tinengotinib   Click here for help

GtoPdb Ligand ID: 11887

Synonyms: Example 6 [US10889586B2] | TT-00420 | TT00420
PDB Ligand
Compound class: Synthetic organic
Comment: The chemical structure for tinengotinib was revealed in WHO proposed INN list 126 (Jan 2022), in which it was described as a tyrosine kinase inhibitor and antineoplastic agent. The SMILES provided a match to TransThera Sciences' clinical lead TT-00420 via PubChem. TT-00420 appears to be an orally administered multi‐kinase inhibitor that targets cell proliferation, angiogenesis, and immune-oncology, through inhibition of Aurora kinases A/B and Janus kinases (involved in cytokine signalling) and receptor tyrosine kinases such as FGFRs and VEGFRs (which play roles in proliferation and angiogenesis) [1].
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 5
Hydrogen bond donors 2
Rotatable bonds 2
Topological polar surface area 82.72
Molecular weight 394.13
XLogP 5.43
No. Lipinski's rules broken 1
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Canonical SMILES Clc1ccccc1c1nc2c(C)n[nH]c2[nH]c2c1cnc(c2)N1CCOCC1
Isomeric SMILES Clc1c(cccc1)c1c2c([nH]c3c(n1)c(n[nH]3)C)cc(nc2)N1CCOCC1
InChI InChI=1S/C20H19ClN6O/c1-12-18-20(26-25-12)23-16-10-17(27-6-8-28-9-7-27)22-11-14(16)19(24-18)13-4-2-3-5-15(13)21/h2-5,10-11H,6-9H2,1H3,(H2,23,25,26)
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Summary of Clinical Use Click here for help
TT-00420 has been advanced to clinical trials in patients with various advanced solid tumours. It was granted FDA Fast Track designation in November 2021.
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT04705922 Relative Bioavailability Study and Food Effect Study of TT-00420 Capsule and Tablet Formulations in Healthy Volunteers Phase 1 Interventional TransThera Sciences (Nanjing), Inc.
NCT03654547 Safety of TT-00420 Monotherapy in Patients With Advanced Solid Tumors and Triple Negative Breast Cancer Phase 1 Interventional TransThera Sciences (Nanjing), Inc.
NCT04919642 Study to Evaluate the Efficacy and Safety of TT-00420 in Cholangiocarcinoma Phase 2 Interventional TransThera Sciences (Nanjing), Inc.
NCT04742959 Study of TT-00420 Tablet as Monotherapy and Combination Therapy in Patients With Advanced Solid Tumors Phase 1/Phase 2 Interventional TransThera Sciences (Nanjing), Inc.