sarizotan

Small moleculeexperimental

Sarizotan (EMD-128,130) is a selective 5-HT1A receptor agonist and D2 receptor antagonist, which has antipsychotic effects, and has also shown efficacy in reducing dyskinesias resulting from long-term anti-Parkinsonian treatment with levodopa. — Wikipedia

Clinical trial activity

6 trials · 5 clinical orgs · 0 marketing orgs

Phase 1

Phase 2

Phase 3

Phase 4

Earliest trial started Jan 1, 2001 (NCT00009048)

Timeline

2000s

Jan 1, 2001
Earliest Phase 2 Sponsor(trial)
Jan 1, 2004
Earliest Phase 3 Sponsor(trial)

Indications

Studied for

Mechanism of action

Dopamine D4 receptorAGONIST
DRD4 agonist
Development discontunued, failed to meet primary efficacy endpoints, no difference between drug and placebo. Newron developing drug for Rett syndrome and received EMA and FDA orphan designation in July 2015. Agonist/partial agonistic/antagonsitic effect depending on dopamine receptor isoform.
- D(4) dopamine receptor (DRD4) ↗
Dopamine D3 receptorAGONIST
DRD3 agonist
Development discontunued, failed to meet primary efficacy endpoints, no difference between drug and placebo. Newron developing drug for Rett syndrome and received EMA and FDA orphan designation in July 2015. Agonist/partial agonistic/antagonsitic effect depending on dopamine receptor isoform.
- D(3) dopamine receptor (DRD3) ↗
Serotonin 1a (5-HT1a) receptorAGONIST
HTR1A agonist
Development discontunued, failed to meet primary efficacy endpoints, no difference between drug and placebo. Newron developing drug for Rett syndrome and received EMA and FDA orphan designation in July 2015. Agonist/partial agonistic/antagonsitic effect depending on dopamine receptor isoform.
- 5-hydroxytryptamine receptor 1A (HTR1A) ↗
Dopamine D2 receptorPARTIAL AGONIST
DRD2 partial agonist
Development discontunued, failed to meet primary efficacy endpoints, no difference between drug and placebo. Newron developing drug for Rett syndrome and received EMA and FDA orphan designation in July 2015. Agonist/partial agonistic/antagonsitic effect depending on dopamine receptor isoform.
- D(2) dopamine receptor (DRD2) ↗

Chemistry & pharmacology

Loading structure…

SMILES

Fc1ccc(-c2cncc(CNC[C@H]3CCc4ccccc4O3)c2)cc1

Mol. weight: 348.42 g/mol
Lipinski Ro5: Pass
Rule of 3: No
Chirality: Single Stereoisomer
Inorganic: No
Polymer: No

Oral

Parenteral

Topical

Sources

Also known as

emd128130
emd 128130
emd 128130
emd-128130
emd-128130
sarizotan
sarizotan
sarizotan
sarizotan
sarizotan hcl
sarizotan hcl
sarizotan hydrochloride
sarizotan hydrochloride
sarizotan hydrochloride

Clinical trials

NCT ID	Phase	Start date	Sponsor(s)
NCT02790034	Phase 2/Phase 3 (Phase 3)	Aug 1, 2016	Newron Pharmaceuticals
NCT00310661	N/A	Dec 1, 2004	Merck KGaA, University of Toronto
NCT00105508	Phase 3	Sep 1, 2004	Merck Serono
NCT00105521	Phase 3	Sep 1, 2004	Merck Serono
NCT00314288	Phase 2	Jul 1, 2002	Merck Serono
NCT00009048	Phase 2	Jan 1, 2001	National Institute of Neurological Disorders and Stroke (NINDS)

Showing 6 of 6 trials

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Organizations

Research & Development (5)

Organization	Org type	Trials	As lead sponsor	Phases	Earliest year
Merck Serono	For profit	3	3	2	2002
Merck KGaA	For profit	1	0	1	2004
National Institute of Neurological Disorders and Stroke (NINDS)	Government	1	1	1	2001
Newron Pharmaceuticals	For profit	1	1	1	2016
University of Toronto	Academic/Hospital	1	1	1	2004

5 organizations

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