Rytelo (imetelstat)

To treat low- to intermediate-1 risk myelodysplastic syndromes Drug Trials Snapshot

FDA Approval: 6/6/2024

Research Synopsis

  • * Recent findings indicate that imetelstat can help reduce minimal residual disease (MRD), allowing patients to take treatment breaks, contributing to improved quality of life.
  • * In AML studies, imetelstat has shown efficacy in reducing cancer cells in specific genetic subtypes, especially when combined with other chemotherapy agents, enhancing treatment outcomes.
  • * Rytelo's action against telomerase, an enzyme that aids many cancers in survival, is central to its mechanism, highlighting its innovative approach in cancer treatment.
  • * Research has indicated that imetelstat may induce ferroptosis, a form of regulated cell death, suggesting a novel therapeutic pathway for aggressive blood cancers like AML.
  • * Experts note that current therapies for myelofibrosis-related anemia are often ineffective, but imetelstat is among the new therapeutic options showing promise for better results.
  • * The drug is part of a broader trend in hematologic oncology, focusing on targeted therapies capable of lasting disease control and lessening the need for constant medication.
  • * Clinical trials continue to explore imetelstat's efficacy, safety, and pharmacokinetics, with ongoing interest in how it might be integrated with existing cancer treatment regimens.
  • * Overall, the sentiment around Rytelo (imetelstat) is cautiously optimistic, as researchers regard it as a potential game-changer in the landscape of therapeutic options for difficult-to-treat hematologic malignancies.
  • * The accumulation of positive early data emphasizes the need for continued research to solidify imetelstat's role in comprehensive cancer treatment strategies.

Related articles

Research articles about Rytelo (imetelstat)

Rytelo (imetelstat)

Developing strategies to reduce the duration of therapy for patients with myeloproliferative neoplasms.

London, UK

2 hours ago

1 Received

  • Myeloproliferative neoplasms (MPN) are diseases that need ongoing treatment, but stem cell transplants (ASCT) might help some patients stop treatment for a while.
  • Researchers are finding new medicines that can reduce small amounts of disease (MRD) so patients might be able to take breaks from their treatments.
  • Some treatments, like busulfan and the experimental drug Imetelstat, show promise in helping patients live longer and potentially go without constant medication.

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$100 - $150

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Treatment of anemia in myelofibrosis: focusing on novel therapeutic options.

London, UK

2 hours ago

1 Received

  • Myelofibrosis is a disease where the body makes too many stem cells, leading to issues like anemia and enlarged organs.
  • This review talks about new treatments for anemia in myelofibrosis, including different types of medicine that help fight the disease.
  • Experts say that current treatments don't work very well and can be harmful, but new drugs are showing better results and can help patients improve.

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Medical treatment of gastrointestinal stromal tumors: state of the art and future perspectives.

London, UK

2 hours ago

1 Received

  • Imatinib mesylate (STI-571) is a key treatment that targets the KIT enzyme, significantly improving outcomes for patients with metastatic GIST but can lead to resistance over time due to mutations.
  • New strategies, including the use of additional drugs like mTOR inhibitors and other KIT inhibitors, are being explored to overcome this resistance and enhance treatment effectiveness.

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AMG 706, an oral, multikinase inhibitor that selectively targets vascular endothelial growth factor, platelet-derived growth factor, and kit receptors, potently inhibits angiogenesis and induces regression in tumor xenografts.

London, UK

2 hours ago

1 Received

  • * AMG 706 is a new small-molecule inhibitor that effectively targets multiple VEGF receptors and other related receptors, showing promise in both preclinical models and clinical trials.
  • * In various experiments, AMG 706 has demonstrated the ability to inhibit tumor growth and promote endothelial cell death while being well-tolerated in test subjects, indicating its potential as a treatment for cancer.

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Beyond imatinib: second generation c-KIT inhibitors for the management of gastrointestinal stromal tumors.

London, UK

2 hours ago

1 Received

  • * Metastatic GISTs that don't respond to imatinib pose significant treatment challenges, prompting research into new therapies, including sunitinib and other investigational TKIs like AMG 706 and AMN 107.
  • * Ongoing trials are exploring a variety of other drugs, including RAD001 and IPI-540, to improve outcomes for patients who do not respond to standard imatinib therapy, indicating a future shift in how GISTs will

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Vascular endothelial growth factor receptor tyrosine kinase inhibitors in non-small cell lung cancer: a review of recent clinical trials.

London, UK

2 hours ago

1 Received

  • * Angiogenesis is crucial for the growth and spread of NSCLC tumors, making the vascular endothelial growth factor (VEGF) pathway a key therapeutic target that has been validated through various early clinical trials.
  • * Early trial data indicates that using angiogenesis inhibitors alongside standard chemotherapy may enhance their effectiveness, but the best combination with minimal side effects is still to be discovered.

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Multitarget tyrosine kinase inhibition: [and the winner is...].

London, UK

2 hours ago

1 Received

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Safety, pharmacokinetics, and efficacy of AMG 706, an oral multikinase inhibitor, in patients with advanced solid tumors.

London, UK

2 hours ago

1 Received

  • - AMG 706 is a new oral drug being tested for its ability to inhibit certain growth factor receptors in patients with advanced solid tumors who have not responded to other treatments.
  • - In a phase I study, 71 patients received varying doses of AMG 706, with the maximum-tolerated dose identified as 125 mg daily; side effects included fatigue, diarrhea, nausea, and hypertension.
  • - The results indicated that while some patients had a partial response or stable disease, AMG 706 was generally well tolerated, paving the way for further research as a standalone treatment or in combination with other therapies.

