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

    Apristor (onapristone XR)

    i
    Other names: ZK 98299, ZK 299, IVV-1001, AR-18, ZK-98299, ONA-XR
    Company:
    Context Therap, Tyligand
    Drug class:
    Progesterone receptor antagonist
    Related drugs:
    7ms
    ELONA: Study of Elacestrant in Combination With Onapristone in Patients With Advanced or Metastatic Breast Cancer (clinicaltrials.gov)
    P1/2, N=4, Terminated, Context Therapeutics Inc. | Phase classification: P1b --> P1/2 | N=67 --> 4 | Active, not recruiting --> Terminated; Sponsor decision to discontinue onapristone development.
    Phase classification • Enrollment change • Trial termination
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    Orserdu (elacestrant) • Apristor (onapristone XR)
    10ms
    Basket study of oral progesterone antagonist onapristone extended-release in combination with anastrozole in progesterone receptor-positive recurrent adult-type granulosa cell tumor of the ovary. (PubMed, Int J Gynecol Cancer)
    The study did not meet its primary end point. Although the combination of onapristone extended-release and anastrozole was well-tolerated, there were no objective responses in patients with progesterone receptor-positive adult-type granulosa cell tumor.
    Journal
    |
    PGR (Progesterone receptor)
    |
    PGR positive
    |
    anastrozole • Apristor (onapristone XR)
    11ms
    A Phase II Trial of Onapristone and Fulvestrant for Patients With ER+ and HER2- Metastatic Breast Cancer. (PubMed, Clin Breast Cancer)
    The study regimen was well-tolerated with no significant toxicities. Future studies may evaluate antiprogestins with various combinations such as targeted therapies.
    P2 data • Journal
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 negative
    |
    fulvestrant • Apristor (onapristone XR)
    11ms
    OATH: Onapristone and Anastrozole for the Treatment of Refractory Hormone Receptor Positive Endometrial Cancer (clinicaltrials.gov)
    P2, N=14, Active, not recruiting, Thomas Jefferson University | Trial completion date: Dec 2024 --> Dec 2025 | Trial primary completion date: Dec 2024 --> Dec 2025
    Trial completion date • Trial primary completion date
    |
    ER (Estrogen receptor) • PGR (Progesterone receptor)
    |
    anastrozole • Apristor (onapristone XR)
    1year
    A Study of Onapristone ER Alone Or In Combination With Anastrozole in Gynecologic Cancers That Respond to Progesterone (clinicaltrials.gov)
    P2, N=34, Completed, Memorial Sloan Kettering Cancer Center | Active, not recruiting --> Completed | Trial completion date: Apr 2025 --> Sep 2024 | Trial primary completion date: Apr 2025 --> Sep 2024
    Trial completion • Trial completion date • Trial primary completion date • Combination therapy • Pan tumor
    |
    PGR expression
    |
    anastrozole • Apristor (onapristone XR)
    over1year
    Basket study of oral progesterone antagonist onapristone extended release in progesterone receptor-positive recurrent granulosa cell, low-grade serous ovarian cancer, or endometrioid endometrial cancer. (PubMed, Gynecol Oncol)
    The study did not meet its primary endpoint. While onapristone-XR was well tolerated in all 3 arms, no objective responses were observed.
    Journal • Pan tumor
    |
    PGR (Progesterone receptor)
    |
    Apristor (onapristone XR)
    over1year
    A Study of Onapristone ER Alone Or In Combination With Anastrozole in Gynecologic Cancers That Respond to Progesterone (clinicaltrials.gov)
    P2, N=34, Active, not recruiting, Memorial Sloan Kettering Cancer Center | Trial completion date: Apr 2024 --> Apr 2025 | Trial primary completion date: Apr 2024 --> Apr 2025
    Trial completion date • Trial primary completion date • Combination therapy • Pan tumor
    |
    PGR expression
    |
    anastrozole • Apristor (onapristone XR)
    2years
    Onapristone and Fulvestrant for ER+ HER2- Metastatic Breast Cancer After Endocrine Therapy and CDK4/6 Inhibitors (The SMILE Study) (clinicaltrials.gov)
    P2, N=11, Terminated, University of Wisconsin, Madison | Trial completion date: Mar 2025 --> May 2023 | Active, not recruiting --> Terminated | Trial primary completion date: Mar 2024 --> Apr 2023; funding
    Trial completion date • Trial termination • Trial primary completion date • Combination therapy • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
    |
    ER positive • HER-2 negative • PGR positive
    |
    fulvestrant • Apristor (onapristone XR)
    over2years
    OATH: Onapristone and Anastrozole for the Treatment of Refractory Hormone Receptor Positive Endometrial Cancer (clinicaltrials.gov)
    P2, N=14, Active, not recruiting, Thomas Jefferson University | N=25 --> 14
    Enrollment change
    |
    PGR expression
    |
    anastrozole • Apristor (onapristone XR)
    over2years
    Onapristone and Fulvestrant for ER+ HER2- Metastatic Breast Cancer After Endocrine Therapy and CDK4/6 Inhibitors (The SMILE Study) (clinicaltrials.gov)
    P2, N=11, Active, not recruiting, University of Wisconsin, Madison | Recruiting --> Active, not recruiting | N=39 --> 11
    Enrollment closed • Enrollment change • Combination therapy • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
    |
    ER positive • HER-2 negative • PGR positive
    |
    fulvestrant • Apristor (onapristone XR)
    over2years
    Z-Endoxifen prevents aggressive mammary cancers in mice by inhibiting cell proliferation and creating a tumor suppressive microenvironment. (PubMed, Biomed Pharmacother)
    We examined the efficacy of the selective ER modulator (Z-endoxifen) as monotherapy and in combination with the selective progesterone receptor modulators (onapristone and ulipristal acetate) in the tamoxifen-insensitive C3(1)/SV40TAg mouse mammary tumorigenesis model. The expression of genes associated with cell cycle, cell proliferation and extracellular matrix remodeling was similarly repressed by endoxifen and UPA however only endoxifen significantly downregulated prominent genes associated with poor prognosis (Col11a1, Il17b, Pdgfa, Tnfrsf11a). Our results indicate that endoxifen can prevent breast cancers, even when tamoxifen-resistant, through its role in favorable tissue remodeling and immunomodulation.
    Preclinical • Journal
    |
    ER (Estrogen receptor) • PGR (Progesterone receptor) • COL1A1 (Collagen Type I Alpha 1 Chain) • PDGFA (Platelet Derived Growth Factor Subunit A) • TNFRSF11A (TNF Receptor Superfamily Member 11a) • COL11A1 (Collagen Type XI Alpha 1 Chain)
    |
    ER positive
    |
    tamoxifen • Apristor (onapristone XR)
    over2years
    A Study of Letrozole, Palbociclib, and Onapristone ER in People With Metastatic Breast Cancer (clinicaltrials.gov)
    P1b; N=28 --> 0 | Trial completion date: Sep 2023 --> Apr 2023 | Recruiting --> Withdrawn | Trial primary completion date: Sep 2023 --> Apr 2023
    Trial completion date • Trial primary completion date • Enrollment change • Trial withdrawal • Circulating tumor DNA • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2) • PGR (Progesterone receptor)
    |
    HER-2 negative
    |
    MSK-IMPACT • MSK-ACCESS
    |
    Ibrance (palbociclib) • letrozole • Apristor (onapristone XR)