Principia Biopharma Inc., a private, clinical-stage biopharmaceutical company, today announced positive Phase 1 results for PRN1008, the company’s reversible covalent Bruton’s Tyrosine Kinase (BTK) inhibitor. PRN1008 safely achieved and exceeded the prospectively defined level of BTK receptor occupancy which the company believes is required for full effect in autoimmune and inflammatory diseases.
The Phase 1, double blind, placebo controlled, single and multiple ascending dose trial evaluated the pharmacokinetics, BTK receptor occupancy, safety and tolerability of PRN1008 given orally to 80 healthy volunteers. The data from this trial will be presented at an upcoming scientific conference.
PRN1008 is an oral, reversible covalent BTK inhibitor designed with Principia’s proprietary Tailored Covalency™ technology. This approach gives PRN1008 antibody-like specificity for BTK, reversible covalent bonding, and potentially enables a safety profile suitable for the treatment of chronic diseases. BTK is a key signaling protein in the regulation of immune and inflammatory functions in many cell types, such as B-cells, neutrophils, mast cells and antigen-presenting cells.
“The data from the trial demonstrate sustained inhibition of BTK with PRN1008 that we believe will translate into a clinical effect for numerous autoimmune and inflammatory diseases,” said Martin Babler, Chief Executive Officer of Principia Biopharma. “To our knowledge, this is the first clinical data of a reversible covalent BTK inhibitor for autoimmune diseases. These clinical results, combined with our preclinical data, show that PRN1008 may have the wide therapeutic margin desirable for long term treatment.”
“The results with PRN1008 validate the principles of our Tailored Covalency platform, on which the company was founded,” said David Goldstein, Senior Vice President, Drug Discovery at Principia Biopharma. “We believe combining the efficacy of a covalent inhibitor with the safety that comes with reversibility will be a distinguishing feature for the treatment of chronic diseases.”
Principia will be presenting at the 33rd Annual J.P. Morgan Healthcare Conference in San Francisco on Tuesday, January 13, 2015 at 2:00 p.m. (PT).
About Principia Biopharma
Principia Biopharma Inc., a private, clinical-stage biopharmaceutical company, has created a revolutionary new way to design and develop oral small molecule therapies that are more potent, selective, durable and safer than currently available drugs. The Company has utilized its proprietary Tailored Covalency™ technology to develop a portfolio of drug candidates that exhibit antibody-like specificity to benefit patients with autoimmune and inflammatory diseases and cancer. Its most advanced drug candidate, PRN1008, a reversible covalent BTK inhibitor, is in Phase 1 development for the treatment of autoimmune and inflammatory diseases. Since Principia began operations in 2011, its highly productive approach has led to the rapid advancement of PRN1008 into the clinic, PRN1371, a covalent pan-FGFR inhibitor drug candidate for oncology as well as research programs in autoimmune and inflammatory diseases. For more information, please visit the company's website at www.principiabio.com.