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Double resistance to imatinib and AMG 706 caused by multiple acquired KIT exon 17 mutations in a gastrointestinal stromal tumour.

London, UK

2 hours ago

1 Received

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[Gastrointestinal stromal tumors: molecular aspects and therapeutic implications].

London, UK

2 hours ago

1 Received

  • - Approximately 90% of gastrointestinal tumors (GISTs) have mutations in the KIT or PDGFR alpha oncogene, which make them sensitive to the drug imatinib, leading to an 80% progression-free survival rate over six months in advanced cases.
  • - Most patients on imatinib eventually develop resistance due to secondary mutations, particularly in those with primary exon 11 mutations.
  • - Sunitinib is another treatment option that can benefit about 25% of imatinib-resistant or intolerant patients, indicating that understanding resistance mechanisms could lead to personalized therapies for GISTs in the future.

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Early clinical studies of novel therapies for thyroid cancers.

London, UK

2 hours ago

1 Received

  • Systemic therapies for advanced thyroid cancers have historically been ineffective, but recent advancements are changing that.
  • Increased understanding of thyroid cancer biology and new targeted therapies have led to significant research and clinical trials in this area.
  • The article discusses major studies that highlight these new treatment approaches and their success.

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Motesanib diphosphate in progressive differentiated thyroid cancer.

London, UK

2 hours ago

1 Received

  • The study evaluates motesanib diphosphate, a new oral drug that inhibits VEGF receptors, in 93 patients with aggressive, radioiodine-resistant differentiated thyroid cancer.
  • Results showed a 14% objective response rate, with 67% achieving stable disease for at least 24 weeks and a median progression-free survival of 40 weeks.
  • Common side effects included diarrhea, hypertension, fatigue, and weight loss, but 81% of patients exhibited decreased serum thyroglobulin levels, suggesting some effectiveness of the treatment.

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[Tumor vasculature as a therapeutic target in non-small cell lung cancer].

London, UK

2 hours ago

1 Received

  • - Despite advancements in traditional treatments, non-small cell lung cancer (NSCLC) patients still have a low survival rate, highlighting the need for new therapies.
  • - Bevacizumab, an anti-VEGF antibody, is currently the most developed antiangiogenic drug for NSCLC, but there are significant questions about its effectiveness and future use.
  • - New drug classes, including vascular disrupting agents and multi-tyrosine kinase inhibitors, are showing promising results in recent studies, warranting further exploration in combination with existing treatments.

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Effect of coadministration of ketoconazole, a strong CYP3A4 inhibitor, on pharmacokinetics and tolerability of motesanib diphosphate (AMG 706) in patients with advanced solid tumors.

London, UK

2 hours ago

1 Received

  • Motesanib diphosphate is a new drug that inhibits angiogenesis by targeting specific receptors and was tested for drug interactions with ketoconazole, a strong inhibitor of the liver enzyme cytochrome P450 3A4.* -
  • In a phase 1b study, 14 patients with advanced solid tumors received escalating doses of motesanib diphosphate while some were also given ketoconazole; the results indicated that ketoconazole increased motesanib’s exposure in the body significantly.* -
  • The treatment was generally well-tolerated, with common mild to moderate side effects including fatigue and hypertension, and no severe adverse events were reported during the study.*

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Safety and pharmacokinetics of motesanib in combination with gemcitabine for the treatment of patients with solid tumours.

London, UK

2 hours ago

1 Received

  • The study investigated the safety and pharmacokinetics of motesanib combined with gemcitabine in patients with advanced solid tumors, aiming to identify any dose-limiting toxicities (DLTs).
  • A total of 26 patients participated, with no DLTs reported, though 62% experienced adverse effects, primarily lethargy, diarrhea, and fatigue.
  • The combination treatment was well tolerated, and while the overall objective response rate was low at 4%, 27% of patients maintained stable disease during the study.

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Motesanib diphosphate in progressive differentiated thyroid cancer.

London, UK

2 hours ago

1 Received

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Broad antitumor activity in breast cancer xenografts by motesanib, a highly selective, oral inhibitor of vascular endothelial growth factor, platelet-derived growth factor, and Kit receptors.

London, UK

2 hours ago

1 Received

  • Angiogenesis is crucial for breast cancer growth, and VEGF is a key factor regulating blood vessel formation; this study explores the effects of motesanib, a new oral inhibitor targeting multiple growth factor receptors.
  • In experiments, mice with different breast cancer tumor types were treated with varying doses of motesanib, alone or alongside chemotherapy drugs like docetaxel, doxorubicin, and tamoxifen.
  • Results showed that motesanib significantly reduces tumor growth and blood vessel density, especially when combined with docetaxel or tamoxifen, indicating its potential as an effective treatment for breast cancer.

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3,4-Disubstituted isothiazoles: novel potent inhibitors of VEGF receptors 1 and 2.

London, UK

2 hours ago

1 Received

  • Novel isothiazole derivatives are identified as strong inhibitors of vascular endothelial growth factor receptors VEGFR-1 and VEGFR-2, showing promise in treating diseases related to these pathways.
  • Some of these compounds demonstrate VEGFR-2 inhibitory activity similar to Vatalanib in both enzymatic and cellular tests.
  • Certain derivatives have a 4- to 8-fold preference for inhibiting VEGFR-2 over VEGFR-1 and display good permeability across cell layers, which is essential for drug development.

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Motesanib diphosphate (AMG 706), an oral angiogenesis inhibitor, demonstrates clinical efficacy in advanced thymoma.

London, UK

2 hours ago

1 Received

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