Emcyt (estramustine) / Pfizer, Nippon Shinyaku - LARVOL DELTA

Impact of Neoadjuvant Chemohormonal Therapy With GnRH Antagonist and Low-Dose Estramustine in Very High-Risk Prostate Cancer Undergoing Robotic Radical Prostatectomy. (PubMed, Prostate) - "In patients with very high-risk PC undergoing robot-assisted laparoscopic prostatectomy, a GnRH antagonist and low-dose EMP yielded better BCR-free survival outcomes than NHT."

Journal • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Trends in novel antiandrogen receptor signal inhibitor use and medical costs in prostate cancer. (PubMed, Cancer Med) - "ARSI usage and medical costs associated with prostate cancer increased significantly from 2016 to 2021. Despite the limited use of ARSIs, a considerable proportion of the medical costs for prostate cancer-specific agents had been spent on ARSIs."

HEOR • Journal • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

The relationship between Sjögren's syndrome and recurrent pregnancy loss: a bioinformatics analysis. (PubMed, Reprod Biomed Online) - "This is one of the first studies to reveal that Sjögren's syndrome shares common biological pathways with RPL. KCNN3 was identified as the hub gene associated with Sjögren's syndrome and RPL, and may be a new target for mechanistic studies on Sjögren's syndrome and RPL."

Journal • Immunology • Sjogren's Syndrome • TLR2 • XIST

Synergistic combination effect of the PCA-1/ALKBH3 inhibitor HUHS015 on prostate cancer drugs in vitro and in vivo. (PubMed, Anticancer Drugs) - "Herein, we investigated the effect of HUHS015 in combination with drugs for prostate cancer approved in Japan (including bicalutamide, cisplatin, mitoxantrone, prednisolone, ifosfamide, tegafur/uracil, docetaxel, dacarbazine, and estramustine) by treating DU145 cells with around IC50 value concentrations of these drugs for 3 days. In conclusion, HUHS015 exhibited a synergistic effect with docetaxel and drugs acting on DNA in vitro, even after drug removal. Since cancer chemotherapy is typically administered during rest periods due to its high toxicity, combining it with an ALKBH3 inhibitor could be a promising strategy for enhancing cancer treatment, as it can elicit an additive effect during treatment, allowing dosage reduction, and synergistically sustain the effect after drug washout during rest periods."

Journal • Preclinical • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Dose compliance of estramustine phosphate in neoadjuvant chemohormonal therapy combined with degarelix acetate predicts the biochemical recurrence in patients with very high-risk prostate cancer who underwent robot-assisted radical prostatectomy. (PubMed, Int J Urol) - "Dose compliance with estramustine phosphate predicted biochemical recurrence in patients with very high-risk prostate cancer undergoing robot-assisted radical prostatectomy with neoadjuvant chemohormonal therapy."

Compliance • Journal • Acute Coronary Syndrome • Cardiovascular • Genito-urinary Cancer • Hematological Disorders • Oncology • Prostate Cancer • Pulmonary Embolism • Respiratory Diseases • Solid Tumor • Venous Thromboembolism

Gösta Jönsson (1909-1978): A pioneer in the hormonal treatment of prostate cancer in Sweden. (PubMed, J Med Biogr) - " Even if the results of Gösta Jönsson's studies could not be confirmed, the subsequent randomized studies of estramustine phosphate may hide the desired action of estramustine phosphate in a subgroup of patients. It has still not been elucidated whether estramustine phosphate has effects in this subgroup of patients with ostrogen-resistant prostate cancer."

Journal • Breast Cancer • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor • Urology

Microtubule depolymerization induces ferroptosis in neuroblastoma cells. (PubMed, IUBMB Life) - "Estramustine (EM), a clinically successful hormone-refractory anti-prostate cancer drug, exhibited potent anti-proliferative activity, depolymerized microtubules, blocked cells at mitosis, and induced cell death in different cancer cells...Ferroptosis inhibitors (deferoxamine mesylate and liproxstatin-1) abrogated the cytotoxic effects of EM, further confirming ferroptosis induction. Vinblastine and nocodazole also increased LIP and induced lipid peroxidation in neuroblastoma cells. This study provides evidence for the coupling of microtubule integrity to ferroptosis. The results also suggest that microtubule-depolymerizing agents may be considered for developing pro-ferroptosis chemotherapeutics."

