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The journey of ASPIRIN The journey of aspirin spans millennia—from ancient herbal remedies to an industrial pharmaceutical icon.  Between 3000 and 1500 BC, Sumerians and Egyptians used willow bark to treat pain and inflammation. The Ebers Papyrus confirms its use as a natural analgesic. Around 400 BC, Hippocrates administered willow leaf tea to ease childbirth.  In 1763, Oxfordshire vicar Edward Stone documented willow bark’s fever-fighting effects to the Royal Society. By 1828, Joseph Buchner isolated…

September 29th Discovery of ZN-c5, an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) with Improved Pharmacokinetics https://pubs.acs.org/doi/abs/10.1021/acs.jmedchem.5c00887 Abstract Here, we report our strategy to design an optimized oral selective estrogen receptor degrader (SERD), including human pharmacokinetics, by exploiting the bicyclo[1.1.1]pentane (BCP) ring system. The BCP has been shown to serve as a surrogate for phenyl rings and alkyl groups in drug candidates, reducing metabolism and improving physicochemical properties. It has not been extensively profiled in…

Given the increased volume of orders in Q4, along with busy suppliers and couriers, we highly recommend placing your orders well in advance to ensure timely delivery and avoid any unexpected delays, such as those that may occur in the purchasing department. Please, include enough time to build and optimize the list of compounds to be ordered, negotiate favorable terms with suppliers, and do the paperwork required by your organization internally. To provide you with…

GSK legacy shaped by Beecham’s Pills and Research Laboratories GSK’s earliest roots include Plough Court Pharmacy, founded in London in 1715 by Silvanus Bevan, which later evolved into Allen & Hanburys, well known for its pioneering work in respiratory medicines. However, thanks to Beecham’s Pills, launched in 1842 by Thomas Beecham (1820–1907), the company experienced a tremendous financial boost that drove its early success and enabled its growth into a primary pharmaceutical business. These popular over-the-counter…

From Apothecary to Alkaloid Pioneer: The Origins of Merck and Modern Drug Discovery Did you know that Merck, one of the oldest pharmaceutical companies in the world, played a foundational role in the development of alkaloid chemistry, laying the groundwork for modern medicinal chemistry and compound screening?  The story begins in 1668, when Friedrich Jacob Merck purchased the Engel-Apotheke (Angel Pharmacy) in Darmstadt, Germany. However, the real transformation occurred in 1827, when Heinrich Emanuel Merck…

Toxicology and Preclinical Testing (Animal Models) Today, I would like to share with you the story of another individual who made a remarkable contribution to the history of drug development. The person who laid the basis for modern preclinical animal model tox evaluations was Johann Wepfer (1620–1695).  A Swiss Pioneer of Toxicology and Preclinical Testing (Animal Models).  Long before modern drug development, Wepfer made groundbreaking strides in toxicological analysis. He is best known for his…

June 23rd Characterizing and understanding the formation of cysteine conjugates and other by-products in a random, lysine-linked antibody drug conjugate https://www.tandfonline.com/doi/full/10.1080/19420862.2021.1974150#abstract Abstract This study describes the characterization of conjugation sites for a random, lysine conjugated 2-iminothiolane (2-IT) based antibody-drug-conjugate synthesized from an IgG1 antibody and a duocarmycin analog-based payload-linker. Of the 80 putative lysine sites, 78 were found to be conjugated via tryptic peptide mapping and LC-HRMS. Surprisingly, seven cysteine-linked conjugated peptides were also detected…

May 12th Real Way to Target Gram-Negative Pathogens: Discovery of a Novel Helicobacter pylori Antibiotic Class https://pubs.acs.org/doi/abs/10.1021/acs.jmedchem.5c00112 Abstract In an era of escalating antibiotic resistance, there is a pressing need for innovative strategies to develop novel antibiotics. Gram-negative bacteria, characterized by their robust dual-membrane, are intrinsically resistant to a wide range of antibiotics and can readily develop new resistances. Members of this bacterial class comprise numerous pathogenic organisms, including the primary cause of gastric cancer, Helicobacter pylori. In…

Dose Makes The Poison Today I’d like to tell you about a Swiss gentleman named Paracelsus.  Often called the “father” of modern toxicology and pharmacology, Paracelsus was the first to articulate a principle that still underpins toxicology today: “The dose makes the poison.” He argued that no substance is inherently toxic; it all depends on how much of it you take. Even substances we consider harmful can be beneficial in tiny amounts. Paracelsus famously used…

April 30th Discovery of Daraxonrasib (RMC-6236), a Potent and Orally Bioavailable RAS(ON) Multi-selective, Noncovalent Tri-complex Inhibitor for the Treatment of Patients with Multiple RAS-Addicted Cancers https://pubs.acs.org/doi/abs/10.1021/acs.jmedchem.4c02314 Abstract Oncogenic RAS mutations are among the most common in human cancers. To target the active, GTP-bound state of RAS(ON) directly, we employed an innovative tri-complex inhibitor (TCI) modality. Formation of a complex with an intracellular chaperone protein CypA, an inhibitor, and a target protein RAS blocks effector binding,…