Contineum Therapeutics Publishes Discovery of Potential Best-in-Class LPAR1 Antagonist PIPE-791 in Journal of Medicinal Chemistry

Key Terms

lpar1 medical

LPAR1 is a protein on the surface of cells that acts like a lock for a small signaling molecule, triggering internal cell responses when activated. Think of it as a light switch that controls processes such as cell movement, scarring, and inflammation. Investors care because drugs that block or activate LPAR1 can change disease outcomes; successful therapies or clinical trial results targeting this receptor can materially affect a biotech’s valuation and regulatory risk.

lysophosphatidic acid receptor 1 medical

A protein on the surface of cells that acts like a receptor for a signalling molecule called lysophosphatidic acid, triggering changes in cell growth, movement and inflammation. It matters to investors because blocking or activating this receptor is a potential way to treat diseases—so companies developing drugs or diagnostics aimed at it face clinical, regulatory and commercial risks and rewards; think of the receptor as a light switch that drugmakers try to turn on or off to change a disease’s course.

adme medical

ADME stands for Absorption, Distribution, Metabolism and Excretion — the four processes that determine how a drug enters the body, moves to target tissues, is chemically changed, and is removed. For investors, ADME profiles signal whether a drug is likely to be effective, safe and practical to dose; weak ADME can sink a program just like delivery problems can ruin a product launch, while strong ADME improves chances of regulatory approval and commercial success.

blood-brain barrier medical

A protective barrier of tightly packed cells and supporting tissue that controls what substances in the blood can enter the brain, acting like a security checkpoint that keeps out most pathogens and many drugs while allowing essential nutrients through. For investors, the barrier matters because whether a therapy can cross or safely bypass it often determines clinical success, regulatory approval and commercial potential for treatments of brain disorders.

central nervous system medical

The central nervous system (CNS) is the body's main control center, made up of the brain and spinal cord, that processes information and directs movement, sensation and basic functions like breathing. For investors, CNS-related products and research matter because they face long development times, strict safety testing and regulatory hurdles; success or failure can dramatically affect a company’s costs, timelines and potential market value.

idiopathic pulmonary fibrosis medical

Idiopathic pulmonary fibrosis is a chronic lung disease in which the air‑carrying tissue becomes progressively thickened and scarred for no identifiable reason, making the lungs stiff and less able to move oxygen—similar to a sponge that hardens and loses its pores. It matters to investors because it is life‑limiting with limited effective treatments, so clinical trial outcomes, regulatory approvals, pricing and reimbursement decisions can strongly affect the commercial value of therapies and the financial prospects of companies developing treatments.

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- Manuscript describes the discovery of LPAR1 antagonist PIPE-791, now in a Phase 2 clinical trial for the treatment of idiopathic pulmonary fibrosis (IPF)

- Blocking LPAR1 inhibits key steps in the fibrosis pathway with potential targets in several therapeutic indications

SAN DIEGO--(BUSINESS WIRE)-- Contineum Therapeutics, Inc. (NASDAQ: CTNM) (Contineum or the Company), a clinical-stage biopharmaceutical company pioneering differentiated therapies for the treatment of neuroscience, inflammation and immunology (NI&I) indications, today announced the publication of a manuscript describing the discovery and characterization of PIPE-791 in the Journal of Medicinal Chemistry. The article, “Discovery of PIPE-791, a Potent and Brain-Penetrant Lysophosphatidic Acid Receptor 1 (LPAR1) Antagonist with Slow Tight Binding Characteristics for the Treatment of Neuroinflammatory Disorders” (Chen et al, J. Med. Chem., June 29, 2026), highlights the Company’s internally discovered, selective LPAR1 antagonist as a potentially best-in-class approach for the treatment of fibrotic conditions.

“This was an incredible effort by our discovery team to enable the exploration of the full potential of LPAR1 as a therapeutic target for a wide range of indications,” said Daniel Lorrain, Ph.D., Chief Scientific Officer, Contineum Therapeutics. “PIPE-791’s chemical structure facilitates a slow on-off rate for our compound, differentiated pharmacokinetics and sustained, high target coverage. We believe these unique properties will allow us to pursue a potentially best-in-class approach in several inflammatory and fibrotic diseases.”

Extensive structural-activity relationship studies led to the identification of a unique scaffold that was responsible for slow but tight binding to LPAR1. Further optimizations that focused on improving brain-penetration and ADME (absorption, distribution, metabolism, excretion) properties afforded PIPE-791, the first LPAR1 antagonist that could effectively traverse the blood-brain barrier and fully occupy the target receptor, with a low, once-daily oral dose. The potential of PIPE-791 to treat both CNS (central nervous system) and peripherally restricted disorders associated with aberrant LPA-LPAR1 signaling was also demonstrated in multiple preclinical disease models.

