CDRI Compound S007-1500 (Novel Orally Active Fracture Healing Drug Candidate)

• Currently there is no orally active FDA approved fracture healing drug available nationally or internationally. 

• CDRI discovered first-in-class orally active fracture healing drug candidate S007-1500, IND application filed on Dec 14, 2020 for Phase I clinical trial approval by DCG (I).

• First-in-Class orally active fracture repairing drug candidate.
• Enhances osteoblast differentiation and mineralization at concentration as low as 1pM (EC₅₀= 3.125 nM).
• Enhances new bone formation and restores bone microarchitecture in adult osteopenic rats.
• Enhances bone regeneration at fracture site at only 1 mg.kg-1.day-1 dose by stimulation of BMP/Smad signaling pathway
• New bone formation at the fracture site is increased by ~40% in rats treated with S007-1500.
• S007-1500 enhances bone mineral density, new bone formation and bone biomechanical strength in ovariectomized osteopenic rat model.
• S007-1500 restores ovariectomized (Ovx) induced deterioration in bone microarchitecture.
• S007-1500 prevents Ovx induced increase in bone resorptive marker, CTx (a collagen breakdown product).
• S007-1500 prevents Ovx induced increase in bone turnover marker like serum OCN.
• Oral administration of S007-1500 at 1 mg/kg in rabbit critical size defect model led to almost complete bone healing at defect site as analyzed by radiography.

S007-1500 is found safe in regulatory toxicity and safety pharmacology in GLP (rodents and non-rodents) as per Schedule “Y” and FDA guidelines.

• Potential osteogenic property and shows accelerated fracture repairing. New bone formation at the fracture site is increased by ~40% in rats.
• Increases callus formation at only 1 mg/kg dose and restores trabecular microarchitecture at fractured site in normal male and female and osteopenic rats.
• Increases bone healing in male and female New Zealand white rabbits at a dose as low as 1.0 mg.kg-1.day-1
• It leads to accelerated fracture repair by BMP-2/Smad signaling pathway.
• Compound found safe in single dose toxicity studies in rodents and in 10 days DRF studies.

• Essential Safety Pharmacology and Regulatory Toxicity study (Rodents and Non-rodents -dog) in GLP as per schedule Y/ FDA is completed and no mortality/adverse effect was observed.
• No orally active drug available in market. FDA has approved rhBMP-2 bone graft for open tibial fractures but it has several side effects and is very expensive.
• S007-1500 synthesis is industrially acceptable five step process. It will be cost effective and easily affordable.
• Will enable return to active life much faster