Zabaglurant

Zabaglurant
Clinical data
Other namesHTL14242; HTL-14242; HTL-0014242; HTL0014242; Heptares 25; TMP-301; TMP301
Routes of
administration		Oral[1]
Drug classMetabotropic glutamate mGlu5 receptor negative allosteric modulator
Identifiers
  • 3-chloro-5-[6-(5-fluoro-2-pyridinyl)pyrimidin-4-yl]benzonitrile
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
ChEMBL
PDB ligand
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC16H8ClFN4
Molar mass310.72 g·mol−1
3D model (JSmol)
  • C1=CC(=NC=C1F)C2=CC(=NC=N2)C3=CC(=CC(=C3)C#N)Cl
  • InChI=1S/C16H8ClFN4/c17-12-4-10(7-19)3-11(5-12)15-6-16(22-9-21-15)14-2-1-13(18)8-20-14/h1-6,8-9H
  • Key:FQAXDSVNYVVQSE-UHFFFAOYSA-N

Zabaglurant (INNTooltip International Nonproprietary Name;[2] developmental code names HTL14242 and TMP-301) is a metabotropic glutamate mGlu5 receptor negative allosteric modulator which is under development for the treatment of alcoholism (alcohol use disorder).[1][3][4][5][6] It is taken orally.[1] The drug was first described in the scientific literature by 2015.[4][5][6] It was developed by Sosei Heptares, Nxera Pharma, and Tempero Bio.[1][3] As of April 2026, the drug is in phase 2 clinical trials for alcoholism.[1][3] It was also under development for cocaine-related disorders, other substance-related disorders, anxiety disorders, neurological disorders, and psychiatric disorders, but no recent development has been reported or development was discontinued for these indications.[1][3] In April 2026, a phase 2 trial for alcoholism was terminated due to serious adverse events.[1][7]

See also

References

  1. 1 2 3 4 5 6 7 "TMP 301". AdisInsight. 27 April 2026. Retrieved 22 July 2026.
  2. ↑ "INN Proposed List 135". World Health Organization. 19 July 2026. Retrieved 21 July 2026.
  3. 1 2 3 4 Quantum Health (18 April 2026). "Delving into the Latest Updates on HTL-0014242 with Synapse". Synapse. Retrieved 22 July 2026.
  4. 1 2 Christopher JA, Aves SJ, Bennett KA, Doré AS, Errey JC, Jazayeri A, et al. (August 2015). "Fragment and Structure-Based Drug Discovery for a Class C GPCR: Discovery of the mGlu5 Negative Allosteric Modulator HTL14242 (3-Chloro-5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzonitrile)". Journal of Medicinal Chemistry. 58 (16): 6653–6664. doi:10.1021/acs.jmedchem.5b00892. PMID 26225459.
  5. 1 2 Tehan BG, Christopher JA (October 2016). "The use of conformationally thermostabilised GPCRs in drug discovery: application to fragment, structure and biophysical techniques". Current Opinion in Pharmacology. 30: 8–13. doi:10.1016/j.coph.2016.06.010. PMID 27400445.
  6. 1 2 Bennett KA, Christopher JA, Tehan BG (2020). "Structure-based discovery and development of metabotropic glutamate receptor 5 negative allosteric modulators". From Structure to Clinical Development: Allosteric Modulation of G Protein-Coupled Receptors. Advances in Pharmacology. Vol. 88. San Diego, Calif. pp. 35–58. doi:10.1016/bs.apha.2020.03.001. ISBN 978-0-12-820187-9. PMID 32416871.{{cite book}}: CS1 maint: location missing publisher (link)
  7. ↑ "A Study to Investigate the Safety and Efficacy of TMP-301 Compared to Placebo in Adult Patients With Alcohol Use Disorder (LIBERATE-A)". ClinicalTrials.gov. 6 April 2026. Retrieved 22 July 2026. Terminated Study was terminated due to serious adverse event (SAE) No longer looking for participants
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