PIPE-791 is now in a global Phase 2 clinical trial for the treatment of patients with IPF. More information on this trial can be found at https://clinicaltrials.gov (NCT07284459).

About Contineum Therapeutics

Contineum Therapeutics (Nasdaq: CTNM) is a clinical-stage biopharmaceutical company pioneering novel, oral small molecule therapies for NI&I indications with significant unmet need. Contineum is advancing a pipeline of internally-developed programs with multiple drug candidates now in clinical trials. PIPE-791 is an LPA1 receptor antagonist in clinical development for idiopathic pulmonary fibrosis and chronic pain. PIPE-307 is a selective inhibitor of the M1 receptor in clinical development for relapsing-remitting multiple sclerosis and major depressive disorder. For more information, please visit www.contineum-tx.com.

Forward-Looking Statements

Certain statements contained in this press release, other than historical information, constitute forward-looking statements within the meaning of the federal securities laws. Forward-looking statements include, but are not limited to, statements regarding the potential for PIPE-791 to be a first-in-class therapy and the pharmacological properties, safety, efficacy, tolerability and therapeutic potential of PIPE-791; the indications, anticipated benefits of, and market opportunities for PIPE-791 and the Company’s other drug candidates; the Company’s business strategies and plans; and the quotations of the Company’s management. These statements involve known and unknown risks, uncertainties and other important factors that are in some cases beyond the Company’s control and may cause its actual results, events, performance or achievements to be materially different from any future results, performance or achievements expressed or implied by the forward-looking statements. These risks and uncertainties, include, but are not limited to, the following: the Company is heavily dependent on the success of PIPE-791 and PIPE-307, both of which are in the early stages of clinical development, and neither of these drug candidates may progress through clinical development or receive regulatory approval; the results of earlier preclinical studies and clinical trials, including those conducted by third parties, may not be predictive of future results and unexpected adverse side effects or inadequate efficacy of the Company’s drug candidates may limit their development, treatment indications, regulatory approval and/or commercialization; the timing and outcome of research, development and regulatory review is uncertain; the FDA or comparable foreign regulatory authorities may disagree as to the design or implementation of our proposed clinical trials; clinical trials and preclinical studies may not proceed at the time or in the manner expected, or at all; the Company may use its capital resources sooner than expected and they may be insufficient to allow the Company to achieve its anticipated milestones; the potential for the Company’s programs and prospects to be negatively impacted by developments relating to the Company’s competitors, including the results of studies or regulatory determinations relating to the Company’s competitors; risks associated with reliance on third parties to successfully conduct clinical trials; the Company’s reliance, pursuant to a global license and development agreement, upon Janssen Pharmaceutica NV, a Johnson & Johnson company, to develop, in its sole discretion, PIPE-307 for relapsing-remitting multiple sclerosis, MDD or for any other indication; the restrictions contained in the Company’s global license and development agreement with Janssen Pharmaceutica NV limiting the Company’s access to, and restricting the Company from disclosing, certain information regarding the development of PIPE-307; the Company has incurred significant operating expenses since inception and it expects that its operating expenses will continue to significantly increase for the foreseeable future; the Company’s ability to operate in a competitive industry and compete successfully against competitors that have greater resources than the Company does; the Company may be unable to obtain, maintain and enforce intellectual property protection for its technology and drug candidates; and unstable market and economic conditions and military conflict may adversely affect the Company’s business and financial condition and the broader economy and biotechnology industry. Additional risks and uncertainties that could affect the Company’s business, operations and results are included under the captions, “Risk Factors” and "Management’s Discussion and Analysis of Financial Condition and Results of Operations” in the Company's periodic filings and in other filings that the Company makes with the Securities and Exchange Commission (SEC) from time to time, which are available on the Company’s website at www.contineum-tx.com under the Investor section and on the SEC’s website at www.sec.gov. Accordingly, readers should not rely upon forward-looking statements as predictions of future events. Except as required by applicable law, the Company undertakes no obligation to update publicly or revise any forward-looking statements contained herein, whether as a result of any new information, future events, changed circumstances or otherwise.

View source version on businesswire.com: https://www.businesswire.com/news/home/20260630868477/en/

Steve Kunszabo
Contineum Therapeutics
Senior Director, Investor Relations & Corporate Communications
858-649-1158
skunszabo@contineum-tx.com

Source: Contineum Therapeutics, Inc.