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Cardiovascular drugs

273 articles

Reserpine

Reserpine, an alkaloid of Rauwolfia serpentina isolated at Ciba in 1952 (brand Serpasil), was the first widely used long-term antihypertensive and an early antipsychotic; it lowers systolic pressure about 8 mmHg but is now withdrawn in the US.

Reteplase

Reteplase (r-PA, Rapilysin) is a nonglycosylated recombinant tPA deletion mutant thrombolytic with kringle-2 and protease domains, given as two 10-unit boluses 30 minutes apart; FDA-approved 1996 for myocardial infarction, EU authorization withdrawn 2024.

Rilmenidine

Rilmenidine (Hyperium) is an imidazoline I1-receptor agonist antihypertensive, 1–2 mg once daily, not available in the US; effective in mild-to-moderate hypertension with less sedation and no rebound than clonidine.

Riociguat

Riociguat (Adempas, BAY 63-2521) is Bayer's oral first-in-class soluble guanylate cyclase stimulator, FDA-approved 2013 for pulmonary arterial hypertension and as the first drug therapy for inoperable or persistent/recurrent CTEPH.

Sacubitril allisartan calcium tablets

Sacubitril allisartan calcium tablets (沙库巴曲阿利沙坦钙片, 信超妥) are Salubris's ARNI co-crystal of sacubitril and allisartan for primary hypertension; first Chinese-developed ARNI, second globally, approved May 2025, dosed 240 mg once daily.

Satavaptan

Satavaptan (SR 121463, Aquilda) is a Sanofi-developed, highly selective vasopressin V2 receptor antagonist (vaptan class) for hyponatremia and cirrhotic ascites; it raised serum sodium in trials but failed phase III endpoints, showed higher mortality with diuretics, and was withdrawn in 2008, never approved.

Selatogrel

Selatogrel (ACT-246475) is an investigational reversible P2Y12 inhibitor given subcutaneously, in Phase 3 (SOS-AMI, NCT04957719) for self-administration at suspected heart attack; developed by Idorsia, now Viatris.

Selexipag

Selexipag (Uptravi, ACT-293987, NS-304) is an oral, non-prostanoid prostacyclin IP receptor agonist prodrug for pulmonary arterial hypertension, hydrolyzed to ACT-333679; approved 2015 after the GRIPHON trial.

Semuloparin sodium

Semuloparin sodium (AVE5026, Mulsevo) is Sanofi's ultra-low-molecular-weight heparin (2000-3000 Da, anti-Xa:anti-IIa >30:1) for VTE prevention; effective in SAVE-ONCO and hip replacement trials, but its EU application was withdrawn in 2012.

Seralutinib

Seralutinib (GB002, PK10571) is Gossamer Bio's inhaled tyrosine kinase inhibitor targeting PDGFRα/β, CSF1R, and cKIT for pulmonary arterial hypertension; phase 2 TORREY met its PVR endpoint, phase 3 PROSERA missed its prespecified alpha, and an NDA is planned for September 2026.

Serelaxin

Serelaxin (recombinant human relaxin-2) is an intravenous vasodilatory peptide drug trialed for acute heart failure in the RELAX-AHF and RELAX-AHF-2 trials, with conflicting mortality evidence.

Sildenafil

Sildenafil (Viagra, Revatio) is a Pfizer-developed PDE5 inhibitor, first synthesized as UK-92,480 in 1989 for angina, approved March 27, 1998 as the first oral erectile dysfunction treatment, later repurposed for pulmonary arterial hypertension.

SILVHIA trial

SILVHIA (Swedish Irbesartan Left Ventricular Hypertrophy Investigation versus Atenolol), NCT00389168: Swedish double-blind trial in 115 hypertensive patients with LVH; irbesartan reduced left ventricular mass more than atenolol (-26 vs -14 g/m2) despite equal blood pressure control.

Sitaxentan

Sitaxentan (sitaxsentan, Thelin), a selective endothelin-A receptor antagonist for pulmonary arterial hypertension, 100 mg once daily; withdrawn worldwide in December 2010 after fatal idiosyncratic liver injury.

