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CDK4/6i
CDK4/6 inhibitors block cyclin-dependent kinases 4 and 6, which prevents phosphorylation of the retinoblastoma protein and halts cell cycle progression in G1 phase.
CDK4/6 inhibitors block cyclin-dependent kinases 4 and 6, which prevents phosphorylation of the retinoblastoma protein and halts cell cycle progression in G1 phase. Used for Hormone receptor-positive, HER2-negative advanced or metastatic breast cancer (in combination with endocrine therapy), Other CDK4/6-dependent malignancies in clinical development.
At a glance
| Generic name | CDK4/6i |
|---|---|
| Sponsor | Hoffmann-La Roche |
| Drug class | CDK4/6 inhibitor |
| Target | CDK4, CDK6 |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | Phase 3 |
Mechanism of action
CDK4/6 inhibitors are small molecules that bind to and inhibit cyclin-dependent kinases 4 and 6, key regulators of the G1/S cell cycle checkpoint. By preventing the phosphorylation of retinoblastoma (Rb) protein, these inhibitors trap cancer cells in G1 phase, preventing their progression to S phase and DNA replication. This mechanism is particularly effective in hormone receptor-positive breast cancers and other malignancies with dysregulated cell cycle control.
Approved indications
- Hormone receptor-positive, HER2-negative advanced or metastatic breast cancer (in combination with endocrine therapy)
- Other CDK4/6-dependent malignancies in clinical development
Common side effects
- Neutropenia
- Leukopenia
- Anemia
- Nausea
- Fatigue
- Diarrhea
- Vomiting
Key clinical trials
- BGB-43395 Plus Letrozole Versus CDK4/6i Plus Letrozole for Patients With Advanced or Metastatic HR+/HER2- Breast Cancer Who Have Not Received Prior Treatment for Advanced or Metastatic Disease (PHASE3)
- Palazestrant in Combination With Ribociclib for the First-line Treatment of ER+/HER2- Advanced Breast Cancer (PHASE3)
- Elacestrant + Everolimus in Patients ER+/HER2-, ESR1mut, Advanced Breast Cancer Progressing to ET and CDK4/6i. (PHASE3)
- Saruparib (AZD5305) Plus Camizestrant Compared With CDK4/6 Inhibitor Plus Endocrine Therapy or Plus Camizestrant in HR-Positive, HER2-Negative (IHC 0, 1+, 2+/ ISH Non-amplified), BRCA1, BRCA2, or PALB2m Advanced Breast Cancer (PHASE3)
- Capivasertib + CDK4/6i + Fulvestrant for Advanced/Metastatic HR+/HER2- Breast Cancer (CAPItello-292) (PHASE3)
- A Study With NKT5097 for Adults With Advanced/Metastatic Solid Tumors (PHASE1)
- A Study to Evaluate Efficacy and Safety of Giredestrant Compared With Fulvestrant (Plus a CDK4/6 Inhibitor), in Participants With ER-Positive, HER2-Negative Advanced Breast Cancer Resistant to Adjuvant Endocrine Therapy (pionERA Breast Cancer) (PHASE3)
- A Vaccine (STEMVAC) With Standard Endocrine-Based Therapy or Chemotherapy for the Treatment of Metastatic Hormone Receptor Positive, HER2 Negative Breast Cancer (PHASE2)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- CDK4/6i CI brief — competitive landscape report
- CDK4/6i updates RSS · CI watch RSS
- Hoffmann-La Roche portfolio CI