trilaciclib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
cyclin dependant kinase inhibitors 5442 1374743-00-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • trilaciclib
  • trilaciclib dihydrochloride
  • cosela
  • G1T28
  • G1T28-1
  • GB3RG-28-1
Trilaciclib is a transient inhibitor of CDK 4 and 6. Hematopoietic stem and progenitor cells (HSPCs) in the bone marrow give rise to circulating neutrophils, RBCs, and platelets. HSPC proliferation is dependent on CDK4/6 activity.
  • Molecular weight: 446.56
  • Formula: C24H30N8O
  • CLOGP: 3.78
  • LIPINSKI: 0
  • HAC: 9
  • HDO: 2
  • TPSA: 91.21
  • ALOGS: -3.23
  • ROTB: 3
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Feb. 12, 2021 FDA G1 THERAPEUTICS Inc

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC V03AF12 VARIOUS
ALL OTHER THERAPEUTIC PRODUCTS
ALL OTHER THERAPEUTIC PRODUCTS
Detoxifying agents for antineoplastic treatment
FDA EPC N0000175605 Kinase Inhibitor
FDA MoA N0000187061 Organic Cation Transporter 2 Inhibitors
FDA MoA N0000191423 Multidrug and Toxin Extrusion Transporter 1 Inhibitors
FDA MoA N0000193921 Cyclin-dependent Kinase 4 Inhibitors
FDA MoA N0000193922 Cyclin-dependent Kinase 6 Inhibitors
FDA MoA N0000193932 Multidrug and Toxin Extrusion Transporter 2 K Inhibitors

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Chemotherapy-induced myelosuppression indication 370569000
Extensive-stage small cell lung cancer indication 458321000124102




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 300MG BASE/VIAL COSELA G1 THERAP N214200 Feb. 12, 2021 RX POWDER INTRAVENOUS 10085992 March 14, 2034 A METHOD TO DECREASE THE INCIDENCE OF CHEMOTHERAPY-INDUCED MYELOSUPPRESSION IN ADULT PATIENTS WHEN ADMINISTERED PRIOR TO A CARBOPLATIN AND ETOPOSIDE-CONTAINING REGIMEN FOR EXTENSIVE-STAGE SMALL CELL LUNG CANCER
EQ 300MG BASE/VIAL COSELA G1 THERAP N214200 Feb. 12, 2021 RX POWDER INTRAVENOUS 10966984 March 14, 2034 A METHOD TO DECREASE THE INCIDENCE OF CHEMOTHERAPY-INDUCED MYELOSUPPRESSION IN ADULT PATIENTS WHEN ADMINISTERED PRIOR TO A PLATINUM/ETOPOSIDE-CONTAINING REGIMEN FOR EXTENSIVE-STAGE SMALL CELL LUNG CANCER
EQ 300MG BASE/VIAL COSELA G1 THERAP N214200 Feb. 12, 2021 RX POWDER INTRAVENOUS 10966984 March 14, 2034 A METHOD TO DECREASE THE INCIDENCE OF CHEMOTHERAPY-INDUCED MYELOSUPPRESSION IN ADULT PATIENTS WHEN ADMINISTERED PRIOR TO A TOPOTECAN-CONTAINING REGIMEN FOR EXTENSIVE- STAGE SMALL CELL LUNG CANCER
EQ 300MG BASE/VIAL COSELA G1 THERAP N214200 Feb. 12, 2021 RX POWDER INTRAVENOUS 9487530 March 14, 2034 A METHOD TO DECREASE THE INCIDENCE OF CHEMOTHERAPY-INDUCED MYELOSUPPRESSION IN ADULT PATIENTS WHEN ADMINISTERED PRIOR TO A PLATINUM/ETOPOSIDE-CONTAINING REGIMEN FOR EXTENSIVE-STAGE SMALL CELL LUNG CANCER
EQ 300MG BASE/VIAL COSELA G1 THERAP N214200 Feb. 12, 2021 RX POWDER INTRAVENOUS 9487530 March 14, 2034 A METHOD TO DECREASE THE INCIDENCE OF CHEMOTHERAPY-INDUCED MYELOSUPPRESSION IN ADULT PATIENTS WHEN ADMINISTERED PRIOR TO A TOPOTECAN-CONTAINING REGIMEN FOR EXTENSIVE- STAGE SMALL CELL LUNG CANCER
EQ 300MG BASE/VIAL COSELA G1 THERAP N214200 Feb. 12, 2021 RX POWDER INTRAVENOUS 11529352 July 23, 2039 A METHOD TO DECREASE THE INCIDENCE OF CHEMOTHERAPY-INDUCED MYELOSUPPRESSION IN ADULT PATIENTS WHEN ADMINISTERED PRIOR TO A PLATINUM/ETOPOSIDE-CONTAINING REGIMEN THAT INCLUDES AN IMMUNE CHECKPOINT INHIBITOR FOR EXTENSIVE-STAGE SMALL CELL CANCER

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 300MG BASE/VIAL COSELA G1 THERAP N214200 Feb. 12, 2021 RX POWDER INTRAVENOUS Feb. 12, 2026 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Cyclin-dependent kinase 6 Kinase INHIBITOR IC50 8.40 DRUG LABEL DRUG LABEL
Cyclin-dependent kinase 4 Kinase INHIBITOR IC50 9 DRUG LABEL DRUG LABEL
Cyclin-dependent kinase 2 Kinase INHIBITOR IC50 5.72 DRUG LABEL
Cyclin-dependent-like kinase 5 Kinase INHIBITOR IC50 5.83 DRUG LABEL
Cyclin-dependent kinase 9 Kinase INHIBITOR IC50 7.30 DRUG LABEL
Receptor-type tyrosine-protein kinase FLT3 Kinase INHIBITOR Kd 9.15 DRUG LABEL
NUAK family SNF1-like kinase 2 Kinase INHIBITOR Kd 9.15 DRUG LABEL
Serine/threonine-protein kinase Nek10 Kinase INHIBITOR Kd 9.57 DRUG LABEL
Cyclin-dependent kinase 7 Kinase INHIBITOR IC50 5.33 DRUG LABEL
Cyclin-dependent kinase 1 Kinase INHIBITOR IC50 5.53 DRUG LABEL

External reference:

IDSource
D11130 KEGG_DRUG
U6072DO9XG UNII
1977495-97-8 SECONDARY_CAS_RN
C4524320 UMLSCUI
CHEMBL3894860 ChEMBL_ID
68029831 PUBCHEM_CID
DB15442 DRUGBANK_ID
CHEMBL4650272 ChEMBL_ID
9626 IUPHAR_LIGAND_ID
018637 NDDF
018638 NDDF
1149152001 SNOMEDCT_US
1149273007 SNOMEDCT_US
1149274001 SNOMEDCT_US
4040108 VANDF
2479690 RXNORM
343885 MMSL
39327 MMSL
d09715 MMSL
C000708352 MESH_SUPPLEMENTAL_RECORD_UI
10565 INN_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Cosela HUMAN PRESCRIPTION DRUG LABEL 1 73462-101 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 300 mg INTRAVENOUS NDA 26 sections
Cosela HUMAN PRESCRIPTION DRUG LABEL 1 73462-101 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 300 mg INTRAVENOUS NDA 26 sections