Nilotinib is widely used for primary treatment of patients with chronic myelogenous leukemia (CML). We previously reported that use of an FRET-based drug sensitivity test at diagnosis efficiently predicts the response to treatment with imatinib or dasatinib. Here, we conducted a phase-II study to evaluate the efficacy and safety of nilotinib treatment and identify useful biomarkers, including results of the FRET-based drug sensitivity test, for predicting treatment response. Data from 42 patients were used in the analysis. Major molecular response (MMR), MR4, and MR4.5 rates at 12 months were 64.3, 42.9, and 28.6%, respectively. Grade 3/4 non-hematologic adverse events occurred in 11 patients (26.2%). The dose intensity of nilotinib (> 76.44%) and halving time (HT, < 13.312 days) were identified as significant factors for MMR at 12 months. However, when we focused on patients whose dose intensity of nilotinib was > 76.44%, the FRET-based drug sensitivity test became a predictive factor of MR4 achievement at 12 months. Our study reconfirmed the efficacy and safety of nilotinib treatment in CML patients. Moreover, our results suggest that the FRET-based drug sensitivity test is an independent predictor for achievement of MR4 in patients treated with a sufficient dose intensity of nilotinib.

Download full-text PDF

Source
http://dx.doi.org/10.1007/s12185-019-02696-wDOI Listing

Publication Analysis

Top Keywords

fret-based drug
20
drug sensitivity
20
sensitivity test
20
efficacy safety
12
safety nilotinib
8
nilotinib treatment
8
dose intensity
8
intensity nilotinib
8
nilotinib
6
fret-based
5

Similar Publications

Fluorescent biosensors offer a powerful tool for tracking and quantifying protein activity in living systems with high temporospatial resolution. However, the expression of genetically encoded fluorescent proteins can interfere with endogenous signaling pathways, potentially leading to developmental and physiological abnormalities. The EKAREV-NLS mouse model, which carries a FRET-based biosensor for monitoring extracellular signal-regulated kinase (ERK) activity, has been widely utilized both in vivo and in vitro across various cell types and organs.

View Article and Find Full Text PDF

EGFP/RFP-based FRET sensors for botulinum neurotoxin A biological activity detection and methodological validation.

Anal Chim Acta

February 2025

Joint Drug Development and Innovation Centre for Neurological Disorders of Lanzhou University-China National Biotec Group-Lanzhou Biotechnology Development Co., School of Pharmacy, Lanzhou University, Lanzhou, Gansu, 730000, PR China; MOE Frontiers Science Center for Rare Isotopes, Lanzhou University, Lanzhou, Gansu, 730000, PR China. Electronic address:

Background: Botulinum neurotoxin type A (BoNT/A) is the most potent and prevalent neurotoxin known to cause botulism, and is also widely used in medical and cosmetic applications. The detection of BoNT/A is of great significance for botulism diagnosis and drug potency determination. Currently, the mouse bioassay (MBA) has long been the gold standard method but has disadvantages of ethical concerns, long testing duration, and high costs.

View Article and Find Full Text PDF

In cardiac muscle, many myosin molecules are in a resting or "OFF" state with their catalytic heads in a folded structure known as the interacting heads motif (IHM). Many mutations in the human β-cardiac myosin gene that cause hypertrophic cardiomyopathy (HCM) are thought to destabilize (decrease the population of) the IHM state. The effects of pathogenic mutations on the IHM structural state are often studied using indirect assays, including a single-ATP turnover assay that detects the super-relaxed (SRX) biochemical state of myosin functionally.

View Article and Find Full Text PDF

Investigating the structural integrity of nanocarriers in vivo is vital for exploring the fate of nanocarriers from ocular surface to the posterior segment of the eye. Most of the published studies adopted the structural integrity ratio of nanocarriers to determine the fate of them, which lacked scientific support. In this study, two methods were used to explore the factors which affected the structural integrity of liposomes.

View Article and Find Full Text PDF

In Vitro Characterization of Inhibition Function of Calcifediol to the Protease Activity of SARS-COV-2 PLpro.

J Med Virol

November 2024

Department of Neurosurgery and Department of Neuroscience, Fujian Key Laboratory of Brain Tumors Diagnosis and Precision Treatment, Xiamen Key Laboratory of Brain Center, The First Affiliated Hospital of Xiamen University, Xiamen, China.

Vitamin D3 and its metabolites calcifediol have been recommended as effective drugs for novel coronavirus disease 2019 (COVID-19) therapy in many studies, since the outbreak of this global dramatic pandemic. In this study, we made a striking discovery that Calcifediol demonstrates robust inhibitive effect on the of the papain-like cysteine protease (PLpro), a critical proteolytic enzyme for the severe acute respiratory syndrome coronavirus-2(SARS-COV-2), through a small-scale FRET-based screening experiment. The practical bindings of Calcifediol to PLpro were also demonstrated by several in vitro interaction studies.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!