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Cardiovascular drugs

273 articles

Acadesine

Acadesine (AICA-riboside, AICAr) is a purine nucleoside AMPK activator and adenosine-regulating agent; developed for CABG cardioprotection, failed phase 3 RED-CABG, orphan-designated for CLL and myeloma.

ACE inhibitor

ACE inhibitors are drugs blocking angiotensin-converting enzyme to treat hypertension and heart failure; developed from Bothrops jararaca venom peptides, first drug captopril (1981), followed by enalapril, lisinopril, ramipril.

Acetazolamide

Acetazolamide (Diamox) is a sulfonamide carbonic anhydrase inhibitor discovered in 1950, FDA-approved for epilepsy in 1953, used for glaucoma, edema, epilepsy, and acute mountain sickness prevention; common side effects include paraesthesias, dysgeusia, polyuria, and fatigue.

Acetyldigitoxin

Acetyldigitoxin (Acylanid, alpha-acetyldigitoxin) is a cardiac glycoside, an acetyl derivative of digitoxin prepared from lanatoside A of Digitalis lanata, used for fast digitalization in heart failure and rate control in atrial arrhythmias; ATC C01AA01, now discontinued.

Acoramidis

Acoramidis, sold as Attruby and Beyonttra, is an oral transthyretin stabilizer developed by BridgeBio Pharma and approved in November 2024 for cardiomyopathy from transthyretin-mediated amyloidosis.

Aficamten tablets

Aficamten tablets (阿夫凯泰片), sold as MYQORZO, are an oral cardiac myosin inhibitor from Cytokinetics for obstructive hypertrophic cardiomyopathy, approved in China in 2025 as the second drug in its class after mavacamten.

Alfuzosin

Alfuzosin (Uroxatral, Xatral) is a quinazoline alpha-1 adrenergic antagonist for benign prostatic hyperplasia symptoms; 10 mg once-daily extended-release tablet, FDA approved 2003, no dose titration, not for hypertension.

Allisartan isoproxil

Allisartan isoproxil (阿利沙坦酯, Xinlitang) is China's first domestically developed class 1.1 ARB antihypertensive, dosed 240 mg daily, activated to EXP3174 by gut esterases, marketed by Shenzhen Salubris since 2013.

Alpha blocker

Alpha blockers (alpha-adrenergic antagonists) are drugs blocking alpha-1 receptors, used as second-line hypertension therapy and first-line drugs for BPH; examples include tamsulosin, silodosin, doxazosin, terazosin, alfuzosin, and prazosin.

Alpha-adrenergic agonist

Alpha-adrenergic agonists are drugs stimulating α1 receptors (phenylephrine, vasoconstriction, reflex bradycardia) or α2/imidazoline receptors (clonidine, lowered sympathetic outflow, sedation), used as vasopressors, decongestants, and antihypertensives.

Ambrisentan

Ambrisentan (Letairis, Volibris) is an oral, ETA-selective endothelin receptor antagonist approved in 2007 for pulmonary arterial hypertension WHO FC II-III; once-daily 5-10 mg dosing, low liver toxicity, edema risk, REMS removed 2025.

Amiloride

Amiloride, a potassium-sparing diuretic and ENaC pore blocker (IC50 ~100 nM) acting in the distal nephron; FDA-approved 1981, used with thiazides for hypokalemia prevention, main risk hyperkalemia.

Amiodarone

Amiodarone (Cordarone) is a plant-derived, iodine-rich class III antiarrhythmic drug developed in Belgium in the 1960s as an antianginal agent, FDA-approved in 1985, used for ventricular arrhythmias and atrial fibrillation but limited by pulmonary, thyroid, hepatic, and cardiac toxicity.

Amlodipine

Amlodipine, a long-acting Pfizer-developed dihydropyridine calcium channel blocker (besylate tablets, US approval 1987), treats hypertension and angina at 5-10 mg once daily; slow receptor binding, dose-related edema, reduced stroke risk versus other regimens.

