Telaglenastat

This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.

Identification

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Name
Telaglenastat
Accession Number
DB15232
Type
Small Molecule
Groups
Investigational
Description

Telaglenastat is under investigation in clinical trial NCT02071862 (Study of the Glutaminase Inhibitor CB-839 in Solid Tumors).

Structure
Thumb
Synonyms
Not Available
External IDs
CB-839
Categories
UNII
U6CL98GLP4
CAS number
1439399-58-2
Weight
Average: 571.58
Monoisotopic: 571.161343324
Chemical Formula
C26H24F3N7O3S
InChI Key
PRAAPINBUWJLGA-UHFFFAOYSA-N
InChI
InChI=1S/C26H24F3N7O3S/c27-26(28,29)39-20-9-5-6-17(14-20)15-22(37)31-21-12-11-18(33-34-21)7-1-2-10-24-35-36-25(40-24)32-23(38)16-19-8-3-4-13-30-19/h3-6,8-9,11-14H,1-2,7,10,15-16H2,(H,31,34,37)(H,32,36,38)
IUPAC Name
N-[6-(4-{5-[2-(pyridin-2-yl)acetamido]-1,3,4-thiadiazol-2-yl}butyl)pyridazin-3-yl]-2-[3-(trifluoromethoxy)phenyl]acetamide
SMILES
FC(F)(F)OC1=CC(CC(=O)NC2=NN=C(CCCCC3=NN=C(NC(=O)CC4=NC=CC=C4)S3)C=C2)=CC=C1

Pharmacology

Indication
Not Available
Pharmacodynamics
Not Available
Mechanism of action
Not Available
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
Toxicity
Not Available
Affected organisms
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

References

General References
Not Available
External Links
ChemSpider
34959639
BindingDB
109086
ChEMBL
CHEMBL3639788

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1Active Not RecruitingTreatmentFumarate Hydratase (FH)-Deficient Tumors / Lung Cancer Non-Small Cell Cancer (NSCLC) / Mesothelioma / Renal Cell Adenocarcinoma / Succinate Dehydrogenase (SDH)-Deficient Gastrointestinal Stromal Tumors (GIST) / Succinate Dehydrogenase (SDH)-Deficient Non-gastrointestinal Stromal Tumors / Triple-Negative Breast Cancer (TNBC) / Tumors Harboring Amplifications in the cMyc Gene / Tumors Harboring Isocitrate Dehydrogenase-1 (IDH1) and IDH2 Mutations / Tumors, Solid1
1CompletedTreatmentAcute Lymphocytic Leukemia (ALL) / Leukemia Acute Myeloid Leukemia (AML)1
1CompletedTreatmentHealthy Volunteers1
1CompletedTreatmentLymphoma, Large B-Cell, Diffuse (DLBCL) / Multiple Myeloma (MM) / Non-Hodgkin's Lymphoma (NHL) / Other B-cell NHL Subtypes, Including WM / T-cell NHL / Waldenström's Macroglobulinemia (WM)1
1Not Yet RecruitingTreatmentOvarian Cancer / Resistant BRCA Wild-Type Ovarian Cancer1
1RecruitingTreatmentAnaplastic Astrocytoma, IDH-Mutant / Diffuse Astrocytoma, IDH-Mutant / IDH1 Gene Mutation / IDH2 Gene Mutation1
1RecruitingTreatmentRecurrent Plasma Cell Myeloma / Refractory Plasma Cell Myeloma1
1, 2RecruitingTreatmentAcute Myeloid Leukemia With Multilineage Dysplasia / Blasts 20-30 Percent of Bone Marrow Nucleated Cells / Blasts 20-30 Percent of Peripheral Blood White Cells / Chronic Myelomonocytic Leukemia / High Risk Myelodysplastic Syndrome / IPSS Risk Category Intermediate-2 / Myelodysplastic Syndrome / Other Diseases of Blood and Blood-Forming Organs1
1, 2RecruitingTreatmentAdvanced Lung Carcinoma / Advanced Lung Non-Small Cell Carcinoma / EGFR Activating Mutation / EGFR Exon 19 Deletion Mutation / EGFR NP_005219.2:p.L858R / EGFR T790M Mutation Negative / Lung Non-Small Cell Carcinoma / Metastatic Lung Carcinoma / Metastatic Lung Non-Small Cell Carcinoma / Stage IV Lung Cancer AJCC v8 / Stage IVA Lung Cancer AJCC v8 / Stage IVB Lung Cancer AJCC v81
1, 2RecruitingTreatmentCcRCC / Clear Cell Renal Cell Carcinoma / Colorectal Cancers / CRC / RCC / TNBC - Triple-Negative Breast Cancer / Tumors, Solid1
1, 2RecruitingTreatmentCRC / KRAS Gene Mutation / Lung Cancer Non-Small Cell Cancer (NSCLC) / Tumors, Solid1
1, 2RecruitingTreatmentClear Cell Renal Cell Carcinoma / Lung Cancer Non-Small Cell Cancer (NSCLC) / Melanoma1
1, 2RecruitingTreatmentColorectal Cancers / Malignant Neoplasm of Colon / Rectal Carcinoma / Tumors, Solid1
1, 2RecruitingTreatmentColorectal Cancers / Metastatic Colorectal Cancer (MCRC) / RAS Wild Type Colorectal Cancer / Refractory Colorectal Cancer1
2Active Not RecruitingTreatmentAdvanced Renal Cell Carcinoma / Metastatic Renal Cell Carcinoma1
2Active Not RecruitingTreatmentClear Cell Renal Cell Carcinoma1
2Active Not RecruitingTreatmentTNBC - Triple-Negative Breast Cancer / Triple Negative Breast Cancer (TNBC)1
2RecruitingTreatmentAdvanced Malignant Solid Neoplasm / KEAP1 Gene Mutation / Metastatic Malignant Solid Neoplasm / NF1 Gene Mutation / NF1 Mutation Positive Malignant Peripheral Nerve Sheath Tumor / NFE2L2 Gene Mutation / STK11 Gene Mutation / Unresectable Malignant Solid Neoplasm1

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
PropertyValueSource
Water Solubility0.00151 mg/mLALOGPS
logP3.73ALOGPS
logP4.74ChemAxon
logS-5.6ALOGPS
pKa (Strongest Acidic)6.94ChemAxon
pKa (Strongest Basic)4.33ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count8ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area131.88 Å2ChemAxon
Rotatable Bond Count13ChemAxon
Refractivity141.14 m3·mol-1ChemAxon
Polarizability55.53 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Taxonomy

Classification
Not classified

Drug created on May 20, 2019 09:02 / Updated on November 02, 2019 03:31