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Under-representation of elderly in clinical trials: An analysis of the initial approval documents in the Food and Drug Administration database.

AIMS: To evaluate the availability of pharmacokinetic, safety and efficacy analyses specifically targeted at elderly, prior to the authorization of drugs. METHODS: A cross-sectional, structured review of publicly available initial approval documents of Food and Drug Administration-approved drugs was performed. The 10 most frequently on-label prescribed drug classes, drugs with known pharmacokinetic differences in the elderly or drugs that are relatively contraindicated in elderly (e.g. anticholinergics or benzodiazepines) were included in the analyses. RESULTS: In total, 1129 unique active p

Lasmiditan in Migraine Management: An Advanced Review of Its Pharmacological Paradigm, Clinical Applications, Safety Considerations, Drug Interaction Spectrum, and Regulatory Approval.

This review offers an in-depth evaluation of Lasmiditan, a novel and selective 5-HT1F receptor agonist, representing a significant breakthrough in migraine pharmacotherapy. Unlike existing reviews, this article consolidates all critical aspects of Lasmiditan into a single, authoritative source encompassing both extensive literature analysis and original findings from our laboratory to provide researchers and clinicians with streamlined access to essential data and minimize the need for exhaustive literature searches.The review provides a comprehensive assessment of Lasmiditan, highlighting its

HBV Drug Resistance Substitutions Existed before the Clinical Approval of Nucleos(t)ide Analogues: A Bioinformatic Analysis by GenBank Data Mining.

Naturally occurring nucleos(t)ide analogue resistance (NUCr) substitution frequencies in the reverse transcriptase (RT) of the hepatitis B virus (HBV) were studied extensively after the clinical approval of nucleos(t)ide analogues (NUCs; year of approval 1998). We aimed to study NUCr substitutions in HBV RT sequences obtained before 1998 and better understand the evolution of RT sequences without NUC pressures. Our strategy was to retrieve HBV sequences from GenBank deposited before 1998. The initial search used the keywords "hepatitis B virus" or "HBV" and 1139 sequences were found. Data anal

Comparison of Labeled Dosages Between Japan and the United States for Drugs Approved in Japan from 2020 to 2025.

INTRODUCTION: Although approved doses in Japan have generally been lower than in Western countries, these differences have been diminished with global drug development. Studies evaluating dose differences between Japan and the United States (US) using post-2010 data are limited, and none have focused on the 2020s. METHODS: This study characterized labeled dosage differences between Japan and the US for new molecular entities approved during 2020-2025. Major differences were defined as a ≥2-fold difference in the maintenance or maximum dose; all others were classified as minor differences. RE

Blockbuster drugs and forecast accuracy: How sponsor type is associated with commercial success of FDA-approved medicines.

We evaluated the commercial performance of 490 FDA-approved new molecular entities (NMEs) and biologic products approved from 2016 through 2025 against analyst forecasts, testing the hypothesis that only a small proportion of approved drugs have the potential to generate substantial returns for their sponsors. We demonstrate that analyst forecasts are subject to considerable limitations, with systematic overestimation of sales particularly prevalent for drugs with biotech sponsors. We further identify a strong association with large, established pharmaceutical companies and their ability to se

Emrelis for c-Met Positive NSCLC: A Breakthrough in Antibody-Drug Conjugate-based Treatment Approved by the FDA.

Telisotuzumab Vedotin (Teliso-V), previously known as ABBV-399, is a novel, first-in-class antibodydrug conjugate developed by AbbVie. It combines an anti-c-Met monoclonal antibody (ABT-700) with monomethyl auristatin E (MMAE), a potent microtubule-disrupting agent, via a cleavable linker. This design allows selective delivery of the cytotoxic payload to c-Met-overexpressing tumour cells, thereby bypassing reliance on MET signalling for efficacy. Preclinical studies demonstrated that ABBV-399 effectively inhibited the growth of xenograft tumors refractory to other MET-targeted inhibitors. In e

Clinical value and cost-effectiveness analysis of conditionally approved anticancer drugs in China from 2015 to 2023.

