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calcitriol + angiotensin converting enzyme inhibitor + angiotensin receptor blocker

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

Overview

This is a **combination therapy** containing three components: **calcitriol**, an **angiotensin converting enzyme inhibitor (ACE inhibitor)**, and an **angiotensin receptor blocker (ARB)**. - **Calcitriol** is the active form of vitamin D3. It acts as a hormone, regulating calcium and phosphate metabolism by promoting absorption in the gut; it is primarily used for conditions related to calcium/phosphate imbalance, including chronic kidney disease, hypoparathyroidism, and osteoporosis. - **ACE inhibitors** block the conversion of angiotensin I to angiotensin II, a potent vasoconstrictor, thereby reducing blood pressure and exerting beneficial effects on cardiovascular and renal outcomes. - **Angiotensin receptor blockers** inhibit the action of angiotensin II at its receptor (AT1), also promoting vasodilation and providing kidney and cardiac protection. The combination of an **ACE inhibitor and ARB** has been studied for additive benefits in hypertension, chronic kidney disease (especially proteinuria), and heart failure, with evidence showing decreased blood pressure, reduced protein excretion, and improved outcomes, although concerns about safety (risk of hyperkalemia, renal insufficiency) exist[2]. Adding **calcitriol** to renin-angiotensin-aldosterone system (RAAS) inhibition may offer further benefit in patients with chronic kidney disease and disordered mineral metabolism, but triple therapy is not a standard fixed-dose or branded combination, and is rarely used in routine clinical practice.

02

Targets

ACE (Angiotensin Converting Enzyme)VDR (Vitamin D receptor)AGTR1 (Angiotensin II Type-1 receptor)

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