Journal • CNS Tumor • Genito-urinary Cancer • Neuroblastoma • Oncology • Prostate Cancer • Solid Tumor • GPX4

Prognostic signature based on S100 calcium-binding protein family members for lung adenocarcinoma and its clinical significance. (PubMed, Comput Methods Biomech Biomed Engin) - "Finally, small molecular compounds targeting prognostic genes were screened using CellMiner database, and molecular docking confirmed the binding of AMG-176, Estramustine, and TAK-632 with prognostic genes. In conclusion, we generated a prognostic signature with robust and reliable predictive ability, which may provide guidance for prognosis and treatment of LUAD."

IO biomarker • Journal • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Radiation Therapy for Locally Advanced Prostate Cancer: How Do We Treat Patients with cN1 Disease? (PubMed, Eur Urol Focus) - "GETUG-AFU-12 showed that addition of docetaxel and estramustine to ADT improved relapse-free survival but not overall survival. STAMPEDE later demonstrated that abiraterone acetate with ADT and RT significantly improved failure-free survival and overall survival...Ongoing studies are testing these options to find the best combination. The aim is to increase the chances of curing prostate cancer, especially as advanced scan techniques are detecting more cases."

Journal • Metastases • Review • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Microtubule-associated protein MAP2 promotes drug resistance and cancer stemness in hepatocellular carcinoma through integrin dysregulation (AACR 2024) - "Estramustine Phosphate (EMP), previously reported to inhibit the interaction of MAP2 with actin filaments, attains a synergistic effect in suppressing tumor initiation and growth of HCC cell lines, HCC patient-derived organoids and NRAS+AKT HCC mouse model when used in combination with sorafenib. In summary, MAP2 inhibition may represent a potential novel therapy for HCC by targeting its cancer stemness roots and altering integrin signaling. Ongoing work is focused on the study of MAP2 regulation of integrin signaling and cell behaviours in the maintenance of a more stemness state in HCC."

Gastrointestinal Cancer • Hepatocellular Cancer • Oncology • Solid Tumor • CD133 • NRAS

Construction of a prognostic model for lung adenocarcinoma based on m6A/m5C/m1A genes. (PubMed, Hum Mol Genet) - "Based on the m6A/m5C/m1A-related genes in LUAD, LUAD patients were divided into 2 subtypes, and a m6A/m5C/m1A-related LUAD prognostic model was constructed to provide a reference for the prognosis prediction of LUAD."

Journal • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • CD4 • CD8

Analysis of genetic biomarkers, polymorphisms in ADME-related genes and their impact on pharmacotherapy for prostate cancer. (PubMed, Cancer Cell Int) - "The pharmacotherapeutic options for PCa include hormonal therapy, chemotherapy (Docetaxel, Mitoxantrone, Cabazitaxel, and Estramustine, etc.), and radiotherapy. Here, we overview the impact of SNPs reported in various genes on the pharmacotherapy for PCa and evaluate current genetic biomarkers with an emphasis on early diagnosis and individualized treatment strategy in PCa."

Biomarker • Journal • Review • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Treating Stage 4 Prostate Cancer (Everydayhealth) - "Stage 4 prostate cancer is considered incurable. But there is good news: New therapies have extended the lives of men with stage 4 prostate cancer. About a decade ago, the length of time men lived after a diagnosis of stage 4 prostate cancer was 18 months to two years, but with the inclusion of newer therapies, three to five years is not uncommon, according to William Dahut, MD...'Men are definitely living longer, but they're not being cured of the cancer,' he says."

