Trilaciclib

Kinase Inhibitor — VARIOUS

Key facts

Trilaciclib is an onp drug in the Kinase Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 2021. Its mechanism of action is classified as Cyclin-dependent Kinase 4 Inhibitors, Cyclin-dependent Kinase 6 Inhibitors and Multidrug and Toxin Extrusion Transporter 1 Inhibitors. DrugCentral lists 10 molecular targets, including NEK10, NUAK2 and FLT3. Recorded indications include Chemotherapy-induced myelosuppression and Extensive-stage small cell lung cancer.

• Approval status: onp (first approved 2021 by the FDA).
• Drug class: Kinase Inhibitor.
• Mechanism of action: Cyclin-dependent Kinase 4 Inhibitors; Cyclin-dependent Kinase 6 Inhibitors; Multidrug and Toxin Extrusion Transporter 1 Inhibitors.
• Molecular targets: NEK10, NUAK2, FLT3 and CDK4 (10 listed in DrugCentral).
• Indications: Chemotherapy-induced myelosuppression and Extensive-stage small cell lung cancer.
• ATC code: V03AF12 (Detoxifying agents for antineoplastic treatment).
• Molecular formula: C24H30N8O; molecular weight 446.56 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (2)

• Chemotherapy-induced myelosuppression
• Extensive-stage small cell lung cancer

Mechanism & targets

• Mechanism of action (MoA): Cyclin-dependent Kinase 4 Inhibitors; Cyclin-dependent Kinase 6 Inhibitors; Multidrug and Toxin Extrusion Transporter 1 Inhibitors; Multidrug and Toxin Extrusion Transporter 2 K Inhibitors; Organic Cation Transporter 2 Inhibitors
• Established pharmacologic class: Kinase Inhibitor

Molecular targets (10)

Target	Gene	Action	Activity
Serine/threonine-protein kinase Nek10	NEK10	inhibitor	Kd 9.57
NUAK family SNF1-like kinase 2	NUAK2	inhibitor	Kd 9.15
Receptor-type tyrosine-protein kinase FLT3	FLT3	inhibitor	Kd 9.15
Cyclin-dependent kinase 4	CDK4	inhibitor	IC50 9.00
Cyclin-dependent kinase 6	CDK6	inhibitor	IC50 8.40
Cyclin-dependent kinase 9	CDK9	inhibitor	IC50 7.30
Cyclin-dependent-like kinase 5	CDK5	inhibitor	IC50 5.83
Cyclin-dependent kinase 2	CDK2	inhibitor	IC50 5.72
Cyclin-dependent kinase 1	CDK1	inhibitor	IC50 5.53
Cyclin-dependent kinase 7	CDK7	inhibitor	IC50 5.33

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
2021-02-12	FDA	—	G1 THERAPEUTICS Inc

ATC classification

ATC code	Therapeutic hierarchy
V03AF12	VARIOUS › ALL OTHER THERAPEUTIC PRODUCTS › ALL OTHER THERAPEUTIC PRODUCTS › Detoxifying agents for antineoplastic treatment

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Myelosuppression	61.1

Chemical structure

• Molecular formula: C₂₄H₃₀N₈O
• Molecular weight: 446.56 g/mol
• CAS number: —
• InChIKey: PDGKHKMBHVFCMG-UHFFFAOYSA-N
• PubChem CID: 68029831

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

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Trilaciclib used for?

DrugCentral lists the following indications for Trilaciclib: Chemotherapy-induced myelosuppression and Extensive-stage small cell lung cancer.

How does Trilaciclib work?

Trilaciclib is classified as Cyclin-dependent Kinase 4 Inhibitors, Cyclin-dependent Kinase 6 Inhibitors and Multidrug and Toxin Extrusion Transporter 1 Inhibitors; its molecular targets in DrugCentral include NEK10 (inhibitor), NUAK2 (inhibitor), FLT3 (inhibitor) and CDK4 (inhibitor).

When was Trilaciclib first approved?

Trilaciclib was first approved by the FDA in 2021.

What drug class does Trilaciclib belong to?

Trilaciclib is in the Kinase Inhibitor class.

What is the chemical formula of Trilaciclib?

Trilaciclib has the molecular formula C24H30N8O and a molecular weight of 446.56 g/mol.

Sources

• DrugCentral drug card 5442 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL3894860 — compound record and bioactivity
• PubChem CID 68029831 — chemical identifiers
• DrugBank DB15442 — drug record
• FDA UNII U6072DO9XG — substance identity
• DailyMed: FDA labels for Trilaciclib — current prescribing information (label search)
• UniProt Q6ZWH5 (NEK10) — target protein
• UniProt Q9H093 (NUAK2) — target protein
• UniProt P36888 (FLT3) — target protein
• UniProt P11802 (CDK4) — target protein
• UniProt Q00534 (CDK6) — target protein
• UniProt P50750 (CDK9) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.