BackgroundThe conditional approval (CA) process in China was established in 2015 to expedite access to urgently-needed drugs, however, the clinical benefits of CA drugs and potential gaps between pre-approval and confirmatory trials remain uncertain. Herein, we aim to compare the clinical values between CA and non-CA anticancer drugs from 2015 to 2023, and to explore the relationship between clinical benefit and average daily cost of treatment of drugs.MethodsThis retrospective study analyzed anticancer drugs first approved in China [2015-2023] using data from National Medical Products Adminis

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… to collect the latest results of these pivotal clinical trials supporting drug approval. … Table 1 Characteristics of pivotal trials for anticancer drugs approved in China Data are presented as n (%). …

A network-driven computational framework for identifying FDA-approved drug repurposing across heterogeneous brain cancers.

BACKGROUND: Brain cancers are notorious for their heterogeneity, which complicates therapeutic decisions because of recurrently dysregulated signaling pathways. Cancer system characterizations have allowed the identification of some key components involved in brain cancer, such as the epidermal growth factor receptor, BRAF, platelet-derived growth factor receptor alpha, TP53, O6-methylguanine-DNA methyltransferase, cyclin-dependent kinase 1/2/3/4, cyclooxygenase 1/2, vascular endothelial growth factor receptor 2, telomerase reverse transcriptase, and CYP2D6, along with the U87 cell line. These

Trends in drug discovery for carbonic anhydrases: FDA approvals, clinical trials, molecular functions, and therapeutic potential.

Human carbonic anhydrases (CAs) catalyse the rapid conversion of CO₂ and bicarbonate, supporting pH balance, ion transport and many metabolic processes. All 15 human CA family proteins share a conserved structure, but they differ in activity, localisation and tissue distribution. Several CA isozymes are directly linked to distinct clinical conditions. Although CA-inhibiting drugs have long been clinically used, research across individual isozymes, chemical compound classes, and therapeutic uses has progressed unevenly. This review brings together current structural, biochemical and pharmacolog

Usefulness of the sulfonamide motif in medicinal chemistry: exploring the pharmacological landscape of FDA-approved and investigational sulfonamide drugs.

The sulfonamide motif is widely used in the design of small molecules owing to its enzymatic stability but also its potentiality to improve target engagement and to provide a beneficial ADME profile. From the commercialization of Prontosil® in 1933 until 2023, a total of 91 compounds containing a sulfonamide moiety have received approval from the FDA. In parallel, analysis of the ChEMBl database revealed that 200 sulfonamide-containing compounds have entered clinical trials between 1998 and 2023. This review aims to present an exhaustive assessment of the sulfonamide motif in approved and inve

An integrated in silico and SPR-based workflow identifies FDA-approved drugs as previously unrecognized SIRT3 binders.

Ataxia-Telangiectasia (AT) is a rare disorder characterized by ATM deficiency and mitochondrial dysfunction. Because SIRT3 contributes to mitochondrial homeostasis in ATM-deficient settings, it represents a relevant molecular context for repurposing-oriented target-engagement studies. Here, we present an integrated computational and biophysical workflow designed to identify experimentally tractable SIRT3 binders within a clinically approved chemical space. A curated dataset of 2342 FDA-approved drugs was screened using hierarchical GNINA-based virtual screening, SAveRUNNER network analysis, tr

Rebamipide (Mucosta®), a clinically approved drug, alleviates neuroinflammation and dopaminergic neurodegeneration in a Parkinson's disease model.

BACKGROUND: Parkinson's disease (PD) is characterized by dopaminergic neuron loss, neuroinflammation, and motor dysfunction. PD is a multifactorial disease, with neuroinflammation driven by NLRP3 inflammasome activation representing an important component of its pathological progression. Therefore, we aimed to evaluate the therapeutic potential of rebamipide (Mucosta®), a clinically approved anti-inflammatory agent, in PD by targeting the NLRP3 inflammasome. Specifically, we examined the effects of rebamipide on neuroinflammation, dopaminergic neuron preservation, and motor deficits using BV2

Current landscape of US Food and Drug Administration use of expedited regulatory approvals for colorectal cancer care.

BACKGROUND: US Food and Drug Administration (FDA) expedited regulatory pathways (ERPs) accelerate the availability of drugs and diagnostic tests for severe conditions and fill unmet medical needs. ERPs accelerate access to new therapeutics but also increase the uncertainty of the benefits of available treatments. OBJECTIVE: To examine how ERPs have influenced the landscape of pharmaceutical treatments for colorectal cancer (CRC), one of the most common forms of cancer in the United States. METHODS: This cross-sectional study used data from public FDA records on all CRC drug approvals before …

Machine learning guided virtual screening of FDA approved drugs targeting GSK-3β in Alzheimer's disease.

