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Epigenetics-targeted drugs: current paradigms and future challenges.

Epigenetics governs a chromatin state regulatory system through five key mechanisms: DNA modification, histone modification, RNA modification, chromatin remodeling, and non-coding RNA regulation. These mechanisms and their associated enzymes convey genetic information independently of DNA base sequences, playing essential roles in organismal development and homeostasis. Conversely, disruptions in epigenetic landscapes critically influence the pathogenesis of various human diseases. This understanding has laid a robust theoretical groundwork for developing drugs that target epigenetics-modifyin

Oncolytic Virus Therapy in a New Era of Immunotherapy, Enhanced by Combination with Existing Anticancer Therapies: Turn up the Heat!

Oncolytic viral therapy is a promising treatment for cancer, where 'cold' tumour cells can become 'hot' to the host immune system. However, with few FDA approved therapies, development of new strategies for more cancer types has been slow and relatively unsuccessful in recent years, Combination therapy has been successful for other types of cancer treatment, therefore, may be a viable alternative to improve the efficacy of oncolytic viral therapy which may reduce some of the adverse events of currently used monotherapies, oncolytic virus therapy and chemotherapy being mutually complimentary wi

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… Comparing duration of response and duration of clinical benefit between fulvestrant treatment groups in the CONFIRM trial: application of new methodology. Breast Cancer Res Treat. 2013;138:149–55. doi: 10.1007/s10549-012-2395-8. 77. Shen X, Pan D, Gong Q, Gu Z, Luo K. …

Promising Therapeutic Strategies for Hematologic Malignancies: Innovations and Potential.

In this review we explore innovative approaches in the treatment of hematologic cancers by combining various therapeutic modalities. We discuss the synergistic potential of combining inhibitors targeting different cellular pathways with immunotherapies, molecular therapies, and hormonal therapies. Examples include combining PI3K inhibitors with proteasome inhibitors, NF-κB inhibitors with immunotherapy checkpoint inhibitors, and neddylation inhibitors with therapies targeting the tumor microenvironment. Additionally, we discuss the potential use of small molecules and peptide inhibitors in hem

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… Significant safety issues Hu8F4 | AML and CMML | - | Limited efficacy and significant toxicity Ivosidenib and Venetoclax with or without Azacitidine | IDH1-mutated HM | Combination of Ivosidenib and Venetoclax, sometimes with Azacitidine | Safety challenges and unmet therapeutic outcomes Afuresertib and Fulvestrant … | HR+/HER2 BC (with implications for HM) | Combination of Afuresertib and Fulvestrant | Insufficient efficacy in Phase III trials Rilotumumab | GC and HM | - | Safety concerns and lack of efficacy in Phase III trials Bavituximab | NSCLC and HM | - | Lack of efficacy in Phase III trials Selinexor | MM …

Holistic Approach to the Diagnosis and Treatment of Patients with Tumor Metastases to the Spine.

The treatment of neoplastic spine metastases requires multi-faceted assessment and an interdisciplinary approach to patients. The metastases do not show specific symptoms but are often the first confirmation of the presence of a primary tumor in a patient. The diagnostic process includes imaging and invasive procedures, e.g., biopsy. It is essential to qualify the patient for an appropriate treatment using dedicated scales. Decompression of the spinal cord is a critical issue to save or restore neurological function in a patient with spine metastases. Surgical treatment ought to meet three cri

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… However, in the light of the latest knowledge, aromatase inhibitors, which include letrozole, exemestane, anastrozole, and fulvestrant, seem to be the right choice [ 97 ]. Another cancer that frequently metastasizes to the spine is prostate cancer. …

Многоцелевые лекарственные препараты: новые 2025 и послерыночного контроля за безопасностью наркотиков, 2022-2024.

Полифармакология предназначена для развития соединений, действующих по крайней мере на two целевые показатели (многоцелевые лиганды, МТДЛ). В 2025, Европейское агентство по медицине (ЕМА), 38 наркотиков, и 11 из них были MTDL. Большинство из них - антитела-наркотики, биконкретные антитела или ингибиторы киназы, все из которых указаны для лечения опухолей, включая датопотамаб дерукстекан (гормон-позитивный рецептор, HER2-negative Рак молочной железы), тизотумаб ведотин (сокращенная шейная карцинома), линвосельтамб (четвёртая линия лечения множественной миеломы) и эрдафитиниб (сокращенная уротел

