Oncocort (pegylated liposomal dexamethasone) / Enceladus - LARVOL DELTA

A Joint-targeting Peptide Enhances the Therapeutic Efficacy of Liposomal Drug Delivery in Experimental Rheumatoid Arthritis (ACR Convergence 2024) - "Another set of animals were treated with liposomal dexamethasone or unpackaged (free) dexamethasone, beginning at the onset of arthritis and then continued on alternate days thereafter... Taken together, the therapeutic profile of dexamethasone was significantly improved by using peptide-displaying liposomes. Our results offer a proof-of concept for the benefits of targeted drug delivery to the joints for arthritis therapy. We hope that after appropriate modifications, this drug delivery platform might also be suitable for use in RA patients."

Clinical • Immunology • Inflammation • Inflammatory Arthritis • Rheumatoid Arthritis • Rheumatology

Neutrophil Hitchhiking Enhances Liposomal Dexamethasone Therapy of Sepsis. (PubMed, ACS Nano) - "Additionally, they mitigate inflammatory cytokines systemically and locally while preserving systemic IL-10 levels, contributing to lower IFN-γ/IL-10 ratios as compared to control liposomes and free dexamethasone. Our strategy addresses sepsis at the cellular level, illustrating the use of neutrophils both as a therapeutic target and as a chariot for drug delivery."

Journal • Infectious Disease • Septic Shock • IFNG • IL10

CRISPR-Cas9 genome and long non-coding RNAs as a novel diagnostic index for prostate cancer therapy via liposomal-coated compounds. (PubMed, PLoS One) - "dose of 3, 2'- dimethyl-4-aminobiphenyl estradiol (DAE) (50mg/kg) followed by treatment via targeted liposomal-coated compounds such as liposomal dexamethasone (DXM), liposomal doxorubicin (DOX) and liposomal Turmeric (TUR) (3mg/kg IP) for four weeks in a comparative study to their non-targeted analogue dexamethasone, doxorubicin and Turmeric...On the other hand, gene expression of apoptotic biomarkers focal adhesion kinase (AKT-1), phosphatidylinistol kinase (PI3K) and glycogen synthase kinase-3 (GSK-3) was also investigated and further confirming these results via histopathological examination. Liposomal loaded dexamethasone; doxorubicin and Turmeric can be considered as promising therapeutic agents for prostate cancer via modulating CRISPR/Cas9 gene editing and long non coding gene MALAT1."

Journal • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor • AKT1 • MALAT1

Autoantigen-dexamethasone Conjugate-Loaded Liposomes Halt Arthritis Development in Mice. (PubMed, Adv Healthc Mater) - "Antigen-pulsed tolerogenic dendritic cells induced by liposomal dexamethasone in vitro enhanced antigen-specific regulatory T cells to a similar extent as dexamethasone-induced tolerogenic dendritic cells...This coincided with systemic tolerance induction and an increase in IL10 expression in the paws of mice. In conclusion, a single administration of autoantigen and dexamethasone-loaded liposomes seems to be a promising antigen-specific treatment strategy for arthritis in mice."

Journal • Preclinical • Immunology • Inflammation • Inflammatory Arthritis • Rheumatoid Arthritis • Rheumatology • IL10

The Utility of Peptide Ligand-Functionalized Liposomes for Subcutaneous Drug Delivery for Arthritis Therapy. (PubMed, Int J Mol Sci) - "Finally, liposomal dexamethasone administered SC was more effective than the unpackaged (free) drug in suppressing arthritis progression in rats. We suggest that with suitable modifications, this SC liposomal treatment modality can be adapted for human RA therapy."

Journal • Immunology • Inflammatory Arthritis • Oncology • Rheumatoid Arthritis • Rheumatology

Evaluation of Cellular Toxicity and Preclinical Safety of Using an Inhalable Liposomal form of Dexamethasone. (PubMed, Pharm Chem J) - "Experiments on laboratory white rats of both sexes revealed that the inhalation use of liposomal dexamethasone insignificantly changed the functional parameters of their respiratory and cardiovascular systems. The study results could be used for conducting clinical trials."

Journal • Preclinical • Cardiovascular

A phase I first-in-man study to investigate the pharmacokinetics and safety of liposomal dexamethasone in patients with progressive multiple myeloma. (PubMed, Drug Deliv Transl Res) - "Thus, despite the limitations of this small first-in-man trial, Dex-PL seems safe and well tolerated without severe side effects. Follow-up studies are needed to confirm this in a larger patient cohort and to evaluate if i.v. Dex-PL can provide a safer and more efficacious dexamethasone treatment option for MM."

Journal • P1 data • PK/PD data • Hematological Malignancies • Infectious Disease • Multiple Myeloma • Oncology

Liposteroid Therapy for Idiopathic Pulmonary Hemosiderosis: A Scoping Review of the Literature. (PubMed, Prague Med Rep) - "This paper reviews and evaluates the efficacy and safety profile of liposomal dexamethasone 21-palmitate (liposteroid) for the treatment of IPH...Liposteroid represents a potential alternative or supplement to conventional CS therapy, as it appears to be more efficacious and associated with fewer side effects. Larger prospective, controlled trials are necessary to be able to define more precisely the therapeutic role of liposteroid in IPH."

