joint inflammation leading to loss of joint function as well as cartilage and bone damage. Chronic, progressive course of the disease results in disability, reduced quality of life, as well as higher comorbidity and mortality rates. It is well documented that JAK kinases play a pivotal role in cytokine receptor signalling to phosphorylate and activate signal transducer and activator of transcription (STAT) proteins. Several of these JAK-controlled cytokine receptor pathways are immediately involved in the initiation and progression of RA pathogenesis. Cytokines promote autoimmunity, maintain chronic inflammatory synovitis and drive the destruction of joint tissue. In consequence on the basis of the preclinical study results the IMP with the active ingredient CPL409116 has been classified as a good clinical candidate for the treatment of RA.

Conditions

  • Healthy

Interventions

DRUG

CPL409116

IMP administration, tablets contain CPL409116 as an active ingredient

DRUG

Placebo

Placebo comparator

Sponsors & Collaborators

  • National Center for Research and Development, Poland

    collaborator OTHER

  • Celon Pharma SA

    lead INDUSTRY

Study Design

Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
DOUBLE
Model
SEQUENTIAL

Eligibility

Min Age
18 Years
Max Age
55 Years
Sex
ALL
Healthy Volunteers
Yes

Timeline & Regulatory

Start
2020-12-08
Primary Completion
2021-09-08
Completion
2021-09-08

Countries

  • Poland

Study Locations

More Related Trials

Entities

Drugs

Read the full study record

This page highlights key information. For complete eligibility criteria, study locations, investigator contacts, and the full protocol, visit the original record on ClinicalTrials.gov.

View NCT04670757 on ClinicalTrials.gov