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    DRUG CLASS:

    Aromatase inhibitor

    Related drugs:
    4d
    High-Plex Digital Spatial Profiling Identified Prolactin-Induced Protein mRNA Associated With Response and Survival of Everolimus and Letrozole Treatment for Hormone Receptor-Positive/Human Epidermal Growth Factor Receptor 2-Negative Advanced Breast Cancer. (PubMed, MedComm (2020))
    PIP mRNA expression and specific immune-stromal features are associated with resistance to EVE. These findings suggest the potential of PIP as a spatially resolved predictive biomarker for patient stratification in HR+/HER2- ABC.
    Journal
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    HER-2 (Human epidermal growth factor receptor 2) • PTPRC (Protein Tyrosine Phosphatase Receptor Type C)
    |
    HR positive • HER-2 negative • EGFR positive
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    everolimus • letrozole
    5d
    Is anastrozole really better than tamoxifen for low-risk breast cancer? (PubMed, Am J Surg)
    In both pre- and postmenopausal women, there is no difference in 10-year OS or LR between anastrozole and tamoxifen for BC patients with low Oncotype RS. We conclude that Stage 1-3, T1-T3 pre- and postmenopausal BC patients with Oncotype RS between 0 and 17 can safely choose either medication. This finding is of particular importance for premenopausal women who wish to avoid the adverse side effects of medically induced menopause and bone deterioration associated with the anastrozole and ovarian suppression approach.
    Journal
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    HR positive
    |
    Oncotype DX Breast Recurrence Score®Test
    |
    tamoxifen • anastrozole
    6d
    Identification of potential novel aromatase inhibitors as therapeutic strategies against breast cancer: insight into molecular docking, MD simulations and ADMET profiling. (PubMed, BMC Cancer)
    The three phytochemicals identified from Ricinus communis show promise as novel aromatase inhibitors with superior binding and favorable pharmacokinetic predictions compared to Letrozole. These compounds warrant further in vitro and in vivo study as potential breast cancer therapeutics.
    Journal
    |
    ER (Estrogen receptor)
    |
    letrozole
    7d
    Grade 3 Dermatitis Secondary to Two Aromatase Inhibitors in Early Hormone Receptor-Positive Breast Cancer: A Case Report. (PubMed, Cureus)
    The patient developed a grade 3 eruptive, maculopapular dermatitis to exemestane and subsequently letrozole. Unusually, a third AI - anastrozole - has been well tolerated. Severe dAEs secondary to AIs are rare, and there is a lack of evidence-based research to guide management of these reactions.
    Journal
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    HER-2 (Human epidermal growth factor receptor 2)
    |
    HR positive • HER-2 negative
    |
    letrozole • anastrozole • exemestane
    11d
    Bushen Huatan formula alleviates polycystic ovary syndrome in rats by activating the PI3K/Akt pathway to inhibit GSDMD-mediated pyroptosis and mitochondrial damage. (PubMed, J Ovarian Res)
    This study shows that BSHT dose-dependently activates the PI3K/Akt pathway, inhibits GSDMD-mediated pyroptosis, and improves mitochondrial dysfunction in PCOS. Its regulation of inflammation, oxidative stress, metabolism, and ovarian function suggests a promising multi-target therapeutic strategy and provides insights for future clinical applications.
    Preclinical • Journal
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    IL6 (Interleukin 6) • TNFA (Tumor Necrosis Factor-Alpha) • IL1B (Interleukin 1, beta) • SLC2A4 (Solute Carrier Family 2 Member 4)
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    letrozole • metformin • LY294002
    13d
    N-Carbobenzoxy-L-Phenylalanine disrupts ErbB2 homodimer formation, blocking autophosphorylation and downstream signaling in breast Cancer: A comprehensive computational approach. (PubMed, Comput Biol Med)
    Compared to the reference endocrine therapy D1 (letrozole), C13 exhibited superior simulation outcomes, with 2D and 3D FEL analyses demonstrating the structural conformation of the complexes. Overall, our findings suggest that C13 is a promising hit compound targeting tyrosine-protein kinase (ErbB2), capable of disrupting homodimer formation in HER2-positive breast cancer progression.
