Compositions and methods of treating pulmonary hypertension

Abstract

Provided are formulations comprising therapeutically effective amounts of ambrisentan or a pharmaceutically acceptable salt thereof and tadalafil or a pharmaceutically acceptable salt thereof and methods of treating and / or preventing pulmonary hypertension by administration of the formulations.

Description

CROSS-REFERENCE TO RELATED APPLICATION[0001]This application claims the benefit and priority to U.S. Provisional Application No. 61 / 393,529 filed Oct. 15, 2010, U.S. Provisional Application No. 61 / 490,454 filed May 26, 2011, and U.S. Provisional Application No. 61 / 497,475 filed Jun. 15, 2011. The entire disclosure of the applications identified in this paragraph is incorporated herein by reference.FIELD[0002]The present disclosure relates to methods of treating and / or preventing pulmonary hypertension by administration of therapeutically effective amounts of a selective type-A endothelin receptor antagonist and a phosphodiesterase type 5 inhibitor. This disclosure also relates to pharmaceutical formulations that are suitable for such administration.BACKGROUND[0003]Pulmonary hypertension (PH) has been previously classified as primary (idiopathic) or secondary. Recently, the World Health Organization (WHO) has classified pulmonary hypertension into five groups:[0004]Group 1: pulmonary...

AI Technical Summary

Benefits of technology

This patent describes a combination therapy using a selective type-A endothelin receptor antagonist (ambrisentan) and a phosphodiesterase type-5 inhibitor (tadalafil) for the treatment and prevention of pulmonary hypertension and related conditions. The combination therapy results in enhanced therapeutic effects when compared to mono-administration of each agent alone. The ratio of the dosages of ambrisentan and tadalafil can vary, but a ratio of about 1:1 to about 1:10 is preferred. The combination therapy can also be used to inhibit endothelin-induced vasoconstriction. Overall, this patent provides a novel treatment approach for pulmonary hypertension and related diseases.

Problems solved by technology

Severe constriction of the blood vessels in the lungs leads to very high pulmonary arterial pressures.

These high pressures make it difficult for the heart to pump blood through the lungs to be oxygenated.

Patients with PAH suffer from extreme shortness of breath as the heart struggles to pump against these high pressures.

Patients with PAH typically develop significant increases in pulmonary vascular resistance (PVR) and sustained elevations in pulmonary artery pressure (PAP), which ultimately lead to right ventricular failure and death.

Patients diagnosed with PAH have a poor prognosis and equally compromised quality of life, with a mean life expectancy of 2 to 5 years from the time of diagnosis if untreated.

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