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DRUG:

letrozole

i
Other names: CGP 20267, CGS 20267, CGS20267
Company:
Generic mfg.
Drug class:
Aromatase inhibitor
2d
ABIGAIL: ABemaciclib, ET ± paclItaxel in aGgressive HR+/HER2- MBC trIaL (clinicaltrials.gov)
P2, N=162, Completed, MedSIR | Active, not recruiting --> Completed
Trial completion
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HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
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HER-2 negative
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paclitaxel • Verzenio (abemaciclib) • fulvestrant • letrozole
2d
Phase II Trial of Ribociclib Plus Letrozole in Women With Recurrent Low-Grade Serous Carcinoma of the Ovary, Fallopian Tube, or Peritoneum: A GOG Partners Trial (GOG 3026). (PubMed, J Clin Oncol)
Ribociclib plus letrozole met the primary end point, achieving meaningful response rates and durable disease control in recurrent LGSOC. The safety profile was consistent with prior CDK4/6 inhibitor studies. This combination represents a therapeutic option in this rare and genomically distinct subtype.
P2 data • Journal
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ER (Estrogen receptor)
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HR positive
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Kisqali (ribociclib) • letrozole
2d
Neoadjuvant Abemaciclib plus Letrozole vs. Chemotherapy in patients with HR+/HER2- Highly Proliferative Breast Cancer. (PubMed, Clin Cancer Res)
CARABELA trial results suggest that 12 months of letrozole/abemaciclib may not offer similar efficacy to that of chemotherapy in achieving RCB 0-I. However, in less proliferative tumors (RS <26 or Ki-67 <30%), outcomes were comparable, suggesting that letrozole/abemaciclib could replace (neo)adjuvant chemotherapy in selected patients.
Journal
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HER-2 (Human epidermal growth factor receptor 2)
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HER-2 negative
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Verzenio (abemaciclib) • letrozole
3d
P021 A case of radiation-induced haemorrhagic bullous lichen sclerosus of the breast. (PubMed, Br J Dermatol)
Her right breast ductal carcinoma, diagnosed 9 months prior, was treated with surgery, adjuvant letrozole and radiotherapy...Management options include topical and systemic corticosteroids, phototherapy and methotrexate (Hobbs L, Tiwari N. Hemorrhagic bullous lichen sclerosus of the breast: a rare complication of radiotherapy...To the best of our knowledge, this is the fifth reported case of RHBLS. Early recognition is crucial to alleviate concerns about breast cancer recurrence and to rule out vulval lichen sclerosus.
Journal
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IL4 (Interleukin 4)
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methotrexate • letrozole
3d
BI14 Case series: exploring the link between psoriasis and cyclin-dependent kinase 4/6 inhibitors in breast cancer treatment. (PubMed, Br J Dermatol)
She was initiated on palbociclib and letrozole treatment in April 2024...She was commenced on ribociclib and letrozole for relapsed metastatic liver disease in April 2023...Understanding the role of CDK4/6 inhibition and the link with psoriasis is important for optimizing therapeutic choices for patients with cancer with pre-existing or newly developed psoriasis. Given the increasing use of CDK4/6 inhibitors in cancer treatment, clinicians should be vigilant of the potential increased prevalence of psoriasis experienced in this patient cohort.
Journal
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HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • IL17A (Interleukin 17A) • IL22 (Interleukin 22)
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HR positive • HER-2 negative • EGFR positive
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Ibrance (palbociclib) • Kisqali (ribociclib) • letrozole
3d
The potential effects of the synergistic interaction between ferulic acid and new generation CDK inhibitor anti-neoplastic drugs on breast cancer anti-tumour activity. (PubMed, Med Oncol)
Ribociclib (Ribo) and Abemaciclib (Abe) are new-generation CDK inhibitors approved for use in breast cancer treatment. Some molecular mechanisms were elucidated by revealing the synergistic effect of FA combined with Ribo and/or Abe in both HR positive and HR negative breast cancer and its possible toxicity or protection on normal breast cells. The present findings suggest that FA is a viable candidate for adjuvant or neoadjuvant treatment in combination with Ribo and/or Abe, as an alternative to Letrozole or Fulvestrant, which have been associated with significant adverse effects in clinical settings.
