Abemaciclib (Verzenio)

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

Abemaciclib is a selective cyclin-dependent kinase (CDK) 4/6 inhibitor that blocks cell cycle progression in cancer cells. In colorectal cancer, abemaciclib is being evaluated in combination with standard chemotherapy agents like 5-fluorouracil and targeted therapies including cetuximab and ERK inhibitors. The drug shows particular interest in tumors harboring KRAS mutations, which are present in approximately 40-50% of colorectal cancers and historically difficult to target effectively.

Mechanism of Action

Abemaciclib specifically inhibits cyclin-dependent kinases 4 and 6, which are essential regulators of the G1/S cell cycle checkpoint. By blocking CDK4/6 activity, the drug prevents phosphorylation of the retinoblastoma protein, leading to cell cycle arrest in the G1 phase and reduced cancer cell proliferation.

Molecular Targets

Side Effects

Diarrhea Neutropenia Nausea Fatigue Abdominal pain Anemia Leukopenia Decreased appetite Vomiting Headache Alopecia Thrombocytopenia

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

Clinical Trials

NCT06654037 Phase 1
Recruiting
Testing the Addition of an Anti-Cancer Drug, Abemaciclib, to the Usual Chemotherapy Treatment (5-Fluorouracil) for Metastatic, Refractory Colorectal Cancer
United States
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
NCT07441369 Phase 2
Enrolling by invitation
Abemaciclib Combined With FOLFOX/FOLFIRI Regimen in Patients With Advanced Colorectal Liver Metastases Cancer
China
NCT05307705 Phase 1
Active, not recruiting
A Study of LOXO-783 in Patients With Breast Cancer/Other Solid Tumors
United States, Australia, Belgium, Canada, China, France, Germany, Japan, Singap
View all 11 clinical trials →