tomivosertib

a selective translation regulator and is part of a new class of cancer treatments known as immunotherapies that are designed to harness the body’s own immune system in fighting cancer. eFT508 is a highly potent and selective, oral inhibitor of MNK1 and MNK2 (MNK1/2).

Also Known As:

6'-((6-Amino-4-pyrimidinyl)amino)-8'-methyl-2'H-spiro(cyclohexane-1,3'-imidazo(1,5-a)pyridine)-1',5'-dione; eFT508; spiro(cyclohexane-1,3'(2'H)-imidazo(1,5-a)pyridine)-1',5'-dione, 6'-((6-amino-4-pyrimidinyl)amino)-8'-methyl-

Networked: 16 relevant articles (3 outcomes, 6 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Heterocyclic Compounds: 198
- 1-Ring Heterocyclic Compounds
  - Pyrimidines: 510
    - tomivosertib: 16
  - Pyridines: 88
    - tomivosertib: 16

Experts

1.	Webster, Kevin R: 3 articles (01/2021 - 01/2019)
2.	Dussor, Gregory: 3 articles (01/2020 - 01/2019)
3.	Sonenberg, Nahum: 2 articles (01/2021 - 01/2019)
4.	Moy, Jamie K: 2 articles (01/2020 - 01/2019)
5.	Pradhan, Grishma: 2 articles (01/2020 - 01/2019)
6.	Price, Theodore J: 2 articles (01/2020 - 01/2019)
7.	Guo, Geyang: 1 article (08/2022)
8.	Liu, Zhenyang: 1 article (08/2022)
9.	Yang, Xiaolin: 1 article (08/2022)
10.	Yin, Xianli: 1 article (08/2022)

Related Diseases

1.	Neoplasms (Cancer) 09/11/2023 - "Notably, eFT508 is currently being investigated in clinical trials for cancer treatment, and our findings may prompt the initiation of clinical trials using eFT508 in radioresistant NPC patients." 01/01/2023 - "Consistent with in vitro findings, eFT508 at non-toxic dose significantly arrested tumor growth in mice throughout the whole duration of treatment. " 01/01/2019 - "We show that this mechanism of PD-L1 translational upregulation was effectively targeted by a potent, clinical compound that inhibits eIF4E phosphorylation, eFT508, which reverses the aggressive and metastatic characteristics of MYCTg;KRASG12D tumors. " 07/05/2021 - "Currently, three inhibitors (BAY1143269, eFT508 and ETC-206) are in various stages of clinical trials for the treatment of solid cancers or leukemia, either alone or combined with inhibitors of other protein kinase. " 08/01/2023 - "Mechanistically, tomivosertib acted on glioblastoma via suppressing MNK-dependent eIF4E phosphorylation and activation in tumor and endothelial cells. "
2.	Neuralgia (Stump Neuralgia) 01/01/2019 - "Our work strongly suggests that MNK1-eIF4E signaling drives CIPN and that a drug in human clinical trials, eFT508, may be a new therapeutic for neuropathic pain." 01/01/2020 - "Reversal of peripheral nerve injury-induced neuropathic pain and cognitive dysfunction via genetic and tomivosertib targeting of MNK." 06/14/2023 - "MNK inhibitor eFT508 (Tomivosertib) suppresses ectopic activity in human dorsal root ganglion neurons from dermatomes with radicular neuropathic pain." 01/01/2020 - "Our results illustrate new testing paradigms for determining preclinical neuropathic pain efficacy and point to the MNK inhibitor tomivosertib (eFT508) as an important drug candidate for neuropathic pain treatment."
3.	Osteosarcoma (Osteogenic Sarcoma) 01/01/2023 - "Our findings highlight the therapeutic value of MNK1/2 inhibition and suggest eFT508 as a promising candidate for the treatment of osteosarcoma." 01/01/2023 - "EFT508 is active against multiple osteosarcoma cell lines via inhibiting growth, survival and migration. " 01/01/2023 - "This study evaluated the efficacy of eFT508, a highly selective inhibitor of MNK1/2, as single drug alone and in combination with paclitaxel in preclinical models of osteosarcoma. " 01/01/2023 - "Combination index shows that eFT508 and paclitaxel is synergistic in osteosarcoma cells. " 01/01/2023 - "MAPK-interacting kinases inhibition by eFT508 overcomes chemoresistance in preclinical model of osteosarcoma."
4.	Stomach Neoplasms (Stomach Cancer) 08/01/2022 - "Rescue studies confirm that tomivosertib inhibits gastric cancer via targeting MNK- eIF4E-β-catenin. " 08/01/2022 - "We firstly demonstrate that tomivosertib displays higher efficacy than other MNK inhibitors in inhibiting gastric cancer cells. " 08/01/2022 - "Our study provides preclinical evidence to initialize clinical trials for gastric cancer using tomivosertib in combination with chemotherapy." 08/01/2022 - "Our work reveals that tomivosertib, a potent and highly selective dual MNK1/2 inhibitor, preferentially sensitizes gastric cancer to chemotherapy via suppressing MNK-eIF4E-β-catenin. " 08/01/2022 - "In addition, tomivosertib significantly augments the inhibitory effects of 5-FU and paclitaxel but not everolimus, suggesting that tomivosertib preferentially sensitizes gastric cancer to chemotherapy. "
5.	Leukemia 07/05/2021 - "Currently, three inhibitors (BAY1143269, eFT508 and ETC-206) are in various stages of clinical trials for the treatment of solid cancers or leukemia, either alone or combined with inhibitors of other protein kinase. "

Related Drugs and Biologics

1.	tomivosertib
2.	Paclitaxel (Taxol)
3.	Interleukin-6 (Interleukin 6)
4.	Protein Kinases (Protein Kinase)
5.	Eukaryotic Initiation Factor-4E
6.	Phosphotransferases (Kinase)
7.	Brain-Derived Neurotrophic Factor (BDNF)
8.	Anthracyclines
9.	Proteins (Proteins, Gene)
10.	Fluorouracil (Carac)

Related Therapies and Procedures

1.	Drug Therapy (Chemotherapy)
2.	Immunotherapy
3.	Duration of Therapy