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A Fast and Clean BTK Inhibitor.

Ronen Gabizon¹, Nir London¹

¹Department of Organic Chemistry, Weizmann Institute of Science, Rehovot 7600001, Israel.

Journal of Medicinal Chemistry

|May 14, 2020

Summary

Remibrutinib is a novel Bruton's tyrosine kinase (BTK) inhibitor with high selectivity, offering a potential new treatment for autoimmune diseases. Its unique properties allow for rapid engagement and clearance, minimizing systemic exposure and side effects.

Area of Science:

Immunology
Pharmacology
Oncology

Background:

Bruton's tyrosine kinase (BTK) is crucial in B-cell malignancies.
Current BTK inhibitors have off-target effects limiting their use in autoimmune diseases.
There is a need for selective BTK inhibitors with improved safety profiles.

Purpose of the Study:

To introduce Remibrutinib (LOU064), a novel covalent BTK inhibitor.
To highlight Remibrutinib's unique selectivity and pharmacokinetic properties.
To discuss its potential therapeutic applications in autoimmune and inflammatory conditions.

Main Methods:

Development of a novel covalent BTK inhibitor, Remibrutinib.
Characterization of Remibrutinib's binding to an inactive BTK conformation.

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Evaluation of in vivo BTK engagement and plasma clearance.

Main Results:

Remibrutinib demonstrates unprecedented selectivity for BTK.
Optimization resulted in rapid BTK engagement in vivo.
Fast clearance of Remibrutinib limits systemic exposure.

Conclusions:

Remibrutinib's high selectivity and favorable pharmacokinetics make it a promising candidate for treating B-cell malignancies.
Its safety profile may allow for use in autoimmune and inflammatory diseases.
Remibrutinib is currently in Phase 2 trials for chronic urticaria and Sjoegren's syndrome.