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    DRUG:

    letrozole

    i
    Other names: CGP 20267, CGS 20267, CGS20267
    Company:
    Generic mfg.
    Drug class:
    Aromatase inhibitor
    Related drugs:
    3d
    Simultaneous gastric and colonic metastasis of invasive lobular carcinoma of the breast. (PubMed, Clin J Gastroenterol)
    Endocrine therapy with letrozole led to systemic improvement. However, diarrhea and abdominal pain persisted until palbociclib was initiated, after which both symptoms markedly improved...In patients with breast cancer, particularly ILC, persistent gastrointestinal symptoms may suggest metastasis. Careful endoscopic evaluation with biopsy is essential for diagnosis and monitoring the treatment response.
    Journal
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    ER (Estrogen receptor) • CDH1 (Cadherin 1)
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    ER positive
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    Ibrance (palbociclib) • letrozole
    3d
    Study of ERW316 as a Single Agent or in Combination With Endocrine Therapy in Patients With HR+/HER2- Breast Cancer and Other Advanced Solid Tumors (clinicaltrials.gov)
    P1/2, N=217, Not yet recruiting, Novartis Pharmaceuticals
    New P1/2 trial • First-in-human
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    HER-2 (Human epidermal growth factor receptor 2) • CCNE1 (Cyclin E1)
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    HER-2 negative
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    fulvestrant • letrozole
    7d
    Alginate-functionalized and PEGylated niosomes co-encapsulating letrozole and berberine for preclinical breast cancer therapy: Overcoming multidrug resistance. (PubMed, Int J Biol Macromol)
    Also, gene expressions of Bax and caspase 3/8/9 increased while the gene expression of Bcl2 (anti-apoptotic) decreased after treatment with coated niosomes compared to uncoated ones. Taken together, this preliminary research indicated that the co-delivery of Let and Ber through coated niosomal formulations (Nio-Let/Ber@PEG and Nio-Let/Ber@AL) was an efficient controlled dual-drug delivery system to increase the effectiveness of breast cancer therapy.
    Preclinical • Journal • IO biomarker
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    BCL2 (B-cell CLL/lymphoma 2) • BAX (BCL2-associated X protein) • CASP3 (Caspase 3) • CASP8 (Caspase 8) • CASP9 (Caspase 9)
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    letrozole
    9d
    Safety and antitumour activity of ipatasertib combined with endocrine therapy and a CDK4/6 inhibitor in HR+/HER2- metastatic breast cancer (TAKTIC): a single-centre, open-label, phase 1b trial. (PubMed, Lancet Oncol)
    The combination of fulvestrant, ipatasertib, and palbociclib showed preliminary signs of clinical activity and showed expected adverse events in heavily pretreated patients with HR+/HER2- metastatic breast cancer, warranting further evaluation in those with CDK4/6 inhibitor-refractory disease.
