Rosuvastatin (Crestor, Ezallor Sprinkle)

Other Medications · Approved since 2003

US Off-label EU EMA Approved ES Funded by SNS other indication Oral 3 Clinical Trials
HMG-CoA reductase

Description

Rosuvastatin is a potent HMG-CoA reductase inhibitor (statin) primarily used to lower cholesterol and prevent cardiovascular disease. In colorectal cancer treatment, rosuvastatin is being evaluated for its potential anti-cancer properties based on preclinical evidence that statins may inhibit tumor growth and metastasis. Clinical trials are examining whether rosuvastatin can improve outcomes when added to standard CRC treatment, particularly in patients with early-stage surgically resected colon cancer.

Mechanism of Action

Rosuvastatin inhibits HMG-CoA reductase, the rate-limiting enzyme in cholesterol biosynthesis, blocking the conversion of HMG-CoA to mevalonate. Beyond cholesterol reduction, this inhibition disrupts the mevalonate pathway, which affects prenylation of proteins involved in cell proliferation, apoptosis, and angiogenesis. The anti-cancer effects may result from reduced protein prenylation affecting oncogenic signaling pathways including Ras and Rho family proteins.

Molecular Targets

Side Effects

Muscle pain Headache Nausea Abdominal pain Weakness Elevated liver enzymes Rhabdomyolysis (rare) Diabetes mellitus

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

Clinical Trials

NCT07372625 Phase 1
Recruiting
A Study to Investigate the Effects of Multiple Doses of Rezatapopt on the Pharmacokinetics of Metformin, Rosuvastatin, Repaglinide, and Midazolam in Patients With Advanced Solid Tumors Harboring a TP53 Y220C Mutation.
United States
NCT05368805 Phase 1
Archived
Fruquintinib DDI Study With P-gp and BCRP Substrates
United States
NCT01011478 Phase 3
Archived
Rosuvastatin in Treating Patients With Stage I or Stage II Colon Cancer That Was Removed By Surgery
United States, Canada