SBIR-STTR Award

The objective of this proposal is to develop a novel folate receptor- based radiopharmaceutical. 111In-DTPA-folate, into a clinical product for the diagnostic imaging of human tumors. The folate receptor has been exploited as a tumor marker because of its significant overexpression in roughly one third of human cancers including over 90% of ovarian and endometrial carcinomas. In the Phase I project period, efforts will be focused on the following Specific Aims: 1) to optimize the method of radiopharmaceutical synthesis, formulation. and determination of product stability; 2) to conduct toxicity studies in two mammalian species to determine product safety; and 3) to prepare an IND application for submission to the FDA to obtain approval to initiate a Phase I/II clinical trial. Aim 1 will be accomplished by contract research in the laboratories of Drs. Mark Green in the Department of Medicinal Chemistry and Philip Low in the Department of Chemistry at Purdue University. Aim 2 will be performed in a contract toxicology laboratory in compliance with GLP standards. Aim 3 will be accomplished at Endocyte. Inc. 111In- DTPA-folate may be developed into a highly sensitive tissue-specific imaging agent that leads to significant improvements in the diagnosis and treatment of many primary and metastatic tumors. PROPOSED COMMERCIAL APPLICATION: The proposed project is aimed at developing ln-111-DTPA-folate into a clinical radiopharmaceutical product to be used in the scintigraphic diagnostic imaging of tumors. This product may significantly impact the clinical management of certain cancer patients by providing a rapid and highly sensitive method of tumor detection.

Thesaurus Terms:
diethylenetriaminepentaacetate, drug design /synthesis /production, folate, indium, radionuclide scanning /imaging, radiopharmacology, vitamin receptor biomarker, neoplasm /cancer radiodiagnosis, radiochemistry, toxicology dog, laboratory ratNational Cancer Institute (NCI)

The objective of this proposal is to develop a novel folate receptor- based radiopharmaceutical. 111In-DTPA-folate, into a clinical product for the diagnostic imaging of human tumors. The folate receptor has been exploited as a tumor marker because of its significant overexpression in roughly one third of human cancers including over 90% of ovarian and endometrial carcinomas. In the Phase I project period, efforts will be focused on the following Specific Aims: 1) to optimize the method of radiopharmaceutical synthesis, formulation. and determination of product stability; 2) to conduct toxicity studies in two mammalian species to determine product safety; and 3) to prepare an IND application for submission to the FDA to obtain approval to initiate a Phase I/II clinical trial. Aim 1 will be accomplished by contract research in the laboratories of Drs. Mark Green in the Department of Medicinal Chemistry and Philip Low in the Department of Chemistry at Purdue University. Aim 2 will be performed in a contract toxicology laboratory in compliance with GLP standards. Aim 3 will be accomplished at Endocyte. Inc. 111In- DTPA-folate may be developed into a highly sensitive tissue-specific imaging agent that leads to significant improvements in the diagnosis and treatment of many primary and metastatic tumors.Proposed commercial application:The proposed project is aimed at developing ln-111-DTPA-folate into a clinical radiopharmaceutical product to be used in the scintigraphic diagnostic imaging of tumors. This product may significantly impact the clinical management of certain cancer patients by providing a rapid and highly sensitive method of tumor detection.Thesaurus termsdiethylenetriaminepentaacetate, drug design /synthesis /production, drug screening /evaluation, folate, indium, lung neoplasm, ovary neoplasm, radionuclide scanning /imaging, radiopharmacology, vitamin receptor biomarker, clinical trial phase I, diagnosis design /evaluation, drug quality /standard, human therapy evaluation, neoplasm /cancer radiodiagnosis, radiochemistry, toxicology clinical research, dog, human subject, laboratory ratNational Cancer Institute (NCI)