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Also known as: 1374743-00-6, G1t28, Cosela, Trilaciclib [usan], U6072do9xg, 2'-((5-(4-methylpiperazin-1-yl)pyridin-2-yl)amino)-7',8'-dihydro-6'h-spiro[cyclohexane-1,9'-pyrazino[1',2':1,5]pyrrolo[2,3-d]pyrimidin]-6'-one

Molecular Formula

C₂₄H₃₀N₈O

Molecular Weight

446.5 g/mol

InChI Key

PDGKHKMBHVFCMG-UHFFFAOYSA-N

FDA UNII

U6072DO9XG

Trilaciclib is a small molecule, competitive inhibitor of cyclin dependent kinases 4 and 6 (CDK4/6), with potential antineoplastic and chemoprotective activities. Upon intravenous administration, trilaciclib binds to and inhibits the activity of CDK4/6, thereby blocking the phosphorylation of the retinoblastoma protein (Rb) in early G1. This prevents G1/S phase transition, causes cell cycle arrest in the G1 phase, induces apoptosis, and inhibits the proliferation of CDK4/6-overexpressing tumor cells. In patients with CDK4/6-independent tumor cells, G1T28 may protect against multi-lineage chemotherapy-induced myelosuppression (CIM) by transiently and reversibly inducing G1 cell cycle arrest in hematopoietic stem and progenitor cells (HSPCs) and preventing transition to the S phase. This protects all hematopoietic lineages, including red blood cells, platelets, neutrophils and lymphocytes, from the DNA-damaging effects of certain chemotherapeutics and preserves the function of the bone marrow and the immune system. CDKs are serine/threonine kinases involved in the regulation of the cell cycle and may be overexpressed in certain cancer cell types. HSPCs are dependent upon CDK4/6 for proliferation.

Trilaciclib is a Kinase Inhibitor. The mechanism of action of trilaciclib is as a Cyclin-dependent Kinase 4 Inhibitor, and Cyclin-dependent Kinase 6 Inhibitor, and Organic Cation Transporter 2 Inhibitor, and Multidrug and Toxin Extrusion Transporter 1 Inhibitor, and Multidrug and Toxin Extrusion Transporter 2 K Inhibitor.

1 2D Structure

Trilaciclib

2 Identification

2.1 Computed Descriptors

2.1.1 IUPAC Name

4-[[5-(4-methylpiperazin-1-yl)pyridin-2-yl]amino]spiro[1,3,5,11-tetrazatricyclo[7.4.0.02,7]trideca-2,4,6,8-tetraene-13,1'-cyclohexane]-10-one

2.1.2 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)

2.1.3 InChI Key

PDGKHKMBHVFCMG-UHFFFAOYSA-N

2.1.4 Canonical SMILES

CN1CCN(CC1)C2=CN=C(C=C2)NC3=NC=C4C=C5C(=O)NCC6(N5C4=N3)CCCCC6

2.2 Other Identifiers

2.2.1 UNII

U6072DO9XG

2.3 Synonyms

2.3.1 MeSH Synonyms

1. 2'-((5-(4-methyl-1-piperazinyl)-2-pyridinyl)amino)-7',8'-dihydro-6'h-spiro(cyclohexane-1,9'-pyrazino(1',2':1,5)pyrrolo(2,3-d)pyrimidin)-6'-one

2. Cosela

3. Spiro(cyclohexane-1,9'(6'h)-pyrazino(1',2':1,5)pyrrolo(2,3-d)pyrimidin)-6'-one, 7',8'-dihydro-2'-((5-(4-methyl-1-piperazinyl)-2-pyridinyl)amino)-

2.3.2 Depositor-Supplied Synonyms

1. 1374743-00-6

2. G1t28

3. Cosela

4. Trilaciclib [usan]

5. U6072do9xg

6. 2'-((5-(4-methylpiperazin-1-yl)pyridin-2-yl)amino)-7',8'-dihydro-6'h-spiro[cyclohexane-1,9'-pyrazino[1',2':1,5]pyrrolo[2,3-d]pyrimidin]-6'-one

7. Spiro(cyclohexane-1,9'(6'h)-pyrazino(1',2':1,5)pyrrolo(2,3-d)pyrimidin)-6'-one, 7',8'-dihydro-2'-((5-(4-methyl-1-piperazinyl)-2-pyridinyl)amino)-

8. 2'-((5-(4-methylpiperazin-1-yl)pyridin-2-yl)amino)-7',8'-dihydro-6'h-spiro(cyclohexane-1,9'-pyrazino(1',2':1,5)pyrrolo(2,3-d)pyrimidin)-6'-one

