Trilaciclib

Cosela / Trilaciclib;

FDA approved Indication is chemotherapy-induced myelosuppression: To decrease the incidence of chemotherapy-induced myelosuppression when administered prior to a platinum/etoposide-containing regimen or topotecan-containing regimen for extensive-stage small cell lung cancer (ES-SCLC) in adults.

Chemotherapy-induced myelosuppression: IV: 240 mg/m2/dose; administered prior to a platinum/etoposide- or topotecan-based regimen for extended-stage small cell lung cancer (Hart 2021; Weiss 2019). Trilaciclib infusion should be completed within 4 hours prior to the start of chemotherapy; administer trilaciclib on each day chemotherapy is administered.

Trilaciclib is a highly potent, selective, and reversible cyclin-dependent kinase 4 and 6 (CDK4/6) inhibitor (Weiss 2019). Hematopoietic stem and progenitor cell (HSPC) proliferation is dependent on CDK4/6 activity. Through CDK4/6 inhibition, trilaciclib transiently induces HSPC G1 cell cycle arrest, preventing the cells from proliferating in the presence of cytotoxic chemotherapy and thus resulting in myelopreservation (Hart 2021).

Cosela / 曲拉西尼

FDA批准的适应症 -- 化疗引起的骨髓抑制。适应症限于小细胞肺癌扩展期（ES-SCLC），只有在给予含铂/依托泊苷方案或含拓扑替康方案之前给药，减少化疗引起的骨髓抑制的发生（Hart 2021；Weiss 2019）。

静脉注射：240 mg/m2/dose；在注射铂/依托泊苷//拓扑替康之前给药。Trilaciclib输液应在化疗开始前4小时内完成；在进行化疗的每一天都要注射Trilaciclib。

Trilaciclib是一种选择性的高效可逆细胞周期蛋白依赖激酶4和6（CDK4/6）抑制剂（Weiss 2019）。造血干细胞和祖细胞（HSPC）的增殖依赖于CDK4/6的活性。通过CDK4/6抑制，trilaciclib可暂时诱导HSPC G1细胞周期停滞，防止细胞在有细胞毒性化疗时增殖，从而导致骨髓保存（Hart 2021）。