Losmapimod: Difference between revisions

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Revision as of 04:10, 1 July 2011 editCheMoBot (talk \| contribs)Bots141,565 edits Updating {{drugbox}} (changes to verified fields - updated 'ChemSpiderID_Ref', 'StdInChI_Ref', 'StdInChIKey_Ref', 'ChEMBL_Ref', 'KEGG_Ref') per Chem/Drugbox validation (report [[Misplaced Pages talk:Wi← Previous edit		Revision as of 06:03, 15 August 2011 edit undoCheMoBot (talk \| contribs)Bots141,565 edits Updating {{drugbox}} (no changed fields - added verified revid - updated 'ChemSpiderID_Ref', 'DrugBank_Ref', 'ChEMBL_Ref', 'ChEBI_Ref', 'KEGG_Ref', 'StdInChI_Ref', 'StdInChIKey_Ref', 'ChEBI_Ref') per [[Misplaced Pages:WikiProject Chemicals/Chembox validatiNext edit →
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		⚫	\| UNII_Ref = {{fdacite\|correct\|FDA}}
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	\| UNII = F2DQF16BXE		\| UNII = F2DQF16BXE
	\| verifiedrevid = ~~386879444~~		\| verifiedrevid = 437173959
	\| IUPAC_name = 6--N-(2,2-dimethylpropyl)pyridine-3-carboxamide		\| IUPAC_name = 6--N-(2,2-dimethylpropyl)pyridine-3-carboxamide
	\| image = Losmapimod_structure.png		\| image = Losmapimod_structure.png
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	\| ATC_suffix =		\| ATC_suffix =
	\| PubChem = 11552706		\| PubChem = 11552706
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	\| DrugBank =		\| DrugBank =
	\| C=22\|H=26\|F=1\|N=3\|O=2		\| C=22\|H=26\|F=1\|N=3\|O=2

Revision as of 06:03, 15 August 2011

Pharmaceutical compound

Losmapimod
Legal status

Legal status	investigational new drug
Identifiers
IUPAC name 6--N-(2,2-dimethylpropyl)pyridine-3-carboxamide
PubChem CID	11552706
UNII	F2DQF16BXE
CompTox Dashboard (EPA)	DTXSID30974109
ECHA InfoCard	100.158.124
Chemical and physical data
Formula	C₂₂H₂₆FN₃O₂
Molar mass	383.458 g/mol g·mol
3D model (JSmol)	Interactive image
SMILES C3CC3NC(=O)c(cc(F)c1C)cc1-c(cc2)ncc2C(=O)NCC(C)(C)C
(verify)

Losmapimod (GW856553X) is a drug developed by GlaxoSmithKline which acts as a selective inhibitor of the enzyme family known as p38 mitogen-activated protein kinases. Inhibiting these enzymes has been shown to produce antidepressant and antipsychotic effects in animal studies, with the mechanism thought to involve increased neurogenesis probably related to BDNF release. Losmapimod has completed Phase II human clinical trials for the treatment of depression although its safety and efficacy have yet to be proven in further trials.

References

Aston N, Bamborough P, Buckton J, Edwards C, Holmes D, Jones K, Patel V, Smee P, Somers D, Vitulli G, Walker A. p38α Mitogen-Activated Protein Kinase Inhibitors: Optimization of a Series of Biphenylamides to Give a Molecule Suitable for Clinical Progression. Journal of Medicinal Chemistry 2009, 52(20), 6257. doi:10.1021/jm9004779
Noh JS, Kang HJ, Kim YE, Sohn S, Chung YK, Kim SU, Gwag BJ. Haloperidol-Induced Neuronal Apoptosis: role of p38 and c-Jun-NH(2)-terminal protein kinase. Journal of Neurochemistry 2000, 75(6), 2327. PMID 11080184 doi:10.1046/j.1471-4159.2000.0752327.x
A Study of GW856553X For the Treatment of Depression

Antidepressants (N06A)

Specific reuptake inhibitors and/or receptor modulators

SSRIsTooltip Selective serotonin reuptake inhibitors	Citalopram Escitalopram Fluoxetine Fluvoxamine Indalpine Paroxetine Sertraline Zimelidine
SNRIsTooltip Serotonin–norepinephrine reuptake inhibitors	Desvenlafaxine Duloxetine Levomilnacipran Milnacipran Tofenacin Venlafaxine
NRIsTooltip Norepinephrine reuptake inhibitors	Atomoxetine Reboxetine Viloxazine
NDRIsTooltip Norepinephrine–dopamine reuptake inhibitors	Amineptine Bupropion Nomifensine
NaSSAsTooltip Noradrenergic and specific serotonergic antidepressants	Mianserin Mirtazapine Setiptiline
SARIsTooltip Serotonin antagonist and reuptake inhibitors	Etoperidone Nefazodone Trazodone
SMSTooltip Serotonin modulator and stimulators	Vilazodone Vortioxetine
Others	Agomelatine Amisulpride Dextromethorphan/bupropion Esketamine Etryptamine Gepirone Indeloxazine Flupentixol Ketamine Medifoxamine Metryptamine Oxaflozane Pivagabine Tandospirone Teniloxazine Tianeptine

Tricyclic and tetracyclic antidepressants

TCAsTooltip Tricyclic antidepressants	Amineptine Amitriptyline Amitriptylinoxide Amoxapine Butriptyline Clomipramine Demexiptiline Desipramine Dibenzepin Dimetacrine Dosulepin Doxepin Imipramine Imipraminoxide Iprindole Lofepramine Melitracen Metapramine Nitroxazepine Nortriptyline Noxiptiline Opipramol Pipofezine Propizepine Protriptyline Quinupramine Tianeptine Trimipramine
TeCAsTooltip Tetracyclic antidepressants	Maprotiline Mianserin Mirtazapine Setiptiline
Others	Tiazesim

Monoamine oxidase inhibitors

Non-selective

Reversible: Caroxazone

Mixed: Bifemelane

MAO_ATooltip Monoamine oxidase A-selective

MAO_BTooltip Monoamine oxidase B-selective

Irreversible: Selegiline

Adjunctive therapies
Atypical antipsychotics (aripiprazole, brexpiprazole, lurasidone, olanzapine, quetiapine, risperidone) Buspirone Lithium (lithium carbonate, lithium citrate) Thyroid hormones (triiodothyronine (T₃), levothyroxine (T₄))

Miscellaneous
Ademetionine (SAMe) GABAkine neurosteroids (brexanolone, zuranolone) Hypericum perforatum (St. John's Wort) Oxitriptan (5-HTP) Rubidium chloride (RbCl) Tryptophan

WHO-EM
Withdrawn from market
Clinical trials:
- Phase III
- Never to phase III

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