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. Author manuscript; available in PMC: 2023 Feb 1.
Published in final edited form as: Biochem Pharmacol. 2021 Jun 12;196:114654. doi: 10.1016/j.bcp.2021.114654

Table 2:

Effects of some cholesterol-targeting therapies in cancer patients

Drug/Study Name Cancer Type Findings References
I. Statins
Lovastatin, Pravastatin, Simvastatin, Atorvastatin: Relationship between statin use and colon cancer recurrence and survival: results from CALGB 89803

Simvastatin, Pravastatin, Atorvastatin, Rosuvastatin, Fluvastatin: Statin use is not associated with improved progression free survival in cetuximab treated KRAS Mutant metastatic colorectal cancer patients: results from the CAIRO2 study
Stage 3 Colorectal Cancer Statin use was not associated with improved cancer prognoses, as measured by overall and disease-free survival.

Patients with metastatic colorectal cancer, treated with chemotherapy and other pharmacological treatment, did not have a significant change in overall survival after statin administration, as compared to other patients.
[187, 188]
Atorvastatin: Statin-induced anti-proliferative effects via cyclin D1 and p27 in a window-of-opportunity breast cancer trial

Atorvastatin: Targeting HMG-CoA reductase with statins in a window-of-opportunity breast cancer trial
Primary Invasive Breast Cancer Statin use led to a decrease in Cyclin D1 expression, and an increase in the expression of the tumor suppressor p27.

Statin use led to a decrease in the expression of the tumor marker Ki67.
[189, 190]
Atorvastatin, Pravastatin, Fluvastatin, Simvastatin: Statin use is associated with improved survival in multiple myeloma: A Swedish population-based study of 4315 patients Multiple Myeloma A dose dependent relationship between statin use and survival was observed in patients with multiple myeloma. [191]
Atorvastatin, Pravastatin, Fluvastatin, Simvastatin: Statin attenuates cell proliferative ability via TAZ (WWTR1) in hepatocellular carcinoma

Pravastatin: Pravastatin combination with sorafenib does not improve survival in advanced hepatocellular carcinoma
Hepatocellular Carcinoma Statin use was associated with longer recurrence free survival in patients with hepatocellular carcinoma.

The use of pravastatin in combination with the current therapy for hepatocellular carcinoma, sorafenib, did not improve survival rates when compared to sorafenib monotherapy.
[192, 193]
Atorvastatin: Global transcriptional changes following statin treatment in breast cancer Breast Cancer Statins induced upregulation of many pro-apoptotic genes. [194]
Fluvastatin, Atorvastatin, Lovastatin, Pravastatin, Simvastatin, Cerivastatin: Statin drug use is not associated with prostate cancer risk in men who are regularly screened

Lovastatin:

Use of statins and prostate cancer recurrence among patients treated with radical prostatectomy

Atorvastatin: Atorvastatin versus placebo before radical prostatectomy—A randomized, double-blind, placebo-controlled clinical trial
Prostate Cancer Statin use was not significantly associated with decreased risk or progression of prostate cancer.

Treatment with atorvastatin did not significantly change the expression of tumor proliferation markers such as Ki67; however, a nonsignificant positive improvement was noted in patients who continued treatment for 28 or more days.
[195197]
Simvastatin: Randomized phase II study of Afatinib plus Simvastatin versus Afatinib alone in previously treated patients with advanced nonadenocarcinomatous non-small cell lung cancer Non-Small-Cell Lung Cancer Patients taking a combination therapy of simvastatin and afatinib did not have a significant change in survival rate or tumor response as compared to monotherapy. [198]
Pravastatin: Multicenter, phase III, randomized, double-blind, placebo-controlled trial of Pravastatin added to first-line standard chemotherapy in small-cell lung cancer (LUNGSTAR) Small-Cell Lung Cancer The administration of Pravastatin in Small-Cell Lung Cancer patients does not significantly change overall survival time or tumor response in patients. [199]
II. Fibrates
Fibrate, fibric acid, fenofibrate, bezafibrate, ciprofibrate, clofibrate, gemfibrozil: Use of fibrates and cancer risk: a systematic review and meta-analysis of 17 long-term randomized placebo-controlled trials. A meta-analysis, showing that fibrate use did not have an impact on the incidence or mortality of cancer [166]
III. Ezetimibe
Ezetimibe is an inhibitor of tumor angiogenesis Prostate Cancer The study showed that ezetimibe use (in animal models) worked to lower tumor angiogenesis via lowering serum cholesterol levels. [167]
IV. Novel Therapies
SREBP-1 inhibitor betulin enhances the antitumor effect of sorafenib on hepatocellular carcinoma via restricting cellular glycolytic activity. Hepatocellular Carcinoma Betulin increases the efficacy of sorafenib in patients who do not respond to sorafenib monotherapy. [168]
Fatostatin blocks ER exit of SCAP but inhibits cell growth in a SCAP-independent manner

Fatostatin suppresses growth and enhances apoptosis by blocking SREBP-regulated metabolic pathways in endometrial carcinoma.

Fatostatin displays high antitumor activity in prostate cancer by blocking SREBP-regulated metabolic pathways and androgen receptor signaling.

Fatostatin inhibits cancer cell proliferation by affecting mitotic microtubule spindle assembly and cell division.
Endometrial Carcinoma, Prostate Cancer Fatostatin has antitumor properties, as observed in multiple in vitro and animal model studies. [169, 170, 172, 173]
Mevalonate metabolism regulates basal breast cancer stem cells and is a potential therapeutic target.

Geranylgeranyl transferase 1 inhibitor GGTI-298 enhances the anticancer effect of gefitinib.

Synergistic effect of Geranylgeranyltransferase Inhibitor, GGTI, and Docetaxel on the growth of prostate cancer cells.

Prenyltransferase inhibitors: treating human ailments from cancer to parasitic infections.
Prostate Cancer Geranylgeranyl-transferase inhibitors favorably prevent the growth of cancer cells, although working better with other prenyloid inhibitors. [178181]