^
    3d
    Identification, synthesis, and characterization of a unique N-glucuronide of an acid metabolite of camizestrant (AZD9833) in humans. (PubMed, Drug Metab Dispos)
    SIGNIFICANCE STATEMENT: Metabolite M14 of camizestrant (AZD9833), a major circulating metabolite in humans, was successfully identified as an N-glucuronide of an acid metabolite of camizestrant, and its unusual chromatographic and stability properties were characterized. The development of a novel hybrid chemical and biological synthesis for M14 has introduced a new approach to synthesizing glucuronides of compounds with acidic functional groups that otherwise interfere with their own in vitro glucuronidation.
    Journal
    |
    ER (Estrogen receptor)
    |
    ER positive
    |
    camizestrant (AZD9833)
    10d
    MEDOPP0555: PHASE II STUDY TO EVALUATE THE EFFICACY AND SAFETY OF CAMIZESTRANT PLUS RIBOCICLIB IN PATIENTS WITH HORMONE RECEPTOR-POSITIVE (HR+) BREAST CANCER? (THE CADILLAC STUDY) (2024-520027-88-00)
    P1/2, N=131, Recruiting, Medica Scientia Innovation Research S.L., Medica Scientia Innovation Research S.L. | Not yet recruiting --> Recruiting
    Enrollment open
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
    |
    HER-2 negative
    |
    Kisqali (ribociclib) • camizestrant (AZD9833)
    29d
    CYCAD-1: A First-in-human Dose Escalation and Expansion Study to Evaluate the Safety, and Tolerability of AZD8421 Alone or in Combination in Participants With Selected Advanced or Metastatic Solid Tumors (clinicaltrials.gov)
    P1/2, N=564, Recruiting, AstraZeneca | Trial completion date: Aug 2026 --> Aug 2027 | Trial primary completion date: Aug 2026 --> Aug 2027
    Trial completion date • Trial primary completion date • First-in-human
    |
    Ibrance (palbociclib) • Verzenio (abemaciclib) • Kisqali (ribociclib) • camizestrant (AZD9833)
    29d
    SERENA-1b: Study to Evaluate the Safety and Tolerability of Camizestrant in Combination With Atirmociclib in Women With Advanced Breast Cancer (clinicaltrials.gov)
    P2, N=24, Not yet recruiting, AstraZeneca
    New P2 trial
    |
    ER (Estrogen receptor) • PGR (Progesterone receptor)
    |
    ER positive
    |
    camizestrant (AZD9833) • atirmociclib (PF-07220060)
    1m
    MEDOPP0555: PHASE II STUDY TO EVALUATE THE EFFICACY AND SAFETY OF CAMIZESTRANT PLUS RIBOCICLIB IN PATIENTS WITH HORMONE RECEPTOR-POSITIVE (HR+) BREAST CANCER? (THE CADILLAC STUDY) (2024-520027-88-00)
    P1/2, N=131, Not yet recruiting, Medica Scientia Innovation Research S.L., Medica Scientia Innovation Research S.L.
    New P1/2 trial
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
    |
    HER-2 negative
    |
    Kisqali (ribociclib) • camizestrant (AZD9833)
    2ms
    Pharmacodynamics of Camizestrant Treatment in Postmenopausal Women With Estrogen Receptor-Positive, Human Epidermal Growth Factor Receptor 2-Negative Primary Breast Cancer: Results From the Randomized, Presurgical SERENA-3 Study. (PubMed, J Clin Oncol)
    SERENA-3 demonstrates that camizestrant 75 mg once daily (Phase III dose) is well-tolerated and achieves maximal reduction in ER through known mechanisms, that is, antagonism and degradation, by 5-7 days, and proliferation suppression determined by Ki67 expression, by 12-15 days. These data support camizestrant 75 mg once daily as the preferred dose for ongoing clinical development and highlight the importance of presurgical WOO studies in guiding dose selection.
