A Phase I, Open Label Study of the Safety, Tolerance and Assessment of HE3286 on Insulin Sensitivity and Hepatic Glucose Production When Administered Orally to Obese Insulin-Resistant Adult Subjects for 28 Days

The objectives of this study are to evaluate the safety and tolerance of 20 mg (10 mg BID) of HE3286 when administered orally over 28 days to obese insulin-resistant adult subjects and, to assess the activity of HE3286 on insulin sensitivity and hepatic glucose production in obese insulin-resistant adult subjects.

Start Date01 Sep 2009

Sponsor / Collaborator

Harbor Therapeutics, Inc.

NCT00716794 / CompletedPhase 1/2

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.

NCT00712114 / CompletedPhase 1/2

A Phase I/II, Open Label, Dose Ranging Study of the Safety, Tolerance, Pharmacokinetics and Potential Anti-Inflammatory Activity of HE3286 When Administered Orally for 29 Days to Patients With Rheumatoid Arthritis on a Stable Dose of Methotrexate

The purpose of this pilot, exploratory study is to evaluate the safety, tolerance, pharmacokinetics and potential anti-inflammatory activity of an investigational agent, HE3286, when administered orally for 29 days to patients with rheumatoid arthritis that are taking a stable dose of methotrexate.

Start Date01 Jul 2008

Sponsor / Collaborator

Harbor Therapeutics, Inc.

100 Clinical Results associated with Harbor Therapeutics, Inc.

0 Patents (Medical) associated with Harbor Therapeutics, Inc.

Literatures (Medical) associated with Harbor Therapeutics, Inc.

11 Sep 2014·Investigative Opthalmology & Visual ScienceQ2 · MEDICINE

HE3286 Reduces Axonal Loss and Preserves Retinal Ganglion Cell Function in Experimental Optic Neuritis

Q2 · MEDICINE

ArticleOA

Author: Dine, Kimberly ; Shindler, Kenneth S. ; Luna, Esteban ; Khan, Reas S. ; Ahlem, Clarence

PURPOSEOptic nerve inflammation, demyelination, and axonal loss are all prominent features of optic neuritis. While corticosteroids hasten visual recovery in optic neuritis, no treatment improves final visual outcomes. HE3286 (17α-ethynyl-5-androstene-3β,7β,17β-triol), a synthetic derivative of a natural steroid, β-AET (5-androstene-3β,7β,17β-triol), exerts anti-inflammatory effects in several disease models and has purported neuroprotective effects as well. HE3286's ability to suppress optic neuritis was examined in experimental autoimmune encephalomyelitis (EAE), a model of multiple sclerosis.METHODSExperimental autoimmune encephalomyelitis was induced in C57/BL6 mice. Mice were treated daily with intraperitoneal vehicle or 40 mg/kg HE3286. Visual function was assessed by optokinetic responses (OKR) at baseline and every 10 days until euthanasia at 40 days post immunization. Retinas and optic nerves were isolated. Inflammation (hematoxylin and eosin and Iba1 staining), demyelination (Luxol fast blue staining), and axonal loss (neurofilament staining) were assessed in optic nerve sections. Retinal ganglion cells (RGCs) were immunolabeled with Brn3a antibodies to quantify RGC survival.RESULTSProgressive decreases in OKR occurred in vehicle-treated EAE mice, and HE3286 treatment reduced the level of this vision loss. HE3286 also attenuated the degree of inflammation, demyelination, and axonal loss in EAE optic nerves as compared to nerves from vehicle-treated EAE mice. Retinal ganglion cell loss that occurred in both vehicle- and HE3286-treated EAE mice was reduced in the temporal retinal quadrant of HE3286-treated mice.CONCLUSIONSHE3286 suppresses inflammation, reduces demyelination and axonal loss, and promotes RGC survival during experimental optic neuritis. Importantly, HE3286 treatment also preserves some RGC function. Results suggest that HE3286 is a potential novel treatment for optic neuritis.

