2ccPA / Orient Europharma - LARVOL DELTA

Lysophosphatidic acid derivative is a novel candidate of therapeutic agents for a mouse model of frontotemporal dementia with progranulin deficiency. (PubMed, Neurobiol Aging) - "Collectively, our findings identify 2ccPA as a promising candidate for the prevention of FTD. This study also represents a conceptual advance by demonstrating that targeting microglial activation is an effective strategy to delay or attenuate neurodegeneration in FTD."

Journal • Preclinical • Alzheimer's Disease • CNS Disorders • Dementia • Frontotemporal Lobar Degeneration • Proteinopathy • CCL8 • TARDBP

The novel autotaxin inhibitor, 2-carba cyclic phosphatidic acid ameliorates bleomycin-induced lung fibrosis in mice. (ERS 2025) - "These findings suggest that 2ccPA is a novel candidate as an antifibrotic agent by blocking the ATX/LPA axis."

Preclinical • Fibrosis • Immunology • Respiratory Diseases • TGFB1

The Effect of Novel Autotaxin Inhibitor, 2-carba Cyclic Phosphatidic Acid, in Lung Fibrosis (ATS 2024) - " For in vivo study, lung fibrosis was induced in mice through intratracheal administration of bleomycin (BLM). These results suggest that 2ccPA may be a novel candidate for antifibrotic agents by blocking the ATX/LPA axis."

Fibrosis • Immunology • Respiratory Diseases • TGFB1

CLINICAL EFFECTIVENESS OF 2-CARBA CYCLIC PHOSPHATIDIC ACID (2CCPA) IN PATIENTS WITH OSTEOARTHRITIS OF THE KNEE: RESULTS OF PHASE I/B STUDY (OARSI 2024) - "Purpose (the aim of the study): 2ccPA, a novel low molecular weight compound with a molecular weight of approximately 400, competitively binds to lysophosphatidic acid (LPA) receptors (LPAR1-LPAR6) on the cell surface in vitro and in vivo and inhibits LPA/ATX signaling. The purpose of this study was to evaluate the safety and pain-relieving effects (WOMAC index) of a single and repeated intra-articular administration of lysophosphatidic acid (LPA) to patients with K-L grade 2~3 of knee OA."

Clinical • Immunology • Osteoarthritis • Pain • Rheumatology • LPAR6

A Study to Evaluate the Safety and Efficacy of 2ccPA in Patients With Symptomatic Knee Osteoarthritis (clinicaltrials.gov) - P1/2 | N=136 | Active, not recruiting | Sponsor: Orient Europharma Co., Ltd. | Recruiting ➔ Active, not recruiting

Enrollment closed • Immunology • Osteoarthritis • Pain • Rheumatology

Two-carba cyclic phosphatidic acid treatment promotes phenotypic switch from M1 to M2 microglia and prevents behavioral abnormalities in a mouse model of neuropsychiatric systemic lupus erythematosus. (PubMed, Hum Cell) - "2ccPA treatment decreased these levels in the MRL/lpr mice. These results suggest that 2ccPA treatment suppresses behavioral abnormalities by promoting a microglial phenotypic switch from M1 to M2 in MRL/lpr mice."

Journal • Preclinical • CNS Disorders • Depression • Immunology • Inflammation • Inflammatory Arthritis • Lupus • Multiple Sclerosis • Psychiatry • Systemic Lupus Erythematosus • Vascular Neurology • ARG1 • CD68

2-Carba cyclic phosphatidic acid regulates blood coagulation and fibrinolysis system for repair after brain injury. (PubMed, Brain Res) - "These results suggest the acute effects of 2ccPA on brain hemostasis. (97 words)."

Journal • CNS Disorders • Inflammation • Vascular Neurology • ITGA2B

Inhibition of the lymphangiogenic actions of human dermal lymphatic endothelial cells in UVB-denatured type I collagen in vitro (WCD 2023) - "In addition, 2-carba cyclic phosphatidic acid (2ccPA), which is a lymphangiogenesis stimulator, enhanced both lymphatic actions... These findings strongly suggest that cutaneous lymphangiogenesis is suppressed by the degeneration of the surrounding type-I collagen due to the action of UVB, which may in turn lead to photoaging such as wrinkles and sagging"

Preclinical

A Phase I-II 2ccPA Study in Patients With Symptomatic Knee (clinicaltrials.gov) - P1/2 | N=136 | Recruiting | Sponsor: Orient Europharma Co., Ltd.

New P1/2 trial • Immunology • Osteoarthritis • Pain • Rheumatology