Tomivosertib
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This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.
Explore a selection of our essential drug information below, or:
Identification
- Generic Name
- Tomivosertib
- DrugBank Accession Number
- DB15219
- Background
Tomivosertib is under investigation in clinical trial NCT03318562 (A PD Study of Oral eFT508 in Subjects With Advanced TNBC and HCC).
- Type
- Small Molecule
- Groups
- Investigational
- Structure
- Weight
- Average: 340.387
Monoisotopic: 340.164773908 - Chemical Formula
- C17H20N6O2
- Synonyms
- 6'-((6-Amino-4-pyrimidinyl)amino)-8'-methyl-2'H-spiro(cyclohexane-1,3'-imidazo(1,5-a)pyridine)-1',5'-dione
- Tomivosertib
- External IDs
- EFT-508
- EFT508
Pharmacology
- Indication
Not Available
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- Pharmacodynamics
Not Available
- Mechanism of action
Target Actions Organism AMAP kinase-interacting serine/threonine-protein kinase 1 inhibitorHumans AMAP kinase-interacting serine/threonine-protein kinase 2 inhibitorHumans - Absorption
Not Available
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
- Not Available
- Route of elimination
Not Available
- Half-life
Not Available
- Clearance
Not Available
- Adverse Effects
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- Toxicity
Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.Not Available
- Food Interactions
- Not Available
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Product Ingredients
Ingredient UNII CAS InChI Key Tomivosertib hydrochloride BW3S40K2UM 1849590-02-8 Not applicable
Categories
- Drug Categories
- Not Available
- Classification
- Not classified
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- U2H19X4WBV
- CAS number
- 1849590-01-7
- InChI Key
- HKTBYUWLRDZAJK-UHFFFAOYSA-N
- InChI
- InChI=1S/C17H20N6O2/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)
- IUPAC Name
- 6'-[(6-aminopyrimidin-4-yl)amino]-8'-methyl-2',5'-dihydro-1'H-spiro[cyclohexane-1,3'-imidazo[1,5-a]pyridine]-1',5'-dione
- SMILES
- CC1=C2N(C(=O)C(NC3=CC(N)=NC=N3)=C1)C1(CCCCC1)NC2=O
References
- General References
- Not Available
- External Links
- ChemSpider
- 57617704
- BindingDB
- 50263263
- ChEMBL
- CHEMBL4073443
- ZINC
- ZINC000575623807
- PDBe Ligand
- N45
- PDB Entries
- 6ck6
Clinical Trials
- Clinical Trials
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Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
- Not Available
- Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Not Available
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 0.527 mg/mL ALOGPS logP 0.53 ALOGPS logP 0.82 Chemaxon logS -2.8 ALOGPS pKa (Strongest Acidic) 10.84 Chemaxon pKa (Strongest Basic) 6.35 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 6 Chemaxon Hydrogen Donor Count 3 Chemaxon Polar Surface Area 113.24 Å2 Chemaxon Rotatable Bond Count 2 Chemaxon Refractivity 97.64 m3·mol-1 Chemaxon Polarizability 35.86 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-0006-0019000000-adde320b502352766f12 Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-000i-0009000000-de67e631602519c3c48e Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-0006-1029000000-d6738225b482a0611697 Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-052r-0029000000-de5e8f7df2fd853ca112 Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-03k9-0095000000-20cdb5f3c887e9746a02 Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-0ab9-2689000000-42521fb13a76cb11f84f Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- May play a role in the response to environmental stress and cytokines. Appears to regulate translation by phosphorylating EIF4E, thus increasing the affinity of this protein for the 7-methylguanosine-containing mRNA cap
- Specific Function
- ATP binding
- Gene Name
- MKNK1
- Uniprot ID
- Q9BUB5
- Uniprot Name
- MAP kinase-interacting serine/threonine-protein kinase 1
- Molecular Weight
- 51341.91 Da
References
- Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F: TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Serine/threonine-protein kinase that phosphorylates SFPQ/PSF, HNRNPA1 and EIF4E. May play a role in the response to environmental stress and cytokines. Appears to regulate translation by phosphorylating EIF4E, thus increasing the affinity of this protein for the 7-methylguanosine-containing mRNA cap. Required for mediating PP2A-inhibition-induced EIF4E phosphorylation. Triggers EIF4E shuttling from cytoplasm to nucleus. Isoform 1 displays a high basal kinase activity, but isoform 2 exhibits a very low kinase activity. Acts as a mediator of the suppressive effects of IFNgamma on hematopoiesis. Negative regulator for signals that control generation of arsenic trioxide As(2)O(3)-dependent apoptosis and anti-leukemic responses. Involved in anti-apoptotic signaling in response to serum withdrawal
- Specific Function
- ATP binding
- Gene Name
- MKNK2
- Uniprot ID
- Q9HBH9
- Uniprot Name
- MAP kinase-interacting serine/threonine-protein kinase 2
- Molecular Weight
- 51874.4 Da
References
- Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F: TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751. [Article]
Drug created at May 20, 2019 15:01 / Updated at August 27, 2024 19:16