01 Jan 2013·Mediators of InflammationQ3 · MEDICINE

An Anti-Inflammatory Sterol Decreases Obesity-Related Inflammation-Induced Insulin Resistance and Metabolic Dysregulation

Q3 · MEDICINE

ArticleOA

Author: Reading, Chris L. ; Stickney, Dwight R. ; Frincke, James M. ; Flores-Riveros, Jaime

Obesity-related inflammation-induced insulin resistance and metabolic dysregulation were investigated in retrospective analysis of placebo hematologic and metabolic laboratory data from trials associated with increasing chronic low-grade inflammation and body mass index. Studies included healthy subjects and those with progressive stages of metabolic dysregulation, including type 2 diabetes mellitus with uncontrolled hemoglobin A1c. Intrasubject variances in erythroid and metabolic values increased with metabolic dysregulation. Random effects were demonstrated in treatment-naïve diabetes for erythroid, glucose, and HbA1c fluctuations. The anti-inflammatory insulin sensitizer, HE3286, was tested for its ability to decrease obesity-related inflammation-induced insulin resistance and metabolic dysregulation in diabetes. HE3286 significantly decreased erythroid and metabolic variances and improved 1,5-anhydroglucitol (a surrogate of postprandial glucose) compared to the placebo group. HE3286 HbA1c decrease correlated with weight loss and inversely with baseline monocyte chemoattractant protein-1 (MCP-1) in metformin-treated diabetics. Normalization of HbA1c to the 84-day average hemoglobin revealed that HE3286 HbA1c decrease correlated with high baseline MCP-1 and MCP-1 decrease in treatment-naïve diabetics. HE3286 decreased insulin resistance, increased the frequency of decreased day 84 HbA1c in metformin-treated subjects, and decreased day 112 HbA1c in treatment-naïve diabetics. HE3286 may be useful to restore metabolic homeostasis in type 2 diabetes.

01 Jan 2012·Parkinson's DiseaseQ4 · MEDICINE

17α-Ethynyl-androst-5-ene-3β,7β,17β-triol (HE3286) Is Neuroprotective and Reduces Motor Impairment and Neuroinflammation in a Murine MPTP Model of Parkinson’s Disease

Q4 · MEDICINE

ArticleOA

Author: Ahlem, Clarence N. ; Reading, Christopher L. ; Frincke, James M. ; Nicoletti, Ferdinando ; Philippens, Ingrid ; Fagone, Paolo ; Auci, Dominick L.

17α-Ethynyl-androst-5-ene-3β,7β,17β-triol (HE3286) is a synthetic androstenetriol in Phase II clinical development for the treatment of inflammatory diseases. HE3286 was evaluated for blood-brain barrier (BBB) permeability in mice, and efficacy in a 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) murine model of Parkinson’s disease (PD). We found that HE3286 freely penetrated the BBB. HE3286 treatment significantly improved motor function compared to vehicle in the rotarod test (mean 58.2 sec versus 90.9 sec,P<0.0001), and reduced inflammatory mediator gene expression in the brain (inducible nitric oxide synthase, 20%,P=0.002; tumor necrosis factorα, 40%,P=0.038, and interleukin-1β, 33%,P=0.02) measured by reverse-transcriptase polymerase chain reaction. Brain tissue histopathology and immunohistochemistry showed that HE3286 treatment increased the numbers of tyrosine hydroxylase-positive cells by 17% compared to vehicle (P=0.003), and decreased the numbers of damaged neurons by 38% relative to vehicle (P=0.029). L-3,4-dihydroxyphenylalanine (L-DOPA) efficacy was not enhanced by concurrent administration of HE3286. HE3286 administration prior to MPTP did not enhance efficacy. Our data suggest a potential role for HE3286 in PD treatment, and provides incentive for further investigation.

100 Deals associated with Harbor Therapeutics, Inc.

100 Translational Medicine associated with Harbor Therapeutics, Inc.

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Drug(Targets)	Indications	Global Highest Phase

Triolex ( ERK x NKRF )	Epilepsy More	Discontinued
HE-3235 ( AR )	Breast Cancer More	Discontinued
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