Novel CDK2/4/6 inhibitor culmerciclib (TQB3616) plus fulvestrant in previously treated, HR-positive, HER2-negative advanced breast cancer: a randomized, double-blind, phase 3 trial

Signal Transduct Target Ther. 2025 Dec 18;10(1):414. doi: 10.1038/s41392-025-02475-6.

Abstract

CDK2 is a principal mediator of CDK4/6 resistance. Concurrent CDK2/4/6 blockade may be effective in treating HR-positive, HER2-negative advanced breast cancer (ABC). This randomized, double-blind, parallel-controlled, phase 3 trial (ClinicalTrials.gov, NCT05375461) assessed the efficacy of culmerciclib, a CDK2/4/6 inhibitor, plus fulvestrant in ABC. Patients with HR-positive, HER2-negative, locally recurrent or metastatic breast cancer were randomized (2:1) to receive culmerciclib plus fulvestrant or matching placebo plus fulvestrant. Between March 18, 2022 and March 3, 2023, 293 pretreated patients (median age 53.0 years; pre- or perimenopausal 42.3%; bone metastasis 65.2%) were randomized to assigned treatments. At this prespecified interim analysis, culmerciclib plus fulvestrant extended the median investigator-assessed progression-free survival (PFS) significantly, the primary endpoint, as compared with placebo plus fulvestrant (16.6 months, 95% CI 13.8 to not evaluable versus 7.5 months, 95% CI 5.3 to 11.0; hazard ratio 0.36, 95% CI 0.26-0.51; stratified log rank test P < 0.001). Consistent effects were observed across diverse subgroups of patients. At a median follow-up duration of 13.8 months, overall survival was immature. The investigators-assessed objective response rate was 40.2% (95% CI, 33.3-47.5) for culmerciclib compared to 12.1% (95% CI 6.4-20.2) for placebo (stratified Mantel-Haenszel χ2 test P < 0.001). Diarrhea (87.1%) and neutropenia (80.4%) were the most common toxicities with culmerciclib plus fulvestrant. In conclusion, this randomized clinical trial met its primary outcome. Culmerciclib plus fulvestrant is well tolerated and leads to a significant gain in PFS of pretreated HR-positive HER2-negative ABC patients.

Publication types

  • Randomized Controlled Trial
  • Clinical Trial, Phase III

MeSH terms

  • Adult
  • Aged
  • Antineoplastic Combined Chemotherapy Protocols* / administration & dosage
  • Antineoplastic Combined Chemotherapy Protocols* / adverse effects
  • Antineoplastic Combined Chemotherapy Protocols* / therapeutic use
  • Breast Neoplasms* / drug therapy
  • Breast Neoplasms* / genetics
  • Breast Neoplasms* / pathology
  • Cyclin-Dependent Kinase 2* / antagonists & inhibitors
  • Cyclin-Dependent Kinase 2* / genetics
  • Cyclin-Dependent Kinase 4* / antagonists & inhibitors
  • Cyclin-Dependent Kinase 4* / genetics
  • Cyclin-Dependent Kinase 6* / antagonists & inhibitors
  • Cyclin-Dependent Kinase 6* / genetics
  • Double-Blind Method
  • Erb-b2 Receptor Tyrosine Kinases / genetics
  • Erb-b2 Receptor Tyrosine Kinases / metabolism
  • Female
  • Fulvestrant* / administration & dosage
  • Fulvestrant* / adverse effects
  • Fulvestrant* / pharmacology
  • Humans
  • Middle Aged
  • Pyrimidines* / administration & dosage

Substances

  • Fulvestrant
  • Erb-b2 Receptor Tyrosine Kinases
  • Cyclin-Dependent Kinase 6
  • Cyclin-Dependent Kinase 4
  • Cyclin-Dependent Kinase 2
  • Pyrimidines
  • ERBB2 protein, human
  • CDK6 protein, human
  • CDK4 protein, human

Associated data

  • ClinicalTrials.gov/NCT05375461