Drug-drug interactions with tyrosine- kinase inhibitors: a clinical perspective. Lancet Oncol 2014;15:e315-26.Van Leeuwen RWF, Van Gelder T, Mathijssen RHJ, Jansman FGA (2014) Drug-drug interactions with tyrosine-kinase inhibitors: a clinical perspective. Lancet Oncol 15:e315-e326...
M. The prediction of drug-glucuronidation parameters in humans: UDP- glucuronosyltransferase enzyme-selective substrate and inhibitor probes for reaction phenotyping and in vitro-in vivo extrapolation of drug clearance and drug-drug interaction potential. Drug Metab Rev 42, 196–208 (2010). 9. ...
Bruton’s tyrosine kinase (BTK) inhibitor is a promising novel agent that has potential efficiency in B-cell malignancies. It took approximately 20 years from target discovery to new drug approval. The first-in-class drug ibrutinib creates possibilities for an era of chemotherapy-free management of...
参考文献 1. Discovery of Selective Irreversible Inhibitors for Bruton’s Tyrosine Kinase. DOI: 10.1002/cmdc.200600221; 2. Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase. DOI: 10.1021/acs.jmedchem.9b00687....
protein tyrosine kinase inhibitorssmall moleculesmolecular descriptorsdrug-likeness scoresNMRThe rate of protein degradation in 3T3, 3T3/41, SV40 virus-... H Otsuka,M Moskowitz - 《Experimental Cell Research》 被引量: 240发表: 1978年 EGFRIndb: Epidermal Growth Factor Receptor Inhibitor Database Thus...
Acute myeloid leukemias (AML) harboring a constitutively active internal tandem duplication (ITD) mutation in the FMS-like kinase tyrosine kinase (FLT3) receptor are associated with poor patient prognosis. Despite initial clinical responses to FLT3 kinase inhibitors, patients eventually relapse. Mechanisms...
Tyrosine kinase inhibitors (TKIs) are indicated for the treatment of a variety of malignancies due to their ability to interfere with cell communication and growth. Interactions that affect TKI metabolism are discussed.
HOW DO ANTINEOPLASTIC TYROSINE KINASE INHIBITORS WORK? Antineoplastictyrosinekinase inhibitors are a class of drugs used to treat nonsmall cell lung cancer,gastrointestinalstromal tumors (a type of tumor that grows in the wall of the stomach and the intestine), mastocytosis (a disorder characterized ...
Bruton's tyrosine kinase (BTK) is a non-receptor protein kinase that plays a crucial role in various biological processes, including immune system function and cancer development. Therefore, inhibition of BTK has been proposed as a therapeutic strategy f
Imatinib is the first FDA approved tyrosine kinase inhibitor (TKI) that has shown potent inhibitory effect on the progression of CML4. Despite imatinib's clinical success, resistance due to mutations and side effects are still a limitation of this drug5. To overcome resistance, second generation ...