- |||||||||| Verzenio (abemaciclib) / Eli Lilly
P2 data, Journal: A Phase II, Two-Stage Study of Letrozole and Abemaciclib in Estrogen Receptor-Positive Recurrent Endometrial Cancer. (Pubmed Central) - Oct 1, 2022 Table: 21MO Parameter PostM PreM RIB + LET n=77 PBO + LET n=77 RIB + NSAI + goserelin n=79 PBO + NSAI + goserelin n=77 Treatment ongoing, n 35 11 27 14 PFS, median, mo Not reached 18.5 27.6 14.7 HR (95% CI) 0.400 (0.258-0.618) 0.672 (0.448-1.009) ORR, % (95% CI)a 60.3 (48.1-71.5) 49.3 (37.2-61.4) 53.6 (41.2-65.7) 38.5 (26.7-51.4) aMeasurable disease. Letrozole/abemaciclib demonstrated encouraging and durable evidence of activity in recurrent ER positive endometrioid EC.
- |||||||||| letrozole / Generic mfg.
Journal: Granulocyte colony stimulating factor (GCSF) did not affect the fertility outcomes in women with unexplained infertility after intrauterine insemination: a randomised clinical trial. (Pubmed Central) - Sep 30, 2022 All participants were stimulated by letrozole, clomiphene and HMG during the cycle...The current study suggests that systemic administration of 300 μg granulocyte colony stimulating factor in the two days after receiving IUI in patients with unexplained infertility does not offer any beneficial clinical related implantation and pregnancy rates.What are the implications of these findings for clinical practice and/or further research? These results may not be generalised to all patients and more randomised controlled trials are needed for the comparison of granulocyte colony stimulating factor effects on women with thin and normal endometrial thickness, efficacy, side effects, and pregnancy outcomes of the intrauterine perfusion versus systemic subcutaneous administration of granulocyte colony stimulating factor in unexplained infertility treated with intrauterine insemination.
- |||||||||| Ibrance (palbociclib) / Pfizer, Keytruda (pembrolizumab) / Merck (MSD)
Trial suspension: Pembrolizumab, Endocrine Therapy, and Palbociclib in Treating Postmenopausal Patients With Newly Diagnosed Metastatic Stage IV Estrogen Receptor Positive Breast Cancer (clinicaltrials.gov) - Sep 30, 2022 P2, N=47, Suspended, These results may not be generalised to all patients and more randomised controlled trials are needed for the comparison of granulocyte colony stimulating factor effects on women with thin and normal endometrial thickness, efficacy, side effects, and pregnancy outcomes of the intrauterine perfusion versus systemic subcutaneous administration of granulocyte colony stimulating factor in unexplained infertility treated with intrauterine insemination. Recruiting --> Suspended
- |||||||||| Retrospective data, Journal: Bone Safety Profile of Steroidal Aromatase Inhibitor in Comparison to Nonsteroidal Aromatase Inhibitors in Postmenopausal Women with Breast Cancer: A Network Meta-Analysis. (Pubmed Central) - Sep 30, 2022
Aromatase inhibitors (AIs) provide an alternative to tamoxifen as an adjuvant therapy for postmenopausal patients with breast cancer (BC)...Although there was no statistical significance, treatment with exemestane lowered the incidence of bone pain (odds ratio [OR] vs. anastrozole and letrozole: 0.63, 0.54), fracture episodes (OR vs. anastrozole and letrozole: 0.84, 0.80), and osteoporosis (OR vs. anastrozole and letrozole: 0.85, 0.73) compared with letrozole and anastrozole...Treatment ranking with the surface under the cumulative ranking curve showed that exemestane was found to reduce the incidence of bone-related adverse events. A lower incidence of bone-related safety events was observed in patients treated with exemestane.
- |||||||||| Herceptin (trastuzumab) / Roche, chlorogenic acid / Jiuzhang Biotech
Journal: In silico approach and molecular docking studies of potent bioactive compounds of Carica papaya as anti-breast cancer agents. (Pubmed Central) - Sep 29, 2022 Potent breast cancer drugs are Tamoxifen, Paclitaxel, Cyclophosphamide, Trastuzumab, etc., and aromatase inhibitors, include Anastrozole, Letrozole, and Exemestane, etc. In general, breast cancer drugs cause numerous adverse effects in humans...Among the five bioactive phytocompounds, Chlorogenic acid has a higher G Score with good binding energy than Tamoxifen, Anastrozole, and Letrozole standards...ADME profiling of the phytocompounds was investigated to find the pharmacokinetic characteristics and drug-likeness Carica papaya derived phytocompounds act as an antiestrogen or aromatase inhibitor to regulate the levels of estrogen and the implications for postmenopausal women and reduce the risk of breast cancer. Therefore, we propose these top five bioactive phytocompound for further investigation through in vitro and in vivo studies.