    Journal
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 positive • HER-2 overexpression
    |
    letrozole
    14d
    Cost-effectiveness analysis of ribociclib versus palbociclib as a first line therapy in HR+/HER2- advanced breast cancer: evidence from the Chilean Public Health system. (PubMed, Expert Rev Pharmacoecon Outcomes Res)
    PSA confirmed a 100% probability of ribociclib being cost-effective at a willingness-to-pay threshold of 1 GDP per capita. Ribociclib plus letrozole is cost-saving and cost-effective compared to palbociclib plus letrozole for the first-line treatment of postmenopausal women with HR+/HER2- advanced BC in Chile.
    Journal • HEOR • Cost-effectiveness
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    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 negative
    |
    Ibrance (palbociclib) • Kisqali (ribociclib) • letrozole
    17d
    An integrated computational, in vitro and metabolomics approach to the discovery of novel aromatase inhibitors with anti-breast cancer activities. (PubMed, Sci Rep)
    Ten molecules were found to inhibit aromatase with IC50 values ranging between 0.04 and 2.31 µM, more potent than the clinical drug, exemestane (IC50 = 2.40 µM)...Molecular docking and dynamics simulations predicted that hydrophobic interactions are most important for aromatase inhibition, whereas chelation activities can also contribute to inhibition. The series have drug-like profiles with acceptable toxicity, and are pharmacokinetically compatible for oral drug administration.
    Preclinical • Journal • Metabolomic study
    |
    ER (Estrogen receptor)
    |
    ER positive
    |
    exemestane
    18d
    Mesonephric-like metaplasia of the endometrium in a woman treated with letrozole: morphological, immunohistochemical and molecular analysis. (PubMed, Pathologica)
    These features appear consistent with a benign endometrial mesonephric-like metaplasia. Its relationships with hormone treatment and with MLA carcinogenesis remain to be defined.
    Journal
    |
    EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2) • KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • ER (Estrogen receptor) • TP53 (Tumor protein P53) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PGR (Progesterone receptor) • NRAS (Neuroblastoma RAS viral oncogene homolog) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS) • IDH1 (Isocitrate dehydrogenase (NADP(+)) 1) • IDH2 (Isocitrate Dehydrogenase (NADP(+)) 2) • FGFR3 (Fibroblast growth factor receptor 3) • HRAS (Harvey rat sarcoma viral oncogene homolog) • PDGFRA (Platelet Derived Growth Factor Receptor Alpha) • NKX2-1 (NK2 Homeobox 1) • MME (Membrane Metalloendopeptidase) • GATA3 (GATA binding protein 3) • PAX8 (Paired box 8)
    |
    PIK3CA mutation • TP53 wild-type
    |
    letrozole
    19d
    Letrozole to prevent breast cancer in postmenopausal women with BRCA1/2 mutations (LIBER study). (PubMed, Eur J Cancer)
    Due to the underpowered nature of the trial and the observed trend, it cannot be ruled out that using AI to prevent invasive breast cancer could be effective for BRCA1/2 carriers overall, or for specific subgroups within a larger sample size. Further randomised controlled trials are needed to determine the potential benefits of AI for gBRCA1/2m carriers.
    Clinical • Journal • BRCA Biomarker
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    BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset)
    |
    letrozole
    20d
    Betaine alleviates letrozole-induced polycystic ovarian syndrome in rats by regulating oxidative stress and inflammation and restoring the proliferation-apoptosis balance. (PubMed, J Ovarian Res)
    This study elucidated the effectiveness of BTN in ameliorating letrozole-induced PCOS in rats by reducing oxidative stress, apoptosis, and inflammation, and modulating PCNA.
    Preclinical • Journal • IO biomarker
    |
    BCL2 (B-cell CLL/lymphoma 2) • NFE2L2 (Nuclear Factor, Erythroid 2 Like 2) • CASP3 (Caspase 3) • PCNA (Proliferating cell nuclear antigen) • CAT (Catalase)
    |
    letrozole • metformin
    25d
    Eccrine Carcinoma Mimicking Breast Cancer: Diagnostic Challenges and Hormone Therapy as an Emerging Treatment. (PubMed, J Med Cases)
    The patient declined chemotherapy and radiation therapy, opting instead for treatment with letrozole and ribociclib. Hormone therapy may be a potential option for hormone receptor-positive cases. Further research is essential to develop clearer diagnostic tools and standardized treatment protocols for this rare malignancy.
    Journal
    |
    ER (Estrogen receptor) • PGR (Progesterone receptor)
    |
    HR positive
    |
    Kisqali (ribociclib) • letrozole