9. G1t28(trilaciclib)

10. G1t28 Di-hcl

11. Trilaciclib [inn]

12. Trilaciclib (usan/inn)

13. Unii-u6072do9xg

14. Trilaciclib [who-dd]

15. Gtpl9626

16. Chembl3894860

17. Schembl10082028

18. Bdbm253928

19. Dtxsid601337125

20. Bcp25013

21. Ex-a4297

22. Nsc816987

23. Db15442

24. Nsc-816987

25. Sb19783

26. Ac-36547

27. Us9464092, T

28. Hy-101467

29. Cs-0021431

30. A17084

31. D11130

32. 2'-((5-(4-methyl-1-piperazinyl)-2-pyridinyl)amino)-7',8'-dihydro-6'h-spiro(cyclohexane-1,9'-pyrazino(1',2':1,5)pyrrolo(2,3-d)pyrimidin)-6'-one

33. 2'-((5-(4-methylpiperazin-1-yl)pyridin-2-yl)amino)-7',8'-dihydro-6'hspiro(cyclohexane-1,9'-pyrazino(1',2':1,5)pyrrolo(2,3-d)pyrimidin)-6'-one

34. 2-[[5-(4-methylpiperazin-1-yl)pyridin-2-yl]amino]spiro[7,8-dihydropyrazino[5,6]pyrrolo[1,2-d]pyrimidine-9,1'-cyclohexane]-6-one

35. 4-[[5-(4-methylpiperazin-1-yl)pyridin-2-yl]amino]spiro[1,3,5,11-tetrazatricyclo[7.4.0.02,7]trideca-2,4,6,8-tetraene-13,1'-cyclohexane]-10-one

2.4 Create Date

2012-11-30

3 Chemical and Physical Properties

Molecular Formula	C₂₄H₃₀N₈O
Molecular Weight	446.5 g/mol
XLogP3	2.6
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	7
Rotatable Bond Count	3
Exact Mass	446.25425761 g/mol
Monoisotopic Mass	446.25425761 g/mol
Topological Polar Surface Area	91.2 Å²
Heavy Atom Count	33
Formal Charge	0
Complexity	707
Isotope Atom Count	0
Defined Atom Stereocenter Count	0
Undefined Atom Stereocenter Count	0
Defined Bond Stereocenter Count	0
Undefined Bond Stereocenter Count	0
Covalently Bonded Unit Count	1

4 Drug and Medication Information

4.1 Drug Indication

5 Pharmacology and Biochemistry

5.1 Pharmacology

Trilaciclib is indicated to reduce the incidence of chemotherapy induced myelosuppression in patients prior to receiving platinum and etoposide-containing or topotecan-containing chemotherapy regimens for extensive-stage small cell lung cancer. It has a short duration of action of approximately 16 hours, and a narrow therapeutic index. Patients should be counselled regarding the risk of injection site reactions, hypersensitivity, and interstitial lung disease.

5.2 FDA Pharmacological Classification

5.2.1 Active Moiety

TRILACICLIB

5.2.2 FDA UNII

U6072DO9XG

5.2.3 Pharmacological Classes

Mechanisms of Action [MoA] - Multidrug and Toxin Extrusion Transporter 2 K Inhibitors

5.3 ATC Code

V - Various

V03 - All other therapeutic products

V03A - All other therapeutic products

V03AF - Detoxifying agents for antineoplastic treatment

V03AF12 - Trilaciclib

5.4 Absorption, Distribution and Excretion

Absorption

C_max and AUC of trilaciclib increase proportionally with dose.

Route of Elimination

79.1% of a radiolabelled dose is recovered in the feces, 7% as the unchanged parent compound. 14% of a radiolabelled dose is recovered in the urine, 2% as the unchanged parent compound.

Volume of Distribution

The volume of distribution of trilaciclib at steady state is 1130 L.

Clearance

The clearance of trilaciclib is 158 L/h.

5.5 Metabolism/Metabolites

Data regarding the metabolism of trilaciclib are not readily available, however it is expected to be extensively metabolised.

5.6 Biological Half-Life

The mean terminal half life of trilaciblib is approximately 14 h.

5.7 Mechanism of Action

Trilaciclib is inhibits cyclin-dependant kinase 4 (CDK4) at a concentration of 1 nmol/L and cyclin-dependent kinase 5 (CDK5) at 4 nmol/L. Inhibition of CDK2, CDK5, and CDK7 is over 1000-fold less at these concentrations and inhibition of CDK9 is 50-fold less. CDK4 and CDK5 are expressed in hematopoietic stem cells and progenitor cells. They are capable of phosphorylating and inactivating the retinoblastoma protien; a tumor suppressor. When trilaciclib is given to patients with retinoblastoma protein-null small cell lung cancer, it does not interfere with the intended chemotherapy induced cytotoxicity of cancer cells. Inhibition of CDK4 and CDK5 leads to a reversible pause in the cell cycle in the G1 phase for approximately 16 hours. The temporary cell cycle arrest prevents chemotherapy induced DNA damage in healthy cells, reducing the activity of caspases 3 and 7, which reduces apoptosis of healthy cells. Other studies have shown inhibitors of CDK4 and CDK6 enhance T-cell activation, upregulating major histocompatibility complex (MHC) class I and II, and stabilize programmed death-ligand 1 (PD-L1). Together these activities increase T-cell activity, increase antigen presentation, and sensitize cells to immune checkpoint inhibitors.

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