A 24 week, MRI based, double-blind, randomised, placebo-controlled, modified dose-escalation trial to evaluate the safety, efficacy and pharmacokinetics of BIRT 2584 XX tablets at doses of 100, 300 and 500 mg administered once daily in patients with relapsing forms of Multiple Sclerosis.

Start Date22 Sep 2006

Sponsor / Collaborator

Boehringer Ingelheim Ltd.

NCT00333411 / CompletedPhase 2

A 12 Week Double-blind, Randomised, Placebo-controlled, Modified Dose-escalation Trial to Investigate Safety, Efficacy, and Pharmacokinetics of BIRT 2584XX Tablets at Doses of 100, 300 and 500 mg Administered Once Daily in Patients With Moderate to Severe Psoriasis With a 12 Week Treatment Extension

The purpose of this clinical study is to determine the effectiveness, pharmacokinetics and safety of several doses of BIRT 2584 XX (100mg, 300mg and 500mg) taken once daily in the treatment of moderate to severe plaque-type psoriasis. This new medicine will be compared to a so-called placebo medicine over 12 weeks with a 12 weeks treatment extension possible.

Start Date01 Jun 2006

Sponsor / Collaborator

Boehringer Ingelheim GmbH

NCT02256813 / CompletedPhase 1

A Study to Evaluate the Effect of Multiple Doses of 500 mg of BIRT 2584 XX Tablets on the Pharmacokinetic Parameters of Warfarin, Omeprazole, Caffeine, and Dextromethorphan Dosed Orally and Midazolam Dosed IV, in Healthy Male Volunteers

The study aimed to investigate the effect of BIRT 2584 XX and its metabolite BI 610100 on the Pharmacokinetics (PK) of five probe substrates for cytochrome P450 isozymes.
The substrates used to monitor enzyme activity were oral warfarin (for CYP2C9), oral omeprazole (for CYP2C19), oral dextromethorphan (for CYP2D6), oral caffeine (for CYP1A2) and intravenous midazolam (for hepatic CYP3A)

Start Date01 Sep 2005

Sponsor / Collaborator

Boehringer Ingelheim GmbH

100 Clinical Results associated with BIRT-2584-XX

100 Translational Medicine associated with BIRT-2584-XX

100 Patents (Medical) associated with BIRT-2584-XX

Literatures (Medical) associated with BIRT-2584-XX

01 May 2024·Journal of Pharmaceutical Sciences

Human Serum Albumin Immobilized On Magnetizable Beads: A Rapid Method for Compound HSA Binding Study

Article

Author: Wang, Ting ; Thomas, Cody ; Byer-Alcorace, Alexander

Immobilized human serum albumin (HSA) was developed by coupling His-tagged HSA onto Ni²⁺-coupled magnetizable beads (HSA-beads), allowing the HSA to be easily removed from incubation components. The HSA-beads system provides a rapid and convenient method to study HSA compound binding. In this study, the HSA-beads system was characterized and evaluated as a tool for assessing compound HSA binding properties. The free fraction (f_u) values of test compounds measured using HSA-beads were comparable to those determined by equilibrium dialysis (ED), which is commonly used to evaluate albumin binding in vitro. The equilibrium dissociation constant (K_d) values determined for a series of compounds using the HSA-beads method demonstrated good correlation with literature data. This good correlation also suggests that the binding of His-HSA to the beads does not impact the conformations of the two compound binding sites of HSA, as the range of compounds tested encompassed binding to both sites. Furthermore, the K_d values of representative compounds itraconazole and BIRT2584 that were difficult to assess using ED, due to significant cellulose membrane adsorption, were successfully determined. The HSA-beads provide several advantages over ED, such as simple preparation, short assay incubation duration, and the ability to quantify both free and HSA-bound species of the test compound, facilitated by the simple separation of HSA-beads from the solution phase using a magnetic field. These properties render the HSA-beads method suitable for high-throughput studies on compound HSA binding.

01 Dec 2021·Drug Metabolism and DispositionQ2 · MEDICINE

HLM-beads: Rapid Assessment of Nonspecific Binding to Human Liver Microsomes Using Magnetizable Beads

Q2 · MEDICINE

Article

Author: Wang, Ting ; Whitcher-Johnstone, Andrea ; Keith-Luzzi, Monica ; Chan, Tom S

In early drug development, drug-drug interaction risk is routinely assessed using human liver microsomes (HLMs). Nonspecific binding of drugs to HLMs can affect the determination of accurate enzyme parameters (K_m, K_i, K_I). Previously, we described a novel in vitro model consisting of HLMs bound to magnetizable beads [HLM-magnetizable-beads system (HLM-beads)]. The HLM-beads enable rapid separation of HLMs from incubation media by applying a magnetic field. Here, HLM-beads were further characterized and evaluated as a tool to assess HLM nonspecific binding of small molecules. The free fractions (f_u,mic) of 13 compounds (chosen based on their pKa values) were determined using HLM-beads under three HLM concentrations (0.025, 0.50, and 1.0 mg/ml) and compared with those determined by equilibrium dialysis. Most f_u,mic values obtained using HLM-beads were within 0.5- to 2-fold of the values determined using equilibrium dialysis. The highest fold difference were observed for high binders itraconazole and BIRT2584 (1.9- to 2.9-fold), as the pronounced adsorption of these compounds to the equilibrium dialysis apparatus interfered with their f_u,mic determination. Correlation and linear regression analysis of the f_u,mic values generated using HLM-beads and equilibrium dialysis was conducted. Overall, a good correlation of f_u,mic values obtained by the two methods were observed, as the r and R² values from correlational analysis and linear regression analysis were >0.9 and >0.89, respectively. These studies demonstrate that HLM-beads can produce comparable f_u,mic values as determined by equilibrium dialysis while reducing the time required for this type of study from hours to only 10 minutes and compound apparatus adsorption. SIGNIFICANCE STATEMENT: This work introduces a new method of rapidly assessing nonspecific microsomal binding using human liver microsomes bound to magnetizable beads.

100 Deals associated with BIRT-2584-XX

R&D Status

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Indication	Highest Phase	Country/Location	Organization	Date
Psoriasis	Phase 2	CA	Boehringer Ingelheim GmbH	01 Jun 2006
Psoriasis	Phase 2	FI	Boehringer Ingelheim GmbH	01 Jun 2006
Psoriasis	Phase 2	FR	Boehringer Ingelheim GmbH	01 Jun 2006
Psoriasis	Phase 2	DE	Boehringer Ingelheim GmbH	01 Jun 2006
Psoriasis	Phase 2	BE	Boehringer Ingelheim GmbH	01 Jun 2006
Psoriasis	Phase 2	DK	Boehringer Ingelheim GmbH	01 Jun 2006
Psoriasis	Phase 2	NL	Boehringer Ingelheim GmbH	01 Jun 2006
Psoriasis	Phase 2	SE	Boehringer Ingelheim GmbH	01 Jun 2006
Psoriasis	Phase 2	ES	Boehringer Ingelheim GmbH	01 Jun 2006
Psoriasis	Discovery	GB	Boehringer Ingelheim GmbH	01 Jun 2006

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