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The Convergence of Digital Health Technologies: The Role of Digital Therapeutics in the Future Healthcare System
Published in Oleksandr Sverdlov, Joris van Dam, Digital Therapeutics, 2023
Joris van Dam, Justin Wright, Graham Jones
Graham Jones is Director of Innovation in the Novartis Technical Research and Development group. He was recruited to Novartis in 2018 from Tufts University Medical Center, where he was Professor of Medicine and Director of Translational Research. He has authored over 175 publications in drug development, drug delivery, process technology, regulatory science, and digital health and served as a government, FDA, and NIH advisor. Graham sits on several editorial boards and has received numerous scientific and technological development awards. He received his doctoral degree from Imperial College London and was awarded the D.Sc. in 2006 for contributions to medicinal chemistry.
Allopathic Medicines
Published in Varma H. Rambaran, Nalini K. Singh, Alternative Medicines for Diabetes Management, 2023
Varma H. Rambaran, Nalini K. Singh
Regarding allopathic medicines, drugs are strictly defined as chemical substances that are used to prevent or heal diseases in humans, animals, and plants, and are grouped according to the manner in which they are utilized. Of particular interest to the medicinal chemist is the structure of the compound as well as its relative pharmacological mechanism of action. However, other categories such as the nature of the illness must also be considered.
Role of Biomarkers in Clinical Development of Cancer Therapies
Published in Sherry X. Yang, Janet E. Dancey, Handbook of Therapeutic Biomarkers in Cancer, 2021
The rapid expansion of our knowledge about cancer genome and biology has provided hypothesis for an increasing number of potential therapeutic targets. Technical advancement in medicinal chemistry and biotechnology has also significantly enhanced the drug design for optimal potency and specificity against the intended targets. Successful development of molecularly targeted agents (MTA), however, must overcome the challenges posed by the very nature of cancer: the pathway complexity within tumors, the heterogeneity between individual patients and the exploitation by cancer cells of the essential survival mechanism of normal tissue. Given the high attrition rate of late-stage clinical trials with MTAs, there is a great need to enhance the robustness of early clinical trials to address the objectives key to future directions: credentialing the agent, optimizing the dose and schedule, obtaining preliminary proof of concept for the target, and identifying patient selection markers for further studies. For most MTAs, incorporation of biomarkers to characterize the tumors and the drug effect on molecular levels is not only desirable but also indispensible for successful transition from target discovery to target validation and clinical benefit.
PROTAC antibiotics: the time is now
Published in Expert Opinion on Drug Discovery, 2023
Jickky Palmae Sarathy, Courtney C. Aldrich, Mei-Lin Go, Thomas Dick
The novel BacPROTAC tool compounds constitute a promising first step toward a generalizable PROTAC approach for the discovery of new antibiotics. The generic medicinal chemistry process of hit-to-lead and lead optimization for PROTACs (optimization of potency, physicochemical properties, and pharmacokinetic parameters) will largely remain similar to that of traditional antibiotics. However, one could argue that optimization of bifunctional and multi-modular antibacterial PROTACs may be more challenging than monofunctional and mono-modular traditional antibiotics [13]. Thus, the infamous ‘valley of death,’ where most drug discovery programs fail due to the challenges associated with multi-property optimization, may lead to higher attrition rates in the case of antibacterial PROTACs. The question is then ‘Why bother?.’ Why engage in medicinal chemistry campaigns that are likely even more challenging than for traditional antibiotics? In the following, we speculate that future PROTAC antibiotics may have a multitude of advantages over traditional antibiotics (Figure 6) and argue that these justify the potentially higher hurdle.
A commentary on the use of pharmacoenhancers in the pharmaceutical industry and the implication for DMPK drug discovery strategies
Published in Xenobiotica, 2022
Vanessa Martins, Lynsey Fazal, Aram Oganesian, Alpesh Shah, Jessie Stow, Hugh Walton, Nicola Wilsher
Many publications have evaluated the changes in practices and technology developments that have led to DMTA cycle improvements including data systems to allow seamless data transfer between collaborators (pharma, CROs and academic groups) (Ballard et al. 2012). However, the direct interaction between medicinal chemist and DMPK scientist is scarcely mentioned. Indeed, it has been suggested that the responsibility to improve the pharmacokinetic properties and tolerability of a drug candidate falls on the shoulders of medicinal chemistry groups (Kerns 2013). However, the drug discovery industry acknowledges that success relies on multifaceted activities within multidisciplinary teams, with emphasis on inter-disciplinary communication as a key aspect to ensure a productive drug pipeline and the reduction of late-stage attrition.
Deciphering the enzymatic target of a new family of antischistosomal agents bearing a quinazoline scaffold using complementary computational tools
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2020
Victor Sebastian-Perez, Alfonso García-Rubia, Sayed H. Seif el-Din, Abdel-Nasser A. Sabra, Naglaa M. El-Lakkany, Samia William, Tom L. Blundell, Louis Maes, Ana Martinez, Nuria E. Campillo, Sanaa S. Botros, Carmen Gil
NPD-1246 shows promising antischistosomal activity potential in vivo, but was found metabolically unstable. A medicinal chemistry programme was therefore designed with the aim of improving its drug-like properties that would enable further development. Computational studies using SmartCyp22 were performed to identify the positions potentially susceptible for metabolic degradation. This software tool predicts CYP3A4, CYP2D6 and CYP2C9 effect on the target molecule and ranks atoms according to their probability to be modified by metabolism (Supplementary Figures S1–S3). Several potential sites were identified (Figure 3). The most important of which are C6 in the quinazoline scaffold and the meta- and para-positions of the benzyl substituent in the N1.