X-165 / X-Rx - LARVOL DELTA

Enhanced Solubilization of Ketoprofen Using Triton X-100, Triton X-165, Brij C10, and Their Binary and Ternary Mixed Micelle Systems. (PubMed, Pharm Res) - "Micellar stability and solubilization efficiency are not always correlated. Brij-rich micelles showed superior ketoprofen solubilization, whereas overly stabilized ternary systems limited drug loading. These findings highlight the need to balance stability and flexibility when designing micellar carriers for hydrophobic BCS class II drugs."

Journal

Interaction of biomimetic lipid membranes with detergents with different physicochemical characteristics. (PubMed, Chem Phys Lipids) - "The detergents chosen were the non-ionic Triton X-100, Triton X-165, C10E5, octyl glucopyranoside (OG) and dodecyl maltoside (DDM) and the ionic sodium dodecyl sulfate (SDS), cetyl trimethyl ammonium bromide (CTAB) and Chaps...The insoluble area fraction left intact was quantified. Overall, the non-ionic detergents were the most effective in solubilizing lipid membranes."

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Adsorption and wetting properties of biosurfactants, Trtions and their mixtures in aqueous and water-ethanol environment. (PubMed, Adv Colloid Interface Sci) - "Adsorption of rhamnolipid (RL) and surfactin (SF) as well as their mixtures with Triton X-100 (TX100) and Triton X-165 (TX165) at the solution-air (S-A), PTFE (polytetrafluoroethylene)-S, PMMA (poly (methyl methacrylate))-S, Q (quartz)-S, PMMA-A, and Q-A as well as their wetting properties regarding the surface tension of the PTFE, PMMA and quartz and its components and parameters were discussed using the literature data...The thermodynamic functions change as a results of RL, SF, TX100, TX165, ET as well as the mixtures of RL and SF with Tritons adsorption at different interfaces were also analyzed based on the literature data. These considerations allow to describe and/or predict changes of the interface tension, contact angle of the mixtures as a function of their composition based on these properties of individual mixture components."

Journal • Review

Wetting Behaviour of Water, Ethanol, Rhamnolipid, and Triton X-165 Mixture in the Polymer-Solution Drop-Air System. (PubMed, Molecules) - "From these considerations, it follows that, depending on the ET concentration, it is possible to form the TX165 + RL layer at the solid-water + ET mixed solvent, as well as the water + ET-air interfaces, but not at the solid-water and water-air ones. This conclusion is in accordance with the Gibbs standard free energy of adsorption of particular components of the studied mixture at the solution-air and solid-solution interfaces."

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Thermodynamic Characterization of Rhamnolipid, Triton X-165 and Ethanol as well as Their Mixture Behaviour at the Water-Air Interface. (PubMed, Molecules) - "This analysis allows to propose a new equation for calculation of the total ethanol concentration at the water-air interface using the Guggenheim-Adam adsorption isotherm. The constants in the Langmuir and Szyszkowski equations for each component of the studied mixtures as well as the composition of the mixed monolayer at the water-air interface were also successfully analysed based on the contribution of particular surface active compounds to the water surface tension reduction as well as based on the Frumkin isotherm of adsorption."

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Wetting Properties of Rhamnolipid and Surfactin Mixtures with Triton X-165. (PubMed, Molecules) - "However, the concentration of the studied mixtures at the PMMA-solution and quartz-solution is greater than zero. The concentration at the PMMA(quartz)-air and PMMA(quartz)-solution interfaces is smaller than that at the solution-air one."

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Thermodynamic Analysis of the Adsorption and Micellization Activity of the Mixtures of Rhamnolipid and Surfactin with Triton X-165. (PubMed, Molecules) - "Taking into account the composition of the mixed monolayer at the water-air interface, the standard Gibbs adsorption free energy was considered. The obtained results allow us to state that the concentration of both mixture components corresponding to their saturated monolayer and the surface tension of their aqueous solution can be predicted using the surfactants' single monolayer pressure and their mole fraction in the mixed monolayer determined in the proposed way."

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A Novel Autotaxin Inhibitor for the Treatment of Idiopathic Pulmonary Fibrosis: A Clinical Candidate Discovered Using DNA-Encoded Chemistry. (PubMed, J Med Chem) - "Optimization of this series led to the discovery of compound 1 (X-165), a highly potent, selective and bioavailable small molecule...After successfully completing IND-enabling studies, compound 1 was approved by the FDA for a Phase I clinical trial. These results demonstrate that DECL hits can be readily optimized into clinical candidates."

Clinical • Journal • Fibrosis • Idiopathic Pulmonary Fibrosis • Immunology • Respiratory Diseases

X-Rx announces FDA acceptance of IND application for X-165 (Businesswire) - "X-Rx, Inc....today announced the US Food and Drug Administration (FDA) has accepted the company’s Investigational New Drug Application (IND) for X-165 being developed for the treatment of Idiopathic Pulmonary Fibrosis....X-165 has demonstrated both promising results in pre-clinical efficacy...and a safety profile in GLP toxicology studies...X-Rx plans to initiate soon a randomized, double-blind, placebo-controlled, single and multiple dose escalation Phase 1 study designed to assess the safety, tolerability and pharmacokinetics of oral X-165 in healthy volunteers."

IND • New P1 trial