Results 11 to 20 of about 284 (126)

Aprocitentan (TRYVIO)

Amrita Journal of Medicine
Aprocitentan (TRYVIO), is the first and only endothelin receptor antagonist for the treatment of high blood pressure not adequately controlled in combination with 3 combined antihypertensive class drugs.
Shalini Thomas
doaj   +3 more sources

Aprocitentan, A Dual Endothelin Receptor Antagonist Under Development for the Treatment of Resistant Hypertension [PDF]

Cardiology and Therapy, 2021
Aprocitentan (ACT-132577) is an orally active, dual endothelin-1 (ET-1) receptor antagonist that prevents the binding of ET-1 to both ETA/ETB receptors. It is an active metabolite of macitentan (obtained by oxidative depropylation), an orphan drug used for the treatment of pulmonary arterial hypertension. Aprocitentan is highly bound to plasma proteins
Fabio Angeli, , Angeli Fabio
exaly   +5 more sources

Aprocitentan and the endothelin system in resistant hypertension

Canadian Journal of Physiology and Pharmacology, 2022
Endothelin has emerged as a target for therapeutic intervention in systemic hypertension. As a vasoconstrictor, comitogenic agent, linking pulse pressure and vascular remodeling, and mediator of aldosterone and catecholamine release, endothelin is a key player in hypertension and end-organ damage.
Martine Clozel
exaly   +4 more sources

Crystal Structures of Large-Volume Commercial Pharmaceuticals [PDF]

Structural Dynamics
As part of a continuing project, the room-temperature crystal structures of 17 commercial pharmaceutical APIs have been solved and refined using synchrotron X-ray powder diffraction data (11-BM at APS and Wiggler Low Energy Beamline at CLS), and ...
James A Kaduk, Anja Dosen, Thomas N Blanton   +2 more
doaj   +3 more sources

Effects of the Dual Endothelin Receptor Antagonist Aprocitentan on Body Weight and Fluid Homeostasis in Healthy Subjects on a High Sodium Diet

Clinical Pharmacology &Therapeutics, Volume 109, Issue 3, Page 746-753, March 2021., 2021
Aprocitentan is a novel, oral, dual endothelin receptor antagonist (ERA) in development in difficult‐to‐control hypertension. As fluid retention and edema are concerns with ERAs, we investigated whether aprocitentan causes weight gain in healthy subjects on a high sodium diet and explored potential mechanisms if occurring. This double‐blind, randomized,
Pierre Gueneau de Mussy, Patricia N. Sidharta, Gregoire Wuerzner, Marc P. Maillard, Nicolas Guérard, Marc Iglarz, Bruno Flamion, Jasper Dingemanse, Michel Burnier   +8 more
wiley   +3 more sources

Endothelin as a Treatment Target in Cardiovascular Diseases: A Recent Step Forward [PDF]

Reviews in Cardiovascular Medicine
Cardiovascular diseases (CVDs) are a leading cause of mortality, significantly influencing quality of life and causing a burden on the healthcare system.
Aleksandra Cole, Kajetan Kiełbowski, Aleksandra Dach, Jacek Szulc, Estera Bakinowska, Andrzej Pawlik   +5 more
doaj   +2 more sources

Dual Endothelin Antagonism with Aprocitentan as a Novel Therapeutic Approach for Resistant Hypertension. [PDF]

Curr Hypertens Rep, 2023
Abstract Purpose of Review Resistant hypertension (RH) defined as uncontrolled blood pressure despite the use of a combination of a renin-angiotensin system blocker, a calcium channel blocker, and a diuretic at maximally tolerated doses is associated with a substantially increased risk of cardiovascular and renal events.
Heidari Nejad S, Azzam O, Schlaich MP.
europepmc   +3 more sources

Endothelin receptor antagonists (ERAs) can potentially be used as therapeutic drugs to reduce hypertension caused by small molecule tyrosine kinase inhibitors (TKIs) [PDF]

Frontiers in Pharmacology
The emergence of targeted anti-tumor drugs has significantly prolonged the lifespan and improved the prognosis of cancer patients. Among these drugs, vascular endothelial growth factor (VEGF) inhibitors, particularly novel small molecule tyrosine kinase ...
Qingjian He, Junling Lin, Chanjuan Mo, Guodong Li, Jianzhong Lu, Qiyin Sun, Lijun Cao, Haojian Gan, Quan Sun, Jiafang Yao, Shengyi Lian, WenJuan Wang   +11 more
doaj   +2 more sources

Aprocitentan in hypertension management: clinical efficacy, safety, and future prospects. [PDF]

Ann Med Surg (Lond)
Hypertension (HTN) is a prevalent medical condition characterized by systolic blood pressure ≥ 130 mm Hg and diastolic blood pressure ≥ 80 mm Hg. In 2010, the global prevalence of HTN was 31.1%, with higher rates in men and low- and middle-income countries (LMICs).
Riaz R, Ahmed U, Naqi U, Afaq L, Shaukat A, Khan Y, Akilimali A.   +6 more
europepmc   +3 more sources

Revolutionizing resistant hypertension: Unlocking the potential of Aprocitentan.

Journal of the Pakistan Medical Association
Madam,  Hypertension is a prevalent disease worldwide; however, the therapies for the treatment of hypertension have been unable to meet the desired blood pressure levels in approximately 15% of patients resulting to resistant hypertension.
Rahemeen Goraya, Mahrukh Nadeem
doaj   +3 more sources