Description

Simple

Clinical

Overview

R411 is a non-steroid oral medicine for the treatment of asthma. It is not immunosuppressive, but blocks the activation and recruitment of cells involved in respiratory inflammation. It is a dual-acting competitive integrin antagonist (as compared to previously developed single integrin antagonists or SIAs) that prevents binding of V-CAM1 to either a4b1 or a4b7.

Pharmacology

Indication

Investigated for use/treatment in asthma.

Pharmacodynamic

R411 is a non-steroid oral medicine for the treatment of asthma. It is not immunosuppressive, but blocks the activation and recruitment of cells involved in respiratory inflammation. It is a dual-acting competitive integrin antagonist (as compared to previously developed single integrin antagonists... Read more

Mechanism of action

R411 prevents binding of V-CAM1 to either a4b1 or a4b7.

Absorption

Information currently not available.

Protein binding

Information currently not available.

Volume of distribution

Information currently not available.

Clearance

Information currently not available.

Half life

Information currently not available.

Route of elimination

Information currently not available.

Toxicity

Good safety profile observed in preclinical and clinical
studies

Adverse Effects

Contraindications

Information currently not available.

Food Interactions

    Information currently not available.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
2 References
  1. 1 . Hijazi Y, Welker H, Dorr AE, Frank K, Renzetti LM, Patel I: Evaluation of the effect of multiple-dose administration of R411, a dual alpha4beta1-alpha4beta7 integrin antagonist on the major CYP isoform activities in healthy volunteers. Eur J Clin Pharmacol. 2006 Jan;62(1):83-5. Epub 2005 Dec 21.PubMed: 16369813
  2. 2 . Hijazi Y, Welker H, Dorr AE, Tang JP, Blain R, Renzetti LM, Abbas R: Pharmacokinetics, safety, and tolerability of R411, a dual alpha4beta1-alpha4beta7 integrin antagonist after oral administration at single and multiple once-daily ascending doses in healthy volunteers. J Clin Pharmacol. 2004 Dec;44(12):1368-78.PubMed: 15545307