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Overview

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Otorhinolaryngologic Diseases

Nervous System Diseases

Small molecule drug

Disease domain score

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Technology Platform

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Targets

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Disease Domain	Count

Nervous System Diseases	1

Top 5 Drug Type	Count

Small molecule drug	1

Top 5 Target	Count

H1 receptor(Histamine H1 receptor)	1

Two important driving forces for oral absorption of active pharmaceutical ingredients are drug dissolution and permeability in the gastrointestinal tract. Poorly soluble weak bases typically exhibit high solubility under fasted gastric conditions. However, the solubility of such drugs usually decreases drastically in the fasted small intestine, constraining drug absorption. Since there is a discrepancy in solubility between the fasted state stomach and intestine, it is crucial to examine the influence of dissolution, supersaturation and precipitation on the oral absorption of poorly soluble weak bases during and after fasted state gastric emptying. Cinnarizine is a poorly soluble weak base with borderline permeability, exhibiting supersaturation and precipitation under simulated fasted state gastric emptying conditions. Interestingly, supersaturation and precipitation of cinnarizine under fed state conditions is not expected to occur, since the drug shows good solubility in fed state biorelevant media and exhibits a positive food effect in pharmacokinetic studies. The present work is aimed at investigating the dissolution, supersaturation and precipitation behavior of marketed cinnarizine tablets under fasted and fed state conditions using biorelevant dissolution and transfer methods. In order to predict the in vivo performance of these cinnarizine formulations, the in vitro results were then coupled with different physiologically based pharmacokinetic (PBPK) models, which considered either only dissolution or a combination of dissolution, supersaturation and precipitation kinetics. The results of the in silico predictions were then compared with in vivo observations. The study revealed that under fasting conditions, plasma profiles could be accurately predicted only when supersaturation and precipitation as well as dissolution were taken into account. It was concluded that for poorly soluble weak bases with moderate permeability, supersaturation and precipitation during fasted state gastric emptying may have an essential influence on oral drug absorption and thus on in vivo drug performance.

Scientific Reports

Neurotensin analogs by fluoroglycosylation at Nω-carbamoylated arginines for PET imaging of NTS1-positive tumors

Article

Author: Gluhacevic von Krüchten, Lara ; Schindler, Lisa ; Wohlfahrt, Katrin ; Keller, Max ; Prante, Olaf ; Maschauer, Simone

AbstractSince neurotensin (NT) receptors of subtype-1 (NTS1) are expressed by different types of malignant tumors, such as pancreatic adenocarcinoma, colorectal and prostate carcinoma, they represent an interesting target for tumor imaging by positron emission tomography (PET) and endoradiotherapy. Previously reported neurotensin-derived NTS1 ligands for PET were radiolabeled by modification and prelongation of the N-terminus of NT(8–13) peptide analogs. In this study, we demonstrate that modifying Arg8 or Arg9 by Nω-carbamoylation and subsequent fluoroglycosylation provides a suitable approach for the development of NT(8–13) analogs as PET imaging agents. The Nω-carbamoylated and fluoroglycosylated NT(8–13) analogs retained high NTS1 affinity in the one-digit nanomolar range as well as high metabolic stability in vitro. In vivo, the radioligand [18F]21 demonstrated favorable biokinetics in HT-29 tumor-bearing mice with high tumor uptake and high retention, predominantly renal clearance, and fast wash-out from blood and other non-target tissues. Therefore, [18F]21 has the potential to be used as molecular probe for the imaging of NTS1-expressing tumors by PET.

100 Deals associated with Hennig Arzneimittel GmbH & Co. KG

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100 Translational Medicine associated with Hennig Arzneimittel GmbH & Co. KG

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Pipeline

Pipeline Snapshot as of 17 Nov 2024

The statistics for drugs in the Pipeline is the current organization and its subsidiaries are counted as organizations,Early Phase 1 is incorporated into Phase 1, Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3

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