scholarly journals On the development of miransertib for rare diseases: an interview with ArQule's Brian Schwartz

2020 ◽  
Vol 2 (1) ◽  
pp. FDD27
Author(s):  
Brian Schwartz
Keyword(s):  
Drug Development ◽  
Precision Medicine ◽  
Small Molecule ◽  
Rare Diseases ◽  
Kinase Inhibitors ◽  
Clinical Stage ◽  
Proteus Syndrome ◽  
Biopharmaceutical Company

Brian Schwartz is CMO of ArQule, a clinical-stage biopharmaceutical company developing small-molecule kinase inhibitors for precision medicine oncology and rare diseases. In this interview he tells us more about the company's current projects, which include drug development for the rare diseases Proteus syndrome and PROS.

scholarly journals 10 years into the resurgence of covalent drugs

2020 ◽  
Author(s):  
Elena De Vita
Keyword(s):  
Clinical Trials ◽  
Drug Discovery ◽  
Drug Development ◽  
Precision Medicine ◽  
Kinase Inhibitors ◽  
Covalent Inhibition ◽  
The Future ◽  
Covalent Inhibitors ◽  
Effective Treatments

In the first decade of targeted covalent inhibition, scientists have successfully reversed the previous trend that had impeded the use of covalent inhibition in drug development. Successes in the clinic, mainly in the field of kinase inhibitors, are existing proof that safe covalent inhibitors can be designed and employed to develop effective treatments. The case of KRASG12C covalent inhibitors entering clinical trials in 2019 has been among the hottest topics discussed in drug discovery, raising expectations for the future of the field. In this perspective, an overview of the milestones hit with targeted covalent inhibitors, as well as the promise and the needs of current research, are presented. While recent results have confirmed the potential that was foreseen, many questions remain unexplored in this branch of precision medicine.

Repositioning Drugs for Rare Immune Diseases: Hopes and Challenges for a Precision Medicine

2018 ◽  
Vol 25 (24) ◽  
pp. 2764-2782 ◽  
Author(s):  
Erica Valencic ◽  
Alenka Smid ◽  
Ziga Jakopin ◽  
Alberto Tommasini ◽  
Irena Mlinaric-Rascan
Keyword(s):  
Precision Medicine ◽  
Rare Diseases ◽  
Business Models ◽  
Drug Repositioning ◽  
Drug Action ◽  
Primary Immunodeficiency Diseases ◽  
Computational Sciences ◽  
Approved Drugs ◽  
Molecular Mode ◽  
Viable Business

Human primary immunodeficiency diseases (PIDs) are a large group of rare diseases and are characterized by a great genetic and phenotypic heterogeneity. A large subset of PIDs is genetically defined, which has a crucial impact for the understanding of the molecular basis of disease and the development of precision medicine. <p> Discovery and development of new therapies for rare diseases has long been de-privileged due to the length and cost of the processes involved. Interest has increased due to stimulatory regulatory and supportive reimbursement environments enabling viable business models. <p> Advancements in biomedical and computational sciences enable the development of rational, designed approaches for identification of novel indications of already approved drugs allowing faster delivery of new medicines. Drug repositioning is based either on clinical analogies of diseases or on understanding of the molecular mode of drug action and mechanisms of the disease. All of these are the basis for the development of precision medicine.

Drug Development of Small-Molecule Inhibitors of AD-Relevant Kinases as Novel Perspective Multitargeted Approach

2016 ◽  
Vol 13 (12) ◽  
pp. 1330-1336 ◽  
Author(s):  
V. Tell ◽  
I. Hilbrich ◽  
M. Holzer ◽  
Frank Totzke ◽  
Christoph Schachtele ◽  
...  
Keyword(s):  
Drug Development ◽  
Small Molecule ◽  
Small Molecule Inhibitors

scholarly journals Feasibility of Extrapolating Randomly Taken Plasma Samples to Trough Levels for Therapeutic Drug Monitoring Purposes of Small Molecule Kinase Inhibitors

2021 ◽  
Vol 14 (2) ◽  
pp. 119
Author(s):  
Ruben A. G. van Eerden ◽  
Esther Oomen-de Hoop ◽  
Aad Noordam ◽  
Ron H. J. Mathijssen ◽  
Stijn L. W. Koolen
Keyword(s):  
Therapeutic Drug Monitoring ◽  
Small Molecule ◽  
Trough Concentration ◽  
Drug Monitoring ◽  
Half Life ◽  
Kinase Inhibitors ◽  
Therapeutic Drug ◽  
Blood Samples ◽  
Elimination Half ◽  
Trough Levels

Small molecule kinase inhibitors (SMKIs) are widely used in oncology. Therapeutic drug monitoring (TDM) for SMKIs could reduce underexposure or overexposure. However, logistical issues such as timing of blood withdrawals hamper its implementation into clinical practice. Extrapolating a random concentration to a trough concentration using the elimination half-life could be a simple and easy way to overcome this problem. In our study plasma concentrations observed during 24 h blood sampling were used for extrapolation to trough levels. The objective was to demonstrate that extrapolation of randomly taken blood samples will lead to equivalent estimated trough samples compared to measured Cmin values. In total 2241 blood samples were analyzed. The estimated Ctrough levels of afatinib and sunitinib fulfilled the equivalence criteria if the samples were drawn after Tmax. The calculated Ctrough levels of erlotinib, imatinib and sorafenib met the equivalence criteria if they were taken, respectively, 12 h, 3 h and 10 h after drug intake. For regorafenib extrapolation was not feasible. In conclusion, extrapolation of randomly taken drug concentrations to a trough concentration using the mean elimination half-life is feasible for multiple SMKIs. Therefore, this simple method could positively contribute to the implementation of TDM in oncology.

scholarly journals FDA-approved small-molecule kinase inhibitors

2015 ◽  
Vol 36 (7) ◽  
pp. 422-439 ◽  
Author(s):  
Peng Wu ◽  
Thomas E. Nielsen ◽  
Mads H. Clausen
Keyword(s):  
Small Molecule ◽  
Kinase Inhibitors
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