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bitopertin

Small moleculeexperimental

Bitopertin is a glycine reuptake inhibitor which was under development by Roche as an adjunct to antipsychotics for the treatment of persistent negative symptoms or suboptimally controlled positive symptoms associated with schizophrenia. Research into this indication has been largely halted as a result of disappointing trial results. As of 2024, it is under development for the management of erythropoietic protoporphyria. — Wikipedia

Clinical trial activity

28 trials · 5 clinical orgs · 0 marketing orgs

Phase 1
15
Phase 2
13
Phase 3
8
Phase 4
0

Earliest trial started Nov 1, 2005 (NCT01636492)

Timeline

2000s

  1. Jan 1, 2005

    Earliest Phase 1 Sponsor(trial)

  2. Jan 1, 2008

    Earliest Phase 2 Sponsor(trial)

2010s

  1. Jan 1, 2010

    Earliest Phase 3 Sponsor(trial)

Indications

Studied for

Mechanism of action

Chemistry & pharmacology

Loading structure…

SMILES

C[C@H](Oc1ccc(S(C)(=O)=O)cc1C(=O)N1CCN(c2ncc(C(F)(F)F)cc2F)CC1)C(F)(F)F
Mol. weight
543.46 g/mol
Lipinski Ro5
1 violation(s)
Rule of 3
No
Chirality
Single Stereoisomer
Inorganic
No
Polymer
No

Oral

No

Parenteral

No

Topical

No

Sources

Also known as

  • (4-(3-fluoro-5-trifluoromethylpyridin-2-yl)piperazin-1-yl)(5-methanesulfonyl-2-(2,2,2-trifluoro-1-methylethoxy)phenyl)methanone
  • bitopertin
  • bitopertin
  • bitopertin
  • bitopertin
  • bitopertin
  • rg1678
  • rg 1678
  • rg-1678
  • ro4917838
  • ro-4917838
  • ro-4917838

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT07123363Phase 1Jan 31, 2026Atrium Medical Center, Wake Forest University
NCT06910358Phase 3Apr 4, 2025Disc Medicine, Inc
NCT05883748Phase 2/Phase 3 (Phase 3)Sep 30, 2023Disc Medicine, Inc
NCT05828108Phase 1/Phase 2 (Phase 2)Jul 25, 2023National Heart, Lung, and Blood Institute (NHLBI)
NCT05308472Phase 2Oct 31, 2022Disc Medicine, Inc
NCT03271541Phase 2Oct 26, 2017Roche
NCT02019290Phase 1Feb 1, 2014Roche
NCT01674361Phase 2Dec 1, 2012Roche
NCT01665976Phase 1Aug 1, 2012Roche
NCT01543529Phase 1Feb 28, 2012Roche
NCT01495104Phase 1Oct 1, 2011Roche
NCT01438749Phase 1Oct 1, 2011Roche
NCT01510899Phase 1Oct 1, 2011Roche
NCT01433575Phase 1Sep 1, 2011Roche
NCT01356550Phase 1Jun 1, 2011Roche
NCT01365403Phase 1Apr 1, 2011Roche
NCT01234779Phase 2Feb 1, 2011Roche
NCT01235520Phase 3Jan 1, 2011Roche
NCT01235559Phase 3Dec 1, 2010Roche
NCT01235585Phase 3Dec 1, 2010Roche
Showing 20 of 28 trials
Page 1 / 2

Organizations

Research & Development (5)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
RocheFor profit232332005
Disc Medicine, IncFor profit3322022
Atrium Medical CenterAcademic/Hospital1012026
National Heart, Lung, and Blood Institute (NHLBI)Government1112023
Wake Forest UniversityAcademic/Hospital1112026
5 organizations
Page 1 / 1