Journal
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ER (Estrogen receptor)
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HR positive
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Verzenio (abemaciclib) • Kisqali (ribociclib) • fulvestrant • letrozole
5d
Enrollment change
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Ibrance (palbociclib) • letrozole
5d
CD8+ T cells in the tumor microenvironment modulate response to endocrine therapy in breast cancer. (PubMed, J Clin Invest)
We analyzed pre- and on-treatment biopsies from patients with HR+ breast cancer treated with letrozole to induce estrogen deprivation (ED)...Finally, deletion combined with silencing of the CXCL11 receptors CXCR3 and CXCR7 in MCF7 cells impaired proliferation in response to exogenous CXCL11 and to co-culture with CD8+ T cells in estrogen-free conditions. These findings suggest that CD8+ T cell-associated CXCL11 in the TIME modulates the response of HR+ breast cancer cells to estrogen suppression.
Journal
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CD8 (cluster of differentiation 8) • CXCL10 (Chemokine (C-X-C motif) ligand 10) • CXCL9 (Chemokine (C-X-C motif) ligand 9) • CXCL11 (C-X-C Motif Chemokine Ligand 11) • CXCR3 (C-X-C Motif Chemokine Receptor 3) • ACKR3 (Atypical Chemokine Receptor 3)
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HR positive
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letrozole
9d
ELEGANCE: Non-interventional Study to Assess the Effectiveness and Safety of Ribociclib in the Adjuvant Therapy of Hormone Receptor Positive (HR+) HER2-negative Stage II and III Breast Cancer in Real Clinical Practice in Russia (clinicaltrials.gov)
P=N/A, N=2766, Not yet recruiting, Novartis Pharmaceuticals | Trial completion date: Jul 2032 --> Dec 2032 | Initiation date: Jul 2025 --> Dec 2025 | Trial primary completion date: Jul 2032 --> Dec 2032
Trial completion date • Trial initiation date • Trial primary completion date
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Kisqali (ribociclib) • letrozole • anastrozole
10d
Novel benzoxazole-based hybrids as multi-target inhibitors of aromatase, EGFR, and PI3K with potential anti-breast cancer activity. (PubMed, Bioorg Med Chem)
MTT assay showed that 6 and 9b were 4.5 and 2 times more potent than doxorubicin against MCF-7 cells, while 9a and 13b were 10 and 7.5 times more effective against MDA-MB-231 cells, respectively...Compound 13b exhibited comparable EGFRL858R inhibition to lapatinib and outperformed pictilisib against PI3Kα, PI3Kβ, and PI3Kδ. Compound 6 showed greater ARO inhibition than letrozole, while being slightly less potent than pictilisib against PI3Kα and PI3Kβ...Docking studies supported the in vitro enzymatic inhibition assays results. Thus, 9b and 13d are potent anti-breast cancer benzoxazoles with selective ARO and PI3kα inhibition activity, respectively, while 6, 9a, and 13b are multi-target inhibitors exhibiting other anticancer synergistic mechanisms.
Journal
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EGFR (Epidermal growth factor receptor) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PIK3CD (Phosphatidylinositol-4 5-Bisphosphate 3-Kinase Catalytic Subunit Delta) • PIK3CB (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta) • CASP9 (Caspase 9) • ANXA5 (Annexin A5) • BECN1 (Beclin 1)
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EGFR L858R • EGFR wild-type
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lapatinib • doxorubicin hydrochloride • letrozole • pictilisib (GDC-0941)
11d
Letrozole, abemaciclib and metformin in endometrial cancer: a non-randomized phase 2 trial. (PubMed, Nat Commun)
Based on preclinical studies showing synergism with simultaneous inhibition of the estrogen receptor (ER), CDK4/6 and PI3K pathways and based on window of opportunity studies showing that metformin suppresses PI3K/mTOR signaling in endometrial cancer (EC), we conduct a non-randomized phase 2 study of letrozole/abemaciclib/metformin in ER positive endometrioid EC (NCT03675893). There are no objective responses among TP53 mutated ECs and among NSMP (no specific molecular profile) tumors with RB1 or CCNE1 alterations; CTNNB1 mutations correlate with clinical benefit. Pharmacokinetic analyses demonstrate that administration of letrozole and abemaciclib with metformin result in a more than 3-fold increase in metformin exposure.
P2 data • Journal
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ER (Estrogen receptor) • TP53 (Tumor protein P53) • RB1 (RB Transcriptional Corepressor 1) • CCNE1 (Cyclin E1) • CDK4 (Cyclin-dependent kinase 4) • CTNNB1 (Catenin (cadherin-associated protein), beta 1)
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TP53 mutation • ER positive
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Verzenio (abemaciclib) • letrozole • metformin
12d
Enrollment open
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Kisqali (ribociclib) • letrozole • palazestrant (OP-1250)