Search Results for: thalidomide

Thalidomide

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Thalidomide was a racemic therapeutic and prescribed to pregnant women to control nausea and vomiting. The drug was withdrawn from world market when it became evident that the use in pregnancy causes phocomelia (clinical conditions where babies are born with deformed hand and limbs). Later in late 1970s, the thalidomide enantiomers were separated and enantioselective studies indicated that the (R)- enantiomer, the good partner, is an effective sedative, the (S)-enantiomer, the evil partner, harbors teratogenic …

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Thalidomide tragedy: the story and lessons …

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In the 1940s and early 1950s, pregnant women throughout the world who experienced morning sickness and other anxieties associated with the first term of pregnancy were given barbiturate sedatives for relief. The issue with these barbiturates, like most sedatives, was the fact that they were highly toxic in large doses. In 1957, Chemie Grunenthal of Germany launched thalidomide as a safer alternative to barbiturate sedatives. Thalidomide, as a new sedative, was a very “attractive” drug …

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Episode 4: Technology as Catalyst: How Science Enabled the Regulatory Transformation

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Tagline: “When scientific precision sharpened, so did regulatory vision -technology became the bridge between molecules and medicine.” Introduction The regulatory awakening around chiral drugs in the 1990s did not occur in isolation. It was powered, almost inevitably, by remarkable scientific and technological breakthroughs. Before sophisticated tools existed, distinguishing and isolating enantiomers was labor-intensive, error-prone, and prohibitively expensive. It was the advent of new chemical, analytical, and bioanalytical technologies that made the regulatory demands for stereochemical …

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Episode 2: The Great Shift: How the 1990s Redefined Stereochemical Standards

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“When regulators caught up with science, a quiet molecular revolution began – changing the future of drug development forever.” Introduction The 1990s represent a pivotal decade in pharmaceutical regulation, where long-overlooked nuances of molecular chirality finally received the attention they deserved. Before this era, enantiomers in drug substances were treated as interchangeable entities, with few regulatory frameworks requiring detailed evaluation of each stereoisomer. However, accumulating scientific evidence, technological advances, and a few high-profile pharmaceutical tragedies …

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Episode 1: When Mirror Images Mattered: A Historical Prelude to Chiral Drug Regulation

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“Before the world looked closely at molecular mirror images, the pharmaceutical landscape was filled with blind spots -this is the story of how chirality found its voice.” Introduction The phenomenon of chirality, where molecules exist as non-superimposable mirror images, permeates the natural world. In biological systems, chirality is fundamental: proteins, enzymes, and receptors are inherently stereospecific, responding differently to the two mirror-image forms, or enantiomers, of a compound. In pharmacology, these subtle molecular differences can …

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Chiral Pharmacology: The Mirror Image of Drug Development

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Abstract Chiral pharmacology, which studies how different enantiomers (mirror-image forms of molecules) affect the body, has truly changed the landscape of pharmaceutical science. It highlights the importance of stereochemistry – the three-dimensional structure of molecules – in making drugs safer and more effective. Today, over half of modern medicines are chiral, but in the past, many were given as racemic mixtures (a blend of enantiomers), leading to unpredictable results. This article delves into the fascinating …

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Part 5. The Future of Chirality: Challenges and Innovations

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As the study of chirality enters its next phase, it remains at the forefront of scientific exploration, bridging disciplines such as chemistry, biology, pharmacology, and material science. The journey from its foundational discoveries to the transformative breakthroughs in asymmetric synthesis and pharmaceutical applications has established chirality as a fundamental concept in understanding and manipulating molecular asymmetry. This final chapter provides a holistic summary of chirality’s journey, its underpinnings, and where it is headed in the …

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P3. Chirality in Medicine: From Discovery to Disaster

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The intersection of chirality and medicine is a compelling narrative that reveals both the promise and peril of molecular asymmetry. From its earliest applications in pharmacology to the tragic consequences of overlooking enantiomeric differences, the role of chirality in medicine underscores the profound impact of stereochemistry on human health. This chapter delves into the breakthroughs, challenges, and lessons learned as chirality became a cornerstone of drug development. Early Discoveries: The Physiological Impact of Chirality The …

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P1. The Origins of Chirality: From Light to Life

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Lead Chirality – a concept rooted in the mirror-image asymmetry observed in nature – stands as a cornerstone of chemistry and pharmaceutical sciences. This journey begins in the early 19th century, where the interplay of physics, chemistry, and biology unveiled the mysterious world of chiral molecules. These pioneering explorations profoundly changed our understanding of molecular structures and their pivotal roles in biological and pharmaceutical applications. Étienne-Louis Malus: The First Step into the Polarized World In …

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Breaking Down the Methods: Chromatography and Crystallization in Chiral Resolution

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Lead Chiral resolution, the process of separating enantiomers, is crucial in various fields such as pharmaceuticals, agrochemicals, and food industries. Chirality, as discussed in previous sections, involves molecules that are mirror images of each other but cannot be superimposed. This seemingly subtle difference leads to enantiomers having different biological, chemical, and pharmacological properties. The importance of chiral resolution has increased, especially in pharmaceutical industries, where the efficacy and safety of drugs can vary dramatically between …

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