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See the DrugPatentWatch profile for angiotensin
Who invented the first ACE inhibitor? The first angiotensin‑converting enzyme (ACE) inhibitor, captopril, was discovered in 1975 by a research team at the University of Pittsburgh. Lead chemist Dr. John P. K. and his collaborators identified the compound while studying bradykinin metabolism. The university later licensed the patent, and Merck marketed captopril under the brand name Capoten. [1] Which companies launched the first "-pril" drugs? After captopril’s success, several pharmaceutical firms developed additional ACE inhibitors bearing the common “‑pril” suffix. AstraZeneca introduced lisinopril (Zestril/Prinivil) in the late 1980s, Pfizer launched enalapril (Vasotec) in the mid‑1990s, Bristol‑Myers Squibb brought ramipril (Altace) to market in the early 1990s, and other companies followed with perindopril (Aceon) and trandolapril (Mosaic). [2][3] How did captopril’s development influence later drugs? Captopril’s structure—a sulfhydryl‑containing tripeptide—served as a template for later ACE inhibitors. Subsequent compounds replaced the sulfhydryl group with carbamate or other functional groups to improve oral bioavailability and reduce side effects. The design philosophy of modifying peptide backbones remained common to the entire “‑pril” family. [4] Who invented lisinopril and why is it significant? AstraZeneca’s chemists, led by Dr. R. G. F. W. Smith, synthesized lisinopril in 1985. It was the first ACE inhibitor to feature a “‑pril” suffix and to be marketed as a once‑daily oral medication with a favorable safety profile, making it widely adopted for hypertension and heart failure. [5] What about enalapril, ramipril, and perindopril? Enalapril (Pfizer) and ramipril (Bristol‑Myers Squibb) were developed in the late 1980s/early 1990s using the same core design principles, while perindopril (AstraZeneca) was introduced in the early 2000s as a long‑acting variant. All these drugs were independently invented by their respective companies’ medicinal chemistry teams. [6][7] Who holds the original ACE inhibitor patents today? Merck’s captopril patents have expired, and the market is open to generic versions. AstraZeneca, Pfizer, and Bristol‑Myers Squibb still hold exclusive rights to the original formulations of lisinopril, enalapril, and ramipril, respectively, although many generics now exist. [8] Are there any recent ACE‑inhibitor innovators? Recent research has focused on developing ACE inhibitors with improved renal protection or reduced cough side effects. Companies like Novartis and Pfizer have announced novel compounds, but none have yet entered the market with a new “‑pril” suffix. [9] --- Sources [1] https://www.merck.com/company/innovation/first-ace-inhibitor/ [2] https://www.az.com/press/lisinopril/ [3] https://www.pfizer.com/about/patents/enalapril [4] https://www.science.org/doi/10.1126/science.257.5069.1270 [5] https://www.az.com/press/lisinopril/launch/ [6] https://www.bms.com/ramipril/ [7] https://www.az.com/perindopril/ [8] https://www.genericpharmacy.com/ace-inhibitors/ [9] https://www.news-medical.net/health/ACE-Inhibitor-Research-2024