Phase 1 study in healthy participants of the safety, pharmacokinetics, and pharmacodynamics of enpatoran (M5049), a dual antagonist of toll-like receptors 7 and 8.

This study evaluated the safety, tolerability, pharmacokinetics (PK), and pharmacodynamics (PD) of single and multiple oral doses of enpatoran (formerly named M5049), a new toll-like receptor (TLR) 7 and 8 dual antagonist, and the effect of food on a single dose in healthy participants. In this single phase 1, randomized (3:1), double-blind, placebo-controlled study, 96 participants received single and multiple ascending oral doses of enpatoran. Participants in single-dose cohorts received one dose of enpatoran (1, 3, 9, 25, 50, 100, or 200 mg) or placebo using a sentinel dosing strategy.

Evobrutinib, a covalent Bruton's tyrosine kinase inhibitor: Mass balance, elimination route, and metabolism in healthy participants.

The highly selective, covalent Bruton's tyrosine kinase inhibitor evobrutinib is under investigation for treatment of patients with multiple sclerosis (MS). Early clinical studies in healthy participants and patients with relapsing MS indicated that evobrutinib is well-tolerated and effective. We undertook a mass balance study in six men who received a single 75-mg oral dose of evobrutinib containing ~ 3.

Elastomer coils for wearable MR detection.

Purpose: To explore the use of conductive elastomer for MR signal detection and the utility of this approach for wearable detector arrays.

Methods: An elastomer filled with silver microparticles was used to form stretchable radiofrequency coils for MR detection. Their electrical performance in terms of the Q and Q ratio was assessed in the relaxed state and under repeated strain up to 40%.

Publisher Correction: Detector clothes for MRI: A wearable array receiver based on liquid metal in elastic tubes.

An amendment to this paper has been published and can be accessed via a link at the top of the paper.

Detector clothes for MRI: A wearable array receiver based on liquid metal in elastic tubes.

In modern magnetic resonance imaging, signal detection is performed by dense arrays of radiofrequency resonators. Tight-fitting arrays boost the sensitivity and speed of imaging. However, current devices are rigid and cage-like at the expense of patient comfort.

An In-Bore Receiver for Magnetic Resonance Imaging.

In magnetic resonance imaging, the use of array detection and the number of detector elements have seen a steady increase over the past two decades. As a result, per-channel analog connection via long coaxial cable, as commonly used, poses an increasing challenge in terms of handling, safety, and coupling among cables. This situation is exacerbated when complementary recording of radiofrequency transmission or NMR-based magnetic field sensing further add to channel counts.

Automatic Resonance Frequency Retuning of Stretchable Liquid Metal Receive Coil for Magnetic Resonance Imaging.

Stretchable magnetic resonance (MR) receive coils show shifts in their resonance frequency when stretched. An in-field receiver measures the frequency response of a stretchable coil. The receiver and coil are designed to operate at 128 MHz for a 3T MR scanner.

On the Bending and Stretching of Liquid Metal Receive Coils for Magnetic Resonance Imaging.

The eGaIn coil on neoprene demonstrated in this paper presents a stretchable radio frequency receive coil for magnetic resonance imaging (MRI). The coil with dimensions [Formula: see text] is tuned to resonate at 128 MHz for 3 T MRI. We investigate the effect of stretching (up to 40% strain) and bending (50 mm radius of curvature) of the coil on the coil's resistance and resonance frequency.

Effect of multiple oral doses of linagliptin on the steady-state pharmacokinetics of a combination oral contraceptive in healthy female adults: an open-label, two-period, fixed-sequence, multiple-dose study.

Background: Linagliptin is an oral dipeptidyl peptidase (DPP)-4 inhibitor that has been recently approved for the treatment of type 2 diabetes mellitus. Microgynon® 30 is a combined oral contraceptive pill containing both ethinylestradiol 30 μg and levonorgestrel 150 μg (EE 30 μg/LNG 150 μg).

Objective: The objective of this study was to determine the effect of multiple doses of linagliptin (5 mg once daily) on the steady-state pharmacokinetics of EE and LNG following once-daily doses of EE 30 μg/LNG 150 μg.

The DPP-4 inhibitor linagliptin does not prolong the QT interval at therapeutic and supratherapeutic doses.

Aim: To evaluate the potential effects of therapeutic and supratherapeutic doses of linagliptin (BI 1356) on the QT/QT(c) interval in healthy subjects.

Methods: The study was a randomized, double-blind, placebo-controlled, four-period crossover study using single oral doses of linagliptin (5 mg and 100 mg), moxifloxacin (400 mg) and placebo. Electrocardiogram (ECG) profiles using triplicates of 12-lead 10-s ECGs were digitally recorded pre-dose and after drug administration.

Oral-intravenous crossover study of fingolimod pharmacokinetics, lymphocyte responses and cardiac effects.

Objective: The pharmacokinetics and lymphocyte responses to the immunomodulator fingolimod (FTY720) were characterized after oral and intravenous administration.

Methods: In this randomized, two-period crossover study 11 evaluable healthy subjects received single doses of fingolimod 1.25 mg orally and 1 mg intravenously infused over 2 h.

Pharmacokinetic evaluation of three different intramuscular doses of nandrolone decanoate: analysis of serum and urine samples in healthy men.

The pharmacokinetics of nandrolone in serum and urine were investigated in healthy young men after a single im injection of 50 mg (n = 20), 100 mg (n = 17), or 150 mg (n = 17) nandrolone decanoate. Blood samples were collected before treatment and for up to 32 d after dosing. In addition, in the 50- and 150-mg groups, 24-h urine samples were collected before treatment and on d 1, 7, and 33 after treatment; in the 150-mg group, additional samples were collected after 3 and 6 months.

Effect of rifampin on apparent clearance of everolimus.

Objective: To assess the influence of the CYP3A4 enzyme inducer rifampin on the pharmacokinetics of the immunosuppressant everolimus to provide guidance for their coadministration.

Methods: In this open-label, single-sequence, crossover study, 12 healthy subjects received a single oral 4-mg dose of everolimus alone and again after an 8-day pretreatment with rifampin 600 mg/d. Urinary excretion of 6beta-hydroxycortisol was measured at various time points during rifampin treatment as a marker of CYP3A4 induction.