denatonium benzoate

Trade name: Bitrex

Small moleculeexperimental

Denatonium, usually available as denatonium benzoate (trade names Bitrex) is the most bitter chemical compound known, with bitterness thresholds of 0.05 ppm for the benzoate and 0.01 ppm for the saccharide. Scientists at Macfarlan Smith, Ltd. of Edinburgh, Scotland discovered Bitrex during research on derivatives of the anesthetic lidocaine. The extremely bitter taste proved effective in reducing ingestion by humans and animals. Denatonium is commonly included in placebo medications used in clinical trials to match the bitter taste of certain medications. Denatonium activates bitter taste receptor, mainly, TAS2R4, TAS2R8, TAS2R10, TAS2R13 on many cell types and plays important roles in chemical release, ciliary beating and smooth muscle relaxation through intracellular Ca(2+)-dependent pathways. — NCATS

Clinical trial activity

5 trials · 3 clinical orgs · 0 marketing orgs

Phase 1
2
Phase 2
0
Phase 3
0
Phase 4
1

Earliest trial started Aug 1, 2011 (NCT02759926)

Timeline

2020s

  1. Jan 1, 2023

    Earliest Phase 1 Sponsor(trial)

Indications

Approved for

Mechanism of action

Chemistry & pharmacology

Loading structure…

SMILES

CC[N+](CC)(CC(=O)NC1=C(C)C=CC=C1C)CC2=CC=CC=C2
Mol. weight
325.4678 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Achiral Molecule
Inorganic
No
Polymer
No

Oral

No

Parenteral

No

Topical

No

Sources

Also known as

  • bitrex
  • denatonium benzoate
  • denatonium benzoate
  • denatonium benzoate

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT06310200Phase 1Aug 1, 2024Wright State University
NCT06003829Phase 1Jul 31, 2023Pfizer
NCT03777787N/AJan 14, 2019Katholieke Universiteit Leuven
NCT03985865Phase 4Mar 2, 2017Katholieke Universiteit Leuven
NCT02759926N/AAug 1, 2011Katholieke Universiteit Leuven
Showing 5 of 5 trials
Page 1 / 1

Organizations

Research & Development (3)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
Katholieke Universiteit LeuvenAcademic/Hospital3322011
PfizerFor profit1112023
Wright State UniversityAcademic/Hospital1112024
3 organizations
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