Drug Discovery

The pharmaceutical industry has over the last decades been confronted with an increased failure rate of (candidate) drugs in late development stages and even after approval and commercialization. Part of this undesirable outcome is clearly linked to the physical chemical properties of the new drugs, which are applied to optimize their target potency. However, this tack seems to be a kiss of death, as just these applied properties increase the risk for Drug-Induced Liver Injury (DILI), and thus the risk for failure of the new drug. Inorbit has developed a unique, groundbreaking chemistry platform to change these properties by replacing the often used sensitive groups and to reduce lipophilicity, but still maintaining potency at the target, thus increasing chances for successful development and commercialization. Inorbit sees it as an opportunity to apply its chemistry platform especially to drugs with demonstrated efficacy in late stage clinical studies, but which have failed due to DILI, thus resuscitating these once promising new drugs.

The InorbitTX Approach:

  • Selective scouting and targeting efficacious drugs, which carry the sensitive group on interest, have high lipophilicity, and thus are at high risk for DILI.
  • Replacement of the sensitive group to reduce the lipophilicity and glucuronidation potential of molecules.
  • Establishment of strong initial assurance of safety and efficacy, optimizing the chances for successful drug development and commercialization.
  • A virtual, flexible way of working, using an extensive, reliable, high quality and cost effective network of collaborators, predominantly in India.

The Inorbit Advantage:

  • Patentable distinct designed compounds based on molecules with proven efficacy in patients.
  • Highly efficient way to identify and characterize lead compounds and candidate drugs.
  • Significantly shortened drug discovery timeline at reduced cost.

Projects and Market

InorbitTX’s efforts are focused on therapeutic areas with a high unmet medical need, a strong market perspective and in which a solid Intellectual Property position can be established. Inorbit’s lead discovery projects include 3 targets  for the treatment of fatty liver diseases (NAFLD / NASH; FXR, DGAT2, and KHK), 2 for Kidney Disease (XO and KHK), and 1 for gout (XO). The Company has identified numerous targets in other highly interesting therapeutic areas to which InorbitTX’s specific chemistry can be applied as well. All targets have demonstrated efficacy in humans.

Current Status

Progress in the NASH projects confirms that Inorbit’s novel compounds show reduced lipophilicity (ΔLogD= -1.5 to -2), show high target potency in cell based assays, and show drug-like properties in in vitro and in vivo test systems. Project progress is in line with initiation of GLP toxicity testing in 9-12 months.