Journal • Review • Hematological Disorders • Pediatrics

Liposomal Dexamethasone Reduces A/H1N1 Influenza-Associated Morbidity in Mice. (PubMed, Front Microbiol) - "The liposomal dexamethasone was mainly distributed into the monocyte/macrophages as a major cell population for inducing the cytokine storm in the lungs. Taken together, the intranasal delivery of liposomal dexamethasone may serve as a novel promising therapeutic strategy for the treatment of influenza A-induced pneumonia."

Journal • Preclinical • Immunology • Infectious Disease • Inflammation • Oncology • Pneumonia • Respiratory Diseases • CCL2 • CXCL2 • IL1B • IL6 • TNFA

ROS-mediated liposomal dexamethasone: a new FA-targeted nanoformulation to combat rheumatoid arthritis via inhibiting iRhom2/TNF-α/BAFF pathways. (PubMed, Nanoscale) - "The anti-inflammatory mechanism of Dex@FA-ROS-Lips was further studied and it was found that it is possibly associated with the down-regulation of iRhom2 and the activation of the TNF-α/BAFF signaling pathway. Therefore, the integration of nanomedicines and the RA microenvironment using multifunctional Dex@FA-ROS-Lips shall be a novel RA treatment modality with full clinical potential, and based on the enhanced therapeutic effect, the signaling pathway of iRhom2/TNF-α/BAFF reasonably explained the mechanism of Dex@FA-ROS-Lips in anti-RA, which suggested a molecular target for RA therapy and other inflammatory diseases."

Journal • Immunology • Inflammation • Inflammatory Arthritis • Rheumatoid Arthritis • Rheumatology • TNFA

An exploratory first-in-man study to investigate the pharmacokinetics and safety of liposomal dexamethasone at a 2- and 1-week interval in patients with metastatic castration resistant prostate cancer. (PubMed, Pharmacol Res Perspect) - "The data presented support further clinical investigation in well-powered studies. Clinical trial registration: ISRCTN 10011715."

Clinical • Journal • PK/PD data • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Hyaluronan-Loaded Liposomal Dexamethasone-Diclofenac Nanoparticles for Local Osteoarthritis Treatment. (PubMed, Int J Mol Sci) - "Single-dose injection could reduce the inflammation volume down to 77.5 ± 5.1% from initial over that time span. Our results provided the novel drug-releasing formulation with safety and efficiency which could be a promising system for osteoarthritis pain control."

Journal • Immunology • Inflammation • Musculoskeletal Diseases • Musculoskeletal Pain • Orthopedics • Osteoarthritis • Pain • Rheumatology

Sialic Acid Conjugate-Modified Liposomal Dexamethasone Palmitate Targeting Neutrophils for Rheumatoid Arthritis Therapy: Influence of Particle Size. (PubMed, AAPS PharmSciTech) - "However, a high intake of large DP-SALs by PBNs inhibited their migration ability and capacity to release the payload at the target site. In contrast, small DP-SALs (75.0 ± 3.9 nm) could maintain the drug delivery potential of PBNs, leading to their efficient accumulation at the inflammatory site, where PBNs would be excessively activated to form neutrophil extracellular traps along with efficient payload release (small DP-SALs) and finally to induce excellent anti-RA effect."

Journal • Immunology • Inflammatory Arthritis • Rheumatoid Arthritis • Rheumatology

AMETHYST: A Evaluation of the Safety of Oncocort IV Pegylated Liposomal Dexamethasone Phosphate in Patients With Progressive Multiple Myeloma (clinicaltrials.gov) - P1/2; N=7; Terminated; Sponsor: Enceladus Pharmaceuticals BV; N=35 ➔ 7; Trial completion date: Mar 2019 ➔ Aug 2020; Not yet recruiting ➔ Terminated; Trial primary completion date: Dec 2018 ➔ Aug 2020; Patient enrolment issues

Clinical • Enrollment change • Monotherapy • Trial completion date • Trial primary completion date • Trial termination • Hematological Malignancies • Multiple Myeloma • Oncology

Liposomal dexamethasone inhibits tumor growth in an advanced human-mouse hybrid model of multiple myeloma. (PubMed, J Control Release) - "The liposomal formulation slightly reduced total body weight of myeloma-bearing mice during the course of treatment, which appeared reversible when treatment was stopped. Liposomal dexamethasone could be further developed as monotherapy or could fit in with existing therapy regimens to improve therapeutic outcomes for multiple myeloma."

Journal • Preclinical • Hematological Disorders • Hematological Malignancies • Multiple Myeloma • Oncology

Liposomal dexamethasone-moxifloxacin nanoparticles combinations with collagen/gelatin/alginate hydrogel for corneal infection treatment and wound healing. (PubMed, Biomed Mater) - "An animal study also confirmed that CGA-Lipo-MFX/DEX could inhibit pathogen microorganism growth and improve corneal wound healing. Our results suggest that CGA-Lipo-MFX/DEX could be a useful anti-inflammatory formulation for ophthalmological disease treatment."

Journal • Immunology • Keratitis • Ocular Infections • Ocular Inflammation • Ophthalmology • CGA, CHGA

Neutrophil-Mediated Delivery of Dexamethasone Palmitate-Loaded Liposomes Decorated with a Sialic Acid Conjugate for Rheumatoid Arthritis Treatment. (PubMed, Pharm Res) - "SA-modified liposomal DP was a promising candidate for RA-targeting treatment through the neutrophil-mediated drug delivery system."

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