
The Module 2, Section 2 lecture introduces the druggable interactome, compiling key resources that map the human druggable genome, protein expression, kinase families, transcription‑factor proteomics, GPCRs, and ion‑channel complexes. It highlights quantitative estimates—over 3,000 proteins deemed druggable and hundreds of actionable kinases—while linking these datasets to disease relevance. The slide deck cites seminal literature that underpins current target‑identification strategies and points to emerging analytical methods for deeper interactome coverage. Together, these references form a roadmap for systematic target discovery across multiple protein families.

The January 2026 Patent Highlights roundup spotlights a wave of new intellectual‑property activity across several cutting‑edge drug discovery areas. Notable filings include lysine‑directed covalent inhibitor chemotypes, strategies to balance potency with drug‑like properties, refined target‑selection frameworks, dozens of Polθ synthetic‑lethal patents...

Dotinurad (FYU‑981), marketed as Urece®, is a URAT1 inhibitor approved for gout and hyperuricemia in Japan and China. The drug was chemically refined from the older uricosuric benzbromarone to retain potency while eliminating rare hepatotoxic events. Crystalys Therapeutics is now...

Balancing potency with oral bioavailability remains a core hurdle as drug candidates grow larger and more complex. Researchers now focus on "chameleonicity"—the ability of a molecule to toggle between polar and lipophilic conformations—to reconcile solubility and permeability. The article outlines...

The module outlines a five‑dimensional framework for target selection, linking biological relevance, drugability, disease impact, competitive landscape, and development risk. It contrasts first‑in‑class and best‑in‑class strategies, highlighting how pioneering mechanisms can command premium market positions. The content identifies oncology as...

Vanda Pharmaceuticals received FDA approval for tradipitant (Nereus®), an oral selective NK1 receptor antagonist, to treat motion‑induced nausea and vomiting. The approval marks the first new drug for motion sickness in more than four decades, highlighting a significant regulatory milestone....

Aceclidine (Vizz®) received FDA approval in 2025 as an ophthalmic solution for presbyopia, targeting age‑related near‑vision loss. The drug acts as a pupil‑selective muscarinic agonist, inducing miosis without significant ciliary muscle activity, thereby enhancing depth of focus through a pinhole...

The article outlines a growing strategy to develop central nervous system (CNS) therapeutics that remain pharmacologically active only within the brain, termed "BrainOnly" pharmacology. By leveraging selective transport mechanisms, pro‑drug designs, and peripheral clearance pathways, researchers aim to minimize off‑target...

The lipid serine hydrolase PNPLA3, especially its I148M mutant, has emerged as a genetically validated driver of MASLD/MASH, prompting a wave of genotype‑focused drug programs. RNA‑based modalities—Arrowhead’s GalNAc‑siRNA ARO‑PNPLA3 and AstraZeneca/Ionis’ GalNAc‑ASO AZD2693—are in clinical trials aiming to lower mutant...

Deciphera Pharmaceuticals received FDA approval for vimseltinib, an oral, selective CSF1R kinase inhibitor, to treat tenosynovial giant cell tumor (TGCT). The drug emerged from structure‑based drug design (SBDD) and extensive SAR optimization, as reported in Bioorganic & Medicinal Chemistry Letters...

Targeted protein degraders that eliminate the transcription factors WIZ and ZBTB7A are shown to raise fetal hemoglobin (HbF) levels, offering a disease-modifying strategy for sickle cell disease and β‑thalassemia. Novartis disclosed a series of CRBN‑based glue degraders, culminating in the...

Drug Hunter has launched a Module 1 Quiz to evaluate learners’ grasp of introductory drug‑discovery concepts. The quiz spans all sections of the first module and is accessible through the platform’s subscription model. Users can take the assessment after reviewing the...

The article outlines modern methods for identifying drug repurposing opportunities, focusing on neurodegenerative diseases such as Alzheimer’s and Parkinson’s. It highlights computational screening, network pharmacology, and real‑world evidence as core techniques, and presents case studies where existing drugs showed disease‑modifying...

Recent disclosures illustrate how multimeric design is reshaping drug discovery in the beyond‑Rule‑of‑5 (bRo5) space. GSK’s dimeric BET inhibitor GSK785 uses a rigid diazaspiro linker to achieve >30‑fold BRD4 selectivity, while Eli Lilly’s muvalaplin dimer‑to‑trimer architecture delivers a 10,000‑fold potency boost...

The blog post emphasizes dose as a pivotal factor distinguishing first‑in‑class from next‑generation therapeutics. It links total dose and dosing regimen to core drug attributes such as potency, pharmacokinetics, and safety. The discussion covers route of administration, dosing schedules, and...