Enzastaurin and FHIT-elevating agents for the treatment of Pulmonary Hypertension

Stanford researchers have developed a method of reducing pulmonary hypertension (PH) in mammals by targeting FHIT (Fragile Histidine Triad), a gene not previously linked to PH but consistently reduced in blood of patients with pulmonary arterial hypertension (PAH). The second aspect of this invention is directed to the therapeutic use of the pharmaceutical Enzastaurin to increase FHIT levels and reduce PH in mammals. In certain embodiments, the method comprises administering Enzastaurin to a mammal having pulmonary hypertension with severe occlusive pulmonary vasculopathy at a dosage sufficient to reduce the pressure in the pulmonary arteries and the occlusive vasculopathy, improve right ventricular hypertrophy and reduce cardiac fibrosis.

Figure description:
(A) Enzastaurin reduces pulmonary hypertension as assessed by reduced right ventricular systolic pressure (RVSP) as well as (B) reduced right ventricular hypertrophy (RV/LV+S). (F) Enzastaurin has anti-remodeling effects and opens previously occluded vessels (D)

Stage of Research