1977495-97-8

Product Details:

CasNo： 1977495-97-8

Molecular Formula： C24H31ClN8O

Appearance： Light yellow to yellow powder

Packing： Aluminium bag

Throughput： 100KG/Month

Purity： 99%

1. Chemical Information

• IUPAC Name: 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 dihydrochlorideDailyMed
• Molecular Formula: \(\boldsymbol{C_{24}H_{30}N_8O \cdot 2HCl}\)
• Molecular Weight: 519.48 g/mol (free base: 446.56 g/mol)DailyMed
• Appearance: Yellow, slightly hygroscopic crystalline powder; water-solubleFDA Access...
• Category: Small-molecule, selective, reversible, short-acting CDK4/6 inhibitor; first-in-class myeloprotective agent先声药业

2. Product Brief (API Version — for your chemical export sheet)

Trilaciclib dihydrochloride is a transient cyclin-dependent kinase 4/6 (CDK4/6) inhibitor. It temporarily arrests hematopoietic stem and progenitor cells (HSPCs) in the G1 phase of the cell cycle before chemotherapy, shielding bone marrow from cytotoxic damage while preserving the anti-tumour activity of chemotherapy regimens. It is indicated to reduce the incidence of chemotherapy-induced myelosuppression (CIM) in adult patients with extensive-stage small cell lung cancer (ES-SCLC) receiving platinum/etoposide or topotecan-based chemotherapy. It is administered by intravenous infusion within 4 hours prior to each chemotherapy dose.COSELA®

3. Formulated Drug (Finished Injectable, COSELA®)

For injection: sterile, preservative‑free yellow lyophilized cake in single‑use vial. Each vial contains trilaciclib dihydrochloride equivalent to 300 mg trilaciclib base. Excipients: citric acid monohydrate, mannitol; HCl / NaOH for pH adjustment. Recommended dose: \(\boldsymbol{240\ mg/m^2}\), infused intravenously over 30 minutes before chemotherapy.G1 Therape...

4. Mechanism of Action

CDK4 and CDK6 drive G1/S transition in proliferating cells. By reversible CDK4/6 inhibition, trilaciclib halts division of bone marrow hematopoietic progenitor cells transiently. Since SCLC tumour cells are largely independent of CDK4/6 signalling, the cytotoxic effect of chemotherapy on cancer cells remains intact. After chemotherapy exposure, bone marrow cells resume normal proliferation.先声药业

5. Key Clinical Summary

• Indication: Reduction of chemotherapy‑induced myelosuppression in extensive‑stage SCLC
• Approval: US FDA Feb 2021 (Breakthrough Therapy designation); NMPA approved in China (Simcere / G1 Therapeutics collaboration)先声药业
• Common adverse events: fatigue, hypocalcaemia, hypokalaemia, hypophosphataemia, elevated hepatic transaminases, headache
• Main benefits: lowers risk of severe neutropenia, reduces neutropenia duration, decreases transfusion requirements, helps maintain planned chemo dosing scheduleCOSELA®