Rineterkib
- Generic Name
- Rineterkib
- Drug Type
- Small Molecule
- Chemical Formula
- C26H27BrF3N5O2
- CAS Number
- 1715025-32-3
- Unique Ingredient Identifier
- 15KFN616FK
- Background
Rineterkib is an inhibitor of extracellular signal-regulated kinase (ERK) being investigated in NCT04097821 (A Randomized, Open-label, Phase I/II Open Platform Study Evaluating Safety and Efficacy of Novel Ruxolitinib Combinations in Myelofibrosis Patients).
Myelofibrosis Treatment Landscape Evolves with Novel Therapies and Combination Strategies
• Emerging therapies like luspatercept, nuvisertib, and pelabresib show promise in addressing myelofibrosis symptoms and anemia, potentially improving patient outcomes.
• Combination strategies, particularly those involving JAK inhibitors with agents like pelabresib or navitoclax, aim to enhance spleen volume reduction and symptom control.
• Research focuses on identifying biomarkers and refining endpoints to better assess disease modification and personalize treatment approaches for myelofibrosis patients.
• Novel agents targeting calreticulin and hemojuvelin, along with advancements in JAK inhibitors, offer potential for more targeted and effective myelofibrosis therapies.
IAG933, a Novel YAP/TAZ-TEAD Inhibitor, Shows Promise in Preclinical Cancer Models
• IAG933 directly disrupts the YAP/TAZ-TEAD protein-protein interaction, leading to YAP eviction from chromatin and reduced Hippo-mediated transcription.
• In preclinical models, IAG933 demonstrates deep tumor regression in Hippo-driven mesothelioma xenografts and shows efficacy in combination with other inhibitors in lung, pancreatic, and colorectal cancer.
• The inhibitor exhibits potent antiproliferative activity in Hippo-dependent cell lines, particularly mesothelioma, and demonstrates a more rapid and profound reduction in cell viability compared to allosteric TEAD inhibitors.
• Clinical evaluation of IAG933 is currently underway, marking a significant step in exploring its potential as a therapeutic agent for various solid tumors.
Drug Development Updates
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