Alzheimer's disease (AD) remains one of the most challenging neurodegenerative disorders, with limited therapeutic options and high failure rates in clinical trials. This work developed a drug repurposing pipeline powered by a machine learning (ML) model to find possible glycogen synthase kinase-3 beta (GSK-3β) inhibitors, a crucial target in AD pathogenesis. We selected, pre-processed, and optimized a dataset of 4,087 experimentally verified GSK-3β inhibitors using dimensionality reduction and descriptor creation. The most excellent prediction performance was obtained by Random Forest (100 de

Resmetirom: The First FDA-Approved Drug for Metabolic Dysfunction-Associated Steatohepatitis (MASH) with a Perspective on Precision Medicine.

Metabolic dysfunction-associated steatohepatitis (MASH) is a progressive form of metabolic dysfunction-associated steatotic liver disease (MASLD) involving hepatocyte destruction, inflammation, and typically pericellular fibrosis, potentially progressing to cirrhosis. Resmetirom, a T3 analogue and an oral agonist of thyroid hormone receptor-β(THR-β), represents a significant advancement in targeted drug therapy for MASH as the first US Food and Drug Administration (FDA)-approved treatment. Clinical trials have shown that resmetirom effectively improves MASH markers, reduces liver fat content,

Reporting of immune-related adverse events in US Food and Drug Administration approvals of immune checkpoint inhibitors.

BACKGROUND: Predicting the occurrence of immune-related adverse events (irAEs) related to immune checkpoint inhibitors (ICI) is complex. Monitoring of irAEs is critical as toxicities cause morbidity and impact quality of life. Thus, we systematically evaluated the patterns and consistency of irAEs reporting in trials leading to US Food and Drug Administration (FDA) ICI approvals. METHODS: We evaluated 75 primary articles from 2011-2021. The authors independently collected data regarding reporting frequency as a binary classification of reported versus not reported and irAE frequency of 24 irA

FDA-approved drugs as potential covalent inhibitors of key SARS-CoV-2 proteins: an in silico approach.

BACKGROUND/AIM: The COVID-19 pandemic caused by SARS-CoV-2 necessitated rapid development of effective therapeutics, prompting this study to identify potential inhibitors targeting key viral and host proteins: RNA-dependent RNA polymerase (RdRp), main protease (Mpro), transmembrane serine protease 2 (TMPRSS2), and angiotensin-converting enzyme 2 (ACE2). METHODS: We used covalent docking and molecular dynamics (MD) simulations to screen FDA-approved compounds against these targets using diverse covalent reaction mechanisms. Top-ranking compounds underwent further evaluation through MD simulati

In-silico study of approved drugs as potential inhibitors against 3CLpro and other viral proteins of CoVID-19.

The global pandemic, due to the emergence of COVID-19, has created a public health crisis. It has a huge morbidity rate that was never comprehended in the recent decades. Despite numerous efforts, potent antiviral drugs are lacking. Repurposing of drugs presents a low-cost and rapid solution for finding new drugs by exploiting known drugs. In this study, we employed an integrated In-Silico approach using molecular docking and machine learning regression models to explore the potential inhibitors against key proteins of SARS-CoV-2. A library of 5903 drugs from the ZINC database was retrieved an

Utilizing neighborhood topological indices for QSPR analysis of clinically approved immunosuppressive drugs in heart transplant therapy.

Heart transplantation is a life-saving transplantation procedure for individuals with advanced heart failure who have gone through all other medicinal options. It is predicted that 5000 heart transplants will be performed annually worldwide. The immunosuppressive drugs are used after a heart transplant to prevent organ rejection. They may be administered both before and throughout the transplant process under specific circumstances. Quantitative Structure-Activity or Property Relationship using topological descriptors is essential in drug design since it allows one to anticipate the physicoche

Eltrombopag, an FDA-approved drug, inhibits dengue virus type 2 by targeting NS2B-NS3 protease.

Dengue viruses (DENV) have spread throughout the world and pose a huge threat to human life. The most widespread serotype is type 2 DENV (DENV 2), which has no specific treatment. NS2B-NS3 protease plays a pivotal role in DENV replication because of its function in cleavage of the viral polyprotein; thus, it is considered a promising target for antiviral discovery. In this study, we developed a high-throughput screening system based on the NS2B-NS3 protease to identify candidates from an FDA-approved drug library. Eltrombopag was screened out of 3273 drugs, and demonstrated inhibition on DENV