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〕 It has been developed as a potential treatment for a number of human cancers. The LHRH receptor is aberrantly present on the cell surface of approximately 80% of endometrial and ovarian cancers, 86% of prostate cancers and about 50% of breast cancers. Whereas in normal tissues, expression of this receptor is mainly confined to the pituitary gland, reproductive organs and hematopoietic stem cells. To a lesser extent the LHRH receptor is also found on the surface of bladder, colorectal, and pancreatic cancers, sarcomas, lymphomas, melanomas, and renal cell carcinomas.〔Cite journal | pmid = 22577891 | year = 2012 | author1 = Engel | first1 = J | title = AEZS-108 : A targeted cytotoxic analog of LHRH for the treatment of cancers positive for LHRH receptors | journal = Expert Opinion on Investigational Drugs | volume = 21 | issue = 6 | pages = 891-9 | last2 = Emons | first2 = G | last3 = Pinski | first3 = J | last4 = Schally | first4 = A. V. | doi = 10.1517/13543784.2012.685128 }}〕 The proposed method of action is that upon administration zoptarelin doxorubicin binds to the LHRH receptor and is subsequently internalized, concentrating the toxic doxorubicin within cancer cells and the small subset of normal tissues, as opposed to the completely systemic distribution observed with untargeted chemotherapeutics. The specific targeting of the doxorubicin to LHRH receptor bearing cells is also proposed to reduce the cardiotoxicity observed in the administration of unconjugated doxorubicin. Zoptarelin doxorubicin is also known as AEZS-108 (previously AN-152). Zoptarelin doxorubicin was developed by Andrew V. Schally while at the Tulane University School of Medicine, New Orleans and subsequently at the Sylvester Comprehensive Cancer Center, University of Miami. The U.S. ] (FDA) has granted it orphan drug status for ovarian cancer and endometrial cancer. ==Clinical trials== Promising results have been reported from a phase II clinical trial for ovarian cancer and endometrial cancer. Phase II trials have also been undertaken for prostate, breast and bladder cancer, although no results for these trials have been reported in peer-reviewed literature. A phase I trial in prostate cancer indicated that nine out ten evaluable patients achieved disease stabilization through administration of zoptarelin doxorubicin. A phase III trial for r = 2014 | author1 = Emons | first1 = G | title = Efficacy and safety of AEZS-108 (LHRH agonist linked to doxorubicin) in women with advanced or recurrent endometrial cancer expressing LHRH receptors: A multicenter phase 2 trial (AGO-GYN5) | journal = International Journal of Gynecological Cancer | volume = 24 | issue = 2 | pages = 260-5 | last2 = Gorchev | first2 = G | last3 = Harter | first3 = P | last4 = Wimberger | first4 = P | last5 = Stähle | first5 = A | last6 = Hanker | first6 = L | last7 = Hilpert | first7 = F | last8 = Beckmann | first8 = M. W. | last9 = Dall | first9 = P | last10 = Gründker | first10 = C | last11 = Sindermann | first11 = H | last12 = Sehouli | first12 = J | doi = 10.1097/IGC.0000000000000044 }}〕 Phase II trials have also been undertaken for prostate, breast and bladder cancer, although no results for these trials have been reported in peer-reviewed literature. A phase I trial in prostate cancer indicated that nine out ten evaluable patients achieved disease stabilization through administration of zoptarelin doxorubicin. A phase III trial for endometrial cancer was initiated in April 2013 and it the primary completion date is estimated to be December 2016.〔Clinicaltrials.gov identifier NCT01767155〕 抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』 ■ウィキペディアで「Zoptarelin doxorubicin」の詳細全文を読む スポンサード リンク
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