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DRUG CLASS:

Androgen receptor modulator

3ms
Dose-Finding Study Evaluating Effect on Body Composition of Enobosarm in Patients Taking a GLP-1 for Chronic Weight Mgmt (clinicaltrials.gov)
P2, N=168, Completed, Veru Inc. | Active, not recruiting --> Completed | Trial completion date: Apr 2025 --> Aug 2025 | Trial primary completion date: Dec 2024 --> Apr 2025
Trial completion • Trial completion date • Trial primary completion date
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Ostarine (enobosarm)
6ms
Protective Role of Harmol Against β-Cell Toxicity And Glucose Dysregulation In Type 2 Diabetes Mellitus. (PubMed, Eur J Pharmacol)
Harmol and ligandrol improved glucose tolerance in diabetic male rats induced by a high-fat diet and streptozotocin. Our results suggest that harmol could serve as a novel anti-diabetic agent for T2DM with a unique mechanism that targets AR for β-cell revival and enhances glucose tolerance.
Journal
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NEUROG3 (Neurogenin 3)
10ms
A Study of HLD-0915 in Patients with Metastatic Castration Resistant Prostate Cancer (mCRPC) (clinicaltrials.gov)
P1/2, N=33, Recruiting, Halda Therapeutics OpCo, Inc. | Not yet recruiting --> Recruiting
Enrollment open
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HLD-0915
10ms
New P1/2 trial
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HLD-0915
1year
Delayed Mandibular Hematoma Following Selective Androgen Receptor Modulator (SARM) Usage. (PubMed, J Craniofac Surg)
This case presents a delayed hematoma following treatment for maxillary hypoplasia. Our findings indicate that the patients' usage of SARMs is responsible for the postoperative complications.
Journal
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HER-2 (Human epidermal growth factor receptor 2)
1year
Polypharmacological profiling across protein target families and cellular pathways using the multiplexed cell-based assay platform safetyProfiler reveals efficacy, potency and side effects of drugs. (PubMed, Biomed Pharmacother)
For example, the neuroleptics clozapine, paliperidone, and risperidone potently inhibited primary targets DRD2 and HTR2A as well as cAMP and calcium pathways...Additionally, precise potency data for LY2452473, an androgen receptor antagonist, that completed a phase 2 clinical trial for prostate cancer, are presented. The non-selective kinase inhibitor staurosporine was observed to potently inactivate the two RTKs EGFR and ERBB4 as well as MAPK signaling, while eliciting stress-related cAMP responses. Our findings underscore the value of comprehensive profiling in elucidating the pharmacological properties of established and novel therapeutics, thereby facilitating the development of novel multi-target drugs with enhanced efficacy and selectivity.
Journal • Adverse events
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EGFR (Epidermal growth factor receptor) • ERBB4 (erb-b2 receptor tyrosine kinase 4) • DRD2 (Dopamine Receptor D2) • HTR2A (5-Hydroxytryptamine Receptor 2A)
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OPK 88004
1year
MED12 and CDK8/19 modulate androgen receptor activity and enzalutamide response in prostate cancer. (PubMed, Endocrinology)
CDK8/19 inhibition significantly decreased PSA secretion in LNCaP and 22Rv1 cells and, when combined with enzalutamide, additively reduced proliferation in 22Rv1 cells. Our study revealed that MED12 and CDK8/19 regulate AR activity and that their inhibition may modulate response to enzalutamide in prostate cancer.
Journal
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MYC (V-myc avian myelocytomatosis viral oncogene homolog) • CDK9 (Cyclin Dependent Kinase 9) • MED12 (Mediator Complex Subunit 12)
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MYC expression • AR expression • AR splice variant 7 • AR-V7 expression • AR splice variant 7 expression
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Xtandi (enzalutamide)
1year
Androgen receptor modulatory miR-1271-5p can promote hormone sensitive prostate cancer cell growth. (PubMed, Front Oncol)
Inhibition or overexpression of miR-1271-5p levels affects prostate cancer cell growth, apoptosis and expression of both androgen receptor target genes and other genes that are likely direct targets, dependent on androgen receptor status, and tumour stage. We conclude that miR-1271-5p has the potential to drive progression of hormone-dependent disease and that the use of specific inhibitors of miR-1271-5p may have therapeutic potential in prostate cancer.
Journal
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MIR127 (MicroRNA 127) • MIR1271 (MicroRNA 1271)
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AR expression
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Xtandi (enzalutamide)
1year
Identification of biomarkers of response and the mechanism of action of a selective androgen receptor modulator in estrogen receptor-positive breast cancer patient-derived xenografts (EORTC-NCI-AACR 2024)
Adding the CDK4/6 inhibitor palbociclib enhanced the antitumor activity of EP0062 or fulvestrant in ESR1-mutant models but not in HER2-enriched or PTEN-mutant PDX models...EP0062 triggers an E2F1 downmodulation which mediates a potent antiproliferative activity. For EP0062-resistant tumors that remain ER-driven, the addition of palbociclib displays a potent antitumor effect.
Clinical
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HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PTEN (Phosphatase and tensin homolog) • AR (Androgen receptor) • FOXA1 (Forkhead Box A1) • HDAC2 (Histone deacetylase 2) • GATA3 (GATA binding protein 3) • E2F1 (E2F transcription factor 1)
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ER positive • PIK3CA mutation • PTEN mutation • ESR1 mutation • AR expression • ER expression • GATA3 mutation
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MSK-IMPACT
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Ibrance (palbociclib) • fulvestrant • vosilasarm (EP0062) • Undisclosed CDK4/6 inhibitor
over1year
Enrollment closed
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Ostarine (enobosarm)
over1year
Enrollment change
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Ostarine (enobosarm)
over1year
Enrollment open
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Ostarine (enobosarm)