Drugs / Esmirtazapine
last change Mar 2015 re-read 9 days ago

Esmirtazapine

Small molecule targets HRH1, HTR2A, HTR2C via inhibition

Developed for
insomnia · mental disorder · sleep disorder, initiating and maintaining sleep
Investigated by
Merck Sharp & Dohme LLC · Parexel

Trials 10

PhaseRegistry idDatesIndicationSponsorStatusOutcome
Phase 11 trial
Phase 1 NCT00798395 Oct 2007 → Sep 2008 mental disorder, sleep disorder, initiating and maintaining sleep Merck Sharp & Dohme LLC Completed No outcome recorded
Phase 39 trials · 4 met primary
Phase 3 NCT00750919 Oct 2008 → Mar 2010 insomnia, mental disorder Merck Sharp & Dohme LLC Terminated No outcome recorded
Phase 3 NCT00631657 Mar 2008 → Nov 2009 mental disorder, sleep disorder, initiating and maintaining sleep Merck Sharp & Dohme LLC Completed Met primary
Phase 3 NCT00561574 Jan 2008 → Feb 2010 insomnia, mental disorder, sleep disorder, initiating and maintaining sleep Merck Sharp & Dohme LLC Completed Mixed
Phase 3 NCT00561821 Nov 2007 → Dec 2009 insomnia, mental disorder, sleep disorder, initiating and maintaining sleep Merck Sharp & Dohme LLC Completed Met primary
Phase 3 NCT00506389 Jun 2007 → Feb 2008 insomnia Merck Sharp & Dohme LLC Completed Met primary
Phase 3 NCT00610675 Dec 2006 → Aug 2009 insomnia Merck Sharp & Dohme LLC Completed No outcome recorded
Phase 3 NCT00482612 Dec 2006 → Aug 2008 insomnia Merck Sharp & Dohme LLC Completed Met primary
Phase 3 NCT00560833 Oct 2004 → Jan 2006 — Merck Sharp & Dohme LLC Completed Mixed
Phase 3 NCT00535288 Sep 2004 → Jan 2006 — Merck Sharp & Dohme LLC Completed Mixed

Evidence & citations 16 cited values

Every value below carries the sentence it was read from. 12 sources stand behind the page.

FieldValueCited text
Known as Esmirtazapine “This trial is a 52-week, open-label extension trial to investigate safety and to explore efficacy of Org 50081 (Esmirtazapine) in participants who completed Protocol 176001...” NCT00610675 ↗
8

NCT00482612 ↗

NCT00631657 ↗

NCT00560833 ↗

NCT00750919 ↗

NCT00535288 ↗

NCT00506389 ↗

NCT00561574 ↗

NCT00561821 ↗

Known as (s)-6-azamianserin ChEMBL registry synonym — accepted as the source's own label CHEMBL1366933 ↗
Known as (s)-mirtazapine ChEMBL registry synonym — accepted as the source's own label CHEMBL1366933 ↗
Known as (s)-org 3770 ChEMBL registry synonym — accepted as the source's own label CHEMBL1366933 ↗
Known as Esmirtazapina ChEMBL registry synonym — accepted as the source's own label CHEMBL1366933 ↗
Known as ESMIRTAZAPINE MALEATE ChEMBL registry synonym — accepted as the source's own label CHEMBL1366933 ↗
Known as MK-8265 “randomized to treatment with 1.5 mg or 3.0 mg of esmirtazapine (Org 50081, SCH 900265, MK-8265) to investigate the safety and tolerability of long-term treatment with...” NCT00561574 ↗
1

“treatment with esmirtazapine (Org 50081, SCH 900265, MK-8265) compared to placebo” NCT00631657 ↗

Known as Org 50081 “This trial is a 52-week, open-label extension trial to investigate safety and to explore efficacy of Org 50081 (Esmirtazapine) in participants who completed Protocol 176001...” NCT00610675 ↗
5

“Twenty-six Week Extension Trial of Org 50081 (Esmirtazapine) in Outpatients With Chronic Primary Insomnia (176003/P05721/MK-8265-007)” NCT00750919 ↗

“The maleic acid salt of Org 4420, code name Org 50081 (esmirtazapine), was selected for development in the treatment of insomnia.” NCT00561574 ↗

“The maleic acid salt of Org 4420, code name Org 50081, known as Esmirtazapine, was” NCT00561821 ↗

“treatment with esmirtazapine (Org 50081, SCH 900265, MK-8265) compared to placebo” NCT00631657 ↗

NCT00798395 ↗

Known as ORG-44-20 ChEMBL registry synonym — accepted as the source's own label CHEMBL1366933 ↗
Known as SCH 900265 “randomized to treatment with 1.5 mg or 3.0 mg of esmirtazapine (Org 50081, SCH 900265, MK-8265) to investigate the safety and tolerability of long-term treatment with...” NCT00561574 ↗
1

“treatment with esmirtazapine (Org 50081, SCH 900265, MK-8265) compared to placebo” NCT00631657 ↗

Action Inhibit “Serotonin 2a (5-HT2a) receptor antagonist” CHEMBL1366933 ↗
3

“Serotonin 2c (5-HT2c) receptor antagonist” CHEMBL1366933 ↗

“a high-affinity antagonist at 5-HT2A” PMID 26047890 ↗ Mar 2015

“Histamine H1 receptor antagonist” CHEMBL1366933 ↗

Modality Small molecule — CHEMBL1366933 ↗
Route Oral “tablets for oral use” NCT00482612 ↗
Target HRH1 “Histamine H1 receptor antagonist” CHEMBL1366933 ↗
Target HTR2A “Serotonin 2a (5-HT2a) receptor antagonist” CHEMBL1366933 ↗
Target HTR2C “Serotonin 2c (5-HT2c) receptor antagonist” CHEMBL1366933 ↗