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probucol

Trade name: lorelco

Small moleculeapproved

Approved

Feb 1, 1977

Probucol is used to lower levels of cholesterol (a fat-like substance) in the blood. Probucol is a drug used to lower LDL and HDL cholesterol yet has little effect on serum-triglyceride or VLDL cholesterol. This may help prevent medical problems caused by cholesterol clogging the blood vessels. Probucol was voluntarily removed from the market in the United States during 1995. The withdrawal from the market was due to safety concern. robucol lowers serum cholesterol by increasing the fractional rate of low-density lipoprotein (LDL) catabolism in the final metabolic pathway for cholesterol elimination from the body. Additionally, probucol may inhibit early stages of cholesterol biosynthesis and slightly inhibit dietary cholesterol absorption. Recent information suggests that probucol may inhibit the oxidation and tissue deposition of LDL cholesterol, thereby inhibiting atherogenesis. It appears to inhibits ABCA1-mediated cellular lipid efflux. — NCATS

Clinical trial activity

22 trials · 19 clinical orgs · 1 marketing orgs

Phase 1
2
Phase 2
5
Phase 3
2
Phase 4
13

Earliest trial started Jan 1, 2004 (NCT00276133)

Timeline

1970s

  1. Feb 1, 1977

    Sanofi-Aventis — Earliest FDA Approval

  2. Feb 1, 1977

    Sanofi-Aventis — NDA Secondary Org

  3. Feb 1, 1977

    Sanofi-Aventis — NDA Organization

2010s

  1. Jan 1, 2010

    Earliest Phase 2 Sponsor(trial)

  2. Jan 1, 2011

    Earliest Phase 3 Sponsor(trial)

  3. Jan 1, 2012

    Earliest Phase 1 Sponsor(trial)

Indications

Approved for

Studied for

Mechanism of action

Approval history

  • approvedPriority reviewFeb 1, 1977

Chemistry & pharmacology

Loading structure…

SMILES

CC(C)(SC1=CC(=C(O)C(=C1)C(C)(C)C)C(C)(C)C)SC2=CC(=C(O)C(=C2)C(C)(C)C)C(C)(C)C
Mol. weight
516.842 g/mol
Lipinski Ro5
2 violation(s)
Rule of 3
No
Chirality
Achiral Molecule
Inorganic
No
Polymer
No
Delivery
Oral
Availability
Discontinued

Oral

Yes

Parenteral

No

Topical

No

Sources

Also known as

  • 4,4'- (isopropylidenedithio)bis(2,6-di-tert-butylphenol)
  • 4,4'- (isopropylidenedithio)bis(2,6-di-tert-butylphenol)
  • acetone bis(3,5-di-tert-butyl-4-hydroxyphenyl) mercaptole
  • acetone bis(3,5-di-tert-butyl-4-hydroxyphenyl) mercaptole
  • biphenabid
  • biphenabid
  • biphenabid
  • bisbid
  • bisbid
  • bisbid
  • bisphenabid
  • bisphenabid
  • bisphenabid
  • dh-581
  • dh-581
  • lesterol
  • lesterol
  • lorelco
  • lorelco
  • lorelco
  • lorelco
  • lurselle
  • lurselle
  • lurselle
  • phenbutol
  • probucol
  • probucol
  • probucol
  • probucol
  • probucol
  • probucol
  • probucol
  • probucol
  • probucol
  • probucol
  • probucol
  • probucol
  • probucolum
  • probucolum
  • serterol
  • serterol
  • sinlestal
  • sinlestal
  • superlipid
  • superlipid

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT06225752Phase 3Jun 15, 2024Capital Medical University, Wannan Medical College
NCT03753555Phase 4Dec 1, 2018People's Liberation Army of China
NCT02707458Phase 1/Phase 2 (Phase 2)Apr 1, 2016McGill University, Weston Brain Institute
NCT02098460Phase 4Oct 1, 2013Beijing Anzhen Hospital, Otsuka
NCT01726816Phase 2Oct 1, 2012Otsuka, Sungkyunkwan University
NCT01590901Phase 1Feb 1, 2012Otsuka, Tsinghua University
NCT01349010Phase 3Apr 1, 2011Central South University, Otsuka
NCT01291641Phase 4Mar 1, 2011Dong-A Pharmaceutical, Otsuka, Seoul National University
NCT01142284Phase 2Apr 1, 2010Otsuka
NCT01252056Phase 4Mar 1, 2010Otsuka, Peking University
NCT01031667Phase 4Nov 1, 2009Otsuka, Yonsei University
NCT01013532Phase 4Jun 1, 2009Otsuka, University of Ulsan
NCT02483169Phase 4Jun 1, 2009Otsuka, University of Ulsan
NCT00823875Phase 4Mar 1, 2009Otsuka, Peking University
NCT02196805N/AMar 1, 2009Otsuka, Tsinghua University
NCT01000467Phase 4Feb 1, 2009Otsuka, Seoul National University
NCT00823849Phase 4Oct 1, 2008Otsuka, Peking University
NCT00655330N/AMay 1, 2008Shantou University
NCT00549978Phase 4Oct 1, 2007Otsuka, Seoul National University
NCT00426348Phase 4May 1, 2007Shantou University
Showing 20 of 22 trials
Page 1 / 2

Organizations

Research & Development (19)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
OtsukaFor profit151152007
Peking UniversityAcademic/Hospital3012008
Seoul National UniversityAcademic/Hospital3112007
Shantou UniversityAcademic/Hospital2222007
Tsinghua UniversityAcademic/Hospital2022009
University of UlsanAcademic/Hospital2212009
Beijing Anzhen HospitalAcademic/Hospital1012013
Capital Medical UniversityAcademic/Hospital1012024
Central South UniversityAcademic/Hospital1012011
Dong-A PharmaceuticalFor profit1012011
McGill UniversityAcademic/Hospital1112016
People's Liberation Army of ChinaGovernment1112018
RiboNova Inc.For profit111—
Sungkyunkwan UniversityAcademic/Hospital1012012
University of PennsylvaniaAcademic/Hospital101—
Wannan Medical CollegeAcademic/Hospital1112024
Weston Brain InstituteAcademic/Hospital1012016
Yokohama City UniversityAcademic/Hospital1112004
Yonsei UniversityAcademic/Hospital1112009
19 organizations
Page 1 / 1

Marketing (2)

OrganizationOrg typeRelationshipDate
Sanofi-AventisFor profitNDA2Feb 1, 1977
Sanofi-AventisFor profitNDAFeb 1, 1977