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… Inavolisib (Itovebi ® ) L01EM06 enzyme inhibitor (-) p110α (+) degradation of mutated p110α PIK3CA -mutated, estrogen receptor-positive, HER2-negative, locally advanced or metastatic breast cancer, in combination with palbociclib and fulvestrant, following recurrence on or within 12 months of completing … neurofibromatosis type 1, aged ≥ 2 years | [ 39 , 40 ] | 2 | + nq 8. | Inavolisib (Itovebi ® ) | L01EM06 | enzyme inhibitor | (-) p110α (+) degradation of mutated p110α | PIK3CA -mutated, estrogen receptor-positive, HER2-negative, locally advanced or metastatic breast cancer, in combination with palbociclib and fulvestrant …

PROTACs: great opportunities for academia and industry (an update from 2020 to 2021).

PROteolysis TArgeting Chimeras (PROTACs) technology is a new protein-degradation strategy that has emerged in recent years. It uses bifunctional small molecules to induce the ubiquitination and degradation of target proteins through the ubiquitin-proteasome system. PROTACs can not only be used as potential clinical treatments for diseases such as cancer, immune disorders, viral infections, and neurodegenerative diseases, but also provide unique chemical knockdown tools for biological research in a catalytic, reversible, and rapid manner. In 2019, our group published a review article "PROTACs:

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… overexpression of estrogen receptor α(ERα) may lead to ER-positive breast cancer, which accounts for 70% of breast cancer. 63 , 64 Approved endocrine therapies include aromatase inhibitors(AIs) such as Letrozole , selective ER modulators (SERMs) such as Tamoxifen , and selective ER degrader (SERDs) such as Fulvestrant … But the long-term use of SERMs is prone to lead to drug resistance and Fulvestrant is limited by poor solubility and low oral bioavailability. 65 , 66 The emergence of PROTACs provides a new method for the development of drugs targeting ERα. …

Proceedings of International Conference on Cell Death in Cancer and Toxicology. February 20-22, 2018. Guest Editors: Kausar M. Ansari, CSIR-IITR, India and Dhyan Chandra, Roswell Park, USA.

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… Fulvestrant (ICI 182,780) is able to destabilize ER and eventually degrade ER. … The peculiarity of Fulvestrant over other antihormonal agents is that the Fulvestrant induced degradation affects the ligand‐independent functions of ER which are not addressed by Tamoxifen thus making it effective under tamoxifen resistance. …

Mechanism and clinical progression of solid tumors bone marrow metastasis.

The rich blood supply of the bone marrow provides favorable conditions for tumor cell proliferation and growth. In the disease's early stages, circulating tumor cells can escape to the bone marrow and form imperceptible micro metastases. These tumor cells may be reactivated to regain the ability to grow aggressively and eventually develop into visible metastases. Symptomatic bone marrow metastases with abnormal hematopoiesis solid tumor metastases are rare and have poor prognoses. Treatment options are carefully chosen because of the suppression of bone marrow function. In this review, we summ

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… Ribociclib plus fulvestrant for postmenopausal women with hormone receptor-positive, human epidermal growth factor receptor 2-negative advanced breast cancer in the phase III randomized MONALEESA-3 trial: updated overall survival . Ann. …

Treatment-induced bone loss and fractures in cancer patients undergoing hormone ablation therapy: efficacy and safety of denosumab.

Hormone ablation therapy (HALT) for breast or prostate cancer accelerates the development of osteoporosis in both men and women by causing estrogen deficiency, which increases the risk for fracture by promoting bone resorption mediated by osteoclasts. Denosumab, a fully human monoclonal antibody that inhibits osteoclast formation and function, increases bone mass in patients undergoing hormone ablation therapy. In the HALT study of 1,468 men with prostate cancer on androgen-deprivation therapy, denosumab significantly reduced the risk of new vertebral fractures, increased bone mineral density

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… Additional endocrine therapies used in the metastatic setting include megesterol acetate, fulvestrant, and fluoxymesterone. …

Potential Immunotherapy Targets for Liver-Directed Therapies, and the Current Scope of Immunotherapeutics for Liver-Related Malignancies.

Liver cancer, including hepatocellular carcinoma and intrahepatic cholangiocarcinoma, is increasing in incidence and mortality across the globe. An improved understanding of the complex tumor microenvironment has opened many therapeutic doors and led to the development of novel pharmaceuticals targeting cellular signaling pathways or immune checkpoints. These interventions have significantly improved tumor control rates and patient outcomes, both in clinical trials and in real-world practice. Interventional radiologists play an important role in the multidisciplinary team given their expertise

Antimitotic drugs in the treatment of cancer.

