drugset / Press release

DMX-200 Competitive Position Further Enhanced

2021-03-24 · Dimerix Bioscience Pty Ltd · original dimerix.com ↗

Immediate Release DMX-200 COMPETITIVE POSITION FURTHER ENHANCED Highlights • DMX-200 has the potential to provide greater potency and efficacy for other compounds in clinical development for inflammatory renal and respiratory diseases • Simultaneous use of a CCR2 inhibitor, such as Dimerix’ lead compound DMX -200, with endothelin A inhibitors, such as sparsentan and atrasentan, result in a significantly greater reduction of signalling in receptors involved in these inflammatory diseases • DMX-200 global patent portfolio expanded with new patent application filing MELBOURNE, Australia, 24 March 2021: Dimerix Limited (ASX: DXB), a clinical-stage drug development company, is pleased to announce new data related to the simultaneous use of Dimeri x’ lead compound DMX -200 (a Phase 3 CCR2 inhibitor) with other compounds in development , such as sparsentan (a Phase 3 dual endothelin and angiotensin receptor blocker) and atrasentan (a Phase 2 endothelin receptor blocker) . These in-vitro study data show that the addition of a CCR2 receptor inhibitor such as DMX -200 alongside sparsentan, provided a significantly greater inhibition of key receptor activation in human kidney cells than either compound alone. DMX-200 as an adjunct to an angiotensin receptor blocker Dimerix is developing DMX-200 for the treatment of kidney diseases and respiratory diseases given to patients already taking an angiotensin receptor blocker (ARB). Previous studies conducted by Dimerix have shown that simultaneous blockade of these receptors causes complete signal interference of key receptors implicated in a range of inflammatory diseases such as chronic kidney disease and respiratory disease. Dimerix has previously generated and published data to support the need to inhibit both CCR2 and angiotensin II type 1 (AT1R) receptors at the same time to fully stop signalling of either receptor, which is further supported by consistent clinical data in patients with various chronic kidney diseases. Dimerix has now confirmed that the blockade of A T1R by sparsentan is indistinguishable from other ARBs in its ability to prevent hyperactivation of CCR2 in the presence of AT1R. This data indicates that sparsentan could be used as an alternative to an ARB, such as irbesartan, as the adjunct therapy with DMX-200. 0 10 20 30 40 50 60 -0.05 0.00 0.05 0.10 0.15 0.20 0.25 Time (minutes) Ligand-induced BRET Sparsentan AT1R inhibitor CCR2 inhibitor & sparsentan No inhibitor • Sparsentan alone provided similar receptor signalling outcome to ARB alone • The addition of a CCR2 inhibitor enhanced that effect DMX-200 as an adjunct to an endothelin receptor blocker Dimerix has now also discovered new evidence of a functional interaction between endothelin A receptor ( ETAR) and CCR2 receptors, whereby Dimerix determined that simultaneous inhibition of CCR2 and ETAR is required to fully stop signalling of these receptors. These data suggest that Dimerix’ lead CCR2 inhibiting compound, DMX-200, may have a strongly beneficial effect for patients receiving new compounds in clinical development such as the endothelin receptor antagonist atrasentan, or the dual angiotensin receptor blocker and endothelin receptor antagonist, sparsentan. Sparsentan is a novel small-molecule candidate in Phase 3 development by Travere Therapeutics for the treatment of focal segmental glomerulosclerosis (FSGS). Sparsentan is a single molecule designed to selectively block both the ETAR and AT1R involved in progression of kidney diseases. In February 2021, Travere reported positive interim data for its Phase 3 study in FSGS patients, whereby 16% more patients achieved a proteinuria reducti on of ≥40% on sparsentan compared to irbesartan (29% of patients demonstrated ≥40% reduction in proteinuria on DMX -200 compared to placebo (irbesartan alone) in the Dimerix Phase 2 study reported in July 2020). Potential benefit to patients This new data clearly demonstrates that DMX -200 has the potential to provide greater potency and efficacy for compounds such as s parsentan and atrasentan that could result in further tangible therapeutic advantage for patients suffering from kidney disease, such as focal segmental glomerulosclerosis (FSGS). As a result of this surprising data demonstrating a coupling between CCR2 and an endothelin receptor, Dimerix has completed a key step in securing ownership over the benefits of DMX -200 by lodging a provisional patent application. The new Australian provisional patent application, titled “Treatment of Inflammatory Diseases” with filing number 2021900862, has a priority date of 23 March 2021 and if granted would expire post 204 2. This new patent filing further supports DMX -200, enhancing the strong competitive position. For further information, please visit our website at www.dimerix.com or contact: Dr Nina Webster Dimerix Limited Chief Executive Officer & Managing Director Tel: +61 1300 813 321 E: [email protected] Rudi Michelson Monsoon Communications Tel: +61 3 9620 3333 Mob: +61 (0)411 402 737 E: [email protected] Authorised for lodgement by the Board of the Company —END— About Dimerix Dimerix (ASX: DXB) is a clinical-stage biopharmaceutical company developing innovative new therapies in areas with unmet medical needs for global markets. Dimerix is currently developing its proprietary product , DMX-200, for Diabetic Kidney Disease, Focal Segmental Glomeruloscler osis (FSGS) and Acute Respiratory Distress Syndrome (ARDS), and is developing DMX-700 for Chronic Obstructive Pulmonary Disease (COPD). DMX-200 and DMX-700 were both identified using Dimerix’ proprietary assay, Receptor Heteromer Investigation Technology (Receptor-HIT), which is a scalable and globally applicable technology platform enabling the understanding of receptor interactions to rapidly screen and identify new drug opportunities. Receptor -HIT is licensed non -exclusively to Excellerate Bioscience, a UK-based pharmacological assay service provider with a worldwide reputation for excellence in the field of molecular and cellular pharmacology. About DMX-200 DMX-200 is the adjunct therapy of a chemokine receptor (CCR2) antagonist administered to patients already receiving irbesartan, an angiotensin II type I (AT1) receptor blocker and the standard of care treatment for hypertension and kidney disease. DMX-200 is protected by granted patents in various territories until 2032. In 2017, Dimerix completed its first Phase 2a study in patients with a range of chronic kidney diseases. No significant adverse safety events were reported, and all study endpoints were achieved. The compelling results from this study prompted the decision to initiate two different clinical studies in 2018: one for patients with Diabetic Kidney Disease; and the second for patients with another form of kidney disease, Focal Segmental Glomerulosclerosis (FSGS). DMX-200 is also under investigation as a potential treatment for acute respir atory distress syndrome (ARDS) in patients with COVID-19. About DMX-700 Chronic Obstructive Pulmonary Disease (COPD) is a progressive and life-threatening lung disease. The most common cause of COPD is exposure to tobacco smoke (either active smoking or secondary smoke) however, COPD is also caused by exposure to indoor and outdoor air pollution, occupational dusts and fumes and long-term asthma. COPD is the fourth-leading cause of death in the world and although treatments exist to improve the symptoms of COPD, there is currently no way to slow progression of the condition or cure it. Moreover, among the top five causes of death globally, this disease is the only one with increasing mortality rates. In 2016, the Global Burden of Disease Study reported a prevalence of 251 million cases of COPD globally, and it was estimated that 3.17 million deaths were caused by the dise ase in 2015, which equates to 5% of all deaths globally in that year (WHO Factsheet – Chronic Obstructive Pulmonary Disease). The global COPD treatment market was valued at US$14 billion in 2017 and is projected to increase at a compound annual growth rate of 4.9% to 2026.

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