INCB-003284 / Incyte - LARVOL DELTA

Choroid plexus CCL2‒CCR2 signaling orchestrates macrophage recruitment and cerebrospinal fluid hypersecretion in hydrocephalus. (PubMed, Acta Pharm Sin B) - "Furthermore, the administration of CCR2 antagonist (INCB 3284) reduces ChP macrophage accumulation and ventriculomegaly. This study not only unveils the ChP CCL2‒CCR2 signaling in the pathophysiology of hydrocephalus but also unveils Bindarit as a promising therapeutic choice for the management of posthemorrhagic hydrocephalus."

Journal • CNS Disorders • Hematological Disorders • Inflammation • Ventriculomegaly • CCL2 • CCR2 • TNFA • TNFRSF1A

A Systems Biology Approach for Investigating Significant Biomarkers and Drug Targets Common Among Patients with Gonorrhea, Chlamydia, and Prostate Cancer: A Pilot Study. (PubMed, Bioinform Biol Insights) - "Three potential therapeutic compounds namely INCB3284, CCX915, and MLN-1202 were found to interact with up-regulated protein C-C chemokine receptor type 2 (CCR2) in protein-drug interaction analysis. The proposed biomarkers and therapeutic potential molecules could be investigated for potential pharmacological targets and activity in the fight against in patients with gonorrhea, chlamydia, and prostate cancer."

Biomarker • Journal • Genito-urinary Cancer • Infectious Disease • Oncology • Prostate Cancer • Solid Tumor • APP • CCR2 • DERL1 • GATA6 • HIVEP1 • KMT2B • MARCKS • MIR7 • PRNP • PROS1 • PTGS1 • SH3BGRL • SLC40A1 • SLFN11

Effects of chemokine (C-C motif) receptor 2 and 3 antagonists in rat models of hemorrhagic shock. (PubMed, PLoS One) - "We reported previously that the CCR2 antagonist INCB3284 prevents cardiovascular collapse and reduces fluid requirements after 30min of hemorrhagic shock (HS), whereas the CCR5 antagonist Maraviroc was ineffective. Series 4: INCB3284 and SB328437 did not affect survival time in a lethal HS model without FR. Our findings further support the assumption that blockade of the major CCL2 receptor CCR2 is a promising approach to improve FR after HS and document that the dosing of INCB3284 can be optimized."

Journal • Preclinical • Cardiovascular • Hematological Disorders • CCL2 • CCR2

The Chemokine (C-C Motif) Receptor 2 Antagonist INCB3284 Reduces Fluid Requirements and Protects From Hemodynamic Decompensation During Resuscitation From Hemorrhagic Shock. (PubMed, Crit Care Explor) - "Our findings suggest that CCR2 is involved in the regulation of normal cardiovascular function and during the cardiovascular stress response to hemorrhagic shock and fluid resuscitation. The present study identifies CCR2 as a drug target to reduce fluid requirements and to prevent death from hemodynamic decompensation during resuscitation from hemorrhagic shock."

Journal • Anesthesia • Cardiovascular • Hematological Disorders • Inflammation • CCL11 • CCL2

Chemokine receptor antagonists with α-adrenergic receptor blocker activity. (PubMed, J Basic Clin Physiol Pharmacol) - "Our data suggest that CCR antagonists should be screened for cross-reactivity with α-adrenoceptors to exclude potential adverse cardiovascular effects when used as anti inflammatory drugs."

Journal • Cardiovascular • CCR10 • CCR4

Activated Hepatic Stellate Cells Induce Infiltration and Formation of CD163 Macrophages via CCL2/CCR2 Pathway. (PubMed, Front Med (Lausanne)) - "To explore whether CCL2/CCR2 axis has a crucial role in macrophage phenotypic changes during liver fibrosis, we treated the M0MΦ with recombinant human CCL2 or its specific receptor antagonist INCB-3284... The expression of the M2 macrophage marker increases during liver fibrosis progression and is associated with fibrosis severity. AHSCs can recruit macrophages through the CCL2/CCR2 pathway and induce M2 phenotypic transformation."

Journal • Fibrosis • Hepatitis B • Hepatology • Immunology • Infectious Disease • Liver Cirrhosis • CCL2 • CD163 • IL10 • TGFB1