Belonging to the category of oral dihydropyridine calcium channel blockers, amlodipine's development traces back to a comprehensive pharmacological study initiated in 1964 in the laboratory of renowned scientist Dr. Paul Godfraind. Pfizer, a leading pharmaceutical company, spearheaded the discovery of amlodipine and successfully secured its patent in 1982 (US patent 4,572,909), marking a significant milestone in cardiovascular medicine.
In the initial stages of drug development, Pfizer explored the feasibility of using a maleate salt form of amlodipine. However, due to inherent challenges related to instability and manufacturing, this approach was discontinued. Undeterred, Pfizer's research team diligently pursued alternative formulations, eventually culminating in the development of the besylate salt form, commercially known as Norvasc, which debuted in 1990. The decision to focus on besylate salt was vindicated by its superior attributes, including enhanced solubility, stability, non-hygroscopicity, and ease of manufacturing, as highlighted in the patent filed in 1986 (US patent 4,879,303). This breakthrough paved the way for amlodipine's widespread adoption and regulatory approval by the FDA in 1987.
Since its approval for medical use in 1990, amlodipine has garnered recognition as an essential medication, earning a coveted spot on the World Health Organization's Essential Medicines List. Its inclusion underscores its clinical efficacy and public health significance. Remarkably, amlodipine's impact extends beyond regulatory recognition, evident in its remarkable prescription statistics. In 2021 alone, amlodipine emerged as the fifth most prescribed medication in the United States, with healthcare professionals issuing over 73 million prescriptions, reaffirming its pivotal role in managing cardiovascular disorders and improving patient outcomes.
Amlodipine: Discovery and Development