Amoproxan

Amoproxan (CERM 730, CAS 22661-76-3) is a withdrawn INN coronary vasodilator and antianginal drug, a trimethoxybenzoate ester with a morpholine ring, C22H35NO7, withdrawn after about a year for skin and sensory toxicity.

Ancrod

Ancrod (Arvin, Viprinex) is a thrombin-like enzyme from Malayan pit viper venom that defibrinogenates blood by cleaving fibrinopeptide A; tested for acute ischemic stroke in STAT and ESTAT trials, never US-approved, production discontinued in 2002.

Angiotensin II receptor blocker

Angiotensin II receptor blocker (ARB) is a class of drugs called sartans that lowers blood pressure by blocking angiotensin II receptors. The first was losartan, approved in 1995.

Anisindione

Anisindione (Miradon) is a synthetic oral anticoagulant of the indanedione class that acts as a vitamin K antagonist. It was approved in 1957 and is discontinued.

Anistreplase

Anistreplase (APSAC, Eminase) is an acylated streptokinase-lys-plasminogen thrombolytic complex, given as a 30-unit IV bolus over 2-5 minutes, half-life about 90 minutes, FDA approved 1989 for acute myocardial infarction.

Anivamersen

Anivamersen (RB007, R01J) is an oligonucleotide antidote that reverses the factor IXa-inhibiting RNA aptamer pegnivacogin in the REG1 anticoagulation system; its phase 3 REGULATE-PCI trial was stopped early for allergic reactions.

Anticoagulation reversal

Anticoagulation reversal is the use of specific antidotes and blood products to counteract anticoagulant drugs in major bleeding or before urgent surgery, using agents like idarucizumab and 4F-PCC.

Antithrombin iii human

Antithrombin III (human), also called AT III or antithrombin concentrate, is an intravenous plasma-derived serpin drug (Thrombate III, Atenativ) that treats and prevents thromboembolism in hereditary antithrombin deficiency; heparin boosts its activity about 1000-fold.

Apabetalone

Apabetalone (RVX-208, RVX-000222) is Resverlogix's investigational BD2-selective BET protein inhibitor for atherosclerosis and diabetes; its phase 3 BETonMACE trial missed the primary MACE endpoint but reduced heart failure hospitalization.

Aprocitentan

Aprocitentan (ACT-132577; Tryvio, Jeraygo) is an oral dual ETA/ETB endothelin receptor antagonist, active metabolite of macitentan, approved 2024 for resistant hypertension; PRECISION trial showed -3.8 mm Hg office systolic BP benefit versus placebo, main side effect edema.

Ardeparin sodium

Ardeparin sodium (Normiflo) is a low-molecular-weight heparin made by peroxidative depolymerization of unfractionated heparin, mean MW about 6000 Da, anti-Xa/anti-IIa ratio about 2; US NDA 20-227, withdrawn in 2001 at the manufacturer's request.

Arotinolol

Arotinolol (アロチノロール, Almarl, S-596) is a Japanese third-generation combined alpha/beta-adrenergic blocker (Sumitomo, 1985) used for hypertension, angina, arrhythmia, and essential tremor, with beta potency about eight times its alpha blockade.

ASP1128

ASP1128 (MA-0217) is Astellas/Mitobridge's intravenous selective PPARδ modulator for acute kidney injury after cardiac surgery; its phase 2 trial 1128-CL-0201 missed its primary endpoint and development was discontinued in 2022.

Atenolol

Atenolol (Tenormin, ICI 66,082) is a beta1-selective beta-blocker approved in the US in 1981 for hypertension, angina, and acute myocardial infarction; renal excretion, 6-7 hour half-life, ISIS-1 mortality benefit.

Atrasentan

Atrasentan, sold as Vanrafia and formerly Xinlay, is an oral endothelin A receptor antagonist approved in 2025 to reduce proteinuria in adults with primary IgA nephropathy.

Avosentan

Avosentan, also known as SPP301, is an endothelin receptor antagonist developed for diabetic nephropathy and abandoned after its phase 3 ASCEND trial was stopped early for congestive heart failure.