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DRUG:

Prolia (denosumab)

i
Other names: AMG 162, AMG162, AMG-162
Company:
Amgen, BeOne Medicines, Daiichi Sankyo
Drug class:
RANK ligand inhibitor
3d
Bufalin suppresses breast cancer bone metastasis through targeting SEC13-mediated osteoclastogenesis. (PubMed, Phytomedicine)
BU demonstrates potent pharmacological activity against breast cancer bone metastasis by targeting SEC13 and suppressing tumor-induced osteoclast differentiation. This effect is mediated through inhibition of HMGB1 release and blockade of the TLR4/NF-κB signaling axis, leading to reduced osteoclast formation and inhibition of metastatic progression.
Journal
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HMGB1 (High Mobility Group Box 1) • TLR4 (Toll Like Receptor 4)
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Prolia (denosumab)
12d
The role of osteoprotegerin in colorectal cancer: Molecular interactions, mechanistic insights, and therapeutic implications. (PubMed, Cytokine Growth Factor Rev)
Current research has predominantly focused on the RANKL signaling pathway, leading to development of anti-RANKL therapeutics such as Denosumab, while OPG-specific therapeutics remain underdeveloped. Collectively, future research could investigate whether compartment-specific OPG levels could serve as a biomarker for CRC and predict responses to immunotherapeutics, alongside drug repurposing of existing anti-RANKL therapeutics, and non-pharmacological strategies targeting OPG.
Review • Journal • IO biomarker
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TNFRSF11B (Tumor necrosis factor receptor superfamily member 11B)
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Prolia (denosumab)
16d
Recombinant LGR4 extracellular domain attenuates osteoclastogenesis and prevents bone metastasis via RANKL inhibition. (PubMed, J Bone Oncol)
Current therapies, such as bisphosphonates and denosumab, offer limited survival benefits and carry significant safety risks, highlighting the need for novel agents that effectively inhibit osteolytic progression...rLGR4-ECD effectively inhibits RANKL-induced osteoclastogenesis and reduces bone metastasis burden through specific suppression of osteoclast activity, leading to improved survival in a preclinical model. Its excellent efficacy and manufacturability support its potential as a novel therapeutic agent for bone metastatic disease.
Journal
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CTSK (Cathepsin K) • NFATC1 (Nuclear Factor Of Activated T Cells 1) • LGR4 (Leucine Rich Repeat Containing G Protein-Coupled Receptor 4)
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Prolia (denosumab)
1m
Successful selpercatinib treatment of metastatic medullary thyroid cancer carrying rare RET variant (PubMed, Magy Onkol)
This case underscores the value of liquid biopsy detected mutations in guiding targeted therapy. Clinical, biochemical, and radiological findings support the potential use of selective RET tyrosine kinase inhibitors for this rare mutation. Serum calcitonin serves as a reliable quantitative biomarker of therapeutic efficacy.
Journal
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RET (Ret Proto-Oncogene)
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RET mutation
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Retevmo (selpercatinib) • Prolia (denosumab)
1m
Enrollment closed
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Prolia (denosumab)
1m
The Association Between Longitudinal Changes in TRACP-5b and Bone Metastasis Progression During Osimertinib Therapy. (PubMed, Anticancer Res)
Serial monitoring of TRACP-5b may provide supplementary information for detecting BM progression in patients with NSCLC treated with osimertinib.
Retrospective data • Journal
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EGFR (Epidermal growth factor receptor)
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EGFR mutation
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Tagrisso (osimertinib) • Prolia (denosumab)
1m
Synergistic effects of denosumab and BMP-2 on bone regeneration in critical-sized femoral defects in ovariectomized rats. (PubMed, J Mater Sci Mater Med)
Moreover, DNB/BMP-2 significantly improved torsional stiffness and maximum compressive force versus either treatment alone (all P < 0.05). The findings demonstrate that systemic DNB combined with local BMP-2 rapidly promotes femoral metaphyseal bone regeneration in osteoporotic rats.
Preclinical • Journal
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TNFA (Tumor Necrosis Factor-Alpha) • SPP1 (Secreted Phosphoprotein 1) • RUNX2 (RUNX Family Transcription Factor 2) • TNFRSF11B (Tumor necrosis factor receptor superfamily member 11B) • BMP2 (Bone Morphogenetic Protein 2)
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Prolia (denosumab)
1m
Targeting RANKL-independent osteoclastogenesis overcomes denosumab resistance in models of ER+ breast cancer bone metastasis. (PubMed, J Clin Invest)
Pharmacological inhibition of CARM1 (TP-064) effectively suppressed osteoclastogenesis and bone metastasis in denosumab-resistant models. These findings revealed a targetable resistance mechanism and provided a clinically actionable strategy to overcome microenvironment-driven metastasis through dual targeting of tumor and bone niches.
Journal
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ER (Estrogen receptor) • CRKL (CRK Like Proto-Oncogene, Adaptor Protein) • NFATC1 (Nuclear Factor Of Activated T Cells 1) • EIF4A3 (Eukaryotic Translation Initiation Factor 4A3)
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ER positive
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Prolia (denosumab)
2ms
Herpes Zoster Following Chemo-Immunotherapy With Pembrolizumab in Metastatic Non-small Cell Lung Cancer: A Case Report. (PubMed, Cureus)
This case illustrates herpes zoster reactivation during Pembrolizumab-based chemo-immunotherapy in metastatic NSCLC. It emphasizes the importance of systematically excluding infectious causes in new cutaneous eruptions under immunotherapy and supports multidisciplinary management. These findings also highlight the need to further explore VZV screening and vaccination strategies in cancer patients undergoing immunosuppressive treatments.
Journal • PD(L)-1 Biomarker • IO biomarker
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PD-L1 (Programmed death ligand 1)
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PD-L1 expression
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Keytruda (pembrolizumab) • carboplatin • pemetrexed • Prolia (denosumab)
2ms
Trial completion
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Prolia (denosumab)
2ms
Integrated Transcriptomic, Proteomic, and Pharmacologic Profiling of 2D and 3D Patient-Derived GCTB Cell Lines Reveals Culture-Dependent Drug Response Determinants. (PubMed, Proteomics)
Giant cell tumor of bone (GCTB) is an intermediate bone neoplasm defined by recurrent H3F3A mutations and limited systemic treatment options beyond denosumab...Functionally, 3D culture generally reduced sensitivity to many agents while preserving compound-dependent vulnerabilities. These results establish culture dimensionality as a key determinant of therapeutic susceptibility in GCTB PDCs and support incorporating proteome-informed 3D models into translational pipelines to prioritize clinically relevant drug candidates and biomarkers.
Preclinical • Journal
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H3-3A (H3.3 Histone A)
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Prolia (denosumab)
2ms
Case Report: Rare gastric and bone metastases after early endocrine therapy discontinuation in hormone receptor-positive breast cancer: lessons and therapeutic insights. (PubMed, Front Oncol)
She received first-line endocrine therapy (letrozole+ribociclib+goserelin) combined with denosumab. Breast cancer gastric metastasis diagnosis relies on medical history, gastroscopy, and immunohistochemistry (GATA3+, CK7+, CK20-). The combination regimen yielded favorable efficacy, providing clinical reference for similar rare cases.
Journal
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HER-2 (Human epidermal growth factor receptor 2) • PGR (Progesterone receptor) • GATA3 (GATA binding protein 3)
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HR positive
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Kisqali (ribociclib) • letrozole • Prolia (denosumab) • goserelin acetate