Cancer is a complex disease since it is adaptive in such a way that it can promote proliferation and invasion by means of an overactive cell cycle and in turn cellular division which is targeted by antimitotic drugs that are highly validated chemotherapy agents. However, antimitotic drug cytotoxicity to non-tumorigenic cells and multiple cancer resistance developed in response to drugs such as taxanes and vinca alkaloids are obstacles faced in both the clinical and basic research field to date. In this review, the classes of antimitotic compounds, their mechanisms of action and cancer cell res

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… Fulvestrant (ICI182780) is an example of such a compound and shows to be more effective when compared to tamoxifen, the current non-steroidal anti-estrogen compound used as standard hormone treatment for breast cancer [ 75 , 77 ]. …

Sternum Metastases: From Case-Identifying Strategy to Multidisciplinary Management.

We aimed to overview the most recent data on sternal metastases from a multidisciplinary approach (diagnosis strategies, outcome, and histological reports). This narrative review based on a PubMed search (between January 2020 and 22 July 2023) using key words such as "sternal", "manubrium", and "metastasis" within the title and/or abstract only included original papers that specifically addressed secondary sternal spreading of cancer in adults, for a total of 48 original articles (14 studies and 34 single case reports). A prior unpublished case in point is also introduced (percutaneous incisio

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… Concomitant fulvestrant with reirradiation for unresectable locoregional recurrent estrogen receptor positive (ER+) breast cancer: A case report and narrative review Medicine 2020 99 e21344 10.1097/MD.0000000000021344 32791733 PMC7387012 18. Mohamed S. Mazhar K. Osman A. Patel A. Srinivasan L. …

Role of Cannabidiol for Improvement of the Quality of Life in Cancer Patients: Potential and Challenges.

There is currently a growing interest in the use of cannabidiol (CBD) to alleviate the symptoms caused by cancer, including pain, sleep disruption, and anxiety. CBD is often self-administered as an over-the-counter supplement, and patients have reported benefits from its use. However, despite the progress made, the mechanisms underlying CBD's anti-cancer activity remain divergent and unclear. Herein, we provide a comprehensive review of molecular mechanisms to determine convergent anti-cancer actions of CBD from pre-clinical and clinical studies. In vitro studies have begun to elucidate the mo

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… For example, with tamoxifen, CBD exerts an additive cytotoxicity in T-47D cells, whereas a triple combination of CBD, fulvestrant, and palbociclib was the most effective in reducing cell viability in both T-47D and MCF-7 cells [ 57 ]. …

The role of noble bumblebee (Bombus terrestris) queen glycosaminoglycan in aged rat and gene expression profile based on DNA microarray.

IL-1 induces a significant number of metabolic and hematological changes. In experimental animals, IL-1 treatments cause hypotension due to rapid reduction of systemic blood pressure, reduced vascular resistance, increased heart rate and leukocyte aggregations. IL-1 causes endothelial dysfunction, the triggering factor of which may be of a different nature including pathogen infection. This dysfunction, which includes macrophage intervention and increased protein permeability, can be mediated by several factors including cytokines and arachidonic acid products. These effects are caused by the

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… Numerous studies have shown that ESR1 mutations are constitutively active and are resistant to the ER antagonists tamoxifen and fulvestrant ( 75 , 76 ). …

Futibatinib, an Irreversible FGFR1-4 Inhibitor for the Treatment of FGFR-Aberrant Tumors.

Fibroblast growth factor receptors (FGFR) are emerging as an important therapeutic target for patients with advanced, refractory cancers. Most selective FGFR inhibitors under investigation show reversible binding, and their activity is limited by acquired drug resistance. This review summarizes the preclinical and clinical development of futibatinib, an irreversible FGFR1-4 inhibitor. Futibatinib stands out among FGFR inhibitors because of its covalent binding mechanism and low susceptibility to acquired resistance. Preclinical data indicated robust activity of futibatinib against acquired res

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… 2020; April 2028 | NCT04093362 Phase II study in metastatic breast cancer (MBC) | MBC harboring FGFR2 amplifications (cohorts 1-3) | Open label | Futibatinib | ORR or CBR | 168 across cohorts | August 30, 2019; June 30, 2023 | NCT04024436 MBC harboring FGFR1 amplifications (cohort 4) | Futibatinib + fulvestrant …

Molecular imaging in oncology: Common PET/CT radiopharmaceuticals and applications.

