Publications related to Bioavailability

Development of cyclic peptides that can be administered orally to inhibit disease targets

Cyclic peptides can bind challenging disease targets, but their oral application is hindered by digestion and absorption issues. We developed a versatile method for the synthesis and functional screening of vast numbers of synthetic cyclic peptides and ide ...

2023

Development of stimuli-responsive chemistry for tumor-targeted immunotherapy

Céline Jasmin Prange

Cancer immunotherapy is the science of boosting the immune response of patients to fight cancer. Recent advances have brought up treatments with huge success in the clinic. Patients with ad-vanced-stage cancers were long-term cured through checkpoint inhib ...

EPFL2023

De novo developed small cyclic peptides that are orally available

Manuel Leonardo Merz

Cyclic peptides are ring-shaped molecules that emerged as a promising class of therapeutics. While it is often difficult to find small molecule binders for challenging disease targets, cyclic peptides can bind to featureless surfaces or inhibit protein-pro ...

EPFL2022

Determination of a clinically effective evobrutinib dose: Exposure-response analyses of a phase II relapsing multiple sclerosis study

Mitchell David Anderson

The pharmacometric analysis of the double-blind, randomized, phase II study (NCT02975349) investigating the safety and efficacy of evobrutinib, explored exposure-response relationships and suitable dosing regimens of evobrutinib for relapsing multiple scle ...

WILEY2022

Identification of broad anti-coronavirus chemical agents for repurposing against SARS-CoV-2 and variants of concern

Gerardo Turcatti, Fabien Kuttler, Michael Bauer, Liliane Yang

Endemic human coronaviruses (hCoVs) 229E and OC43 cause respiratory disease with recurrent infections, while severe acute respiratory syndrome (SARS)-CoV-2 spreads across the world with impact on health and societies. Here, we report an image-based multicy ...

2022

Structures of ABCG2 under turnover conditions reveal a key step in the drug transport mechanism

Henning Paul-Julius Stahlberg, Dongchun Ni

ABCG2 is a multidrug transporter that affects drug pharmacokinetics and contributes to multidrug resistance of cancer cells. In previously reported structures, the reaction cycle was halted by the absence of substrates or ATP, mutation of catalytic residue ...

Nature Research2021

Towards the Development of Orally Available Peptide Therapeutics

Christian Heinis, Xudong Kong

Peptides have a number of attractive properties that make them an interesting modality for drug development, including their ability to bind challenging targets, their high target specificity, and their non-toxic metabolic products. However, a major limita ...

2021

Catalytic effects of photogenerated Fe(II) on the ligand-controlled dissolution of Iron(hydr)oxides by EDTA and DFOB

Janet Gordon Hering

Low bioavailability of iron due to poor solubility of iron(hydr)oxides limits the growth of microorganisms and plants in soils and aquatic environments. Previous studies described accelerated dissolution of iron(hydr)oxides under continuous illumination, b ...

Pergamon-Elsevier Science Ltd2021

A reduced form of nicotinamide riboside defines a new path for NAD(+) biosynthesis and acts as an orally bioavailable NAD(+) precursor

Carlos Canto Alvarez, Richardus Houtkooper, Sofia Moco

Objective: A decay in intracellular NAD(+) levels is one of the hallmarks of physiological decline in normal tissue functions. Accordingly, dietary supplementation with NAD(+) precursors can prevent, alleviate, or even reverse multiple metabolic complicati ...

2019

Optimized Sampling Rate for Voltammetry-Based Electrochemical Sensing in Wearable and IoT Applications

Sandro Carrara, Danilo Demarchi, Simone Aiassa

The recent advancements in electrochemical measurements are guiding the development of new platforms for in situ point-of-care monitoring of human-metabolite, markers, and drugs. Despite this, the application of voltammetry-based sensing (VBS) techniques i ...

