23 May 2022 - - US-based specialty pharmaceutical company Tenax Therapeutics, Inc. (NASDAQ: TENX) has completed its comparative pharmacokinetic study of TNX-201, for the treatment of pulmonary arterial hypertension, the company said.

Tenax Therapeutics' efforts to optimize its formulation of imatinib mesylate, TNX-201, have culminated in a modified release tablet that effectively minimizes gastric release while preserving bioavailability.

The pharmacokinetic data from this trial showed that TNX-201 significantly exceeded Tenax' relative bioavailability threshold (area under the curve) when compared to reference Gleevec tablets.

These pharmacokinetic results are consistent with earlier in vitro dissolution data that indicated the formulation should limit gastric release while optimizing intestinal absorption.

Based on these positive pharmacokinetic findings, Tenax Therapeutics and its formulation partner are now manufacturing TNX-201 at the target scale for both the Phase 3 trial and future market demand.

IMPROVE is the Phase 3 clinical trial of imatinib for PAH sponsored by Tenax Therapeutics. Clinical sites are now being recruited, with patient enrolment expected to start in 2H 2022.

Tenax Therapeutics is a specialty pharmaceutical company focused on identifying, developing, and commercializing products that address cardiovascular and pulmonary diseases with high unmet medical need.

The company has world-class scientific advisory teams, including recognized global experts in pulmonary hypertension.

The company owns North American rights to develop and commercialize subcutaneous and oral formulations of levosimendan and has recently released detailed results from the Phase 2 HELP Study of levosimendan in Pulmonary Hypertension associated with Heart Failure and preserved Ejection Fraction (PH-HFpEF) at the Heart Failure Society of America Virtual Annual Scientific Meeting, and in the Journal of the American College of Cardiology: Heart Failure.

Tenax Therapeutics is also developing a unique oral formulation of imatinib designed to minimize the gastric irritation observed in a previous Phase 3 trial of the marketed version of the therapy while assuring that the dose achieved is at the level necessary for the drug to be effective.

Tenax Therapeutics expects to conduct a single pivotal trial pursuant to the 505(b) (2) pathway for regulatory approval.

Tenax Therapeutics is developing novel dosing and a unique formulation of imatinib mesylate, a kinase inhibitor that has received FDA's orphan designation (March 2020) for the treatment of pulmonary arterial hypertension.

The IMPRES trial, a previous Phase 3 trial, demonstrated that oral imatinib may produce a markedly greater, and much more durable, treatment effect on exercise tolerance, than any other available PAH treatment, alone or in combination, in those patients who were maintained on the full imatinib dose for the majority of the trial.

Despite the availability of several classes of pulmonary vasodilators, no existing treatment has been shown to halt progression or induce regression of the disease. Imatinib acts on underlying cellular proliferative pathways associated with PAH and has the potential to be the first disease modifying therapy for PAH.

Tenax Therapeutics intends to commence a Phase 3 trial of TNX-201 in 2H 2022.

Levosimendan is a unique potassium ATP channel activator and calcium sensitizer that affects the heart and vascular system through multiple mechanisms of action. Initially discovered and developed by Orion Corp. in Finland, intravenous levosimendan is approved in over 60 countries outside the United States for use in hospitalized patients with acutely decompensated heart failure.

Tenax Therapeutics has North American rights to develop and commercialize oral (TNX-103) and subcutaneous (TNX-102) formulations of levosimendan.

Results of Tenax Therapeutics' Phase 2 trial of levosimendan in patients with pulmonary hypertension and heart failure with preserved ejection fraction (HFpEF) demonstrated that IV levosimendan produces potent dilation of the central and pulmonary venous circulations which translates into an improvement in exercise capacity.

Patients have now completed the open-label transition study from weekly IV to a more convenient daily, oral regimen, TNX-103.

The discovery that venous dilation of the splanchnic circulation with levosimendan leads to increased exercise capacity in PH-HFpEF patients forms the basis for the Phase 3 investigation of Tenax Therapeutics' potential groundbreaking therapy.

To date, no other drug therapy has improved exercise tolerance in patients with PH associated with HFpEF, recently referred to as the greatest unmet need in cardiovascular disease.