PET/CT is a commonly used modality in cancer imaging, as it can help in diagnosis, staging and assessment of treatment response in many cancer types. A better understanding of the tumor microenvironment and identification of multiple selective targets are promoting further investigation into different radiotracers for diagnosis and therapy. In the past few decades many radiopharmaceuticals have emerged for specific oncologic indications providing superior detection rate than some morphologic modalities. The purpose of this review is to provide an update on the most current radiopharmaceuticals

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… Fig. 8 Limitations and pitfalls One of the main limitations is that the sensitivity of FES decreases if there is concomitant treatment with ER down-regulator or modulator such as Fulvestrant or Tamoxifen and patients ideally would need to be off therapy for several weeks prior to the scan. …

Genetic Therapy and Molecular Targeted Therapy in Oncology: Safety, Pharmacovigilance, and Perspectives for Research and Clinical Practice.

The impressive advances in the knowledge of biomarkers and molecular targets has enabled significant progress in drug therapy for crucial diseases such as cancer. Specific areas of pharmacology have contributed to these therapeutic outcomes-mainly targeted therapy, immunomodulatory therapy, and gene therapy. This review focuses on the pharmacological profiles of these therapeutic classes and intends, on the one hand, to provide a systematic definition and, on the other, to highlight some aspects related to pharmacovigilance, namely the monitoring of safety and the identification of potential t

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… Endo) | Recruiting | 3 | •Metastatic breast cancer | •Drug: Pertuzumab •Drug: Trastuzumab •Drug: Capecitabine •Drug: Paclitaxel •Drug: Vinorelbine •Drug: Docetaxel •Drug: Exemestane •Drug: Letrozole •Drug: Anastrozole •Drug: Fulvestrant •Drug: Ribociclib •Drug: Nab-Paclitaxel •Drug: Eribulin •Drug: Leuprorelin …

Safety, tolerability, and pharmacokinetics/pharmacodynamics of JMT103 in patients with bone metastases from solid tumors.

Bone metastases are common complications of solid tumors. The outcome is poor despite major progress in cancer therapies. We describe a multicenter, open-label, phase 1, dose escalation and expansion trial of JMT103, a novel fully humanized receptor activator of nuclear factor kappa-B ligand (RANKL)-targeting monoclonal antibody, in adults with bone metastases from solid tumors. The study assessed the safety, tolerability, and pharmacokinetics/pharmacodynamics of JMT103. Patients received JMT103 at doses of 0.5, 1.0, 2.0, and 3.0 mg/kg every 4 weeks for 3 cycles. Among 59 patients enrolled, 20

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… During the study, 50 patients (84.7%) received concomitant cancer treatments: 36 patients (61.0%) received hormonal therapy with the most common used being fulvestrant, exemestane, anastrozole, letrozole, and tamoxifen; 34 patients (57.6%) received chemotherapy with the most common used being anthracycline …

Next-generation antibody-based therapeutics in cancer: antibody-drug conjugates bispecific antibodies across hematologic malignancies and solid tumors.

The therapeutic paradigm in oncology is undergoing a profound transformation driven by antibody-drug conjugates (ADCs) and bispecific antibodies (bsAbs). This review comprehensively summarizes recent clinical advances of these platforms across both hematologic malignancies and solid tumors. ADCs such as trastuzumab deruxtecan have expanded the concept of targetable HER2 expression, demonstrating meaningful intracranial activity and redefining standards of care in HER2-low breast cancer and beyond. The landscape continues to broaden with novel ADC targets (TROP2, CLDN18.2, B7-H3, HER3) and bisp

Global first-in-class drugs approved in 2023-2024: Breakthroughs and insights.

First-in-class (FIC) drugs are considered the main drivers of new drug discovery and have novel targets and mechanisms. The proportion of FIC drugs among new drugs provides fundamental guidance for both academic and pharmaceutical research. From a global perspective, 81 FIC drugs were approved in 2023 and 2024. Among them, small-molecule drugs account for a greater percentage (51.9%), illustrating the discovery of new chemical entities. Macromolecule drugs (48.1%), which mainly consist of antibody analogs, represent a growing trend as new biotechnology techniques have emerged. In terms of FIC

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… Kinases, as modulators of protein phosphorylation, are involved in many aspects of biological function and disease mechanisms. 123 The first protein kinase B (AKT) kinase inhibitor, 124 AstraZeneca’s capivasertib (Truqap), was approved by the FDA 125 in combination with fulvestrant for adults with hormone …