Sitokiren

Sitokiren (SPH3127, Sintolan, Xintuoan) is an oral non-peptide direct renin inhibitor developed by Shanghai Pharmaceuticals; approved in China 9 December 2025 for hypertension, noninferior to valsartan in a phase III trial.

Sotalol

Sotalol (Betapace, Sotylize) is a racemic Class II/III antiarrhythmic, beta-blocker and I_Kr blocker approved in the US in 1992 for ventricular arrhythmias and AF rhythm control, with QT-prolongation and torsades risk requiring monitored initiation.

Sotatercept

Sotatercept (Winrevair, ACE-011) is a first-in-class activin signaling inhibitor, a fusion protein approved in the United States in March 2024 to improve exercise capacity in pulmonary arterial hypertension.

Spirapril

Spirapril (Renormax, SCH-33844) is a non-sulfhydryl ACE inhibitor prodrug hydrolyzed to active spiraprilat; 50% oral bioavailability, dual renal-hepatic elimination, 6 mg once daily for hypertension; FDA-approved 1994, discontinued in North America.

Spironolactone

Spironolactone (Aldactone) is a steroidal mineralocorticoid receptor antagonist and potassium-sparing diuretic discovered at Searle in the 1950s, launched 1960, used for edema, hypertension, heart failure, and PCOS, with hyperkalemia and gynecomastia as key risks.

SRSD107

SRSD107: investigational long-acting GalNAc siRNA by Sirius Therapeutics (靖因药业) targeting factor XI mRNA for anticoagulation; Phase 2 VTE and CAD/PAD trials, co-developed with CRISPR Therapeutics.

Streptokinase (drug)

Streptokinase, a 47 kDa protein from beta-hemolytic streptococci (S. equisimilis H46A), is the first plasminogen-activator thrombolytic drug, discovered by Tillett in 1933, dosed at 1.5 million IU IV, and still the low-cost (~US$200) clot-buster of developing countries.

Strophanthin

Strophanthin is a family of steroidal cardiac glycosides extracted from Strophanthus vine seeds, historically used as injectable drugs for heart failure and including ouabain, still used in the laboratory to inhibit the sodium pump.

Succinobucol

Succinobucol (AGI-1067), a monosuccinate ester of probucol developed by AtheroGenics, is an antioxidant anti-inflammatory drug candidate for atherosclerosis that reached Phase 3 (ARISE) without approval.

Suloctidil

Suloctidil (Sulocton, Duolcitil), a peripheral vasodilator and antiplatelet propanolamine drug introduced in 1975 for arterial disease and withdrawn worldwide in the mid-1980s after hepatitis deaths.

Sulodexide

Sulodexide (Vessel, KRX-101) is an orally active glycosaminoglycan drug, 80% fast-moving heparin and 20% dermatan sulfate, used for venous thromboembolism prevention, chronic venous disease, and peripheral arterial disease.

Tamsulosin

Tamsulosin, marketed as Flomax and generics, is a selective alpha-1 adrenoceptor antagonist used to treat benign prostatic hyperplasia, an enlargement of the prostate obstructing urine flow.

Tecarfarin

Tecarfarin (ATI-5923), an investigational oral vitamin K antagonist anticoagulant inhibiting VKORC1 like warfarin but metabolized by carboxylesterases instead of CYP450; phase 3, not approved.

Tedisamil

Tedisamil (KC-8857), a class III antiarrhythmic potassium channel blocker developed as a bradycardic agent; intravenous tedisamil converts recent-onset atrial fibrillation to sinus rhythm in about half of patients, with torsade de pointes as the main risk.

Telcagepant

Telcagepant (MK-0974) was Merck's first oral CGRP receptor antagonist (gepant) for acute migraine, with efficacy comparable to zolmitriptan but no vasoconstriction; development was discontinued in 2011 over hepatotoxicity in daily-dosing prophylaxis trials.

Telmisartan

Telmisartan (MICARDIS) is an angiotensin II receptor blocker approved in 1998 for hypertension and cardiovascular risk reduction, distinguished among ARBs by partial PPARγ agonism, high lipophilicity, and biliary elimination.