trilaciclib   Click here for help

GtoPdb Ligand ID: 9626

Synonyms: G1T28
Immunopharmacology Ligand
Compound class: Synthetic organic
Comment: Trilaciclib (G1T28) is an investigational short-acting CDK4/6 inhibitor being developed by G1 Therapeutics [2].
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 8
Hydrogen bond donors 2
Rotatable bonds 3
Topological polar surface area 91.21
Molecular weight 446.25
XLogP 3.65
No. Lipinski's rules broken 0
SMILES / InChI / InChIKey
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Canonical SMILES CN1CCN(CC1)c1ccc(nc1)Nc1ncc2c(n1)n1c(c2)C(=O)NCC21CCCCC2
Isomeric SMILES CN1CCN(CC1)c1ccc(nc1)Nc1ncc2c(n1)n1c(c2)C(=O)NCC21CCCCC2
InChI InChI=1S/C24H30N8O/c1-30-9-11-31(12-10-30)18-5-6-20(25-15-18)28-23-26-14-17-13-19-22(33)27-16-24(7-3-2-4-8-24)32(19)21(17)29-23/h5-6,13-15H,2-4,7-12,16H2,1H3,(H,27,33)(H,25,26,28,29)
InChI Key PDGKHKMBHVFCMG-UHFFFAOYSA-N
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Summary of Clinical Use Click here for help
Pre-chemotherapy intravenous administration of G1T28 is being evaluated in a number of Phase 2 clinical trials, in patients with advanced solid tumours- small cell lung cancer (NCT03041311) and triple-negative breast cancer (NCT02978716).
Mechanism Of Action and Pharmacodynamic Effects Click here for help
G1T28 represents a novel strategy for targeting CDK4/6-independent tumours. By transiently inhibiting CDK4/6 in normal hematopoietic stem cells, and thereby protecting them from chemotherapy-induced exhaustion, it is predicted that this strategy will deliver better outcomes for cancer patients receiving chemotherapy (i.e. reduced chemotherapy-induced myelosuppression) [1].
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT02978716 Trilaciclib (G1T28), a CDK 4/6 Inhibitor, in Combination With Gemcitabine and Carboplatin in Metastatic Triple Negative Breast Cancer (mTNBC) Phase 2 Interventional G1 Therapeutics, Inc.
NCT03041311 Carboplatin, Etoposide, and Atezolizumab With or Without Trilaciclib (G1T28), a CDK 4/6 Inhibitor, in Extensive Stage Small Cell Lung Cancer (SCLC) Phase 2 Interventional G1 Therapeutics, Inc.