Drug intelligence / Profile preview

aliskiren + spironolactone + lisinopril

Development stage
Preclinical
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination of three antihypertensive agents, each with distinct mechanisms targeting the renin-angiotensin-aldosterone system (RAAS) and fluid balance. Aliskiren is a direct renin inhibitor that blocks the conversion of angiotensinogen to angiotensin I, thereby reducing downstream production of angiotensin II and aldosterone[4][10]. Spironolactone is a potassium-sparing diuretic and mineralocorticoid receptor antagonist that inhibits aldosterone’s effects in the distal renal tubule, promoting sodium excretion while retaining potassium[8]. Lisinopril is an angiotensin-converting enzyme (ACE) inhibitor that prevents the conversion of angiotensin I to angiotensin II, leading to vasodilation and reduced aldosterone secretion[2][5]. This triple combination would theoretically provide potent antihypertensive effects by blocking RAAS at multiple points; however, it carries significant risks including hyperkalemia, hypotension, and acute kidney injury due to overlapping pharmacological actions on potassium retention and renal hemodynamics[1][2][3][7].

02

Targets

REN (Renin)ACE (Angiotensin Converting Enzyme)MR (Mineralocorticoid receptor)

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