A Phase I/II, Open-Label, Dose Ranging Study of the Safety, Tolerance, Pharmacokinetics and Potential Activity of HE3235 When Administered Orally to Patients With Prostate Cancer

This is a phase I/II, open-label, dose escalation study of HE3235 administered orally to patients with advanced prostate cancer who have failed hormone therapy and at least one taxane based chemotherapy regimen.

Start Date01 Jul 2008

Sponsor / Collaborator

Harbor Therapeutics, Inc.

100 Clinical Results associated with HE-3235

100 Translational Medicine associated with HE-3235

100 Patents (Medical) associated with HE-3235

Literatures (Medical) associated with HE-3235

01 Feb 2012·Investigational New DrugsQ3 · MEDICINE

17α-Alkynyl 3α, 17β-androstanediol non-clinical and clinical pharmacology, pharmacokinetics and metabolism

Q3 · MEDICINE

Article

Author: Theodore Page ; David Bell ; Michael Kennedy ; Clarence Ahlem ; Evelyn Delorme ; Steven White ; Dwight Stickney ; Chris Reading ; James Frincke ; Sonia Villegas

17α-ethynyl-5α-androstane-3α, 17β-diol (HE3235, Apoptone) is an orally bioavailable synthetic analogue of 3β-androstanediol, that is active in rodent models of prostate and breast cancer, and is in Phase IIa clinical trials for the treatment of early- and late-stage prostate cancer. In preparation for clinical studies, nuclear hormone receptor and P450 interactions for HE3235 and major metabolites were characterized in vitro, and pharmacokinetics and metabolite profiles were studied in rodents, dogs, and monkeys. Four-week safety studies conducted in rats and dogs indicated a substantial margin of safety for clinical use, and no evidence of electrocardiographic or neurological effects, although anorexia, thrombocytopenia, and hypokalemia were identified as potentially dose-limiting toxicities at superpharmacological exposures. Pharmacokinetics and drug metabolism have been studied in prostate cancer patients.

01 Jan 2012·Case Reports in Oncology

Sequencing of Cabazitaxel in Metastatic Castrate-Resistant Prostate Cancer: A Case Report

Author: Colbourn, Donald

Prostate cancer is a common cancer in men; for metastatic disease, it has a 5-year survival rate of 30%. No FDA-approved therapy for castrate-resistant prostate cancer (CRPC) known to improve survival was available until 2004, when based on a significant survival benefit over mitoxantrone, docetaxel in combination with prednisone was approved. In combination with prednisone, cabazitaxel, which was approved in the United States in 2010, is indicated for patients with metastatic CRPC previously treated with a docetaxel-containing regimen. This case report describes the treatment of a man 58 years of age who was diagnosed with advanced prostate cancer in 2006. He was initially managed with radical prostatectomy followed by androgen deprivation therapy, but a rising prostate-specific antigen (PSA) level led to enrollment in a clinical trial of HE3235 for 6 months. Subsequently, with progression of disease, he was treated with docetaxel for 4 months and then palliative radiation therapy. Cabazitaxel was initiated in October 2010; his condition stabilized within weeks, and he experienced a progressive decline in his PSA level from a peak of 5,424 ng/ml. Continued treatment with cabazitaxel resulted in his being weaned off pain medications and resuming his normal activities. After 16 cycles of cabazitaxel, his PSA declined to 994 ng/ml as of January 2012. He tolerated the cabazitaxel well and occasionally received myeloid growth factors for treatment of neutropenia; otherwise, he experienced only mild diarrhea. This response to cabazitaxel is notable, particularly in light of prior failure of multiple therapies.

01 Jan 2011·International Journal of Breast Cancer

17α-Ethynyl-5α-androstane-3α, 17β-diol Treatment of MNU-Induced Mammary Cancer in Rats

Article

Author: Ahlem, Clarence N. ; Lakshmanaswamy, Rajkumar ; White, Steven K. ; Frincke, James M. ; Reading, Christopher L. ; Trauger, Richard J.

N-methyl-N-nitrosourea (MNU) induces estrogen-dependent mammary tumors in female Lewis rats. We explored the antineoplastic activity of a synthetic androstane derivative, 17α-ethynyl-5α-androstane-3α, 17β-diol (HE3235), as a single agent or in combination with docetaxel compared to tamoxifen, anastrazole, and docetaxel monotherapies against MNU-induced mammary tumors in female Lewis rats. Treatment with HE3235 alone rapidly reduced tumor burden, similar in effect to tamoxifen and anastrozole. The combination of HE3235 with docetaxel was more effective than any single agent, although without apparent toxicity. Only HE3235 or HE3235 plus docetaxel continued to suppress tumor growth after cessation of treatment. HE3235 treatment increased immunohistochemical markers of apoptosis and expression of proapoptotic genes and estrogen receptor beta and decreased expression of antiapoptotic genes, androgen receptor, and estrogen receptor alpha. These data warrant clinical investigation of HE3235 for breast cancer treatment.

100 Deals associated with HE-3235

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Indication	Highest Phase	Country/Location	Organization	Date
Breast Cancer	Phase 2	US	Harbor Therapeutics, Inc.	-
Prostatic Cancer	Phase 2	-	Harbor	-
Prostatic Cancer	Phase 2	-	Harbor	-
Prostatic Cancer	Phase 2	-	China State Institute of Pharmaceutical Industry	-
Prostatic Cancer	Phase 2	-	China State Institute of Pharmaceutical Industry	-

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ASCO2010	Phase 1/2	Castration-Resistant Prostatic Cancer	32	HE3235	(cdvacbyuhe) = lpyzfhuqpt nbxtlvbbvm (mxnwsdvonv ) View more	-	20 May 2010

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