Small molecules for bone diseases

Abstract

Importance of the field: Bones play many roles in the body, providing structure, protecting organs, anchoring muscles and storing calcium. Over 100 million people worldwide suffer from bone diseases, mainly osteoporosis, cancer-related bone loss, osteoarthritis and inflammatory arthritis. Osteoporosis itself has no specific symptoms, and the main consequence is the increased risk of bone fractures. Therefore, the prevention of bone diseases is important to maintain the quality of life in the human society. However, treatment options are still insufficient.

Areas covered in this review: This review article gives a summary of the low molecular mass modulators of bone diseases targets disclosed in patent applications and articles, mainly during the last 5 years.

What the reader will gain: Readers will rapidly gain an overview of these modulators not only for historical targets, but also of emerging and re-visited targets. Readers will also be able to see the current research trend and the main players in this field.

Take home message: Drug discovery for bone diseases has made progress in the last years. The research area has dynamically shifted from historical targets (bisphosphonate, parathyroid hormone and calcitonin) to newly confirmed targets or targets re-visited which were biologically validated in the past. Cathepsin K inhibitors should be very close to launching in the market.

Keywords::

• α_vβ₃ antagonists
• bisphosphonate
• bone disease
• cathepsin K
• cyclooxygenase-2
• MMP
• prostaglandin EP4 receptor
• secreted Frizzled-related protein
• vacuolar H⁺-ATPase

Acknowledgements

The authors are grateful to C McCarthy for the critical reading of the manuscript.

Notes

This box summarizes key points contained in the article.