BHQ880

First-in-class, fully human, anti-DKK-1 neutralizing antibody

• The Wnt pathway is a major regulator of mesenchymal stem cell (MSC) differentiation into osteoblasts as well as an important survival factor for active osteoblasts.⁶⁶
• Dickkopf-1 (DKK-1) is a soluble Wnt pathway antagonist expressed predominantly in adult bone and upregulated in myeloma patients with osteolytic lesions.⁶⁶
• Overexpression of DKK-1 by myeloma cells may upset the normal balance between osteoblasts and osteoclasts by blocking osteoblast differentiation and turning off anabolic bone formation, thus promoting bone resorption.⁶⁶
• Certain antitumor treatments used for myeloma, such as dexamethasone, have been reported to upregulate DKK-1.⁶⁷
• Agents targeting DKK-1 may play a role in preventing osteolytic bone disease in multiple myeloma patients.
• BHQ880 is a first-in-class, fully human, anti-DKK-1 neutralizing antibody.⁶⁸ Preclinical studies support the hypothesis that BHQ880 promotes bone formation and thereby inhibits tumor-induced osteolytic disease.
• BHQ880 is currently in Phase I/II clinical trials in multiple myeloma.

All compounds are either investigational or studied in new indications. Efficacy and safety have not been established. There is no guarantee that they will become commercially available.

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