Rosuvastati (Crestor)

Other · Approved since 2003

US Off-label Oral 3 Clinical Trials
HMG-CoA reductase

Description

Rosuvastatin is a high-potency HMG-CoA reductase inhibitor (statin) primarily used for lowering cholesterol levels. In colorectal cancer, rosuvastatin has been evaluated as an adjuvant therapy for early-stage colon cancer patients following surgical resection, based on preclinical evidence suggesting statins may have anti-cancer properties. The drug's potential role in CRC stems from observations that statin use may be associated with improved outcomes in certain cancer patients. Clinical trials have specifically examined its use in stage I and II colon cancer patients with mismatch repair deficiency markers.

Mechanism of Action

Rosuvastatin inhibits HMG-CoA reductase, the rate-limiting enzyme in cholesterol biosynthesis, leading to reduced cholesterol production and increased LDL receptor expression. In the cancer context, statins may exert anti-neoplastic effects through multiple pathways including inhibition of protein prenylation, which affects oncogenic signaling proteins like Ras, and potential modulation of inflammatory pathways. The mevalonate pathway disruption may also impact cancer cell proliferation and survival mechanisms.

Molecular Targets

Side Effects

Muscle pain and weakness Headache Abdominal pain Nausea Elevated liver enzymes Constipation Dizziness Memory problems

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