Ralmitaront

Investigational antipsychotic drug

Ralmitaront
Clinical data

Other names	RG-7906; RO-6889450
Identifiers
IUPAC name 5-Ethyl-4-methyl-N-[4-[(2S)-morpholin-2-yl]phenyl]-1H-pyrazole-3-carboxamide
CAS Number	2133417-13-5
PubChem CID	130429734
ChemSpider	88298290
UNII	QA8MW1Q80P
KEGG	D11830
ChEMBL	ChEMBL4594376
Chemical and physical data
Formula	C₁₇H₂₂N₄O₂
Molar mass	314.389 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES CCC1=C(C(=NN1)C(=O)NC2=CC=C(C=C2)[C@H]3CNCCO3)C
InChI InChI=1S/C17H22N4O2/c1-3-14-11(2)16(21-20-14)17(22)19-13-6-4-12(5-7-13)15-10-18-8-9-23-15/h4-7,15,18H,3,8-10H2,1-2H3,(H,19,22)(H,20,21)/t15-/m1/s1 Key:XHHXGKRFUPEPFM-OAHLLOKOSA-N

Ralmitaront (INNTooltip International Nonproprietary Name, USANTooltip United States Adopted Name; developmental code names RG-7906 and RO-6889450) is an investigational antipsychotic drug which is undergoing a clinical trial for the treatment negative symptoms in schizophrenia and schizoaffective disorder.^[1]^[2]^[3] Another clinical trial targeting acute psychotic symptoms of schizophrenia has been terminated due to lack of efficacy.^[4] It is a partial agonist of the TAAR1.^[5] The medication is being developed by the pharmaceutical company Hoffmann-La Roche.^[1] Ralmitaront had completed phase 1 clinical trials.^[1]^[6]

References

^ ^a ^b ^c "Ralmitaront - Roche". AdisInsight. Springer Nature Switzerland AG.
^ Gomes FV, Grace AA (April 2021). "Beyond Dopamine Receptor Antagonism: New Targets for Schizophrenia Treatment and Prevention". International Journal of Molecular Sciences. 22 (9): 4467. doi:10.3390/ijms22094467. PMC 8123139. PMID 33922888.
^ Clinical trial number NCT04512066 for "Phase 2, Randomized, Double-Blind, Placebo-Controlled Study to Assess the Effects of RO6889450 (Ralmitaront) in Patients With Schizophrenia or Schizoaffective Disorder and Negative Symptoms" at ClinicalTrials.gov
^ Clinical trial number NCT03669640 for "A Trial of the Efficacy and the Safety of RO6889450 (Ralmitaront) vs Placebo in Patients With an Acute Exacerbation of Schizophrenia or Schizoaffective Disorder" at ClinicalTrials.gov
^ "Ralmitaront: Relationships: Trace Amine-Associated Receptor 1". Global Substance Registration System (GSRS). U.S. Food and Drug Administration.
^ Clinical trial number NCT02699372 for "The Safety, Tolerability, Pharmacokinetics and Pharmacodynamics Study of RO6889450 in Healthy Volunteers" at ClinicalTrials.gov

Human trace amine-associated receptor ligands

TAAR1

Agonists

Endogenous^†	Classical monoamine neurotransmitters Dopamine Histamine Norepinephrine Serotonin Trace amines 3-Iodothyronamine 3-Methoxytyramine N-Methylphenethylamine N-Methyltyramine m-Octopamine p-Octopamine Phenethylamine Phenylethanolamine Synephrine Tryptamine m-Tyramine p-Tyramine
Synthetic^‡	Amphetamine DOB DOET 4-Hydroxyamphetamine Isoprenaline MDA (tenamfetamine) MDMA (midomafetamine) 2-Methylphenethylamine 3-Methylphenethylamine 4-Methylphenethylamine β-Methylphenethylamine Methamphetamine 3-MMA Norfenfluramine Phentermine o-PIT Propylhexedrine Ralmitaront (RG-7906, RO-6889450) RO5166017 N,N-Dimethylphenethylamine Ulotaront (SEP-363856)

Neutral antagonists

Inverse agonists

EPPTB (RO5212773)

TAAR2

Agonists^‡
Neutral antagonists

TAAR5

Agonists^‡	N,N-Dimethylethylamine Trimethylamine
Neutral antagonists
Inverse agonists^‡	3-Iodothyronamine

^† References for all endogenous human TAAR1 ligands are provided at List of trace amines

^‡ References for synthetic TAAR1 agonists can be found at TAAR1 or in the associated compound articles. For TAAR2 and TAAR5 agonists and inverse agonists, see TAAR for references.

See also: Receptor/signaling modulators