- |||||||||| letrozole / Generic mfg., exemestane / Generic mfg.
Journal: Genome-wide association study of aromatase inhibitor discontinuation due to musculoskeletal symptoms. (Pubmed Central) - Sep 29, 2022 Our GWAS findings identify several candidate variants that may be associated with AIMSS risk from AI generally or letrozole specifically. Validation of these associations in independent cohorts is needed before translating these findings into clinical practice to improve treatment outcomes in patients with HR + breast cancer.
- |||||||||| letrozole / Generic mfg.
Mechanistic Insights into Cytotoxic Effects of Letrozole Against Glioblastoma Cells (West/Central Hall) - Sep 28, 2022 - Abstract #SNO2022SNO_1242; Our study suggests that the cytotoxic effects of LTZ against GBM are mediated, at least partially, by the inhibition of aromatase activity which results in estrogen deprivation. These mechanistic insights are important to facilitate repurposing LTZ as a novel anti-GBM drug.
- |||||||||| Legalon (silibinin) / Mylan
Preclinical, Journal: Therapeutic Effects of Silibinin Against Polycystic Ovary Syndrome Induced by Letrozole in Rats via Its Potential Anti-Inflammatory and Anti-Oxidant Activities. (Pubmed Central) - Sep 20, 2022 Silibinin alone or in combination with metformin was found to be effective in restoring the regularity of estrous cycle by ameliorating the abnormal alterations of LH, TS, EST, tumor necrosis factor (TNF)-α, and oxidative status and by resuming the appearance of corpora lutea and decreasing or even total absence of cystic follicles in the ovaries. Silibinin was effective in restoring estrous regularities and alleviating hormonal and histomorphological abnormalities of the ovarian and uterine tissues, this could be due to its anti-androgenic, anti-inflammatory and antioxidant properties.
- |||||||||| Legalon (silibinin) / Mylan
Preclinical, Journal: Effect of Silibinin on Dyslipidemia and Glycemic Alteration Associated with Polycystic Ovarian Syndrome: An Experimental Study on Rats. (Pubmed Central) - Sep 20, 2022 This study investigated the efficacy of the flavonolignan silibinin in restoring the metabolic alterations associated with letrozole-induced PCOS in rats...On day 21, six animals from the first group and six animals from the second group were sacrificed to confirm the development of PCOS, and the rest of the animals (n=24) in the second group were distributed equally into four groups: the PCOS group received vehicle, the metformin (MET) group received 300 mg/kg metformin orally, and the low-dose silibinin (LD-100) and high-dose silibinin (HD-200) groups received 100 and 200 mg/kg silibinin intraperitoneally, respectively...This could be related to the decreased insulin resistance, and antiandrogenic and phytoestrogenic activity of silibinin. Further study with longer term therapy is recommended to clarify more potential effects of silibinin and its mechanism of action in PCOS.
- |||||||||| letrozole / Generic mfg.
Journal: Estrogen promotes fetal skeletal muscle myofiber development important for insulin sensitivity in offspring. (Pubmed Central) - Sep 20, 2022 Importantly, fetal skeletal muscle development, including fascicle organization, myofiber size and composition was normal in baboons treated with letrozole and estradiol benzoate. Collectively, these and our previous findings support our proposal that exposure of the fetus to estrogen is important for fetal skeletal muscle development and glucose homeostasis in adulthood.
- |||||||||| letrozole / Generic mfg.
Aromatase Inhibitor Induced Musculoskeletal Inflammation Is Observed Independent of Oophorectomy in a Novel Mouse Model (Virtual Poster Hall) - Sep 17, 2022 - Abstract #ACRConvergence2022ACR_CONVERGENCE_3531; This suggests that the pathogenesis of AIIA may not be mediated by E2 deficiency, as previously hypothesized, and indicates that AI-induced inflammation is not regulated directly through immune cell activation. Future studies will characterize this inflammatory mechanism in vivo with a focus on synovial cells and chondrocytes to provide insight into putative therapeutic strategies directed at mitigating disease pathology
- |||||||||| letrozole / Generic mfg., clomifene citrate / Generic mfg.
