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Inverse Agonists of the TSH Receptor for the Treatment of Thyroid Cancer and Hyperthyroidism

Posted Oct 11 2010 8:00pm

Description of Invention:
This technology features small molecule inverse agonists of the thyroid-stimulating hormone (TSH) receptor that may be readily synthesized, and are likely to prove effective for oral administration. These compounds may potentially be used to treat recurrent thyroid cancer and some cases of hyperthyroidism, and also represent unique tools for investigating the role of TSH receptor signaling in these diseases.

According to the National Cancer Institute, over 37,000 new cases of thyroid cancer were diagnosed in the United States in 2008. Approximately 10% to 30% of patients thought to be disease-free after initial treatment will develop recurrent cancer or metastases, and unless the recurrence is detected early, the prognosis is generally poor.

As the TSH receptor is known to stimulate proliferation of thyroid cancer cells, it has been suggested that suppression of basal TSH receptor signaling may improve outcomes in the treatment of recurrent thyroid cancer. The compounds disclosed in this technology suppress basal signaling by the TSH receptor, and are thus excellent candidates for a suppression-based treatment approach.

  • Lead compounds for the development of therapeutics for recurrent or metastatic thyroid cancer.
  • Lead compounds for the development of therapeutics for hyperthyroidism associated with constitutive TSH receptor signaling.
  • Tool for probing the role of basal TSH signaling in normal endocrine function and in disease states.

Development Status:
In vitro studies in primary human thyrocytes have been performed.

Marvin C Gershengorn (NIDDK)
Susanne E Neumann (NIDDK)
Craig J Thomas (NIDDK)
Wenwei Huang (NHGRI)

Patent Status:
HHS, Reference No. E-067-2010/0
US, Application No. 61/322,138 filed 08 Apr 2010

Related Technologies:
US, Application No. 60/801,370 filed 17 May 2006, Reference No. E-223-2006/0
US, Application No. 12/291,932 filed 14 Nov 2008, Reference No. E-223-2006/1
PCT, Application No. PCT/US2008/011958 filed 20 Oct 2008, Reference No. E-284-2008/0

Relevant Publication:
  1. S Neumann, W Huang, E Eliseeva, S Titus, CJ Thomas, MC Gershengorn. A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. Endocrinology. 2010 Jul;151(7):3454-3459. [ PubMed: 20427476 ]
  2. S Moore, H Jaeschke, G Kleinau, S Neumann, S Costanzi, JK Jiang, J Childress, BM Raaka, A Colson, R Paschke, G Krause, CJ Thomas, MC Gershengorn. Evaluation of small-molecule modulators of the luteinizing hormone/choriogonadotropin and thyroid stimulating hormone receptors: structure-activity relationships and selective binding patterns. J Med Chem. 2006 Jun 29;49(13):3888-3896. [ PubMed: 16789744 ]
  3. S Neumann, G Kleinau, S Costanzi, S Moore, BM Raaka, CJ Thomas, G Krause, MC Gershengorn. A low molecular weight antagonist for the human thyrotropin receptor with therapeutic potential for hyperthyroidism. Endocrinology. 2008 Dec;149(12):5945-5950. [ PubMed: 18669595 ]

Licensing Status:
Available for licensing.

Collaborative Research Opportunity:
The NIDDK Office of Technology Transfer and Development is seeking statements of capability or interest from parties interested in collaborative research to further develop inverse agonists of the TAS receptor. Please contact Marguerite J. Miller at 301-496-9003 or for more information.

Cancer - Therapeutics
Cancer - Research Materials
Internal Medicine
Internal Medicine - Therapeutics
Internal Medicine - Research Materials

For Licensing Information Please Contact:
Tara Kirby Ph.D.
NIH Office of Technology Transfer
6011 Executive Blvd. Suite 325,
Rockville, MD 20852
United States
Phone: 301-435-4426
Fax: 301-402-0220

Ref No: 2172

Updated: 10/2010

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