Media quote

Microtubule-associated protein MAP2 promotes drug resistance and cancer stemness in hepatocellular carcinoma through integrin dysregulation (EACR 2023) - "Estramustine Phosphate (EMP), reported to inhibit the interaction of MAP2 with actin filaments, attained a synergistic effect in suppressing tumor initiation cell frequency and growth of HCC cell lines and patient-derived organoids when used in combination with sorafenib.ConclusionMAP2 inhibition may represent a potential novel therapy for HCC by targeting its CSC roots and altering integrin signaling. Future research will focus on the study of MAP2 regulation on integrin signaling and cell behaviors in the maintenance of a more stemness state in HCC."

Gastrointestinal Cancer • Hepatocellular Cancer • Oncology • Solid Tumor • CD133 • NRAS • PROM1

Very Long-Term Complete Remission Can Be Achieved in Men With High-Risk Localized Prostate Cancer and a Very High PSA Value: An Analysis of the GETUG 12 Phase 3 Trial. (PubMed, Clin Genitourin Cancer) - "Men with apparently localized prostate cancer and a high baseline PSA value have a reasonable chance of being long-term disease-free when treated with curative intent combining systemic and local therapy."

Journal • P3 data • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

A Systematic Literature Review (SLR) of Health State Utility Values (HSUV) in Metastatic Castration-Resistant Prostate Cancer (MCRPC) (ISPOR 2023) - "Therapies included novel hormone therapy, chemotherapy (docetaxel, cabazitaxel, mitoxantrone, estramustine), anti-androgen therapy (bicalutamide), and immunotherapy (sipuleucel-T). HSUVs trended towards lower values with progressing lines of therapy. As novel treatments for mCRPC have emerged in the past decade, this study provides a comprehensive synthesis of current HSUV evidence in adults with mCRPC receiving 1L and later-line therapy. Limitations include hampered comparability between studies due to heterogeneity in study designs (e.g., measuring, quantifying, and reporting HSUVs) and treatments assessed."

Metastases • Review • Genito-urinary Cancer • Oncology • Palliative care • Prostate Cancer • Solid Tumor

Assessment of polyphenolic secondary metabolites and small molecules against the xenobiotic metabolic and cell cycle regulatory proteins in prostate cancer (AACR 2023) - "Cyproterone acetate, Flutamide, and Bicalutamide are prominent medications that induce acute and long-term toxicity and create drug resistance in patients and remission...Additionally, we have performed molecular simulation at 100ns and furthermore, we will perform cytotoxicity analysis. Diosmetin (58.72), Lapatinib Ditosylate (121.61), and Estramustine Phosphate Sodium (143.38) has the highest binding affinity for CDKN2 (4EK3), CYP17A1(3RUK), and CYP19A1(3S79), respectively, and are stable throughout 100ns simulation studies... As a result of our findings, these four Flavonoids may be viable candidates for additional research into PCa prevention or management.Keywords: Diosmetin, Lapatinib Ditosylatye, Prostate cancer, In-silico, Simulation"

Genito-urinary Cancer • Lung Cancer • Oncology • Prostate Cancer • Solid Tumor • CDKN2A • CYP17A1 • CYP19A1

Activity and safety of KEES - an oral multi-drug chemo-hormonal metronomic combination regimen in metastatic castration-resistant prostate cancer. (PubMed, BMC Cancer) - "KEES demonstrated meaningful efficacy in heavily pre-treated CRPC patients, especially those with PS 0-1 and lower baseline ALP, and had an acceptable toxicity profile."

Journal • Metastases • Retrospective data • Cardiovascular • Fatigue • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor • AR

