in vitro efficacy
˙ SW1 is a specific ADAM9 inhibitor targeting its protease function and reducing its protein amounts
˙ SW1 broadly reduces KRAS proteins in KRAS wild-type and mutants
˙ A combination of SW1 and gemcitabine shows potent anti-cancer effects
in vivo efficacy
˙ SW1 suppresses tumor growth and prolongs survival in the KrasG12D spontaneous pancreatic cancer model
˙ The combination of SW1 and gemcitabine suppresses tumor growth and prolongs survival in the syngeneic pancreatic cancer model
˙ Potent efficacy of the combination of SW1 and gemcitabine in the patient-derived cell xenograft model (CR:70%; PR:20%; SD: 10%)
Safety pharmacology and general toxicology
Mice are tolerant in the 2-month daily treatment of SW1 without any blood cell count change or liver/kidney damage.
SW1 is very stable on the physical and chemical properties at 4 weeks under acceleration conditions.