Modulating Target Engagement of Small Molecules Via Drug Delivery – Approaches and Applications in Drug Discovery and Development

Drug delivery technologies for modified drug release have been in existence for a long time, but their utilization has been largely limited to extending market exclusivity and improving patient adherence to therapy. Recently, they are gaining renewed importance as pharmaceutical industry is steadily shifting to a more integrated discovery-development approach. In discovery, modulating target engagement via drug delivery technologies can enable crucial pharmacology studies for building a strong foundation and well-defined criteria for molecular design. In development, earlier implementation of delivery technologies can enhance the value of drug products through reduced dosing frequency, improved tolerability and/or safety profile, thereby leading to better adherence and therapeutic effectiveness

Smart design of patient centric long-acting products: from preclinical to marketed pipeline trends and opportunities.

We see a development in the field of long-acting products to serve patients with chronic diseases by providing benefits in adherence, efficacy and safety of the treatment. This review investigates features of long-acting products on the market/pipeline to understand which drug substance (DS) and drug product (DP) characteristics likely enable a successful patient-centric, low-dosing frequency product.This review evaluates marketed/pipeline long-acting products with greater than one week release of small molecules and peptides by oral and injectable route of administration (RoA), with particular focus on patient centricity, adherence impact, health outcomes, market trends, and the match of DS/DP technologies which lead to market success.Emerging trends are expected to change the field of long-acting products in the upcoming years by increasing capability in engineered molecules (low solubility, long half-life, high potency, etc.), directly developing DP as long-acting oral/injectable, increasing the proportion of products for local drug delivery, and a direction towards more subcutaneous, self-administered products. Among long-acting injectable products, nanosuspensions show a superiority in dose per administration and dosing interval, overwhelming the field of infectious diseases with the recently marketed products

Clinically established biodegradable long acting injectables: An industry perspective

Long acting injectable formulations have been developed to sustain the action of drugs in the body over desired periods of time. These delivery platforms have been utilized for both systemic and local drug delivery applications. This review gives an overview of long acting injectable systems that are currently in clinical use. These products are categorized in three different groups: biodegradable polymeric systems, including microparticles and implants; micro and nanocrystal suspensions and oil-based formulations. Furthermore, the applications of these drug delivery platforms for the management of various chronic diseases are summarized. Finally, this review addresses industrial challenges regarding the development of long acting injectable formulations

Clinically established biodegradable long acting injectables: An industry perspective

Long acting injectable formulations have been developed to sustain the action of drugs in the body over desired periods of time. These delivery platforms have been utilized for both systemic and local drug delivery applications. This review gives an overview of long acting injectable systems that are currently in clinical use. These products are categorised in three different groups: biodegradable polymeric systems, including microparticles and implants; micro and nanocrystal suspensions and oil-based formulations. Furthermore, the applications of these drug delivery platforms for the management of various chronic diseases are summarized. Finally, this review addresses industrial challenges regarding the development of long acting injectable formulations