Details
Stereochemistry | ACHIRAL |
Molecular Formula | C17H20N6O2.ClH |
Molecular Weight | 376.841 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.CC1=C2N(C(=O)C(NC3=NC=NC(N)=C3)=C1)C4(CCCCC4)NC2=O
InChI
InChIKey=WBGPPUUXCGKTSC-UHFFFAOYSA-N
InChI=1S/C17H20N6O2.ClH/c1-10-7-11(21-13-8-12(18)19-9-20-13)16(25)23-14(10)15(24)22-17(23)5-3-2-4-6-17;/h7-9H,2-6H2,1H3,(H,22,24)(H3,18,19,20,21);1H
Tomivosertib (eFT-508) is a dual inhibitor of MAP kinase-interacting kinases (MNK1 and MNK2) thereby controlling translation. It has potent in vivo antitumor activity in models of diffuse large cell B-cell lymphoma and solid tumors. Tomivosertib acts on multiple points in the cancer immunity cycle simultaneously, underscoring its therapeutic potential as both a monotherapy and in combination with existing checkpoint inhibitor treatments. Preclinical studies suggest combining tomivosertib with a checkpoint inhibitor can overcome mechanisms of resistance to checkpoint inhibitors, resulting in enhanced sensitivity to checkpoint inhibitors and a higher response rate. In addition, preclinical data demonstrate that tomivosertib as a single agent promotes antitumor immunity that persists after stopping drug treatment. Tomivosertib is currently being evaluated in Phase 2 clinical trials in solid tumors and lymphoma. Additionally, tomivosertib may be a new therapeutic for neuropathic pain.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: Q9BUB5 Gene ID: 8569.0 Gene Symbol: MKNK1 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/29526098 |
2.4 nM [IC50] | ||
Target ID: Q9HBH9 Gene ID: 2872.0 Gene Symbol: MKNK2 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/29526098 |
2.4 nM [IC50] |
PubMed
Title | Date | PubMed |
---|---|---|
Mitogen-activated Protein Kinase (MAPK) Interacting Kinases 1 and 2 (MNK1 and MNK2) as Targets for Cancer Therapy: Recent Progress in the Development of MNK Inhibitors. | 2017 |
|
Structure-based Design of Pyridone-Aminal eFT508 Targeting Dysregulated Translation by Selective Mitogen-activated Protein Kinase Interacting Kinases 1 and 2 (MNK1/2) Inhibition. | 2018 Apr 26 |
|
Nociceptor Translational Profiling Reveals the Ragulator-Rag GTPase Complex as a Critical Generator of Neuropathic Pain. | 2019 Jan 16 |
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1849590-02-8
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C171899
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118598855
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BW3S40K2UM
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300000011146
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FG-109
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ACTIVE MOIETY
SUBSTANCE RECORD