Latest research
Drug Brand Switching: A Regulatory Perspective
in Drug SafetyThe replacement of expensive medications marketed by companies that bore the cost of development and testing, by low-cost “generics” once patent protection ends, is a common step in the life cycle of most drugs. Although generics are required to...
Vepdegestrant: the first FDA-approved oral PROTAC and a milestone in targeted protein degradation
Vepdegestrant (ARV-471, Veppanu) represents an important milestone in targeted protein degradation (TPD) as the first FDA-approved heterobifunctional proteolysis-targeting chimera (PROTAC). Designed to selectively degrade estrogen receptor α (ERα)...
Personalized drug discovery from rare diseases to cancer
Precision medicine selects individual treatments from a small toolbox of therapies already available. Personalized drug discovery (PDD) brings this concept one step ahead, developing drugs for individual patient’s diseases. Currently, PDD is being...
Exploring Novel Strategies for Improving the Bioavailability of Docetaxel
In today’s world, research has evolved a lot in the field of cancer and docetaxel (DTX) has been intensively studied for its ability to cure different types of cancers. However, the intravenous delivery of DTX puts forth various undesirable side...
A Strategic Formulation to Enhance the Safety and Anti-Hyperlipidaemic Activity of Simvastatin: Prototype Development
Statins are widely regarded as the gold standard first-line treatment for hyperlipidemia, as they inhibit HMG-CoA reductase in the liver. This effectively reduces LDL cholesterol levels and reduces cardiovascular risks, such as heart attack and...
In-Silico Identification and Molecular Dynamics Characterization of FDA-Approved Drug Candidates Targeting MAO-B for Parkinson’s Disease Drug Repurposing
Parkinson’s disease (PD) is characterized by striatal dopamine depletion, a process exacerbated by upregulation of monoamine oxidase B (MAO-B), whose activity accelerates dopamine catabolism and contributes to oxidative stress. This computational...
The application, development and challenge of digital twin in drug evaluation
With the improvement of computational resources and development of artificial intelligence, current digital twins (DT) can achieve the integration of multi-omics data via hybrid mechanism- and data-driven models, thereby enabling personalized...
Camizestrant: First Approval
in DrugsCamizestrant (Etcamah®) is an orally available, potent selective estrogen receptor degrader (SERD) and complete estrogen receptor (ER) α antagonist being developed by AstraZeneca for the treatment of breast cancer. It received its first approval in...
Real-world Italian experience with asciminib in chronic myeloid leukaemia–chronic phase: case series and drug profile overview
Asciminib selectively targets the myristoyl pocket of ABL1, offering high specificity and a potentially improved safety profile. Its efficacy has been demonstrated in both clinical trials and real-world settings, including heavily pretreated...
Design, synthesis, SAR, in silico and in vitro evaluation of 1, 3, 4-oxadiazole derivatives against breast cancer
The 1,3,4-oxadiazole scaffold is well recognized for its anticancer potential. Based on our previous work, we designed and synthesized nine 1,3,4-oxadiazole derivatives (R1–R9) viaSchiff base formation followed by cyclization. The compounds were...
Synthesis of Imidazole-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine-Linked 1,2,3-Triazole Hybrids as Potent EGFR-Targeting Anti-Lung Cancer Agents
Abstract Objective: This study describes the design, synthesis, and biological evaluation of novel imidazole-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine-1,2,3-triazole hybrids acting as potent inhibitors of the epidermal growth factor receptor (EGFR)...
Development of an isavuconazole physiologically-based pharmacokinetic model for adult and pediatric populations
Isavuconazonium sulfate is the water-soluble prodrug of the active triazole antifungal agent isavuconazole. Isavuconazonium sulfate is approved for the treatment of invasive aspergillosis and invasive mucormycosis in pediatric and adult populations....
Temporal Trends and Predictors of P2Y12 Inhibitor Selection and Switching Following Percutaneous Coronary Intervention in Acute Coronary Syndrome Patients
Introduction Dual antiplatelet therapy (DAPT) with aspirin and a P2Y12 inhibitor is standard care after percutaneous coronary intervention (PCI) for acute coronary syndrome (ACS). While ticagrelor provides potent ischemic protection, bleeding risk,...
Targeting type 2 diabetes mellitus through novel thiazolidinedione derivatives: design, synthesis, and integrated biological evaluation
The present study aimed to design, synthesize, and evaluate a series of novel thiazolidinedione derivatives (4a–4f) as potential anti-diabetic agents targeting peroxisome proliferator-activated receptor gamma (PPAR-γ). The synthesized...
The evolving landscape of drug targets
Since the turn of the century, drug discovery has been transformed by advances in genetics, genomics and proteomics, as well as automation, data science and the diversification of therapeutic modalities beyond synthetic small molecules and natural...
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