Ruxolitinib (Jakafi, Opzelura)

Targeted Therapy · Approved since 2011

US Off-label EU EMA Approved ES Hospital use off-label in CRC Oral 4 Clinical Trials
JAK1 JAK2

Description

Ruxolitinib is a selective Janus kinase (JAK) inhibitor that blocks JAK1 and JAK2 signaling pathways. While approved for certain blood cancers and inflammatory conditions, ruxolitinib is being explored in colorectal cancer through combination approaches with other targeted agents. In CRC, it is primarily tested alongside MEK inhibitors like trametinib to target multiple oncogenic pathways simultaneously.

Mechanism of Action

Ruxolitinib selectively inhibits JAK1 and JAK2 kinases, which are critical components of the JAK-STAT signaling pathway involved in cell proliferation, survival, and immune responses. By blocking these kinases, ruxolitinib disrupts cytokine signaling that can promote tumor growth and inflammation in the tumor microenvironment.

Molecular Targets

Side Effects

Thrombocytopenia Anemia Neutropenia Diarrhea Peripheral edema Fatigue Dizziness Headache

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

Clinical Trials

NCT07566897 Phase 1
Not yet recruiting
A Phase I Study to Evaluate the Safety and Efficacy of L19IL2 in Combination With Ruxolitinib in Patients With Advanced Solid Tumors
Italy
NCT04303403 Phase 1
Unknown
Study of Trametinib and Ruxolitinib in Colorectal Cancer and Pancreatic Adenocarcinoma
Singapore
NCT02955940 Phase 2
Active, not recruiting
An Open-Label Study to Enable Continued Treatment Access for Subjects Previously Enrolled in Studies of Ruxolitinib
United States, Poland
NCT02119676 Phase 2
Archived
Study of Ruxolitinib in Colorectal Cancer Patients
United States, Australia, France, Germany, Israel, South Korea, Spain, United Ki