    P1 data • Journal
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    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 negative
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    Ibrance (palbociclib) • fulvestrant • letrozole • ipatasertib (RG7440) • anastrozole • exemestane
    10d
    Morpheus-TNBC: A Study Evaluating the Efficacy and Safety of Multiple Treatment Combinations in Patients With Metastatic or Locally Advanced Breast Cancer (clinicaltrials.gov)
    P1/2, N=792, Recruiting, Hoffmann-La Roche | N=56 --> 792
    Enrollment change
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    PD-L1 (Programmed death ligand 1)
    |
    Avastin (bevacizumab) • Tecentriq (atezolizumab) • Ibrance (palbociclib) • carboplatin • gemcitabine • Enhertu (fam-trastuzumab deruxtecan-nxki) • capecitabine • Verzenio (abemaciclib) • albumin-bound paclitaxel • Kisqali (ribociclib) • fulvestrant • Halaven (eribulin mesylate) • letrozole • ipatasertib (RG7440) • Trodelvy (sacituzumab govitecan-hziy) • Itovebi (inavolisib) • Actemra IV (tocilizumab) • atirmociclib (PF-07220060) • ladiratuzumab vedotin (SGN-LIV1A) • selicrelumab (RG7876)
    10d
    OPERA-01: OP-1250 (Palazestrant) vs. Standard of Care for the Treatment of ER+/HER2- Advanced Breast Cancer (clinicaltrials.gov)
    P3, N=510, Recruiting, Olema Pharmaceuticals, Inc. | N=382 --> 510
    Enrollment change
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    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
    |
    HER-2 negative
    |
    fulvestrant • letrozole • anastrozole • exemestane • palazestrant (OP-1250)
    10d
    OPERA-02: Palazestrant in Combination With Ribociclib for the First-line Treatment of ER+/HER2- Advanced Breast Cancer (clinicaltrials.gov)
    P3, N=1000, Recruiting, Olema Pharmaceuticals, Inc. | N=360 --> 1000
    Enrollment change • Trial initiation date
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    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
    |
    HER-2 negative
    |
    Kisqali (ribociclib) • letrozole • palazestrant (OP-1250)
    10d
    Case Report: Rare gastric and bone metastases after early endocrine therapy discontinuation in hormone receptor-positive breast cancer: lessons and therapeutic insights. (PubMed, Front Oncol)
    She received first-line endocrine therapy (letrozole+ribociclib+goserelin) combined with denosumab. Breast cancer gastric metastasis diagnosis relies on medical history, gastroscopy, and immunohistochemistry (GATA3+, CK7+, CK20-). The combination regimen yielded favorable efficacy, providing clinical reference for similar rare cases.
    Journal
    |
    HER-2 (Human epidermal growth factor receptor 2) • PGR (Progesterone receptor) • GATA3 (GATA binding protein 3)
    |
    HR positive
    |
    Kisqali (ribociclib) • letrozole • Prolia (denosumab) • goserelin acetate
    10d
    Palbociclib and Letrozole or Fulvestrant in Treating Patients With Estrogen Receptor Positive, HER2 Negative Metastatic Breast Cancer (clinicaltrials.gov)
    P2, N=93, Completed, Alliance for Clinical Trials in Oncology | Active, not recruiting --> Completed | Trial completion date: Aug 2024 --> Feb 2026
    Trial completion • Trial completion date
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    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
    |
    ER positive • HER-2 negative • HER-2 negative + ER positive
    |
    Ibrance (palbociclib) • fulvestrant • letrozole
    10d
    PLUM: Prescription of Letrozole for Uterine Myoma (clinicaltrials.gov)
    P4, N=140, Recruiting, University of California, San Francisco | Trial primary completion date: Jan 2027 --> Jun 2027
    Trial primary completion date
    |
    letrozole
    10d
    OPERA-02: Palazestrant in Combination With Ribociclib for the First-line Treatment of ER+/HER2- Advanced Breast Cancer (clinicaltrials.gov)
    P3, N=360, Recruiting, Olema Pharmaceuticals, Inc. | Not yet recruiting --> Recruiting
    Enrollment open
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
    |
    HER-2 negative
    |
    Kisqali (ribociclib) • letrozole • palazestrant (OP-1250)
    11d
    A Precision Medicine Approach (SMMART-ACT) for the Treatment of Patients With Advanced Sarcoma, Prostate, Breast, Ovarian or Pancreatic Cancer (clinicaltrials.gov)
    P2, N=6, Terminated, OHSU Knight Cancer Institute | N=30 --> 6 | Trial completion date: Jun 2033 --> Mar 2026 | Active, not recruiting --> Terminated | Trial primary completion date: Dec 2027 --> Mar 2026; Loss of support.
    Enrollment change • Trial completion date • Trial termination • Trial primary completion date
    |
    HER-2 (Human epidermal growth factor receptor 2) • BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset)
    |
    HER-2 positive • BRCA2 mutation • BRCA1 mutation • HR positive • HER-2 negative • EGFR positive
    |
    Tagrisso (osimertinib) • gemcitabine • tamoxifen • Verzenio (abemaciclib) • pemetrexed • letrozole • exemestane