The Central Drug Research Institute (CDRI), the public sector premier institution for drug discovery, has developed some concrete leads in key therapeutic areas like cancer and diabetes and is looking for industry partners to further develop the same into drugs.
One of the potential new leads is to fight osteoporosis and is open for licensing. The compound (S007-1500) is for rapid fracture healing. Mechanism of action studies show that compound stimulates osteoblast differentiation by activating ER/BMP2 signalling pathway. Further studies are in progress. It is safe in Single Dose Toxicity Studies in Rat and mice by oral route (50,100 mg/kg bw), according to a report by the CDRI.
Two compounds have been found to fight cancer. The anti-leukaemic compound (S007-1235) was found be having higher efficacy than salinomycin. The other compound (S-009-131) is an oral administration which resulted in regression of tumours induced by HeLa cell xenografts in nod SCID mice. The institute is scouting for partner for this also.
Two other compounds are against diabetes and dyslipidemia. Antidyslipidemic agent ( CDR267F018) is standardised fraction from mangrove fruit and has potent anti-dyslipidemic activity in various animal models of dyslipidemia having both preventive and curative potential. The compound has been found safe in monkey toxicity studies and have been recommended for filing IND.
CDR914K058, the other compound, showed protection against dex-induced insulin resistance. “In db/db mice K058 induced robust glucose clearance, drastically improved lipid profile, eliminated hepatic steatosis, protected pancreatic beta cells against diabetes-induced apoptosis and induced browning in white adipose tissue. Detailed mechanistic analysis revealed that K058 is the first in class,” the report said.
The premier institution is also in talks with some companies to license two other compounds to fight thrombosis. The anti-thrombotic chiral compound (S007-867) exhibited potential anti-thrombotic efficacy in various experimental models of thrombosis with nominal increase in the bleeding time. Safety pharmacology and toxicity studies have found it safe. It is a first in class approach for potential anti-platelet molecule.
S002-333 is yet another prototype to prevent platelet collagen interaction and potential anti-platelet racemic molecule. Safety studies conducted so far have demonstrated it to be safe, the report said.