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    DRUG:

    Zonalta (Z-endoxifen hydrochloride)

    Company:
    Intas, Jina Pharma, National Cancer Institute
    Drug class:
    Estrogen receptor antagonist, Selective estrogen receptor modulator
    Related drugs:
    21d
    Z-Endoxifen Hydrochloride in Treating Patients With Metastatic or Locally Recurrent Estrogen Receptor-Positive Breast Cancer (clinicaltrials.gov)
    P1, N=62, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Oct 2025 --> Oct 2026
    Trial completion date
    |
    ER (Estrogen receptor)
    |
    ER positive
    |
    Zonalta (Z-endoxifen hydrochloride)
    9ms
    Efficacy and Safety of Endoxifen in Bipolar I Disorder Patients (clinicaltrials.gov)
    P3, N=490, Active, not recruiting, Jina Pharmaceuticals Inc. | Recruiting --> Active, not recruiting | Trial completion date: Sep 2025 --> Dec 2025
    Enrollment closed • Trial completion date
    |
    Zonalta (Z-endoxifen hydrochloride)
    9ms
    Tamoxifen Citrate or Z-Endoxifen Hydrochloride in Treating Patients With Locally Advanced or Metastatic, Estrogen Receptor-Positive, HER2-Negative Breast Cancer (clinicaltrials.gov)
    P2, N=81, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Feb 2025 --> Feb 2026
    Trial completion date
    |
    ER (Estrogen receptor) • NCOA3 (Nuclear Receptor Coactivator 3)
    |
    ER positive • HER-2 negative • ER positive + HER-2 negative • HER-2 negative + ER positive
    |
    Zonalta (Z-endoxifen hydrochloride) • Soltamox (tamoxifen citrate)
    1year
    Z-Endoxifen Hydrochloride in Treating Patients With Metastatic or Locally Recurrent Estrogen Receptor-Positive Breast Cancer (clinicaltrials.gov)
    P1, N=62, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Oct 2024 --> Oct 2025
    Trial completion date
    |
    EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor) • AKT1 (V-akt murine thymoma viral oncogene homolog 1) • mTOR (Mechanistic target of rapamycin kinase) • IGF1R (Insulin-like growth factor 1 receptor) • NCOA3 (Nuclear Receptor Coactivator 3) • PI3K (Phosphoinositide 3-kinases)
    |
    ER positive • HER-2 expression • EGFR expression
    |
    Zonalta (Z-endoxifen hydrochloride)
    1year
    Efficacy and Safety of Endoxifen in Bipolar I Disorder Patients (clinicaltrials.gov)
    P3, N=490, Recruiting, Jina Pharmaceuticals Inc.
    New P3 trial
    |
    Zonalta (Z-endoxifen hydrochloride)
    1year
    Evaluate Efficacy and Safety of Endoxifen in Bipolar I Disorder Patients (clinicaltrials.gov)
    P3, N=124, Completed, Jina Pharmaceuticals Inc. | Recruiting --> Completed
    Trial completion
    |
    Zonalta (Z-endoxifen hydrochloride)
    over1year
    Endoxifen in Adults With Hormone Receptor Positive Solid Tumors (clinicaltrials.gov)
    P1, N=40, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Jun 2024 --> Jun 2026
    Trial completion date
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    tamoxifen • Zonalta (Z-endoxifen hydrochloride)
    almost2years
    Tamoxifen Citrate or Z-Endoxifen Hydrochloride in Treating Patients With Locally Advanced or Metastatic, Estrogen Receptor-Positive, HER2-Negative Breast Cancer (clinicaltrials.gov)
    P2, N=81, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: May 2024 --> Feb 2025
    Trial completion date • Metastases
    |
    ER (Estrogen receptor) • NCOA3 (Nuclear Receptor Coactivator 3)
    |
    ER positive • HER-2 negative • ER positive + HER-2 negative
    |
    Zonalta (Z-endoxifen hydrochloride) • Soltamox (tamoxifen citrate)
    almost2years
    A randomized Phase I pre-operative window trial of transdermal endoxifen in women planning mastectomy: Evaluation of dermal safety, intra-mammary drug distribution, and biologic effects. (PubMed, Biomed Pharmacother)
    We formulated the tamoxifen metabolite (E/Z)-endoxifen for transdermal delivery and tested it in a placebo-controlled, double-blinded Phase I trial with dose escalation from 10 to 20 mg daily. At the endoxifen doses and duration used, and the tissue concentration achieved, we observed a non-significant overall reduction of tumor proliferation (Ki67 LI) and significant downregulation of gene signatures known to promote cancer invasion (FN1, SERPINH1, PLOD2, PDGFA, ITGAV) (p = 0.03). Transdermal endoxifen is an important potential breast cancer prevention agent but formulations with better dermal penetration are needed.
    P1 data • Journal
    |
    SERPINH1 (Serpin family H member 1) • PDGFA (Platelet Derived Growth Factor Subunit A) • PLOD2 (procollagen-lysine,2-oxoglutarate 5-dioxygenase 2)
    |
    tamoxifen • Zonalta (Z-endoxifen hydrochloride)
    2years
    Presurgical Oral Tamoxifen vs Transdermal 4-Hydroxytamoxifen in Women With Ductal Carcinoma In Situ: A Randomized Clinical Trial. (PubMed, JAMA Surg)
    P2b; The median 4-hydroxytamoxifen concentrations deep in the breast were nonsignificantly higher in the oral tamoxifen group (5.7 [IQR, 4.0-7.9] vs 3.8 [IQR, 1.3-7.9] ng/g), whereas endoxifen was abundant in the oral tamoxifen group and minimal in the 4-hydroxytamoxifen gel group (median, 13.0 [IQR, 8.9-20.6] vs 0.3 [IQR, 0-0.3] ng/g; P < .001). New transdermal approaches must deliver higher drug quantities and/or include the most potent metabolites. ClinicalTrials.gov Identifier: NCT02993159.
    Journal • Clinical
    |
    ER (Estrogen receptor)
    |
    ER positive
    |
    Oncotype DX Breast DCIS Score test
    |
    tamoxifen • Zonalta (Z-endoxifen hydrochloride)
    over2years
    Tamoxifen Citrate or Z-Endoxifen Hydrochloride in Treating Patients With Locally Advanced or Metastatic, Estrogen Receptor-Positive, HER2-Negative Breast Cancer (clinicaltrials.gov)
    P2, N=81, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: May 2023 --> May 2024
    Trial completion date • Metastases
    |
    ER (Estrogen receptor)
    |
    ER positive • HER-2 negative • ER positive + HER-2 negative
    |
    Zonalta (Z-endoxifen hydrochloride) • Soltamox (tamoxifen citrate)
    over2years
    Endoxifen in Adults With Hormone Receptor Positive Solid Tumors (clinicaltrials.gov)
    P1, N=40, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Jun 2023 --> Jun 2024
    Trial completion date
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    tamoxifen • Zonalta (Z-endoxifen hydrochloride)