Ribociclib (Kisqali)

Other Medications · Approved since 2017

US Off-label EU EMA Approved ES Hospital use off-label in CRC Oral 11 Clinical Trials
CDK4 CDK6

Description

Ribociclib is a selective cyclin-dependent kinase 4 and 6 (CDK4/6) inhibitor that blocks cell cycle progression from G1 to S phase. While primarily approved for hormone receptor-positive breast cancer, ribociclib is being explored in colorectal cancer through combination approaches with other targeted agents. In CRC, it is studied particularly in tumors with KRAS mutations as part of combination regimens with MEK inhibitors like trametinib.

Mechanism of Action

Ribociclib selectively inhibits cyclin-dependent kinases 4 and 6, which are key regulators of cell cycle progression. By blocking CDK4/6 activity, ribociclib prevents phosphorylation of the retinoblastoma protein, leading to cell cycle arrest in the G1 phase and ultimately inducing apoptosis in rapidly dividing cancer cells.

Molecular Targets

Side Effects

Neutropenia Fatigue Nausea Diarrhea Vomiting Alopecia Headache Decreased appetite

Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.

Clinical Trials

NCT06726148 Phase 1
Recruiting
Study of ECI830 Single Agent or in Combination in Patients With Advanced HR+/HER2- Breast Cancer and Other Advanced Solid Tumors
United States, Australia, Canada, China, Czechia, Denmark, France, Germany, Isra
NCT06625775 Phase 1
Recruiting
Open-Label Study of BBO-10203 in Subjects With Advanced Solid Tumors
United States, Australia, Brazil, France, Spain
NCT06239467 Phase 1
Recruiting
First-in-Human Study of OKI-219 in Advanced Solid Tumors and Advanced Breast Cancer
United States, Belgium, France, Italy, South Korea, Spain
NCT06188520 Phase 1
Recruiting
A First-in-human Dose Escalation and Expansion Study to Evaluate the Safety, and Tolerability of AZD8421 Alone or in Combination in Participants With Selected Advanced or Metastatic Solid Tumors
United States, Australia, South Korea, Spain, United Kingdom
NCT05867251 Phase 1
Recruiting
Study of AVZO-021 in Patients With Advanced Solid Tumors
United States, Australia
NCT05768139 Phase 1
Recruiting
First-in-Human Study of Tersolisib (STX-478) as Monotherapy and in Combination With Other Antineoplastic Agents in Participants With Advanced Solid Tumors
United States, Belgium, France, Germany, Ireland, Italy, Japan, Netherlands, Spa
View all 11 clinical trials →