fluvastatin
Trade name: lescol
Approved
Dec 31, 1993
Fluvastatin is an antilipemic agent that competitively inhibits hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase. Fluvastatin is marketed under the trade names Lescol, Canef, Vastin. LESCOL/LESCOL XL is an HMG-CoA reductase inhibitor (statin) indicated as an adjunctive therapy to diet to: Reduce elevated TC, LDL-C, Apo B, and TG, and to increase HDL-C in adult patients with primary hypercholesterolemia and mixed dyslipidemia Reduce elevated TC, LDL-C, and Apo B levels in boys and post-menarchal girls, 10 to 16 years of age, with heterozygous familial hypercholesterolemia after failing an adequate trial of diet therapy Reduce the risk of undergoing revascularization procedures in patients with clinically evident CHD Slow the progression of atherosclerosis in patients with CHD. Fluvastatin selectively and competitively inhibits the hepatic enzyme hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase. HMG-CoA reductase is responsible for converting HMG-CoA to mevalonate, the rate-limiting step in cholesterol biosynthesis. Inhibition results in a decrease in hepatic cholesterol levels which stimulates the synthesis of LDL receptors and increases hepatic uptake of LDL cholesterol. The end result is decreased levels of plasma total and LDL cholesterol. — NCATS
Clinical trial activity
51 trials · 42 clinical orgs · 7 marketing orgs
Earliest trial started Sep 1, 2001 (NCT00565474)
Timeline
1990s
- Dec 31, 1993
Earliest FDA Approval
- Dec 31, 1993
Novartis — NDA Secondary Org
2000s
2010s
- Apr 11, 2012
Mylan — Marketing Organization
- Jun 12, 2012
Teva — Marketing Organization
- Sep 11, 2015
PHARMOBEDIENT — Marketing Organization
2020s
- Apr 26, 2021
Beijing Pearl Biotechnology Limited Liability Company — Marketing Organization
Indications
Approved for
Studied for
- Adipose Tissue, Brown · Phase 4
- Aging · Phase 2
- Antiphospholipid Syndrome · Phase 2
- Aortic Valve Stenosis · Phase 4
- Atherosclerosis · Phase 4
- Breast Neoplasms · Phase 2
- Cardiovascular Diseases · Phase 3
- Clinical Trial · Phase 4
- Coronary Artery Disease · Phase 4
- Coronary Disease · Phase 4
- Diabetes Mellitus, Type 2 · Phase 4
- Drug Interactions · Phase 4
- Dyslipidemias · Phase 4
- Erectile Dysfunction · Phase 3
- Glioma · Phase 1
- Healthy Volunteers · Phase 1
- Heart Transplantation · Phase 4
- Hepacivirus · Phase 2
- Hepatitis C · Phase 2
- Hepatitis C, Chronic · Phase 2
- Homozygous Familial Hypercholesterolemia · Phase 3
- Hypercholesterolemia · Phase 4
- Hypertension · Phase 4
- Inflammation · Phase 2
- Insulin Resistance · Phase 4
- Ischemic Attack, Transient · Phase 4
- Ischemic Stroke · Phase 4
- Kidney Diseases · Phase 3
- Kidney Transplantation · Phase 4
- Lipid Metabolism Disorders · Phase 4
- Livedoid Vasculopathy · Phase 4
- Melanoma · Early Phase 1
- Metabolic Syndrome · Phase 4
- Myocardial Infarction · Phase 4
- Nephritis, Hereditary · Phase 2
- Osteoporosis · Phase 4
- Prostatic Neoplasms · Phase 2
- Proteinuria · Phase 3
Mechanism of action
- HMG-CoA reductaseINHIBITOR
HMGCR inhibitor
Approval history
- approvedDec 31, 1993
Chemistry & pharmacology
SMILES
CC(C)n1c(/C=C/C(O)CC(O)CC(=O)O)c(-c2ccc(F)cc2)c2ccccc21- Mol. weight
- 411.47 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Racemic Mixture
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL2220442 ↗
- WikipediaFluvastatin ↗
- NCATS4L066368AS ↗
- ChEMBLCHEMBL333442 ↗
- ChEMBLCHEMBL2218894 ↗
- ChEMBLCHEMBL1078 ↗
Also known as
- (3s,5s)-fluvastatin
- 7-(3-(4-fluorophenyl)-1-(1-methylethyl)-1h-indol-2-yl)-3,5-dihydroxy-6-heptenoate
- dorisin xl
- fluindostatin
- fluvastatin
- fluvastatin
- fluvastatin
- fluvastatin
- fluvastatin
- fluvastatin
- fluvastatin
- fluvastatin
- fluvastatin
- fluvastatina
- fluvastatina
- fluvastatine
- fluvastatine