Theranostic inorganic-organic hybrid nanoparticles with a cocktail of chemotherapeutic and cytostatic drugs. (PubMed, J Mater Chem B) - "Theranostic inorganic-organic hybrid nanoparticles (IOH-NPs) with a cocktail of chemotherapeutic and cytostatic drugs and a composition Gd[(PMX)(EMP)], [Gd(OH)][(PMX)(AlPCS)], or [Gd(OH)][(PMX)(TPPS)] (PMX: pemetrexed, EMP: estramustine phosphate, AlPCS: aluminum(III) chlorido phthalocyanine tetrasulfonate, TPPS: tetraphenylporphine sulfonate) are presented for the first time. The synergistic anti-cancer effect of the IOH-NPs with a chemotherapeutic cocktail is shown in a murine breast-cancer cell line (pH8N8) and a human pancreatic cancer cell line (AsPC1), whereas the synergistic cytotoxic and phototoxic efficacy is verified in response to illumination of HeLa-GFP cancer cells, MTT assays with human colon cancer cells (HCT116), and normal human dermal fibroblasts (NHDF). HepG2 spheroids as 3D cell cultures prove the effective uptake of the IOH-NPs with high uniform distribution and the release of the chemotherapeutic drugs with the strong synergistic effect of the..."

Journal • Breast Cancer • Colon Cancer • Colorectal Cancer • Gastrointestinal Cancer • Hepatology • Oncology • Pancreatic Cancer • Solid Tumor

Hormone Therapy With or Without Docetaxel And Estramustine in Treating Patients With Prostate Cancer That is Locally Advanced or At High Risk of Relapse (clinicaltrials.gov) - P3 | N=413 | Completed | Sponsor: UNICANCER | Active, not recruiting ➔ Completed

Metastases • Trial completion • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Androgen receptor axis-targeted agents are not superior to conventional hormonal therapy for treatment of metastatic prostate cancer. (PubMed, Oncol Lett) - "However, there was some clinical benefit when ARAT agents were used after patients developed castration-resistant prostate cancer. These findings suggest that up-front therapy using ARAT agents at the time of the initial hormone therapy can impart clinical benefit in Japanese patients with metastatic prostate cancer."

Journal • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Significance of pelvic lymph node dissection during radical prostatectomy in high-risk prostate cancer patients receiving neoadjuvant chemohormonal therapy. (PubMed, Sci Rep) - "We retrospectively analyzed 516 patients with high-risk localized PC (< cT4N0M0) who received neoadjuvant androgen-deprivation therapy plus estramustine phosphate followed by RP between January 2010 and March 2020...The inverse probability of treatment weighting-Cox analysis revealed limited PLND had no significant impact on BCR-FS (hazard ratio, 1.44; P = 0.469). Limited PLND during RP after neoadjuvant chemohormonal therapy showed quite low rate of positive nodes, higher rate of complications, and no significant impact on BCR-FS."

Journal • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Efficacy of Combination Chemotherapy With Docetaxel, Estramustine and Carboplatin in Men With Castration-resistant Prostate Cancer. (PubMed, Cancer Diagn Progn) - "Median overall survival was 11 months, prostate-specific antigen progression-free survival was 6.5 months, and radiographic progression-free survival was 7 months. Docetaxel and carboplatin with oral estramustine shows efficacy against castration-resistant prostate cancer."

Journal • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Seawater fungi-derived compound screening to identify novel small molecules against dengue virus NS5 methyltransferase and NS2B/NS3 protease. (PubMed, Inform Med Unlocked) - "Both licensed medications, estramustine (DB01196) and quinestrol (DB04575), were found to be similar to Chevalone E, with prediction scores of 0.818 and 0.856, respectively. In addition, cholic acid (DB02659), acitretin (DB00459), and mupirocin (DB00410) are similar to Sterolic acid, zidovudine (DB00495), imipenem (DB01598), and nadolol (DB01203) are similar to Brocazine A, and budesonide (DB01222) and colchicine (DB01394) are related to Brevione K. These findings suggest that these could be feasible dengue virus treatment options, meaning that more research is needed."

Journal • Dengue Fever • Infectious Disease • Novel Coronavirus Disease

Hormone Therapy With or Without Docetaxel And Estramustine in Treating Patients With Prostate Cancer That is Locally Advanced or At High Risk of Relapse (clinicaltrials.gov) - P3 | N=413 | Active, not recruiting | Sponsor: UNICANCER | Trial completion date: Dec 2021 ➔ Dec 2022

Trial completion date • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor