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A phase I trial of AEZS-108 (AN-152) in castration- and taxane-resistant prostate cancer

Liu, Stephen V. and Schally, Andrew V. and Dorff, Tanya B. and Tsao-Wei, Denice D. and Groshen, Susan G. and Xiong, Shigang and Hawes, Debra and Quinn, David I. and Tai, Yu-Chong and Block, Norman L. and Engel, Juergen and Pinski, Jacek K. (2012) A phase I trial of AEZS-108 (AN-152) in castration- and taxane-resistant prostate cancer. Journal of Clinical Oncology, 30 (5). Art. No. 60. ISSN 1527-7755.

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Background: The prognosis for patients with castration-resistant prostate cancer (CRPC) remains suboptimal and targeted therapies should be explored. One potential target is the receptor for luteinizing hormone-releasing hormone (LHRH-R), which is highly expressed on prostate cancer cells. AEZS-108 (AN-152) is an LHRH-cytotoxic hybrid whose rational design covalently couples an LHRH agonist and the cytotoxic doxorubicin. AEZS-108 exploits the presence of these receptors to target delivery of the cytotoxic. We report the phase I trial of AEZS-108 in men with taxane-resistant CRPC. We also report correlative studies of a novel circulating tumor cell (CTC) capture device that will provide both enumeration of CTCs and LHRH-R expression on captured CTCs as well as results from AEZS-108 internalization studies that exploit the auto-fluorescence of doxorubicin in captured CTCs. Methods: This is a single-arm, dose-escalation phase I study in men with CRPC to confirm the dose established in a completed phase I trial in females. Eligibility criteria included adequate organ function and progression of disease despite prior therapy with an LHRH agonist and at least one taxane-based regimen. Patients were required to discontinue LHRH agonists to avoid receptor competition. Patients received AEZS-108 every 21 days until progression or unacceptable toxicity for up to 6 cycles. The primary endpoint was safety. Results: Enrollment began in November 2010 and completed in September 2011. Twelve patients were accrued onto 3 dose levels. No DLTs have been noted. At the time of submission, a decrease in PSA was noted in 5 of the 10 evaluable patients. The grade 3 or 4 toxicities were primarily hematologic. Final reports detailing toxicity, RECIST response and PSA response will be reported. All correlative studies will also be reported. Conclusions: AEZS-108 is well tolerated and has demonstrated early signs of antitumor activity in men with CRPC. We will report the recommended dose for the planned phase II study.

Item Type:Article
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Tai, Yu-Chong0000-0001-8529-106X
Additional Information:© 2012 American Society of Clinical Oncology.
Issue or Number:5
Record Number:CaltechAUTHORS:20170104-134516800
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Official Citation:10.1200/jco.2012.30.5_suppl.60 Journal of Clinical Oncology 30, no. 5_suppl (February 2012) 60-60
Usage Policy:No commercial reproduction, distribution, display or performance rights in this work are provided.
ID Code:73214
Deposited By: Tony Diaz
Deposited On:04 Jan 2017 22:01
Last Modified:03 Oct 2019 16:25

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