Drug intelligence / Profile preview

ACT-280778

Development stage
Phase 2
Lead developer
Johnson & Johnson
Modality
Small Molecules
Administration
Oral
01

Overview

ACT-280778 is a novel, oral, non-dihydropyridine dual L-/T-type calcium channel blocker developed for the potential treatment of hypertension and angina pectoris. It acts by inhibiting both L-type and T-type voltage-operated calcium channels in cardiac and vascular smooth muscle cells, thereby reducing calcium influx associated with cardiovascular disorders. Clinical studies have shown that single and multiple doses up to 15 mg were well tolerated in healthy subjects, but higher doses led to abnormal electrocardiogram findings. In a phase 2a trial for mild-to-moderate essential hypertension, ACT-280778 did not demonstrate significant blood pressure lowering compared to placebo[1][2][4][7]. The drug was developed by Actelion Pharmaceuticals.

02

Targets

CaV3 (Caveolin-3)LTCC (Voltage-gated calcium channel (L-type))

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