The liver or ileum lysates from hamsters were homogenized to detect the protein levels of HMGR, LDLR, CYP7A1 and ASBT by commercial ELISA kits (Biovalue, China) and by western blotting.
To explore the molecular mechanisms for the antihypercholesterolemic efficiency of jatrorrhizine, the mRNA and the protein expression level of related genes including HMGR, LDLR, CYP7A1 and ASBT were investigated by qRT-PCR, ELISA and western blot.
LUM001 is a novel, once-daily, orally-administered, potent and selective ASBT inhibitor that works by preventing recycling of bile acids back to the liver and is thought to reduce bile acid accumulation, improve liver function and potentially relieve the extreme itching associated with cholestatic liver disease.
LUM002 is a novel, once daily, orally-administered, highly potent and selective inhibitor of ASBT, in development for the treatment of nonalcoholic steatohepatitis (NASH), a common and often "silent" liver disease characterized by fat deposits in the liver and inflammation which can progress to significant fibrosis.
About LUM001 LUM001 is a novel, once-daily, orally-administered, potent and selective ASBT
inhibitor, which reduces bile acid intestinal absorption leading to an increase in bile acid excretion and lower levels of bile acids in the liver and systemic circulation.
We see a lot of promise in the therapeutic approach of inhibiting ASBT for the treatment of both rare cholestatic liver diseases as well as the increasingly common NASH," said Ed Mathers, partner, NEA, who will join Lumena's board of directors in conjunction with the financing.
About LUM002 Lumena's second product candidate, LUM002, is a novel, once-daily, orally-administered, highly-potent and selective inhibitor of ASBT being developed for the treatment of NASH, a common, often "silent" liver disease characterized by fat deposits in the liver, leading to inflammation and significant fibrosis.
The study showed that inhibiting ASBT with SC-435, a close analog of LUM001, the company's lead drug candidate for the treatment of cholestatic liver disease, significantly improved markers of liver function in rats that had undergone partial bile duct ligation (pBDL) surgery to induce a state of cholestasis.
ASBT recycles intestinal bile acids back into the circulation and blocking it with a once-daily oral presentation, such as LUM001, reduces serum bile acids and may offer a novel therapeutic approach for alleviating the severe itching and progressive liver damage associated with many cholestatic liver diseases.
Lumena also licensed the patent rights and a package of clinical and non-clinical data from Sanofi for LUM002, a highly potent, selective inhibitor of ASBT