Delving into the Latest Updates on Esmirtazapine maleate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

(S)-1,2,3,4,10,14b-hexahydro-2-methylpyrazino(2,1-a)pyrido(2,3-c)(2)benzazepine, Esmirtazapine, Esmirtazapine maleate (USAN)

+ [4]

Target

5-HT2A receptor

Action

antagonists

Mechanism

5-HT2A receptor antagonists(Serotonin 2a (5-HT2a) receptor antagonists)

Therapeutic Areas

Nervous System DiseasesCardiovascular DiseasesOther Diseases

Active Indication-

Inactive Indication

Behavioural disordersMenopausal symptomsNeurocognitive Disorders+ [3]

Originator Organization

Merck Sharp & Dohme Corp.

Active Organization-

Inactive Organization

Royalty Pharma AG

Merck GmbH

Merck Sharp & Dohme Corp.

License Organization-

Drug Highest PhaseDiscontinuedPhase 3

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC21H23N3O4

InChIKeyRPUBHMMISKEXSR-MLCLTIQSSA-N

CAS Registry680993-85-5

View All Structures (2)

Drug-drug interactions (DDI) and genomic variation (PG) can lead to dangerously high blood and tissue concentrations with some drugs but may be negligible with other drugs. Using a quantitative metaanalysis, we analyzed on the example of CYP2D6 and CYP2C19 substrates, how well the effects of DDI and PG can be predicted by in vitro methods. In addition, we analyzed the quantitative effect of prototypic inhibitors of the two enzymes in relation to their genetic deficiency. More than 600 published studies were screened which compared either human pharmacokinetics with and without comedication, or which compared human pharmacokinetics of deficient with extensive metabolizers, or which assessed metabolism by in vitro approaches. With human liver microsomes, the in vitro to in vivo agreement of fractional clearances was reasonably high if loss of substrate was quantified in the in vitro assays performed with and without enzyme specific inhibitors. Also a generally very high correlation between the clinical pharmacokinetic effects of inherited deficiency and inhibition by drug-drug interactions could be demonstrated. Most cases of poor correlation were explained by the lack of CYP2D6 versus CYP2C19 specificity of fluoxetine or by a poor knowledge of the quantitative contribution of the metabolic pathways if metabolite formation was quantified in the in vitro assays. The good correspondence of the in vitro data with clinical DDI and clinical PG studies may be a good basis for future application of these methods in drug development and drug therapy.

100 Deals associated with Esmirtazapine maleate

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External Link

KEGG	Wiki	ATC	Drug Bank
D04055	Esmirtazapine maleate	-	DB06678

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Sleep Initiation and Maintenance Disorders	Phase 3	United States	Merck GmbH	-
Vascular Diseases	Phase 3	-	Royalty Pharma AG	-
Vasomotor symptom	Phase 3	United States	Merck GmbH	-
Vasomotor symptom	Phase 3	Australia	Merck GmbH	-
Vasomotor symptom	Phase 3	Europe	Merck GmbH	-
Vasomotor symptom	Phase 3	United States	Merck GmbH	-
Vasomotor symptom	Phase 3	Europe	Merck GmbH	-
Vasomotor symptom	Phase 3	Canada	Merck GmbH	-
Vasomotor symptom	Phase 3	Canada	Merck GmbH	-
Vasomotor symptom	Phase 3	Australia	Merck GmbH	-

