Title:
TRICARBONYL TECHNETIUM-99M OR RHENIUM-188 LABEL RING RGD DERIVATIVE, A PREPARATION METHOD THEREOF, AND A PHARMACEUTICAL COMPOSITION CONTAINING THE DERIVATIVE AS AN ACTIVE INGREDIENT FOR USE IN THE DIAGNOSIS OR TREATMENT OF ANGIOGENESIS-RELATED DISEASES
Document Type and Number:
WIPO Patent Application WO/2011/149250
Kind Code:
A3
Abstract:
The present invention relates to a tricarbonyl technetium-99m or rhenium-188 label ring RGD derivative, a preparation method thereof, and a pharmaceutical composition containing the derivative as an active ingredient for use in the diagnosis or treatment of angiogenesis-related diseases. The tricarbonyl technetium-99m or rhenium-188 label ring RGD derivative of the present invention has a high subnanomolar affinity to αvβ3 integrin (also called as a vitronectin receptor that is activated in an angiogenic action induced by a tumor, reflects a high tumor image after an animal in which cancer cells are transplanted received an initial intake of the tricarbonyl technetium-99m label ring RGD derivative, and acts exclusively upon cancer cells having selectively activated αvβ3 integrin because of a substantially low intake into the liver and intestines, compared to existing known radioactive isotope label ring RGD derivatives. These results show that the rhenium-188 label derivative, a therapeutic nuclide using the same precursor as used in the technetium-99m label, effectively inhibits the growth of a tumor and demonstrates therapeutic efficacy when administered via tail vein injection to an animal model of a tumor, compared to a case where only saline has been injected, thereby making it useful as a medicine for the diagnosis or treatment of angiogenesis-related diseases.
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Inventors:
LEE BYUNG CHUL (KR)
KIM SANG EUN (KR)
KIM JI SUN (KR)
MOON BYUNG SEOK (KR)
JUNG JAE HO (KR)
KIM SANG EUN (KR)
KIM JI SUN (KR)
MOON BYUNG SEOK (KR)
JUNG JAE HO (KR)
Application Number:
PCT/KR2011/003801
Publication Date:
March 22, 2012
Filing Date:
May 24, 2011
Export Citation:
Assignee:
SNU R&DB FOUNDATION (KR)
LEE BYUNG CHUL (KR)
KIM SANG EUN (KR)
KIM JI SUN (KR)
MOON BYUNG SEOK (KR)
JUNG JAE HO (KR)
LEE BYUNG CHUL (KR)
KIM SANG EUN (KR)
KIM JI SUN (KR)
MOON BYUNG SEOK (KR)
JUNG JAE HO (KR)
International Classes:
C07D273/06; A61K31/5395; A61K51/04; A61P35/00; C07D498/06; C07D498/16; G01N33/60
Foreign References:
| US20080219921A1 | 2008-09-11 |
Other References:
LEE, BYEONG CHEOL ET AL.: "Synthesis of Tc-99m labeled glucosamino-Asp-cyclic (Arg- Gly-Asp-D-Phe-Lys) as a potential angiogenesis imaging agent", BIOORGANIC & MEDICINAL CHEMISTRY, vol. 15, no. 24, 2007, pages 7755 - 7764, XP022302070, DOI: doi:10.1016/j.bmc.2007.08.054
JUNG, GYEONG HO ET AL.: "Favorable Biokinetic and Tumor-Targeting Properties of 99mTc-Labeled Glucosamino RGD and Effect ofPaclitaxel Therapy", JOURNAL OF NUCLEAR MEDICINE, vol. 47, no. 12, 2006, pages 2000 - 2007
SUSANA ALVES ET AL.: "In Vitro and In Vivo Evaluation of a Novel 99mTc (CO)3- Pyrazolyl Conjugate of cyclo-(Arg-Gly-Asp-D-Tyr-Lys)", BIOCONJUGATE CHEMISTRY, vol. 18, no. 2, 2007, pages 530 - 537
JUNG, GYEONG HO ET AL.: "Favorable Biokinetic and Tumor-Targeting Properties of 99mTc-Labeled Glucosamino RGD and Effect ofPaclitaxel Therapy", JOURNAL OF NUCLEAR MEDICINE, vol. 47, no. 12, 2006, pages 2000 - 2007
SUSANA ALVES ET AL.: "In Vitro and In Vivo Evaluation of a Novel 99mTc (CO)3- Pyrazolyl Conjugate of cyclo-(Arg-Gly-Asp-D-Tyr-Lys)", BIOCONJUGATE CHEMISTRY, vol. 18, no. 2, 2007, pages 530 - 537
Attorney, Agent or Firm:
LEE, Won Hee (Sung-ji Heights II642-16 Yoksam-dong, Kangnam-ku, Seoul 135-080, KR)
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Claims: