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trilaciclib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| cyclin dependant kinase inhibitors | 5442 | 1374743-00-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 2.472 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 3.499 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 17.179 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 10 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 30.290 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 55.730 | % | High | 1 |
| herg | hERG pIC50 | 4.777 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 3.041 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 31.046 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 30.530 | % | High | 1 |
| kinase-safety-class | AAK1,ABL1,ABL2,ACVR2A,ACVR2B,ACVRL1,AKT3,ALK,AURKA,AURKB,AURKC,AXL,BLK,BMX,BRAF,BTK,CAMK2A,CAMK2B,CAMK2D,CAMK2G,CDK1,CDK14,CDK16,CDK19,CDK2,CDK3,CDK4,CDK5,CDK6,CDK7,CDK8,CDK9,CHEK1,CHEK2,CHUK,CLK1,CLK2,CLK4,CSF1R,CSK,CSNK1G2,CSNK2A2,DDR1,DYRK1A,DYRK1B,DYRK2,DYRK3,EGFR,EIF2AK3,EPHA2,EPHB1,EPHB4,ERBB2,ERBB4,FGFR1,FGFR4,FLT1,FLT3,FLT4,FYN,GAK,GRK1,GRK2,GSK3A,GSK3B,HASPIN,HIPK2,IGF1R,IKBKB,INSR,INSRR,IRAK1,IRAK3,IRAK4,ITK,JAK1,JAK2,JAK3,KDR,KIT,LCK,LRRK2,LYN,MAP2K1,MAP2K4,MAP2K6,MAP3K1,MAP3K10,MAP3K11,MAP3K14,MAP3K19,MAP3K2,MAP3K21,MAP3K3,MAP3K7,MAP3K9,MAP4K1,MAP4K2,MAP4K3,MAP4K5,MAPK1,MAPK10,MAPK15,MAPK3,MAPK7,MAPK8,MAPK9,MARK1,MARK2,MARK3,MARK4,MELK,MET,MINK1,MKNK1,MKNK2,MST1R,MTOR,MYLK,NTRK1,NTRK2,NTRK3,NUAK1,PAK1,PAK2,PAK4,PAK5,PDGFRB,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CD,PIK3CG,PIM1,PIM2,PIM3,PLK1,PLK2,PLK3,PLK4,PRKAA1,PRKAA2,PRKACA,PRKCA,PRKCD,PRKCI,PRKCZ,PRKD1,PRKDC,PTK2,RET,RIPK3,ROCK1,ROCK2,RPS6KA1,SGK1,SIK2,SIK3,SRC,STK10,STK16,STK17A,STK3,STK33,STK4,SYK,TBK1,TEK,TGFBR1,TNIK,TNK1,TTK,TYRO3,UHMK1,ULK1,ULK2,YES1,ZAP70 | 180 | |||
| kinase-selectivity-class | AAK1,ABL2,ACVR2B,ALK,AURKB,AURKC,AXL,BLK,BMX,BRAF,CAMK2A,CAMK2B,CAMK2D,CDK1,CDK16,CDK3,CDK4,CDK6,CDK7,CDK9,CHEK1,CLK2,CLK4,CSF1R,DDR1,DYRK1B,DYRK3,EGFR,EIF2AK3,EPHA2,EPHB4,ERBB2,FGFR1,FLT1,FLT3,FYN,GAK,GSK3B,HIPK2,IGF1R,INSR,IRAK1,IRAK3,IRAK4,JAK1,JAK2,JAK3,KDR,KIT,LCK,LRRK2,LYN,MAP2K1,MAP3K10,MAP3K11,MAP3K14,MAP3K21,MAP3K7,MAP3K9,MAP4K1,MAP4K3,MAP4K5,MAPK1,MAPK7,MARK1,MARK2,MARK3,MARK4,MELK,MET,MINK1,MKNK2,MST1R,NTRK1,NUAK1,PAK1,PAK4,PDGFRB,PDK1,PDK4,PIM3,PLK2,PLK3,PLK4,PRKAA1,PRKAA2,PRKCD,PTK2,RET,RIPK3,SIK2,SIK3,SRC,STK16,STK33,STK4,SYK,TNIK,TNK1,TTK,TYRO3,ULK1,ULK2,YES1 | 104 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 16.331 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 26.669 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 21.990 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 24.210 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 36.370 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 14.521 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 61.800 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 18.050 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 15.066 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| 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:
| Source | Code | Description |
|---|---|---|
| ATC | V03AF12 | VARIOUS ALL OTHER THERAPEUTIC PRODUCTS ALL OTHER THERAPEUTIC PRODUCTS Detoxifying agents for antineoplastic treatment |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D047428 | Protein Kinase Inhibitors |
| 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 |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
Related Drugs by ATC class:
V03AF Detoxifying agents for antineoplastic treatment 10 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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 strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| EQ 300MG BASE/VIAL | COSELA | PHARMACOSMOS | 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 | PHARMACOSMOS | 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 | PHARMACOSMOS | 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 | PHARMACOSMOS | N214200 | Feb. 12, 2021 | RX | POWDER | INTRAVENOUS | 11717523 | March 14, 2034 | A METHOD FOR REDUCING 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 | PHARMACOSMOS | N214200 | Feb. 12, 2021 | RX | POWDER | INTRAVENOUS | 11717523 | March 14, 2034 | A METHOD FOR REDUCING 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 | PHARMACOSMOS | 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 | PHARMACOSMOS | 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 | PHARMACOSMOS | N214200 | Feb. 12, 2021 | RX | POWDER | INTRAVENOUS | 12527798 | Dec. 5, 2037 | 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 LUNG CANCER |
| EQ 300MG BASE/VIAL | COSELA | PHARMACOSMOS | 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 LUNG CANCER |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| EQ 300MG BASE/VIAL | COSELA | PHARMACOSMOS | N214200 | Feb. 12, 2021 | RX | POWDER | INTRAVENOUS | Feb. 12, 2026 | NEW CHEMICAL ENTITY |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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:
| ID | Source |
|---|---|
| D11130 | KEGG_DRUG |
| U6072DO9XG | UNII |
| 1977495-97-8 | SECONDARY_CAS_RN |
| C4524320 | UMLSCUI |
| CHEBI:231087 | CHEBI |
| CHEMBL3894860 | ChEMBL_ID |
| 68029831 | PUBCHEM_CID |
| DB15442 | DRUGBANK_ID |
| CHEMBL4650272 | ChEMBL_ID |
| 10565 | INN_ID |
| C000708352 | MESH_SUPPLEMENTAL_RECORD_UI |
| 9626 | IUPHAR_LIGAND_ID |
| 1149152001 | SNOMEDCT_US |
| 1149273007 | SNOMEDCT_US |
| 1149274001 | SNOMEDCT_US |
| 4040108 | VANDF |
| 343885 | MMSL |
| 39327 | MMSL |
| d09715 | MMSL |
| 018637 | NDDF |
| 018638 | NDDF |
| 2479690 | RXNORM |
| U6072DO9XG | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| 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 | 73594-0101 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 300 mg | INTRAVENOUS | NDA | 28 sections |