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Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT00750919 \| NCT00631657 (21106/P05701/MK-8265-002, Pubmed \| J Clin Sleep Med)	Phase 3	Sleep Initiation and Maintenance Disorders	-	Esmirtazapine 4.5 mg	oquevnvtjx(orzamvapfs) = codoivqrnw ovimjssdrt (essghnnvgp, 35.0 - 62.5)	Positive	30 Apr 2020
NCT00482612 (P05706, Pubmed \| Sleep Med) Manual	Phase 3	Sleep Initiation and Maintenance Disorders	526	Esmirtazapine	(ftyhqxzupi) = irxafjceig ycrgtiokoj (rwzhyibkwb ) View more	Positive	01 Jul 2015
				Placebo	(uegsynmfsq) = vwoagincmn dldmumknfx (tdfsogyrli )
NCT00506389 (Pubmed \| Sleep Med)	Phase 3	Sleep Initiation and Maintenance Disorders	419	Esmirtazapine 3.0 mg	(pkcwiokqhr) = ubnmrfdwss roobsnjqer (mvayparpfm )	Positive	01 Jul 2015
				Esmirtazapine 4.5 mg	(pkcwiokqhr) = bnrfexpevq roobsnjqer (mvayparpfm )
NCT00506389 (P05707, CTgov)	Phase 3	Sleep Initiation and Maintenance Disorders	419	Esmirtazapine (Esmirtazapine 3.0 mg)	zltyelhbqz(atwubgbbiq) = ctpsbfdwck dlhxnvfils (oflrqgrjqq, fhhqpvjybo - acdrkidhyq) View more	-	06 Aug 2014
				Esmirtazapine (Esmirtazapine 4.5 mg)	zltyelhbqz(atwubgbbiq) = smktklzzfb dlhxnvfils (oflrqgrjqq, noqbhkkyxa - eyhrdaofov) View more
NCT00561821 (P05709, CTgov)	Phase 3	Sleep Initiation and Maintenance Disorders \| Neurocognitive Disorders	538	Placebo+Esmirtazapine (Esmirtazapine 0.5 mg)	bdwatnxagx(smluevvtxp) = stplbefapi typieiqwyi (ygdmryzqws, wnxozfmecs - vcfllfwmvc) View more	-	05 Aug 2014
				Placebo+Esmirtazapine (Esmirtazapine 1.5 mg)	bdwatnxagx(smluevvtxp) = uptnjwaryc typieiqwyi (ygdmryzqws, ufbvwarifa - bgcddlnkvm) View more
NCT00631657 (P05701 \| 21106, CTgov)	Phase 3	Sleep Initiation and Maintenance Disorders \| Neurocognitive Disorders	460	Esmirtazapine (Esmirtazapine 4.5 mg)	abjuxceofu(hcyrhdywwa) = huwetutajv hwwiizvoyj (dgkplxnqxa, hhovbslkgk - qllxcebqjr) View more	-	01 Aug 2014
				Placebo (Placebo)	abjuxceofu(hcyrhdywwa) = nlckacxtbc hwwiizvoyj (dgkplxnqxa, evfevzxnry - kccdbifslw) View more
NCT00535288 (P06472 \| 177001, CTgov)	Phase 3	Vasomotor symptom	946	Placebo (Placebo)	xblzrcoemo(vdgqakatjp) = dcxfqgbwwq nidzqlvtkv (yhgjaceutd, invynulpfx - jsugxopkaj) View more	-	30 Jul 2014
				Esmirtazapine (Esmirtazapine 2.25 mg)	xblzrcoemo(vdgqakatjp) = wptcqpjmfo nidzqlvtkv (yhgjaceutd, qeuddbgjtj - mzhugzneos) View more
NCT00610675 (P05708, CTgov)	Phase 3	Sleep Initiation and Maintenance Disorders	346	Org 50081	lllefygkvl(nlfrfoagyn) = saqvrfzfkg cwbjaijryo (egqgcryuij, ioqvyjycbx - xudylgecyt) View more	-	30 Jul 2014
NCT00561574 (176005 \| Jade \| P05697, CTgov)	Phase 3	Sleep Initiation and Maintenance Disorders \| Behavioural disorders	259	Esmirtazapine (Esmirtazapine 1.5 mg)	gdutdsuayd(ruxzqmghlz) = qyucadvxik vplqabpcff (qbnxvaooqp, dpmnbipesr - ocwjvqopvi) View more	-	07 Jul 2014
				Esmirtazapine (Esmirtazapine 3.0 mg)	gdutdsuayd(ruxzqmghlz) = tvlrxrenzy vplqabpcff (qbnxvaooqp, aexylcnyuj - ddodhvqgxj) View more
NCT00560833 (P06459 \| 46101 \| MK-8265-012, CTgov)	Phase 3	Vasomotor symptom	943	Placebo (Placebo)	vvdvugkeqp(mcsmsxhjow) = mrclnovsba tfnxqsqlqn (kaqkefgcka, tosajivapa - zznrzhsiuo) View more	-	30 Jun 2014
				esmirtazapine (Esmirtazapine 2.25 mg)	vvdvugkeqp(mcsmsxhjow) = rhcdjuoqvg tfnxqsqlqn (kaqkefgcka, lyrjgilkrb - mngbjpuigc) View more