Journal: Modeling Pregnancy Outcomes through Sequentially Nested Regression Models. (Pubmed Central) - Sep 14, 2022 By analyzing the PPCOS data, we successfully uncover the hidden influence of risk factors on live birth, which confirm clinical experience. Moreover, we provide novel infertility treatment recommendations (e.g., letrozole vs clomiphene citrate) for women with PCOS to improve their chances of live birth.
- |||||||||| letrozole / Generic mfg.
Preclinical, Journal: Roles of HIF-1α/BNIP3 mediated mitophagy in mitochondrial dysfunction of letrozole-induced PCOS rats. (Pubmed Central) - Sep 14, 2022 Finally, we detected the HIF-1α/BNIP3 pathway and found HIF-1α-mediated mitophagy is impaired in the ovaries of PCOS rats. Together, these results clearly demonstrated excessive ROS causes mitochondrial dysfunction via the abnormal mitochondrial quality control system, and attenuates HIF-1α/BNIP3-mediated mitophagic defense in the granulosa cells of PCOS rats, which will provide a new direction for further understanding the role of HIF-1α in the molecular mechanism of mitochondrial dysfunction in PCOS ovaries.
- |||||||||| letrozole / Generic mfg.
CYP19A1 mediated sex hormone metabolism promotes severe SARS-CoV-2 disease outcome in males (HALL 1A) - Sep 13, 2022 - Abstract #OPTIONSXI2022OPTIONS_XI_184; Our findings highlight the role of the lung as a yet unrecognized but critical organ regulating metabolic responses upon respiratory virus infection. Furthermore, inhibition of CYP19A1 by the clinically approved drug letrozole may pose a new therapeutic strategy to reduce poor long-term COVID-19 outcome.
- |||||||||| NN1213 / Novo Nordisk
Trial completion date, Trial primary completion date, Real-world evidence, Real-world, Metastases: Treat ER+ight: Treatment of Canadian Men and Pre/Peri/Post-menopausal Women With ER+ Advanced Breast Cancer in the Real-World Setting With Hormone Therapy (clinicaltrials.gov) - Sep 13, 2022 P=N/A, N=440, Active, not recruiting, Furthermore, inhibition of CYP19A1 by the clinically approved drug letrozole may pose a new therapeutic strategy to reduce poor long-term COVID-19 outcome. Trial completion date: Aug 2022 --> Dec 2022 | Trial primary completion date: Aug 2022 --> Dec 2022
- |||||||||| letrozole / Generic mfg., spironolactone / Generic mfg.
Preclinical, Journal: Low-dose spironolactone ameliorates adipose tissue inflammation and apoptosis in letrozole-induced PCOS rat model. (Pubmed Central) - Sep 11, 2022 Clinical management must be tailored on a case-by-case basis by a gynecologic oncologist and reproductive physician meeting. Altogether, the present study suggests that low-dose spironolactone confers protection against adipose dysfunction in experimental PCOS animals by attenuating inflammation, oxidative stress and cellular apoptosis.
- |||||||||| letrozole / Generic mfg., clomifene citrate / Generic mfg.
Review, Journal: Recent Advances in the Management of Polycystic Ovary Syndrome: A Review Article. (Pubmed Central) - Sep 11, 2022 Other than reproductive symptoms, PCOS symptoms include insulin resistance (IR), metabolic syndrome (MS), and chronic low-grade inflammation. Our understanding of the pathophysiological process, diagnosis, and therapy of PCOS has advanced recently.
- |||||||||| Prolia (denosumab) / Amgen, Daiichi Sankyo, Ibrance (palbociclib) / Pfizer
AN UNCOMMON CAUSE OF CHEST PAIN: CEMENT EMBOLISM (Convention Center Exhibit Hall: Poster Area) - Sep 11, 2022 - Abstract #CHEST2022CHEST_4085; Fortunately majority of them are peripheral, asymptomatic and only need surveillance. For symptomatic, central pulmonary cement embolism long term anticoagulation therapy has been recommended.
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