- fluvastatin sodium
- fluvastatin sodium
- fluvastatin sodium
- fluvastatin sodium
- fluvastatin sodium
- fluvastatin sodium hydrate
- fluvastatin sodium salt
- fluvastatin sodium salt
- fluvastatinum
- fluvastatinum
- leschol
- lescol
- lescol
- lescol
- lescol
- lescol
- lescol
- lescol
- luvinsta xl
- nandovar xl
- pinmactil
- stefluvin xl
- xu 62320
- xu 62-320
- xu-62320
- xu-62320
- xu-62320
- xu-62-320
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT06785727 | Phase 4 | Feb 1, 2025 | University of Amsterdam |
| NCT06679036 | Phase 1/Phase 2 (Phase 2) | Nov 25, 2024 | Suzhou Suncadia Biopharmaceuticals Co., Ltd. |
| NCT04285749 | Early Phase 1 (Phase 1) | May 6, 2020 | Case Western Reserve University |
| NCT03510715 | Phase 3 | Sep 3, 2018 | Regeneron, Sanofi |
| NCT03510884 | Phase 3 | May 31, 2018 | Regeneron, Sanofi |
| NCT03189511 | Phase 4 | May 31, 2017 | University of Basel, University of Zurich |
| NCT03393377 | N/A | Sep 30, 2014 | University of Ljubljana |
| NCT02115074 | Phase 1 | Jun 1, 2014 | Reliable Cancer Therapies, University of Lille |
| NCT02107898 | Phase 3 | Mar 1, 2014 | Regeneron, Sanofi |
| NCT01992042 | Phase 2 | Feb 1, 2014 | University of Toronto |
| NCT03309618 | N/A | Nov 30, 2012 | University of Ljubljana |
| NCT01715714 | Phase 4 | Oct 1, 2012 | German Federal Ministry of Education and Research, University of Cologne |
| NCT01681199 | Phase 4 | Jul 1, 2012 | Capital Medical University, Novartis |
| NCT01644175 | Phase 3 | Jul 1, 2012 | Regeneron, Sanofi |
| NCT01514682 | N/A | Jun 1, 2012 | University of Maryland |
| NCT01507831 | Phase 3 | Jan 1, 2012 | Regeneron, Sanofi |
| NCT01551173 | Phase 4 | Jan 1, 2012 | Novartis |
| NCT00814606 | Phase 2 | Feb 1, 2010 | University of Chicago |
| NCT01045512 | Phase 2 | Oct 1, 2009 | Martin Luther University, Novartis |
| NCT00752843 | Phase 1 | Sep 1, 2008 | Corcept Therapeutics, MDS Pharma |
Organizations
Research & Development (42)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Novartis | For profit | 18 | 14 | 3 | 2001 |
| Regeneron | For profit | 5 | 0 | 1 | 2012 |
| Sanofi | For profit | 5 | 5 | 1 | 2012 |
| Universitaetsklinikum Schleswig-Holstein | Academic/Hospital | 3 | 3 | 2 | 2003 |
| Department of Veteran Affairs | Government | 2 | 2 | 2 | 2006 |
| Mario Negri Institute | Academic/Hospital | 2 | 2 | 2 | 2003 |
| University of Ljubljana | Academic/Hospital | 2 | 2 | 1 | 2012 |
| University of Oklahoma | Academic/Hospital | 2 | 0 | 2 | 2006 |
| Yokohama City University | Academic/Hospital | 2 | 1 | 1 | 2006 |
| AORTICA Group | For profit | 1 | 1 | 1 | 2006 |
| Capital Medical University | Academic/Hospital | 1 | 1 | 1 | 2012 |
| Case Western Reserve University | Academic/Hospital | 1 | 1 | 1 | 2020 |
| Corcept Therapeutics | For profit | 1 | 1 | 1 | 2008 |
| German Federal Ministry of Education and Research | Government | 1 | 0 | 1 | 2012 |
| Government of Czech Republic | Government | 1 | 0 | 1 | 2003 |
| Kitasato University | Academic/Hospital | 1 | 1 | 1 | 2006 |
| Martin Luther University | Academic/Hospital | 1 | 1 | 1 | 2009 |
| MDS Pharma | For profit | 1 | 0 | 1 | 2008 |
| Medical University of Graz | Academic/Hospital | 1 | 1 | 1 | 2005 |
| Merck | For profit | 1 | 1 | 1 | 2005 |
Marketing (10)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Beijing Pearl Biotechnology Limited Liability Company | Government | MKTG | Apr 26, 2021 |
| Mylan | For profit | MKTG | Apr 11, 2012 |
| Mylan | For profit | SYN | Sep 11, 2015 |
| Novartis | For profit | NDA2 | Dec 31, 1993 |
| PHARMOBEDIENT | For profit | MKTG | Sep 11, 2015 |
| Par Pharmaceuticals | For profit | MKTG | Sep 15, 2009 |
| Sandoz | For profit | NDA | — |
| Sandoz | For profit | MKTG | Oct 6, 2000 |
| Teva | For profit | MKTG | Jun 12, 2012 |
| Teva | For profit | SYN | Jan 27, 2016 |