BHQ880 / Novartis - LARVOL DELTA

THE EMERGING ROLE OF DKK1 IN GASTRIC CARCINOGENESIS AND TARGETING DKK1 BY APTAMER-BASED PROTAC (UEGW 2025) - "Dickkopf-1 (DKK1), frequently overexpressed in GC, is implicated in critical oncogenic processes such as tumorigenesis, epithelial-mesenchymal transition (EMT), cisplatin resistance, and immune evasion...However, clinical outcomes from therapeutic antibodies targeting extracellular DKK1 (e.g., DKN-01, BHQ880) have been disappointing, highlighting the potential importance of intracellular DKK1 functions in cancer progression and underscoring the need for innovative therapeutic strategies addressing both extracellular and intracellular roles... Intracellular DKK1 promotes the progression of GC through the stabilization of β-catenin. Apc102, a novel aptamer-based PROTAC, which has recently been granted the FDA Orphan Drug Designation (DRU-2024-10338), exhibits potent anti-tumor efficacy and safety. This offers a breakthrough for DKK1 - positive gastric cancer."

Dyslipidemia • Gastric Cancer • Oncology • Targeted Protein Degradation • CRBN • DKK1

Enhancing motor functional recovery in spinal cord injury through pharmacological inhibition of Dickkopf-1 with BHQ880 antibody. (PubMed, Biomed Pharmacother) - "Collectively, our findings highlight the therapeutic potential of BHQ880 treatment in the context of SCI."

Journal • CNS Disorders • Orthopedics • DKK1

Identification and characterization of four immune-related signatures in keloid. (PubMed, Front Immunol) - "Through interactive network analysis, we found that these DEIGs were associated with drugs currently used to treat keloid, such as hydrocortisone, androstanolone, irinotecan, oxaliplatin, BHQ-880, and lecoleucovorin. These immune-related signaling molecules may be important modules in the pathogenesis of keloid. Additionally, we developed novel therapeutic targets for the treatment of this challenging disease."

Journal • Fibrosis • CD4 • CD8 • DKK1 • JAG1

[VIRTUAL] Analysis of clinical trials targeting the Wnt signaling pathway for cancer therapy (ASHP 2020) - "The most commonly used drugs, investigated in 3 or more clinical trials included DKN-01 [DKK1 neutralizing monoclonal antibody] (9.9%), PRI-724 [CBP/ β-catenin complex inhibitor] (4%), OMP-54F28 [Decoy Receptor for Wnt lignads] (4%), Vantictumab [monoclonal antibody against Frizzled receptors] (4%), Cirmtuzumab [monoclonal antibody against ROR1] (4%), and BHQ880 [monoclonal antibody against DKK1] (3%). Based on our analysis, we reckon that DKK1 is the most investigated Wnt pathway target in cancer clinical trials, with DKN-01 being the most explored drug. Out of the 91 studies, the highest number of trials were carried out in colorectal cancer, followed by multiple myeloma. The preponderance of the clinical trials in early phases and active status could be the possible reasons for the deficit of Wnt pathway modifiers for cancer therapy in clinical practice."

Clinical • Colorectal Cancer • Gastrointestinal Cancer • Hematological Malignancies • Hepatology • Leukemia • Multiple Myeloma • Oncology • Pancreatic Cancer • Solid Tumor • DKK1 • ROR1 • SPON1

A study to assess BHQ880 in combination with zoledronic acid in relapsed or refractory myeloma patients (clinicaltrials.gov) - P2, N=28 -> 36; Completed -> Active, not recruiting

Enrollment • Enrollment closed • Multiple Myeloma

Study of BHQ880 in Patients With High Risk Smoldering Multiple Myeloma (clinicaltrials.gov) - P2; N=41; Completed; Sponsor: Novartis Pharmaceuticals; Active, not recruiting -> Completed

Trial completion • Biosimilar • Hematological Malignancies • Multiple Myeloma • Oncology

Correlations of DKK1 with pathogenesis and prognosis of human multiple myeloma. (PubMed, Cancer Biomark) - "DKK1 is closely related to the pathogenesis and prognosis of human MM, which might be a potential biomarker for the diagnosis of MM."

Biomarker • Journal