Literature DB >> 9179196

The development of estrogen and progestin radiopharmaceuticals for imaging breast cancer.

J A Katzenellenbogen1, M J Welch, F Dehdashti.   

Abstract

BACKGROUND: The presence of receptors for estrogens and progestins in many breast tumors provides a means for imaging these tumors using positron emission tomography (PET) with appropriate fluorine-18 labeled estrogen and progestin radiopharmaceuticals. In this context, the estrogen analog 16 alpha-[18F]fluoroestradiol (FES) has already proven to be an effective imaging agent for estrogen receptor-positive tumors.
METHODS: Clinical studies comparing FES images with those based on the metabolic probe 2-[18F]fluoro-2-deoxyglucose (FDG) in patients before and after tamoxifen hormone therapy are underway. Several fluorine-18 labeled progestins have been prepared, and efforts are underway to develop methods for labeling steroid receptor imaging agents with the widely available radionuclide technetium-99m, using both pendant and integrated approaches. RESULTS AND
CONCLUSION: Breast tumor imaging with FES and FDG shows an interesting relationship between tumor metabolic response (assessed with FDG) and tumor estrogen receptor levels (assessed with FES). The fluorine-18 labeled progestins show excellent target tissue selective distribution in experimental animals and are ready for imaging studies in humans. The development of steroids labeled with technetium-99m poses special challenges because of the metallic nature of this radioisotope.

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Year:  1997        PMID: 9179196

Source DB:  PubMed          Journal:  Anticancer Res        ISSN: 0250-7005            Impact factor:   2.480


  15 in total

1.  Small-animal PET of steroid hormone receptors predicts tumor response to endocrine therapy using a preclinical model of breast cancer.

Authors:  Amy M Fowler; Szeman Ruby Chan; Terry L Sharp; Nicole M Fettig; Dong Zhou; Carmen S Dence; Kathryn E Carlson; M Jeyakumar; John A Katzenellenbogen; Robert D Schreiber; Michael J Welch
Journal:  J Nucl Med       Date:  2012-06-05       Impact factor: 10.057

Review 2.  Characterizing tumors using metabolic imaging: PET imaging of cellular proliferation and steroid receptors.

Authors:  D A Mankoff; F Dehdashti; A F Shields
Journal:  Neoplasia       Date:  2000 Jan-Apr       Impact factor: 5.715

Review 3.  Current and future use of positron emission tomography (PET) in breast cancer.

Authors:  David A Mankoff; William B Eubank
Journal:  J Mammary Gland Biol Neoplasia       Date:  2006-04       Impact factor: 2.673

4.  Imaging readouts as biomarkers or surrogate parameters for the assessment of therapeutic interventions.

Authors:  Markus Rudin
Journal:  Eur Radiol       Date:  2007-03-06       Impact factor: 5.315

5.  Factors influencing the uptake of 18F-fluoroestradiol in patients with estrogen receptor positive breast cancer.

Authors:  Lanell M Peterson; Brenda F Kurland; Jeanne M Link; Erin K Schubert; Svetlana Stekhova; Hannah M Linden; David A Mankoff
Journal:  Nucl Med Biol       Date:  2011-05-05       Impact factor: 2.408

6.  GPER-targeted, 99mTc-labeled, nonsteroidal ligands demonstrate selective tumor imaging and in vivo estrogen binding.

Authors:  Tapan K Nayak; Chinnasamy Ramesh; Helen J Hathaway; Jeffrey P Norenberg; Jeffrey B Arterburn; Eric R Prossnitz
Journal:  Mol Cancer Res       Date:  2014-07-16       Impact factor: 5.852

7.  Breast imaging: A survey.

Authors:  Subbhuraam Vinitha Sree; Eddie Yin-Kwee Ng; Rajendra U Acharya; Oliver Faust
Journal:  World J Clin Oncol       Date:  2011-04-10

Review 8.  International Union of Basic and Clinical Pharmacology. XCVII. G Protein-Coupled Estrogen Receptor and Its Pharmacologic Modulators.

Authors:  Eric R Prossnitz; Jeffrey B Arterburn
Journal:  Pharmacol Rev       Date:  2015-07       Impact factor: 25.468

9.  Preclinical development of a neutral, estrogen receptor-targeted, tridentate 99mTc(I)-estradiol-pyridin-2-yl hydrazine derivative for imaging of breast and endometrial cancers.

Authors:  Tapan K Nayak; Helen J Hathaway; Chinnasamy Ramesh; Jeffrey B Arterburn; Donghai Dai; Larry A Sklar; Jeffrey P Norenberg; Eric R Prossnitz
Journal:  J Nucl Med       Date:  2008-05-15       Impact factor: 10.057

10.  Predicting Breast Cancer Endocrine Responsiveness Using Molecular Imaging.

Authors:  Erin Currin; Hannah M Linden; David A Mankoff
Journal:  Curr Breast Cancer Rep       Date:  2011-12
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