Technology

Terpenoid Therapeutics, Inc. is a privately-held biotechnology company focused on anti-cancer therapeutics. We use the platform of terpene chemistry to develop candidate drug molecules. Our team is creating, testing, and developing novel drug candidates using cutting-edge technologies. We seek to generate a robust pipeline of terpene-derived therapeutic agents. Two projects are in advanced preclinical testing with lead compounds identified in both projects. One project is focused on discovering small molecule inhibitors of geranylgeranyl diphosphate synthase, a novel target with applicability towards cancer and other indications. Another project is focused on the schweinfurthins, a family of novel cytotoxic agents that disrupt cholesterol metabolism with applicability towards cancer.

Terpenoid Bisphosphonates

Terpenoid’s bisphosphonate project is based on proprietary terpenoid-modified bisphosphonate inhibitors of geranylgeranyl diphosphate synthase (GGDPS), a novel target for which there is no approved drug at this time. Terpenoid predicts that inhibition of GGDPS will result in efficacy in the treatment of primary tumors and metastases (including, but not limited to, bone metastases).

GGDPS forms a key product that is added to specific proteins in a post-translational modification process known as geranylgeranylation and this process is critical to the proper functioning of these proteins. Among the proteins that are geranylgeranylated are ones which are important in cancer and osteoporosis. Inhibition of geranylgeranylation by a Terpenoid GGDPS inhibitor is expected to be beneficial in cancer because geranylgeranylation is crucial to cancer cell growth and cancer spread. The validation of GGDPS as a target in prostate cancer is quite advanced. Additionally, the metabolic pathway that is targeted has already been successfully inhibited, albeit at earlier steps for the treatment of diseases other than cancer. This preclinical profile is differentiated from existing drugs (including the nitrogen-containing bisphosphonates) and indicates that the Terpenoid GGDPS inhibitors will be important additions to the treatment of prostate cancer.

  • U.S. Patent Application Serial No. 60/604,309, entitled “Geranylgeranyl Pyrophosphate Synthase Inhibitors”, filed August 25, 2004, by David Wiemer and Raymond Hohl
  • International Patent Application Serial No. PCT/US05/30304, entitled “Geranylgeranyl Pyrophosphate Synthase Inhibitors”, filed August 25, 2005, by David Wiemer and Raymond Hohl
  • European Patent Application Serial No. 0579154.6, entitled “Geranylgeranyl Pyrophosphate Synthase Inhibitors”, priority date August 25, 2005, by David Wiemer and Raymond Hohl
  • US Patent Issued September 11, 2007 US no. 7,268,124


Terpenoid Schweinfurthins

Terpenoid’s second oncology program is focused on developing a drug with activity against primary brain tumors by interfering with the tumor requirement for a key metabolite, cholesterol. This project is based on the rare schweinfurthin natural products, chemicals whose unique profile of anti-cancer activity was first reported by the National Cancer Institute (NCI) in 1998.

Because the natural source of schweinfurthins is not commercially viable, the TTI founders have synthesized both natural products and numerous analogs which have been patented and exclusively licensed. Over one hundred proprietary compounds have been designed, synthesized, and assayed to assess structure-activity relationships. Some of these compounds potently inhibit human brain tumor cell proliferation, and have direct tumor cell killing effects. A lead candidate and back-up compounds are undergoing efficacy testing currently.

  • U.S. Patent Application Serial No. 60/557,243, entitled “Analogs of Schweinfurthins as Potential Anticancer Agents”, filed March 29, 2004, by David Wiemer, Jeffrey Neighbors, and John Beutler
  • International Application Serial No. PCT/US05/10482, entitled “Analogs of Schweinfurthins as Potential Anticancer Agents”, filed March 29, 2005, by David Wiemer, Jeffrey Neighbors, and John Beutler
  • European Patent Application Serial No. 05760943.0, entitled “Analogs of Schweinfurthins as Potential Anticancer Agents”, priority date March 29, 2005, by David Wiemer, Jeffrey Neighbors, and John Beutler
  • US Patent Issued April 15, 2008, no. 7,358,377.