2019

Evaluation of the ray-casting analytical algorithm for pencil beam scanning proton therapy

Ye Zhang, Sojin Shim

For pencil beam scanned (PBS) proton therapy, analytical dose calculation engines are still typically used for the optimisation process, and often for the final evaluation of the plan. Recently however, the suitability of analytical calculations for planni ...

2019

Scalable Production of AAV Vectors in Orbitally Shaken HEK293 Cells

Florian Maria Wurm, Bernard Schneider, Vivianne Padrun, Nicole Déglon, Daniel Roman Blessing, Gabriel Vachey

Adeno-associated virus (AAV) vectors are currently among the most commonly applied for in vivo gene therapy approaches. The evaluation of vectors during clinical development requires the production of considerable amounts of highly pure and potent vectors. ...

2019

More Medicines for Tuberculosis: Fuelling Drug Discovery against Mycobacterium tuberculosis

Shi-Yan Caroline Foo

Tuberculosis (TB), whose etiological agent is Mycobacterium tuberculosis (M. tuberculosis), has plagued humanity since antiquity. Even with chemotherapy available today, TB is the leading cause of death due to an infectious disease. Modern day factors, suc ...

EPFL2018

Microdevice-integrated immunoassays for Point-of-Care Therapeutic Drug Monitoring

Elena-Diana Bojescu

A significant number of drugs exhibit narrow therapeutic windows and high inter-individual pharmacokinetic variability. In such cases, Therapeutic Drug Monitoring (TDM) is compulsory in order to optimize the efficacy of the drug while avoiding adverse effe ...

EPFL2018

Controlling and Monitoring Intracellular Delivery of Anticancer Polymer Nanomedicines

Harm-Anton Klok, Claudia Battistella

Polymer nanomedicines are very attractive to improve the delivery of chemotherapeutics. Polymer conjugates and other polymer-based nanocarriers allow to increase plasma half-life and drug bioavailability and can also be guided toward tumors using passive a ...

2017

Controlling and Monitoring Intracellular Drug Delivery Using PHPMA-Based Polymer Nanomedicines

Claudia Battistella

Polymer nanomedicine is an attractive approach for the delivery of anticancer drugs. Firstly designed to increase drug bioavailability, polymer conjugates and polymer nanoparticles have rapidly emerged in the field of cancer therapy after the discovery of ...

EPFL2017

Rapid Production of Submicron Drug Substance Particles by Supersonic Spray Drying

Esther Amstad

Many newly developed active pharmaceutical ingredients (APIs) are poorly soluble in water and thus have a dissolution-limited bioavailability. The bioavailability of Biopharmaceutical Classification System (BCS) class II APIs increases if they dissolve fas ...

Amer Chemical Soc2017

Antitubercular drugs for an old target: GSK693 as a promising InhA direct inhibitor

John McKinney, Neeraj Dhar, François Signorino-Gelo

Despite being one of the first antitubercular agents identified, isoniazid (INH) is still the most prescribed drug for prophylaxis and tuberculosis (TB) treatment and, together with rifampicin, the pillars of current chemotherapy. A high percentage of ison ...

Elsevier Science Bv2016

Crystallization of undercooled liquid fenofibrate

Esther Amstad

Formulation of hydrophobic drugs as amorphous materials is highly advantageous as this increases their solubility in water and therefore their bioavailability. However, many drugs have a high propensity to crystallize during production and storage, limitin ...

Royal Society of Chemistry2015

Label-Free Detection of Tobramycin in Serum by Transmission-Localized Surface Plasmon Resonance

Carlotta Guiducci, Thierry Buclin, Anna Ferretti, Giulia Cappi, Fabio Mario Spiga, Laurent Décosterd, Michael Beyeler

In order to improve the efficacy and safety of treatments, drug dosage needs to be adjusted to the actual needs of each patient in a truly personalized medicine approach. Key for widespread dosage adjustment is the availability of point-of-care devices abl ...

Amer Chemical Soc2015