Category: Sci&Tech
Pharmaceutical
Sci&Tech
How to Solve Metabolic Stability Issues in Early Drug Discovery
You’ve designed a molecule with exceptional oral absorption and carefully tuned its physical chemistry to hit the optimal tissue distribution sweet spot. Yet, when you dose it in a rodent model, the drug’s systemic concentration plummets...
Chemical
Pharmaceutical
Sci&Tech
How bench scientist select a reactionsolvent (part-2)
Once you move past simple substitutions and start building carbon-carbon or carbon-nitrogen bonds, the solvent stops being a passive host and becomes a critical referee. In this phase of process chemistry, your choice of solvent is...
Pharmaceutical
Sci&Tech
How to Solve the Drug Distribution Issue in Early Discovery
You’ve optimized your lead molecule for flawless oral absorption and verified that it binds its target with nanomolar potency in biochemical assays. But when you dose it in vivo, the therapeutic effect is completely absent. You check...
Pharmaceutical
Sci&Tech
How to solve oral absorption issues in early drug discovery
1. What is Absorption? In drug discovery, absorption is the process by which a drug transitions from its site of administration (most commonly the gastrointestinal lumen after oral dosing) into the systemic circulation. To achieve this, a dissolved drug...
Chemical
Pharmaceutical
Sci&Tech
How bench scientist select a reactionsolvent (part-1)
You look up a prep in the literature, you see the authors used DCM, so you grab the DCM bottle without a second thought. If the reaction fails, you blame the catalyst, you question the purity...
Molecule Digest
Pharmaceutical
Sci&Tech
The Nonclinical Studies Lead to the First FDA Approved PROTAC-Veppanu
As a PROTAC (Proteolysis-Targeting Chimera), vepdegestrant represents a novel class of heterobifunctional degraders, and its non-clinical package focused heavily on its unique mechanism and potential for off-target effects. Based on the FDA approval documentation for VEPPANU...
Pharmaceutical
Regulation
Sci&Tech
VEPPANU A Breakthrough of PROTAC
The drug ARV-471, now known by its generic name vepdegestrant and brand name VEPPANU, has made history. As of May 1, 2026, it became the first-ever PROTAC (Proteolysis-Targeting Chimera) to receive FDA approval. Discovered through the pioneering work at Arvinas and detailed in...
GLP
Pharmaceutical
Sci&Tech
The challenges and solutions of testing peptide drugs in Ames assay
The Ames assay (OECD 471) is the standard first step for genotoxicity screening. However, testing a peptide drug in an Ames assay is technically challenging because the assay was originally designed for small, stable, non-nutritional chemicals. When...
Pharmaceutical
Sci&Tech
The comparison of the two FDA approved aptamers
The two FDA-approved aptamer drugs, Macugen (pegaptanib) and Avacincaptad Pegol (ZIMURGA), represent two distinct generations in pharmaceutical history. Macugen, approved in 2004, was the pioneer—the first aptamer to market—but ultimately lost its dominance in the Wet AMD market to more...
Chemical
Pharmaceutical
Sci&Tech
Aptamer Drug Development Status and Pipeline
The development of therapeutic aptamers has evolved from a niche technology challenged by pharmacokinetic (PK) issues (stability and renal clearance) to a robust platform. While only two RNA aptamers are currently FDA-approved, the pipeline contains dozens...