trilaciclib

China [CN]

I. Basic Information

Item | Details

English Name | (4R)-6-amino-4-(4-(cyclopentylamino)-2-methoxyphenyl)-3,4-dihydro-2H-chromen-2-one

Chinese Name | (4R)-6-amino-4-(4-(cyclopentylamino)-2-methoxyphenyl)-3,4-dihydro-2H-chromen-2-one (Trilaciclib)

CAS Number | 1374743-00-6

Molecular Formula | C₂₄H₃₀N₈O

Molecular Weight | 446.55

Target | CDK4 (IC₅₀=1 nM), CDK6 (IC₅₀=4 nM)

R&D / Market Launch | Developed by G1 Therapeutics, approved by the FDA in 2021, approved in China in 2022

Dosage Form and Specifications | Powder for injection: 300 mg/vial (single-use vial)

II. Physicochemical Properties

Parameter | Data

Appearance | White to off-white crystalline powder

Solubility | Slightly soluble in water, slightly soluble in DMSO, readily soluble in methanol

Dissociation Constant (pKa) | 9.2 (amino group), 7.8 (lactam) (predicted value)

Stability | Stable for 3 years when stored sealed and dry at 2-8℃; stable for 24 hours at 2-8℃ after dissolution, stable for 8 hours at room temperature

Chiral Characteristics | Single R configuration, optical purity >99.5%

Partition Coefficient (logP) | 4.5 (neutral pH, predicted value)

III. Mechanism of Action (Core Advantages)

Short-acting CDK4/6 inhibition: Reversibly inhibits CDK4/6, causing hematopoietic stem/progenitor cells (HSPCs) to temporarily arrest in the G1 phase, avoiding the killing effect of chemotherapy drugs on dividing cells, and protecting bone marrow hematopoietic function.

Full-spectrum bone marrow protection: Simultaneously protects neutrophil, erythrocyte, and platelet production, reducing the risk of multi-lineage myelosuppression and reducing the need for supportive treatments such as G-CSF and blood transfusions (COSELA®). Does not affect chemotherapy efficacy: It only acts on HSPCs, does not inhibit tumor cell CDK4/6, and does not reduce the cytotoxic activity of chemotherapy against tumors (NCBI).

Convenient intravenous administration: Administered 30 minutes before chemotherapy, completed in a single 30-minute infusion, does not affect the chemotherapy process, and has high patient compliance.