^
    Contact us  to learn more about
    our Premium Content:  News alerts, weekly reports and conference planners
    DRUG CLASS:

    Selective androgen receptor modulator

    Related drugs:
    17d
    Dose-Finding Study Evaluating Effect on Body Composition of Enobosarm in Patients Taking a GLP-1 for Chronic Weight Mgmt (clinicaltrials.gov)
    P2, N=90, Recruiting, Veru Inc. | Not yet recruiting --> Recruiting
    Enrollment open
    |
    Ostarine (enobosarm)
    2ms
    Phase II Study of GTx024 in Women With Metastatic Breast Cancer (clinicaltrials.gov)
    P2, N=22, Terminated, GTx | Completed --> Terminated
    Trial termination • Metastases
    |
    ER (Estrogen receptor) • AR (Androgen receptor)
    |
    ER positive • AR positive
    |
    Ostarine (enobosarm)
    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=90, Not yet recruiting, Veru Inc.
    New P2 trial
    |
    Ostarine (enobosarm)
    3ms
    ENABLAR-2: Efficacy & Safety Evaluation of Enobosarm in Combo With Abemaciclib in Treatment of ER+HER2- Metastatic Breast Cancer (clinicaltrials.gov)
    P3, N=5, Terminated, Veru Inc. | N=186 --> 5
    Enrollment change
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • AR (Androgen receptor)
    |
    HER-2 negative
    |
    Ibrance (palbociclib) • everolimus • Verzenio (abemaciclib) • fulvestrant • exemestane • Ostarine (enobosarm)
    3ms
    Pembrolizumab and Enobosarm in Treating Patients With Androgen Receptor Positive Metastatic Triple Negative Breast Cancer (clinicaltrials.gov)
    P2, N=18, Completed, City of Hope Medical Center | Active, not recruiting --> Completed
    Trial completion • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor) • AR (Androgen receptor)
    |
    HER-2 negative • AR positive • ER expression • PGR expression
    |
    Keytruda (pembrolizumab) • Ostarine (enobosarm)
    3ms
    Activity and safety of enobosarm, a novel, oral, selective androgen receptor modulator, in androgen receptor-positive, oestrogen receptor-positive, and HER2-negative advanced breast cancer (Study G200802): a randomised, open-label, multicentre, multinational, parallel design, phase 2 trial. (PubMed, Lancet Oncol)
    Enobosarm has anti-tumour activity in patients with ER-positive, HER2-negative advanced breast cancer, showing that AR activation can result in clinical benefit, supporting further clinical investigation of selective AR activation strategies for the treatment of AR-positive, ER-positive, HER2-negative advanced breast cancer.
    P2 data • Journal • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
    |
    ER positive • HER-2 negative • AR positive • ER positive + HER-2 negative
    |
    Ostarine (enobosarm)
    10ms
    In vitro anti-carcinogenic effect of andarine as a selective androgen receptor modulator on MIA-PaCa-2 cells by decreased proliferation and cell-cycle arrest at G0/G1 phase. (PubMed, Biochem Biophys Res Commun)
    Furthermore, we established that the anti-carcinogenic activity of andarine is not mediated by the PI3K/AKT/mTOR signaling pathway, a crucial regulator of cell survival. Our findings suggest that andarine might be considered as a prospective drug for PC.
    Preclinical • Journal
    |
    CDKN1A (Cyclin-dependent kinase inhibitor 1A)
    11ms
    Phase 1/2 Study to Evaluate EP0062 in Patients With Relapsed Locally Advanced or Metastatic Androgen Receptor Positive (AR+)/HER2-/ER+ Breast Cancer (clinicaltrials.gov)
    P1/2, N=128, Recruiting, Ellipses Pharma | Not yet recruiting --> Recruiting
    Enrollment open • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 negative
    |
    vosilasarm (EP0062)
    1year
    Pembrolizumab and Enobosarm in Treating Patients With Androgen Receptor Positive Metastatic Triple Negative Breast Cancer (clinicaltrials.gov)
    P2, N=18, Active, not recruiting, City of Hope Medical Center | Trial completion date: Jan 2023 --> Dec 2023
    Trial completion date • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor) • AR (Androgen receptor)
    |
    HER-2 negative • AR positive • ER expression • PGR expression
    |
    Keytruda (pembrolizumab) • Ostarine (enobosarm)
    1year
    A Selective Androgen Receptor Modulator, S4, Displays Robust Anti-cancer Activity on Hepatocellular Cancer Cells by Negatively Regulating PI3K/AKT/mTOR Signaling Pathway. (PubMed, Gene)
    Since PI3K/AKT/mTOR signaling is frequently activated in HCC and contributes to its aggressiveness and poor prognosis, its negative regulation by the downregulation of critical components via S4 was a prominent finding. Further studies are necessary to investigate the S4 action mechanism and anti-tumorigenic capacity in in-vivo.
    Journal
    over1year
    Pharmacological targeting of androgen receptor elicits context-specific effects in estrogen receptor-positive breast cancer. (PubMed, Cancer Res)
    However, both a selective AR agonist (RAD140) and an AR inhibitor (enzalutamide, ENZ) have shown a therapeutic effect on ER+ breast cancer, so the potential for clinical application of AR-targeting therapy for ER+ breast cancer is still in dispute. In contrast, RAD140 activated AR signaling and suppressed AR-high tumor growth by deregulating ERα expression and blocking ERα function. Overall, analysis of the dynamic efficacies and outcomes of AR agonist and antagonist in the presence of different AR and ERα levels reveals regulators of response and supports the clinical investigation of ENZ in selected ER+ tumors with a low AR/ER ratio and AR agonists in tumors with a high AR/ER ratio.
    Journal
    |
    ER (Estrogen receptor)
    |
    ER positive • AR expression • AR underexpression
    |
    Xtandi (enzalutamide capsule) • vosilasarm (EP0062)
    over1year
    Phase 1/2 Study to Evaluate EP0062 in Patients With Relapsed Locally Advanced or Metastatic Androgen Receptor Positive (AR+)/HER2-/ER+ Breast Cancer (clinicaltrials.gov)
    P1/2, N=128, Not yet recruiting, Ellipses Pharma
    New P1/2 trial • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 negative
    |
    vosilasarm (EP0062)
    over1year
    A phase 1/2 study to evaluate the safety and efficacy of EP0062, an oral Selective Androgen Receptor Modulator (SARM), for the treatment of AR+/HER2-/ER+ advanced breast cancer (SABCS 2022)
    Clinic follow-up will be at 2 and 4 weeks, then every 4 weeks until disease progression. Recruitment is scheduled to initiate in Q4 2022.
    Clinical • P1/2 data
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
    |
    HER-2 negative • AR expression
    |
    vosilasarm (EP0062)