    PK/PD data • Journal
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
    |
    ER positive • HER-2 negative • EGFR positive
    |
    camizestrant (AZD9833)
    2ms
    SERENA-1: Study of AZD9833 Alone or in Combination in Women With Advanced Breast Cancer. (clinicaltrials.gov)
    P1, N=396, Active, not recruiting, AstraZeneca | Trial completion date: Dec 2026 --> Jun 2027
    Trial completion date • First-in-human
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
    |
    HER-2 negative
    |
    Ibrance (palbociclib) • everolimus • Verzenio (abemaciclib) • Kisqali (ribociclib) • Truqap (capivasertib) • anastrozole • camizestrant (AZD9833)
    2ms
    Camizestrant in combination with capivasertib for women with ER-positive, HER2-negative advanced breast cancer: results from SERENA-1. (PubMed, ESMO Open)
    In these pretreated participants, camizestrant 75 mg in combination with capivasertib 400 mg was well tolerated, with a side effect profile consistent with each drug as monotherapy, and showed encouraging evidence of clinical efficacy.
    Journal
    |
    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) • AKT1 (V-akt murine thymoma viral oncogene homolog 1)
    |
    ER positive • HER-2 negative • EGFR positive • HER-2 negative + ER positive
    |
    fulvestrant • Truqap (capivasertib) • camizestrant (AZD9833)
    2ms
    CYCAD-1: A First-in-human Dose Escalation and Expansion Study to Evaluate the Safety, and Tolerability of AZD8421 Alone or in Combination in Participants With Selected Advanced or Metastatic Solid Tumors (clinicaltrials.gov)
    P1/2, N=564, Recruiting, AstraZeneca | N=348 --> 564
    Enrollment change • First-in-human
    |
    Ibrance (palbociclib) • Verzenio (abemaciclib) • Kisqali (ribociclib) • camizestrant (AZD9833)
    2ms
    Selective Estrogen Receptor Degraders Induce Bradycardia by Modulating Nuclear Estrogen Signaling. (PubMed, JACC Basic Transl Sci)
    Giredestrant and camizestrant induced significant bradycardia in wild-type zebrafish embryos, whereas fulvestrant and amcenestrant (SERDs that do not induce bradycardia in patients) did not alter heart rate. Mutations in gper, esr2a, and esr2b did not confer resistance to SERD-induced bradycardia, whereas esr1 mutant embryos were protected. These findings demonstrate that SERD-associated bradycardia is mediated through Esr1 signaling, supporting an on-target adverse effect.
    Journal
    |
    ER (Estrogen receptor)
    |
    ER positive • BRAF wild-type • ESR1 mutation
    |
    fulvestrant • amcenestrant (SAR439859) • camizestrant (AZD9833) • giredestrant (RG6171)
    5ms
    Patient-reported outcomes in the SERENA-6 trial of camizestrant plus CDK4/6 inhibitor in patients with advanced breast cancer and emergent ESR1 mutations during first-line endocrine-based therapy. (PubMed, Ann Oncol)
    Together with the clinical efficacy and manageable safety profile of camizestrant-CDK4/6i, and reduced risk of GHS/QoL deterioration, the PROs from the SERENA-6 trial support switching to this combination as a potential new treatment strategy to optimise and improve outcomes in patients with HR+/HER2- advanced breast cancer and ESR1m emergence, ahead of disease progression, during first-line AI-CDK4/6i.
    Journal
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
    |
    HER-2 negative • ESR1 mutation
    |
    camizestrant (AZD9833)
    5ms
    SERENA-1: Study of AZD9833 Alone or in Combination in Women With Advanced Breast Cancer. (clinicaltrials.gov)
    P1, N=396, Active, not recruiting, AstraZeneca | Trial completion date: Nov 2025 --> Dec 2026
    Trial completion date • First-in-human
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
    |
    HER-2 negative
    |
    Ibrance (palbociclib) • everolimus • Verzenio (abemaciclib) • Kisqali (ribociclib) • Truqap (capivasertib) • anastrozole • camizestrant (AZD9833)